dinda2015

Journal of Ethnopharmacology 161 (2015) 255–278
Contents lists available at ScienceDirect
Journal of Ethnopharmacology
journal homepage: www.elsevier.com/locate/jep
Review
Oroxylum indicum (L.) Kurz, an important Asian traditional medicine:

From traditional uses to scientific data for its commercial exploitation
B. Dinda a,n, I. SilSarma a, M. Dinda b, P. Rudrapaul a
a
Department of Chemistry, Tripura University, Suryamaninagar, Agartala-799022, Tripura, India
b
Department of Life Science and Biotechnology, Jadavpur University, Jadavpur, Kolkata-700032, India
art ic l e i nf o a b s t r a c t
Article history: Ethnopharmacological relevance: Oroxylum indicum\ (L.) Kurz has been used for centuries as a traditional
Received 26 August 2014 medicine in Asia in ethnomedicinal systems for the prevention and treatment of several diseases, such as
Received in revised form jaundice, arthritic and rheumatic problems, gastric ulcers, tumors, respiratory diseases, diabetes, and
18 December 2014
diarrhea and dysentery, among others. The present review provides scientific evidence supporting the
Accepted 19 December 2014
therapeutic potency of the plant for ethnomedicinal uses and identifies gaps for future research to
Available online 25 December 2014
facilitate commercial exploitation.
Keywords: Methods: This review is based on available information on traditional uses and phytochemical,
Oroxylum indicum (L.) Kurz pharmacological, clinical and toxicity data for Oroxylum indicum that was collected from electronic
Oroxylum flavum Rehder (SciFinder, PubMed, Science Direct, and ACS, among others) and library searches.
Bignoniaceae
Keyfinding: A variety of traditional medicinal uses of Oroxylum indicum in different Southeast and South
Traditional medicine
Asian countries have been reported in books describing the uses of these plants. Phytochemical
Asian countries
Scientific data
investigations of the different parts of the plant resulted in identification of approximately 111
compounds, among which flavonoids, naphthalenoids and cyclohexylethanoids are the predominant
groups. The crude extracts and their isolates exhibit a wide spectrum of in vitro and in vivo
pharmacological activities involving antimicrobial, anti-inflammatory, anti-arthritic, anticancer, anti-
ulcer, hepatoprotective, antidiabetic, antidiarrheal and antioxidant activities. Flavonoids are the major
constituents of all parts of the plant. From a toxicity perspective, only aqueous and ethanolic extracts of
stem bark, root bark and fruits have been assessed and found to be safe.
The major flavonoids of the stem bark, such as baicalein, chrysin and oroxylin A, were reported for
the first time as natural flavonoids with potent inhibitory activity against endoprotease enzymes and
proprotein convertases, which play a key role in the growth of cancer and in viral and bacterial infections.
Flavonoids are the active components of bioactive extracts. Several Ayurvedic medicines have been
formulated either singly using this plant or along with other herbs for the treatment of different diseases.
Conclusions: Pharmacological results have supported some traditional medicinal uses of Oroxylum
indicum. Several extracts and their isolates have been reported to exhibit interesting pharmacological
properties. These components could be useful as sources of modern medicines following future detailed
studies to elucidate their underlying mechanisms, toxicity, synergistic effects and clinical trials. Attention
should also be focused on pharmacological studies investigating the traditional uses of the plant, which
have not been yet addressed, as well as clinical studies investigating commercial Ayurvedic medicines
Abbreviations: ABTS, 2,20 -azino bis-(3-ethylbenzothiazoline-6-sulfonic acid; AGE, advanced glycation end products; AIU, aspirin-induced ulceritis; ALP, alkaline
phosphatase; ALT, serum alanine aminotransferase; Aq. MeOH, aqueous methanolic; AST, serum aspartate aminotransferase; BSA, bovine serum albumin; bw, body
weight; CRU, cold restrain induced ulcer; DCM, dichloromethane; DNBS, dinitrobenzene sulfonic acid; DNFB, 2,4-dinitrofluoro benzene; DPPH, 2-diphenyl-1-picrylhydrazyl;
EE, ethanolic extract; EIA, enzyme immune assay; EIU, ethanol-induced ulcer; ELISA, enzyme-linked immunosorbent assay; FAS, cell surface death receptor; FRAP, ferric ion
reducing antioxidant powder; FPS, fluorogenic peptide substrate; GLUT-4, glucose transporter-4; Gy, gray (SI unit of absorbed radiation per sec.); HDL, high density
lipoprotein; IC50, concentration that causes 50% inhibition; i.p., intraperitoneally; LC50, concentration that kills 50% of the larvae within 24 h; LD50, dose of extract in g per kg
body weight of mice to kill 50% of tested mice; LPL, lipoprotein lipase; LPO, lipid peroxidase; LPS, lipopolysaccharide; MIC, minimum inhibitory concentration; MTD,
maximum tolerated dose; MPO, myeloperoxidase; MTT, 2-(4,5-dimethylthiazol-2 yl)-3, 5-diphenyl-2H-tetrazolium bromide; ND, new castle disease (¼ Ranikhet disease);
WIRS, water immersion plus restraint stress; N/S, not stated; ORAC, oxygen radical absorbance capacity; PE, petroleum ether, b.p. 60-80 1C; p.o., per oral; PLU, pylorus
ligation-induced ulcer (gastric lesions); PMA, phorbol 12-myristate 13-acetate; PPAR-γ, peroxisome proliferator-activated receptor gamma; SGOT, serum glutamate
oxaloacetate transaminase; SGPT, serum glutamic pyruvate transaminase; STZ, streptozotocin; SALP, serum alkaline phosphatase; TBE, trypan blue exclusion; XTT, 2, 3-bis(2-
methoxy-4-nitro-5-sulphenyl)-2H-tetrazolium-5-carboxanilide
n
Corresponding author. Tel.: þ 91 3812519006.
E-mail address: dindabtu@gmail.com (B. Dinda).
http://dx.doi.org/10.1016/j.jep.2014.12.027
0378-8741/& 2014 Elsevier Ireland Ltd. All rights reserved.
256 B. Dinda et al. / Journal of Ethnopharmacology 161 (2015) 255–278
and other ethnomedicinal preparations in human subjects based on this plant to confirm the safety and
quality of the preparations.
& 2014 Elsevier Ireland Ltd. All rights reserved.
Contents
1. Introduction . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 256
1.1. Taxonomy and synonyms . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 256
1.2. Geographical distribution . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 257
1.3. Traditional medicinal usage . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 257
1.4. Scope of the review . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 257
1.5. Methods . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 259
2. Chemical constituents and their structures . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 259
2.1. Flavonoids . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 259
2.2. Isoflavonoids . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 261
2.3. Naphthalenoids . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 261
2.4. Phenylethanoids. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 261
2.5. Cyclohexylethanoids . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 261
2.6. Triterpenoids . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 261
2.7. Steroids . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 261
2.8. Stilbenoids . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 261
2.9. Miscellaneous compounds . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 261
3. Pharmacological activities . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 261
3.1. Antimicrobial activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 266
3.2. Anti-inflammatory activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 266
3.3. Anti-arthritic activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 269
3.4. Anticancer/anti-tumor activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 269
3.5. Anti-ulcer activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 269
3.6. Radioprotective activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 269
3.7. Immunostimulant activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 269
3.8. Anti-diarrheal activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 270
3.9. Antidiabetic activity. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 270
3.10. Anti-gout activity. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 270
3.11. Anthelminthic activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 270
3.12. Hepatoprotective activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 270
3.13. Antioxidant activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 271
3.14. Nephroprotective activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 271
3.15. Analgesic activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 271
3.16. Anticolitis activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 271
3.17. Antimutagenic activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 272
3.18. Wound-healing activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 272
3.19. Proprotein convertase inhibitory activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 272
3.20. Anti-leishmanial activity . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 272
4. Toxicity studies . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 272
5. Clinical trials . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 272
6. Discussion . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 272
7. Conclusion . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 273
Acknowledgements . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 274
References . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 274
1. Introduction
other Southeast Asian countries are as follows: Indonesia: pongporang
1.1. Taxonomy and synonyms (Sundanese), Kayu lanang, mungli (Javanese); Malaysia: beko, bonglai,
kulai; Philippines: pingka-pingkahan (Tagalog), abong-abong (Bisaya),
Oroxylum indicum (L.) Kurz (earlier name: Oroxylum flavum Rehder; kamkampilan (Iloko); Cambodia: pika; Laos: lin may, ung ka; Thailand:
Bignoniaceae) is a medium-sized tree that grows in Asian tropical and phe kaa (central), litmai (northern), lin faa (northeastern) (Rasadah,
subtropical low-altitude open forests and is cultivated on road sides 2001). Its leaves are opposite ternately bipinnate and up to 2-m long,
and slopes (Anonymous, 1972; Kochummen, 1978). In India, it is called with leaflets that are broad and entirely ovate and glabrous. The
“Syonakh” or “Trumpet tree” due to the resemblance of its flowers to pinkish flowers of the plant are arranged in long, terminal erect
the trumpet (Chopra et al., 1992). In Sri Lanka, it is called ‘Thotila’ racemes. The fruits are long and sword-like with capsules that have
(Jayawera, 1981), and in Malaysia, it is called “Midnight Horror” bec- kidney-shaped, yellowish-green seeds that are surrounded by a light-
ause the flowers open at night, emitting a powerful stink that attracts brown papery wing (Deb, 1983). Per the taxonomical classification of
bats to facilitate pollination (Kochummen, 1978). Its local names in the plant, it belongs to the class Dicotyledon, sub-class Sympetaleae,
B. Dinda et al. / Journal of Ethnopharmacology 161 (2015) 255–278 257
order Tubiflorae, family Bignoniaceae, genus Oroxylum, and species herbal medicine in many Asian countries to cure various diseases
Oroxylum indicum (Engler and Prantle, 1887–1995). (Biswas and Ghosh, 1994). The root and stem bark are used for
fever, bronchitis, intestinal worms, leucoderma, asthma, inflam-
Synonyms of Oroxylum indicum (L.) Kurz mation, anal troubles, diarrhea and dysentery. The fruits and seeds
are used as an expectorant, purgative and bitter tonic (Kirtikar and
Homotypic: Basu, 1996). In Indian Ayurvedic medicine, the root bark, stem and
Bignonia indica L., sp. PL.: 625 (1753) leaf are prescribed for snake bite, diarrhea and dysentery (Ghani,
Calosanthes indica Bl., Bijdr.: 761 (1826) 1998). In Traditional Chinese medicine, the seeds of the plant,
Hippoxylon indica Raf., Sylv. Tellur.: 78(1838) which are named Mu Hu Die in Chinese, have been widely used for
Spathodea indica L. (Pers.), synop. PL: (1807) the treatment of cough, bronchitis, pharyngitis, pertussis and
other respiratory disorders (National Commission of Chinese
Heterotypic: Pharmacopoeia, 2010).
Arthrophyllum ceylanicum Miq, Ann. Mus. Bot. Lugduno-Batavi In India, several Ayurvedic medicines are commercially available
1: 27 (1863), WCSP that utilize different parts of this plant. For example, the roots are used
Arthrophyllum reticulatum Blume, Ann. Mus. Bot. Lugduno- extensively along with other herbs to prepare ‘Dasamoola’, which is
Batavi 1: 27 (1863), WCSP considered to be effective as an anti-inflammatory, anthelmintic,
Bignonia lugubris Salisb, Prodr. Strip. Chap. Allerton: 106 (1796) antibronchitic, antileucodermic, antirheumatic, and antianorexic, as
Bignonia tripinnata Noronha, V. B. G. Kunsten 5(4): 8 (1790) well as for the treatment of thyroid dysfunction, viral hepatitis, and
Bignonia tuberculata Roxb. Ex DC, Prodr. 9: 177 (1845) gallstone disease, among others. (Anonymous, 1995). Another pre-
Bignonia quadripinnata Blanco, Fl. Filip.: 499 (1837) paration, Chitraka Haritaki Avaleha, is specifically used for the treat-
Bignonia pentandra Lour., Fl. Cochinch: 379 (1790) ment of nasal disorders, including cough and asthma disorders of
Oroxylum flavum Rehder, C. S. Sargent, Trees & Shrubs: 193 Pthisis, chronic rhinitis, helminthiasis, hemorrhoids and digestive
(1927) impairment (Atara et al., 2014). The different parts of the plant, mainly
the fruits, seeds, stem-bark and roots, are also used with other herbs in
several Ayurvedic formulations such as Amartarista, Dantyadyarista,
Narayan taila, Dhanawantara ghrita, Brahma rasayan and Chyavana-
1.2. Geographical distribution prasa, Dasamularistha, Misraka sneha, Dasamoola rasayan, Syonaka
thailam, Pashanabhedadhi gritham, Dasamoola hareethaki, Sidhartha-
Oroxylum indicum (L.) Kurz is found throughout Southeast and kadhi agadam, Mahat-panchamoola thailam, Sathahwadhi dhooma,
South Asian countries. It is native to the Indian sub-continent, in the Pushyanuga choornam, Agastya hareethaki, Maha tailam, Dasamoola
Himalayan foot hills, and extends into Southern China, Indo-China and kwatham, Veerathavadhi kashayam, and Syonaka putapakam, among
the Malaysia ecozone (Theobald, 1981). In India, it is found in the others, to alleviate thirst, reheumatism, dysentery, anorexia, bronchitis,
Himalayan foothills and Eastern and Western Ghats, and it is culti- eruptive fevers and dropsy, among others. (Anonymous, 1998; Radhika
vated throughout India in forest areas (Sasidharan, 2004). It grows et al., 2011).
wild in Bangladesh in Chittagong, as well as other Hill Tracts districts In Malaysia, Ayurvedic formulations, ‘Rymanyl’ capsules and
(Yusuf et al., 2009). It is found in Fujian, Guangdong, Guangxi, ‘Arthrella’ ointment consisting of Oroxylum indicum as an ingre-
Guizhou, Sichuan, Taiwan, Yunan, Myanmar, Vietnam, Laos, Thailand, dient, are used to treat rheumatoid arthritis and osteoarthritis
Cambodia, Malaysia, Philippines, Indonesia (Java, Sumatra), Nepal, (Singh et al., 2010).
Bhutan, Bangladesh, Pakistan and Sri Lanka (Zhang and Santisuk,
1998; Kochummaen, 1978). It is usually grown in low altitude open
forests and slopes at 500–900 m (Zhang and Santisuk, 1998). Fig. 1
shows a map of Southeast and South Asia that indicates the geogr- 1.4. Scope of the review
aphical distribution of Oroxylum indicum (L.) Kurz.
The extremely diverse range of recorded traditional uses,
wide geographical distribution in different Southeast and South
1.3. Traditional medicinal usage Asian countries and promising phytochemical profile and phar-
macological studies of the plant have created an opportunity for
The traditional uses of Oroxylum indicum (L.) Kurz are listed in greater development of the medicinal properties of the plant at
Table 1. The plant has been used for centuries as an important both local and international levels. Hence, a critical review of
this plant is needed. Previous review articles on this plant by Yin
et al. (2007), Dev et al. (2010), Harminder et al. (2011), Ahad
et al. (2012) and Deka et al. (2013) have highlighted primarily
the taxonomy and ethnobotany and partially the phytochemis-
try and pharmacology of this plant. None of these articles has
focused on detailed traditional uses in different Asian countries
or the future course of studies on the plant to examine its use
in modern medicines. Therefore, in this review, we highlight
detailed traditional uses, scientific data on phytochemistry,
pharmacology, toxicity and for clinical studies and future per-
spectives regarding research and precautionary measures for
the commercial utilization of the plant in modern medicines. In
this review, separate tables for folklore usages, isolated phyto-
chemicals, pharmacological activities of extracts and isolates
(Tables 1, 2 and 3) and geographical distributions and chemical
Fig. 1. The map of Southeast and South Asia showing geographical distribution of structures of isolated compounds in Figs. 1, 2 provide a quick
Oroxylum indicum (L.) Kurz [●]. overview for the reader.
Table 1
Traditional uses of Oroxylum indicum (L.) Kurz.
Plant part Traditional use(s) Country Preparation(s) Reference(s)

(s)
Root/root (a) Hepatoprotective India Paste of root bark Jamir and Takatemjen (2010)
bark
(b) Jaundice Vietnam Decoction of dried root bark Rasadah (2001)
(c) Antidiarrheal India N/S Prakash (2005)
Thailand N/S Rasadah (2001)
Bangladesh N/S Ghani (1998)
Sri Lanka N/S Jayawera (1981)
Vietnam Decoction of dried root bark Rasadah (2001)
(d) Antidysenteric Philippines Decoction Rasadah (2001)
and
Thailand
Nepal Decoction Kunwar et al. (2009)
India N/S Prakash (2005)
Sri Lanka N/S Jayawera (1981)
Laos N/S Perry (1980)
Mayanmar N/S Perry (1980)
(e) Antidiabetic Laos Decoction with other herbs Libman et al. (2006)
(f) Antirheumatic Philippines Decoction Rasadah (2001)
India N/S Prakash (2005)
(g) Urinary disorders including India N/S Sreedevi et al., (2011a)
diuretic
Philippines Decoction Rasadah (2001)
(h) Asthma, sore throat India Mixed with other herbs Kalaivani and Mathew (2009), Kirtikar
and Basu (2001)
Vietnam Decoction of dried root Rasadah (2001)
(i) Leprosy, tuberculosis rheumatic pain India Mixed with other herbs Kalaivani and Mathew (2009)
and bowels
(j) Gastralgia Vietnam Decoction of dried root bark Rasadah (2001)
(k) Leucoderma, intestinal worms anal India N/S Kirtikar and Basu (2001)
troubles and biliousness
(l) Impotence Bangladesh Aqueous extract is mixed with 3 drops of water Faruque and Uddin (2014)
from three different ponds and 2–3 tea spoonful
is taken twice a day for 3 days
(m) Gonorrhoea India Dry roots mixed with roots Rivea hypocrateriformis Kumari et al. (2012)
and Salmalia malabarica are powdered and
1–2 teaspoonful powder in milk is given
for a week
Stem/stem (a) Jaundice and heart problem India Decoction of bark powder in water Tangjang et al., (2011), Badgujar and Patil
bark (2008)
Paste of fresh stem bark with turmeric Hemadri and Rao (1984)
Crushed bark soaked in water overnight Sharma et al. (2012)
Two tablespoons juice of stem bark, one hen’s Sarkar and Das (2010)
egg and common salt are blended and fried
Bangladesh N/S Rahim et al. (2012)
Vietnam N/S National Institute of Medicinal Materials
(2004)
(b) Antidiabetic India Decoction of powder or fresh juice of stem bark Chhetri et al. (2005)
Thailand Fresh juice of stem bark Wuthithamvech (1997)
(c) Arthritic and rheumatic pains Thailand Hot water extract Laupattarakasem et al. (2003)
Sri Lanka Decoction Jayawera (1981)
(d) Gastritis, ulcer, mouth cancer scabies India Decoction Mao (2002), Bhushan and Kumar (2013)
and abscesses
Java Decoction with water Rasadah (2001)
(e) Allergic dermatitis Vietnam Alcoholic maceration of fresh bark externally Rasadah (2001)
(f) Anti dysenteric Malaysia N/S Burkill (1966)
(g) Wounds and burns India Bark powder is used topically on wounds; Gaur and Sharma (2011)
bark paste is applied topically on burns
(h) Wounds of animals to kill Maggots India Paste of bark Warrier et al. (1995)
and deworming of animals
(i) Bronchitis and other respiratory China Mixed with other herbs Wu et al. (2005), Liang (2007)
problems
Vietnam Decoction of dried bark Rasadah (2001)
India N/S Patil et al. (2008)
Panghal et al. (2010)
(j) Bleeding Sulawesi Paste of fresh inner bark Rasadah (2001)
(k) Malaria India Powdered bark is taken for 5–6 days Shankar et al. (2012)
(l) Menstruation complaints India Fresh bark is mixed with immature seeds of Carica Majumdar and Datta (2007)
papaya
in a ratio of 2:1 and the mixture is grinded into a paste
and made into small pills; 2–3 pills are given with betal
leaf
(m) Swelling Malaysia Bark soaked in hot water and rubbed on the affected Kulip (2003)
area
Table 1 (continued )
Plant part Traditional use(s) Country Preparation(s) Reference(s)

(s)
Leaf (a) Enlarged spleen India Decoction Drury (2006)

Malaysia Boiled leaves as poultice Rasadah (2001)
Sikkim Decoction Singh et al. (2002)
(b) Toothache, headache, Stomach-ache, India Decoction Drury (2006), Bhushan and Kumar (2013)
ulcer and rheumatic pain
Malaysia Poultice Rasadah (2001), Burkill (1966)
Nepal Chewed Limbu and Rai (2013)
Philippines N/S Rasadah (2001)
(c) Snake bite India Decoction Nadkarni (1982)
Bangladesh N/S Ghani (1998)
(d) Piles India Decoction Deb et al. (2011)
(e) Child birth Malaysia Boiled leaves as poultice Rasadah (2001)
(f) Anti dysenteric Malaysia Boiled leaves as poultice Rasadah (2001)
(g) Cholera Malaysia Decoction externally Rasadah (2001)
(h) Low blood pressure weakness India Decoction Majumdar and Datta (2007)
(i) Scorpion sting India Decoction is mixed crushed garlic and used Naturu et al. (2013)
as poultice
Fruits (a) Intestinal worms India Dcoction Drury (2006)
(b) Bronchitis and cough expectorant India Decoction Drury (2006), Bhushan and Kumar (2013)
(c) Cardiac ailments and piles India N/S Bhushan and Kumar (2013)
(d) Anti-diarrhea Nepal Aqueous extract Limbu and Rai (2013)
Seed (a) Tonsillitis pain India Poultice externally Mao (2002)
(b) Epilepsy India Decoction of powdered seed Sharma et al. (2013), Gairola et al. (2013)
(c) Boils and wounds Nepal Paste externally Kunwar et al. (2009), Rijal (2008)
(d) Analgesic, anti tussive cough, China N/S National Commission of Chinese
bronchitis, pharyngitis and other Pharmacopoeia (2010), Jiansu New
respiratory problems Medical College (1997)
Vietnam Decoction Rasadah (2001)
India N/S Patil et al. (2008), Panghal et al. (2010)
(e) Laxative Thailand N/S Rasadah (2001)
(f) Gastritis Vietnam Decoction Rasadah (2001)
(g) Ulcers and tumor Vietnam Poultice externally Rasadah (2001)
Thailand Hot water extract Palasuwan et al. (2005)
(h) Anti dysenteric India Decoction of powdered seeds in water Gairola et al. (2013)
(i) Anti diarrheal Thailand Hot water extract Palasuwan et al. (2005)
(j) High fever and pneumonia India Seeds with bark are powdered and mixed Pradhan and Badola (2008)
with water, and strained; the concoction is fed to
patients
(k) Purgative and headache India N/S Kala (2005)
Plant part (a) Tumor India N/S Balachandran and Govindarajan (2005)
N/S
(b) Gynaecological inflammation China Mixed with other herbs Lu (2007)
(c) Tonsillitis China Mixed with other herbs Ning and Wang (2006)
N/S: Not stated.
1.5. Methods 2013), as well as in the petiole, leaf, seed, fruit wall and root
(Samatha et al., 2012). Among them, B-ring unsubstituted flavones
The literature search was conducted via SciFinder (http://cas. and their glycosides are the major types of flavonoids distributed in
org/products/scifinder/index.html) covering the period from 1933 different parts of the plant. These flavonoids are mainly bioactive
to 2014. Additional information was collected from PubMed components that are present in the bioactive fractions of the
(http://www.ncbi.nlm.nih.gov/pubmed) and journal and book extracts.
searches.
2.1. Flavonoids
2. Chemical constituents and their structures To date, 50 flavonoids have been reported (Table 2, Fig. 2). Among
the flavonoids, baicalein (1), chrysin (2) and oroxylin A (3) are the
Table 2 and Fig. 2 summarize the phytochemicals with chemical major flavones present in stem bark (Dinda et al., 2007; Hari Babu
structures that have been reported for different parts of Oroxylum et al., 2010). Baicalein, chrysin, baicalein 7-O-glucoside (4), baicalein
indicum to date. These include the following: 50 flavonoids, 6 iso- 7-O-diglucoside (7) and chrysin 7-O-diglucoside (13) are the major
flavonoids, 14 napthalenoids, 3 phenyl ethanoids, 9 cyclohexyl etha- chemical constituents of seeds (Yan et al., 2011). In fruits, baicalein
noids, 3 triterpenoids, 4 steroids, 5 stilbenoids and 17 miscellaneous (1) was present as the major constituent and represented approxi-
compounds. Each phytochemical is numbered (1 to 111) (Fig. 2) and mately 4% of freeze-dried fruits (Roy et al., 2007). In root bark,
is cited in the text. oroxylin A and baicalein are the major constituents (Ali et al., 1998,
Flavonoids, the most abundant constituents of this plant, Khandhar et al., 2006). In leaves, baicalein, scutellarein (26) and their
demonstrated the highest levels (346.6715.2 mg quercetin equiv./g 7-O-glucuronides (5 and 30) are the major chemical constituents
ext.) in the MeOH extract of the stem bark (Moirangthem et al., (Subramanian and Nair, 1972a).
Table 2
An overview of the chemical constituents reported from different parts of Oroxylum indicum (L.) Kurz.
Phytochemical Chemical constituents Reference(s)

group
(a) Phytochemicals reported from leaves

Flavonoids Baicalein (1), baicalein 7-O-glucuronide (¼ baicalin, 5), baicalein 6-O-glucuronide (9), scutellarein (26) and Subramanian and Nair (1972a)
scutellarein 7-O-glucuronide (¼ scutellarin, 30)
Chrysin (2), baicalein 7-O-glucoside (4), baicalein 7-O-diglucoside (7), chrysin-7-O-glucuronide (11) and Yuan et al. (2008)
chrysin -7-O-diglucoside (13)
Anthraquinone
Aloe-emodin (95) Dey et al. (1978)
(b) Phytochemicals reported from fruits
Flavonoids
Baicalein (1) and chrysin (2) Roy et al. (2007)
Phenylethanoids
Salidroside (71), 2(3,4-dihydroxyphenyl)-ethyl glucoside (72) and acteoside (73) Teshima et al. (1996)
Cyclohexylethanoids
Rengyol (74), ketoform of rengyoxide (75), ( 7 )5,6-dihydrocornoside (76), ( 7 ) 6α- Teshima et al. (1996)
hydroxydihydrocornoside (77), cornoside (78), regyolone (80), dihydrorengyolone (81) and 6α-
methoxydihydrorengyolone (82)
Triterpenoid
Ursolic acid (83) Roy et al. (2007)
(c) Phytochemicals reported from seeds
Flavonoids
Chrysin-7-O-glucoside (12), chrysin-7-O-β-D-glucuronide Et ester (14), norwogonin (21), chrysin-8-C-β-D- Wen et al. (2011)
glucopyranoside (24), acacetin (34), hispidulin (35), isorhamnetin (45), kaempferol 7-O-β-D-
glucopyranoside (46), and isoquercetin (50)
Baicalein (1), and baicalein-6-O-glucoside (¼ tetuin, 8) Mehta and Mehta (1953)
Oroxylin A (3), baicalin (5), baicalein-7-O-β-D-glucuronopyranosyl-(1-3)-[β-D-glucopyranosyl-(1-6)-β- Yan et al. (2011)
D-glucopyranoside (10), chrysin 7-O-glucuronide (11), chrysin-6-C-β-D-glucopyranosyl-8-C-α-L-
arabinopyranoside (25), chrysin-6-C-β-D-glucopyranosyl 7-O-β-D-glucuronopyranoside (15), scutellarein
7-O-glucoside (27), scutellarein-7-O-β-D-glucopyranosyl (1-6)-β-D-glucopyranoside (28), pinocembrin
(41) and pinobanksin (42)
Baicalein-7-O-glucoside ( ¼ oroxin A, 4) Tomimori et al. (1988), Chen et al.
(2003), Chen et al., (2005)
Baicalein-7-O-β-gentiobioside ( ¼oroxin B, oroxylin B, 7) Tomimori et al. (1988), Chen et al.
(2003)
Chrysin (2) and chrysin 7-O-diglucoside (13) Chen et al. (2003)

Wogonin-7-O-β-D-glucuronide ( ¼ oroxindin, wogonoside, 22) Nair and Joshi (1979)
Apigenin (36), kaempferol (47), quercetin (48) and quercetin-3-O-arabinopyranoside (49) Wei et al. (2013b)
Triterpenoids
Lupeol (84) and 2α-hydroxylupeol (85) Yan et al. (2011)
Steroids
β-Sitosterol (86) Yan et al. (2011)
Cholest-5-ene-3,7-diol (89) and β-sitosterol glucoside ( ¼ daucosterol, 87) Wei et al. (2013b)
Stilbenoids
(E)-Dihydropinosylvin-2-carboxyl-5-O-β-D-glucopyranoside (90), E)-dihydropinosylvin-3-O-β-D- Xie et al. (2014)
glucopyranoside (91), (E)-pinosylvin-3-O-β-D-glucopyranoside (92), pinosylvin (93) and dihydropinosylvin
(94)
Cyclohexylethanoids
Rengyol (74) and isorengyol (79) Wei et al. (2013b)
Fatty acids
Caprylic acid (99), lauric acid (100), myristic acid (101), myristoleic acid (104), palmitoleic acid (105) and Grover and Rao (1980)
linoleic acid (107)
Palmitic acid (102), stearic acid (103) and oleic acid (106) Mehta (1939)
Others
2-Methyl-6-phenyl-4H-pyran-4-one (98), echinulin (108), adenosine (109) and dimethylsulfone (110) Yan et al. (2011)
Zarzissine (111) Wei et al. (2013a,b)
(d) Phytochemicals reported from stem bark
Flavonoids
Baicalein (1), chrysin (2), oroxylin A (3), baicalein 7-O-glucuronide ( ¼ baicalin, 5), scutellarein (26) and Subramanian and Nair (1972b)
scutellarein 7-O-rutinoside (29)
Baicalein 7-O-glucoside (4), baicalein 7-O-caffeate (6), 8, 8″-bisbaicalein (23), 6-hydroxyluteolin (37) and Dinda et al. (2007)
6-methoxyluteolin (38)
7-O-Methylchrysin (16), 5-hydroxy-7,40 -dimethoxyflavone (33), 5,20 -dihydroxy-7,60 -dimethoxyflavone-20 - Hari Babu et al. (2010)
O-β-D-glucopyranoside (39), dihydrooroxylin A (40) and dihydrooroxylin A 7-O-methylglucuronide (43)
Scutellarein 40 -O-methyl ether (31), pectolinarigenin (32) and (2S)-dihydrobaicalein 7-O-(6″- SilSarma et al. (2014)
benzoylglucopyranoside) (44)
Oroxylin A 7-O-glucoside (17) Lalou et al. (2013)
Chrysin A-7-O-β-D-glucuronide (11), oroxylin A 7-O-β-D-glucuronide (18), oroxylin A 7-O-β-D- Tran et al. (2014)
methylglucuronide (19), baicalein A 7-O-β-D-methylglucuronide (20) and hispidulin (35)
Isoflavonoids
Methyl oroxylopterocarpan (53), dodecanyl oroxylopterocarpan (54), hexyl oroxylopterocarpan (55) and Ali et al. (1999)
heptyl oroxylopterocarpan (56)
Naphthalenoids
Lapachol (57) and dehydro iso-α-lapachone (58) Ali et al. (1998)
Phytochemical Chemical constituents Reference(s)

group
Steroids
β-Sitosterol (86) Dinda et al. (2007)
β-Sitosterol glucoside (87) SilSarma et al. (2014)
Others (Phenolic)
p-Coumaric acid (97) Subramanian and Nair (1972b)
(e) Phytochemicals reported from heart wood
Isoflavonoid
Prunetin (51) Joshi et al. (1977)
Steroid
β-Sitosterol (86) Joshi et al. (1977)
(f) Phytochemicals reported from roots and its bark
Flavonoids
Baicalein (1) and chrysin (2) Zaveri et al. (2008)
Oroxylin A (3) Ali et al. (1998)
Baicalein 6-O-glucoside ( ¼ tetuin, 8) Dinda et al. (2012)
Isoflavonoid
Biochanin A (52) Zaveri et al. (2008)
Naphthalenoids
Lapachol (57) Ali et al. (1998)
Dehydro iso-α-lapachone (58), 2-(1-hydroxymethylethyl)-4H, 9H-naphtho-[2,3-b]-furan-4,9-dione (59), Kizu et al. (1994)
2-acetylnaphtho [2,3-b]-furan-4, 9-dione (60), (3R,4R)-3,4-dihydro-4-hydroxy-3 (3-hydroxymethyl-(2Z)-
butenyl)-1-(2H)-naphthalenone (61), catalponol (62), (3R,4R)-3,4-dihydro-4-hydroxy-3(3-methyl-2-
butenyl)-1(2H)-naphthalenone (63), (2S,3S,4R)-3,4-dihydro-3,4 dihydroxy-2(3-methyl-2-butenyl)-1(2H)-
napthalenone (64), (2R, 3aS, 9S, 9aR) 9-hydroxy-2-isopropenyl-2,3,9,9a-tetrahydro-3aH-naphtho [2,3-b]-
furan-4-one (65), (2Rn,3aRn,5Sn,9bRn)-2,3,3a,4,5,9b-hexahydro-2-(1-hydroxy-1-methylethyl)-5-naphtho-
[1,2-b]-furanol (66), (2Rn,3aRn,9bRn)-2-(1-hydroxy-1-methyl ethyl)-2,3,3a,9b-tetrahydro-4H-naphtho-
[1,2-b]-furan-5-one (67), [3S, 4aR, 10bR]-2,2-dimethyl-3-hydroxy-3,4,4a,10b-tetrahydro-5H-naphtho [1,2-
b]-pyran-6-one (68), faramol (69) and spiro [(1aS, 2R, 7aS)-2,3-dihydroxy-1a,2,7,7a-tetrahydronaphtho
[2,3-b]-oxirene-7,20 -naphtho-[1,8-de]-10 ,30 -dioxin] (70)
Steroids
β-Sitosterol (86) Ali et al. (1998)
β-Sitosterol glucoside (87) and stigmasterol glucoside (88) Dinda et al. (2012)
Phenolic
Ellagic acid (96) Vasantha et al. (1991)
2.2. Isoflavonoids 2.7. Steroids
Among the isoflavonoids (51–56), five were isolated from stem, β-Sitosterol and its glucoside and stigmasterol glucoside (86–88)
and one (56) was isolated from root bark (Joshi et al., 1977; Ali have been shown to be present in root bark (Dinda et al., 2012). The
et al., 1999; Zaveri et al., 2008). The bioactivity of the isolated iso- antimicrobial and anti-inflammatory activities of β-sitosterol have
flavonoids was not studied. been reported (Ali et al., 1998).
2.3. Naphthalenoids 2.8. Stilbenoids
Among fourteen naphthalene analogues (57–70), lapachol (57) All of the stilbinoids (90–94) have been reported in seeds (Xie
and dehydro-iso-α-lapachone (58) were isolated from stem bark et al., 2014)
(Ali et al., 1998); the remainder were from root bark (Kizu et al.,
1994). Compounds 58 and 61 were the major constituents of the
root bark (Kizu et al., 1994). 2.9. Miscellaneous compounds
Miscellaneous compounds (95–111) of anthraquinone, pheno-

2.4. Phenylethanoids
lic, fatty acids, and alkaloids, among others, have been reported as
minor constituents.
Among the phenylethanoids (71–73), salidroside (71) and
acteoside (73) are the major constituents of fruits (Teshima et al.,
1996).
3. Pharmacological activities
2.5. Cyclohexylethanoids A number of pharmacological studies have been reported in the

literature to justify the indigenous folklore uses of Oroxylum indicum.
Among cyclohexylethanoids (74–82), cornoside (78) was found Table 3 summarizes the pharmacological studies undertaken to
to be a major constituent of fruits (Teshima et al., 1996). investigate the extracts and their pure isolates from different parts
of Oroxylum indicum to support many of the traditional uses of the
2.6. Triterpenoids plant. Some of the listed pharmacological activities (Table 3) may not
relate to the traditional uses of the plant, but they may provide some
Among triterpenoids (83–85), ursolic acid (83) was isolated from insight regarding their potential bioactive role(s) in new areas of
fruits (Roy et al., 2007), and lupeol (84) and 2α-hydroxylupeol (85) application. Some other interesting pharmacological activities of
were isolated from the seeds of the plant (Yan et al., 2011). these compounds that are not discussed in this review have also
Table 3
Summary of pharmacological activities of the extracts/pure isolated compounds from different parts of Oroxylum indicum (L.) Kurz.
Activity tested Extract/ Compound Plant In vitro/ Model Effect Dosage Reference
part in vivo
Antimicrobial EtOH Leaf In vitro Growth inhibition Moderate antibacterial activity 250 μg/ml Phatthalung et al.
against Acinetobacter baumannii (2012)
DCM Stem In vitro Disc diffusion Mild antibacterial and antifungal 100 μg/disc Ali et al. (1998),
bark activity against Bacillus sublitis Houghton et al.
(BS), Staphylococcus aureus (SA), (1997)
Candida albicans (CA),
Pseudomonas aeruginosa (PA)
Isolated baicalein and Stem In vitro Disc diffusion Moderate to strong antibacterial 5.0 μg/disc Ali et al. (1998)
lapachol bark activity against Bacillus subtilis
and Staphylococcus aureus
Isolated chrysin Stem In vitro Disc diffusion Antibacterial and antifungal 5.0 μg/disc Ali et al. (1998)
bark activity against Candida albicans
and Pseudomonas aeruginosa,
which were comparable to that
of standard drugs, nystatin and
streptomycin
EtOH Stem In vitro Disc diffusion Moderate antibacterial activity 50 μl/disc Radhika et al. (2011)
bark of stem bark extract against
and Escherischia coli, Klebsiella spp.,
root Pseudomonas aeruginosa and
Staphylococcus aureus while root
extract exhibited activity against
Proteus spp., and Staphylococcus
aureus
MeOH Stem In vitro Disc diffusion Moderate antibacterial activity 1000 μg/disc Moirangthem et al.
bark against Klebsiella pneumonia, (2013)
Bacillus cereus and antifungal
activity against Aspergillus
fumigates and Macrofomina
phaeolina
Isolated chrysin Stem In vitro Broth dilution Inhibited the growth of Bacillus 25–50 μg/ml SureshBabu et al.
bark subtilis (BS), Bacillus sphaericus, (MIC) (2006)
Staphylococcus aureus, Klebsiella
aerogenes and Chromobacterium
violaceum
DCM Root In vitro Disc diffusion Mild antibacterial and antifungal 100 μg/disc Ali et al. (1998),
activity against BS, SA and CA Houghton et al.
(1997)
Isolated oroxylin A and β- Root In vitro Disc diffusion Significant and moderate 5 μg/ml Ali et al. (1998)
sitosterol bark antibacterial activity against
Bacillus subtilis and
Staphylococcus aureus,
respectively
EtOH and H2O Root In vitro Disc diffusion Moderate antibacterial and 1000 μg/disc Vinod and Kamlesh
bark antifungal activity against (2009)
Escherischia coli, Shigella
dysenteriae, Streptococcus
mutant, Staphylococcus aureus,
Candida albicans and Aspergillus
niger
Anti- DCM Stem In vitro Soya Lipoxygenase 31% and 15.5% inhibition against 83.3 μg/ml Ali et al. (1998)
inflammatory bark inhibition soya 5-lipoxygenase (soya lip)
and with IC50 of 18.9 and 42.4 μg/ml,
root respectively
Isolated baicalein, chrysin and Stem In vitro Lipoxygenase inhibition Inhibited the activity of 0.5 to 10 μl/ml Ali et al. (1998)
lapachol bark 5-lipoxygenase with IC50 value from 8.33 μg/ml
of 1.64, 1.73 and 0.79 μg/ml, stock
respectively
H2O Stem In vitro Release of myeloperoxi- Reduced 64% of MPO release 500 μg/ml Laupattarakasem
bark dase (MPO) from rat et al. (2003)
peritoneal leukocytes
DCM Stem In vitro Luciferase reporter Significantly inhibited NF-κB 10 μg/ml Tran et al. (2014)
bark activation in TNF-α-stimulated
HEK-293 cells
Isolated oroxylin A, chrysin, Stem In vitro Luciferase reporter Potent to weak inhibition of NF- 95% inhibition Tran et al. (2014)
hispidulin and baicalein bark κB activation in TNF-α- in the conc.
stimulated HEK-293 cells with 3.5–4.4, 6.0–8.8,
IC50 of 3.9, 7.2, 9.0 and 28.1 μM,7.9–10.2 and
respectively 24.6–32.0 μM,
respectively
EtOAc Stem In vitro LPS-induced pro- Significantly inhibited the 50–1 μg/ml Siriwatanametanon
bark inflammatory mediators release of PGE2, IL-6, IL-1β, TNF- et al. (2010)
release in human α with IC50 of 26.98, 27.98, 44.12,
monocytes 22.33 μg/ml, respectively
part in vivo
EtOAc Stem In vitro PMA-induced activation Significantly inhibited the 200-0.2 μg/ml Siriwatanametanon
bark of NF-κB in HeLa cells activation of NF-κB with IC50 of et al. (2010)
47.45 μg/ml
H2O Stem In vivo Carrageenan-induced Both the doses of extract 150 and Upaganlawar et al.
bark rats’ paw oedema showed significant (Po 0.05) 300 mg/kg bw (2009)
anti inflammatory activity
Decoction in H2O Stem In vivo Carrageenan-induced Both the decoctions showed 14 ml/kg bw Doshi et al. (2012)
bark paw oedema in rats significant anti-inflammatory
and activity by reducing the volume
root of paw edema by 26.3 and 22.7%,
bark respectively
DCM Root In vitro Leukocyte lipoxygenase 100% inhibition against rat 50 μg/ml Ali et al. (1998)
inhibition leukocytes, 5-lipoxygenase
(LTB4) and cyclooxygenase
(TXB2)
Isolated oroxylin A and β- Root In vitro Lipoxygenase inhibition Strong and weak anti- 0.5 to 10 μl/ml Ali et al. (1998)
sitosterol bark inflammatory activity with IC50 from 8.33 μg/ml
of 1.87 and 2.71 μg/ml, stock
respectively
PE, CHCl3, EtOAc, n-BuOH Root In vivo Carrageenan-induced rat Tested doses of BuOH extract 100 and Zaveri and Jain
bark paw oedema and cotton showed significant anti- 300 mg/kg (2010)
pellet induced granuloma inflammatory activity in both
formation in rats models
Anti-arthritic CHCl3, EtOAc, n-BuOH Root In vivo Adjuvant induced EtOAc extract showed significant 300 mg/kg bw Karnati et al. (2013)
bark arthritis in rats anti-arthritic activity compared
to other extracts
Anticancer EtOH Stem In vitro MTT Strong anti proliferative activity N/S Khan et al. (2002)
bark against leukemia K562 cells
EtOH Stem In vitro MTT Significant cytotoxicity against 2–125 μg/ml for Costa-Lotufo et al.
bark tumor HL-60, CEM, and B-16 72 h (2005)
cells with IC50 of 14.2, 19.6 and
17.2 μg/ml, respectively
EtOH Stem In vitro MTT Significant anti proliferative N/S Lambertini et al.
bark activity against MCF-7 and (2004)
MDA-MB-231 breast cancer cells
PE Stem In vitro MTT and XTT Moderate cytotoxic effect 200–0.2 μg/ml Siriwatanametanon
bark against HeLa and leukaemia et al. (2010)
CCRF-CEM and CEM/ADR 5000
cells with cell viability of 85.61%,
24.35% and 60.37%, respectively
at 10 μg/ml
EtOAc Stem In vitro MTT and XTT Moderate cytotoxicity against 200–0.2 μg/ml Siriwatanametanon
bark HeLa, CCRF-CEM and CEM/ADR et al. (2010)
5000 cells with cell viability of
87.81%, 29.35% and 38.99%,
respectively at 10 μg/ml
MeOH and H2O Stem In vitro Cellular DNA Significant cytotoxicity and 25–400 μg/ml Rajkumar et al.
bark fragmentation and apoptosis of MDA-MB- 435 S, (2011)
ELISA Hep3B and PC-3 cells
PE and CHCl3 Stem In vitro XTT Both PE and CHCl3 extracts at a 12.5-200 μg/ml Naveen Kumar et al.
bark dose of 200 μg/ml exhibited (2012)
significant cytotoxicity against
tumor MDA-MB-231 and non-
tumor WRL-68 cells. Hot PE
extract showed apoptotic
induction in MDA-MB-231 and
MCF-7 cells in a dose-dependent
manner
Isolated baicalein Stem In vitro MTT Completely blocked the 0–50 μM Lalou et al. (2013)
bark proliferation of CT-26 tumor
cells after 5 d with IC50 value of
10 μM
EtOH Stem In vivo Sea urchin eggs Inhibited the egg development 10–1000 μg/ml Costa-Lotufo et al.
bark of sea urchin, Lytechinus (2005)
variegates with IC50 of 13 μg/
ml
EtOAc Stem In vivo Brine shrimp lethality Significant cytotoxic activity 400–0.781 μg/ Asaduzzaman et al.
bark with LC50 of 1.58 μg/ml ml (2011)
MeOH Leaf In vitro MTT Significant cytotoxicity against 20 μg/ml Ong et al. (2009)
HL-60 cells
MeOH Leaf In vitro Methylene blue Significant anti-proliferative 0.39–99 μg/ml Zazali et al. (2013)
effect against HeLa cells with
IC50 of 3.87 μg/ml
MeOH Fruits In vitro MTT Inhibited proliferation of HL-60 N/S Roy et al. (2007)
cells
part in vivo
Isolated baicalein Fruits In vitro MTT Inhibited proliferation of HL-60 25–30 μM Roy et al. (2007)
cells
Antiulcer 50% EtOH, PE and n-BuOH frs. Root In vivo EtOH-induced gastric Significant reduction of gastric 100 and Khandhar et al.
bark ulcer in rats mucosal damage 300 mg/kg bw (2006)
n-BuOH Root In vivo WIRS ulcer model in About 99% inhibition of gastric 100 and Zaveri and Jain
bark rats lesions 300 mg/kg bw (2007)
Hexane and acetone Stem In vivo EtOH-induced ulcer Mild and moderate gastro 100 and Hari Babu et al.
bark (EIU), cold restrain- protective activity in all models 250 mg/kg bw (2010)
induced ulcer (CRU)
pylorus-induced ulcer
(PIU) and aspirin-
induced ulcer (AIU) in
rats
Isolated chrysin Stem In vivo Gastric ulceration in rats Significant gastroprotective 25 mg/kg bw Hari Babu et al.
bark potential in PLU and CRU models (2010)
Isolated oroxylin A Stem In vivo Gastric ulceration in rats Significant gastroprotective 25 mg/kg bw Hari Babu et al.
bark activity in EIU (2010)
Isolated dihydro oroxylin A-7- Stem In vivo Gastric ulceration in rats Strong and moderate 25 mg/kg bw Hari Babu et al.
O-methyl glucuronide and bark gastroprotective activity in PLU, (2010)
5,20 -Dihydroxy-7,60 -dimethoxy CRU, EIU and AIU models
flavone-20 -O-glucoside
Radio- 60% EtOH Fruits In vitro Comet assay of Significant protection of DNA 20–600 μg/ml Thokchom et al.
protective irradiated plasmid against 5 and 10 Gy γ radiation (2014)
PBR322 DNA
60% EtOH Fruits In vivo Comet assay in Significantly reduced radiation 1–2 g/kg bw Thokchom et al.
irradiated rats (1,3 and 5 Gy)-induced DNA (2014)
damage in bone marrow cells of
rats
Immuno- EtOH, n-BuOH fr. Root In vivo Histopatho- logical Enhanced both humoral and 100 mg/kg bw Zaveri et al. (2006)
stimulant bark analysis of lymphoid cell-mediated immune
tissues in rats responses
Powder Root In vivo In broiler chicks against Root bark showed higher 250 mg/kg bw Kumari et al. (2011)
bark ND virus humoral and cell mediated
and immune response than that of
stem stem bark
bark
Anti-diarrheal n-BuOH medium polarity fr. Root In vivo Castor oil and MgSO4- Higher dose significantly 50 and 100 mg/ Joshi et al. (2012)
bark induced diarrhea in reduced the extent of diarrhea in kg bw
mice both models
MeOH Stem In vivo Castor oil- induced Significant anti-diarrheal effect 400 mg/kg bw Asaduzzaman et al.
bark diarrhea in mice by reducing the number of stool (2011)
by 52.17% and prolonging the
onset of diarrheal episode by
61.07 min
Antidiabetic 50% Aq. EtOH Stem In vitro α-Glucosidase inhibition Significant inhibitory activity 0.025–10.0 Singh and Kakkar
bark against α-Glucosidase with IC50 /200 μl (2013)
2.87 μg/ml
50% Aq. EtOH Stem In vitro BSA-glycation inhibition High inhibitory effect against 0.01-5.0 μg/ml Singh and Kakkar
bark AGEs formation with IC50 (2013)
2.10 μg/ml
50% Aq. EtOH Stem In vitro 3T3-L1 mature About 2 fold increase of GLUT-4 15 μg/5 105 Singh and Kakkar
bark adipocytes translocation to elevate glucose cells (2013)
up take in adipocytes
Isolated oroxylin A Stem In vitro Adipogenesis in 3T3-L1 Inhibited adipogenesis, 10–40 μM Singh and Kakkar
bark cells increased lypolysis and induced (2014)
apoptosis in matured 3T3-L1
cells acting as agonist of PPAR-γ
EtOH Stem In vivo STZ-induced diabetic Significant antidiabetic activity 250 mg/kg bw, Singh and Kakkar
bark rats orally (2013)
MeOH and H2O Leaf In vivo Alloxan-induced Significant antidiabetic effect 300 mg/kg bw, Kaldate et al. (2011)
diabetic rats p.o. for 21 d
EtOH and H2O Root In vivo Alloxan and Higher dose (500 mg/kg) 300 and Tamboli et al. (2011)
dexamethasone- exhibited significant antidiabetic 500 mg/kg bw,
induced diabetic rats effect in both models oral
Antigout MeOH Seed In vitro Xanthine oxidase (XO) Significant inhibitory activity 100 mg/ml Li et al. (2014)
inhibition against XO
Isolated baicalein, oroxin A, Seed In vitro Xanthine oxidase (XO) Strong to weak XO inhibitory 20 μl Li et al. (2014)
oroxin B and baicalin inhibition activity with IC50 valu of 71.5,
543.5, 845.4 and 801.3 μM,
respectively
Anti- N/S N/S In vitro Against equine Exhibited 0% hatching of eggs 2 10 1 g/ml Downing (2000)
helminthic strongyle eggs
part in vivo
Hepato- EtOH, PE and n-BuOH Root In vivo CCl4-induced liver Significant hepatoprotective 300 and Zaveri and Jain
protective bark damage in mice and rats activity by lowering the 100 mg/kg bw (2009)
elevated serum enzymes, SGOT, p.o. for 7 d
SGPT, ALP and total bilirubin
levels
H2O Root In vivo Paracetamol- induced Exhibited better 100, 200 and Sastry et al. (2011)
bark liver damage in rats hepatoprotective activity at a 400 mg/kg bw
dose of 400 mg/kg bw compared
to lower doses
EtOH Stem In vivo CCl4-induced liver Significant hepatoprotective 250 and Tripathy et al.
bark damage in rats activity at a dose of 500 mg/kg 500 mg/kg bw (2011)
bw
Aq. MeOH Stem In vivo Acetaminophen induced Significant hepatoprotective 50 and 100 mg/ Bharali et al. (2014)
bark liver injury in rats activity at higher doses by kg bw p.o.
reducing serum ALT, AST and
LPO levels
EtOH, H2O, CHCl3, PE Leaf In vivo CCl4- induced liver Ethanolic extract showed better 300 mg/kg bw Tenpe et al. (2009)
damage in rats hepatoprotective activity than
that of other extracts.
Anti-oxidant EtOAc and MeOH Stem In vitro DPPH and lipid per- EtOAc and MeOH extracts N/S Siriwatanametanon
bark oxidation showed antioxidant activity et al. (2010)
with IC50 of 0.73 and13.39 μg/ml
in DPPH assay; and 0.08 and
1.05 μg/ml in lipid peroxidation
assay, respectively.
EtOH, H2O, PE and CHCl3 Leaf In vitro DPPH, superoxide, nitric All the EtOH, H2O, PE and CHCl3 10–150 mcg/ml Tenpe et al. (2009)
oxide extracts showed antioxidant
activity with IC50 of 18.8, 21.36,
25.25 and 28.08 μg/ml against
DPPH; 4.44, 6.95, 7.4 and
8.12 μg/ml against superoxide;
and 21.64, 23.58, 28.27 and
33.13 μg/ml against nitric oxide,
respectively
H2O Seed In vitro Inhibition of Heinz body Completely inhibited the Heinz 1:20 of extract Palasuwan et al.
and ABTS body formation and showed dilution (2005)
strong antioxidant activity
Isolated baicalein, baicalin, Seed In vitro DPPH Moderate anti-oxidant activity 100 μl Yan et al. (2011)
baicalein-7-O-glucoside, with IC50 value of 51.64, 114.35,
baicalein-7-O-gentiobioside, 101, 139.62, 112.95 and
scutellarein-7-O-glucoside and 136.59 μg/ml, respectively
scutellarein-7-O-gentiobioside
Isolated baicalein, chrysin, Seed In vitro ORAC Strong to weak anti-oxidant 50 μl Yan et al. (2011)
oroxylin A, baicalin, baicalein- activity with 2.15, 0.51, 2.00,
7-O-glucoside, baicalein-7-O- 2.08, 1.34, 0.75, 7.55 abd 6.77 μM
gentiobioside, scutellarein-7- Trolox/μM, respectively
O-glucoside and scutellarein-
7-O-gentiobioside
Nephro- EtOH Root In vivo Cisplatin-induced renal Significant nephroprotective 200 and Sreedevi et al.
protective bark injury in rats activity 400 mg/kg bw (2011a)
Isolated chrysin Root In vivo Cisplatin-induced injury Significant nephroprotective 20 and 40 mg/ Sreedevi et al.
in rats activity at 40 mg/kg bw kg bw (2011b)
Analgesic n-BuOH Root In vivo Tail-flick and acetic- Significant analgesic effect in 100 mg/kg bw Zaveri and Jain
bark induced writhing both models. In tail flick (2010)
response in rats method, the result was
moderate compared to that of
standard drug, morphine
(10 mg/kg bw).
MeOH Stem In vivo Acetic acid-induced Produced 21.36% inhibition of 500 mg/kg bw Asaduzzaman et al.
bark writhing test in mice writhing (2011)
Anticolitis H2O Root In vivo DNBS-induced colitis in Higher dose exhibited 100, 200 and Joshi et al. (2011)
rats significant anti-colitis effect 400 mg/kg bw
Anti-mutagenic MeOH Fruits In vitro Try-P-1-induced Significantly inhibited (91 75%) 138 μg Nakahara et al.
mutagenesis in Ames the mutagenicity (2001)
test
Isolated baicalein Fruits In vitro Ames test Inhibited Trp-P-1-induced 10–1000 nM Nakahara et al.
mutagenesis with IC50 value of (2001)
2.78 μM
Wound-healing MeOH Root In vivo Partial thickness burn Significant wound healing effect 1.0 and 2.5% Singh et al. (2011)
bark wound in mice at the higher dose extract as
ointment
PC inhibitory Isolated baicalein Stem In vitro FPS Inhibited the activity of PC-4 4–30 μM Majumdar et al.
bark enzyme with IC50 value of (2010)
12.2 μM
part in vivo
Isolated baicalein, chrysin and Stem In vitro FPS Inhibited furin activity with IC50 4–30 μM Majumdar et al.
oroxylin A bark value of 13.36, 13.65 and 4.8 μM, (2010)
respectively
Antileish- Baicalein Stem In vitro TBE Inhibited the growth of CPT- 1–15 μM Das et al. (2012)
manial bark resistant Leishmania donovani
with IC50 value of 1.5 μM
Extracts: DCM: Dichloromethane; PE: Petroleum ether; N/S: not stated; bw: body weight; FPS: Fluorogenic peptide substrate; TBE: Trypan blue exclusion.
Flavonoids
1 21
2 22
3
O 4 23
5
O 6
O O
7
O 8
O 9
O
24
10
O- 11 25
O- 12
O- 13
O-
O- 14
O 15
O 16
O 17
O 18
O 19
O 20 26
O- 27
O-di 28
O- 29
30
31
32
33
34
35
36
Fig. 2. Chemical structures of isolated compounds from Oroxylum indicum (L.) Kurz.
been reported during their isolation from other plants or purchase the root showed inhibition against Proteus spp. and Staphylococcus
from pharmaceutical industries. aureus, with inhibition zones of 20 and 14 mm, respectively (Radhika
et al., 2011).
3.1. Antimicrobial activity The EE of the leaf demonstrated a moderate antibacterial effect
against the nosocomial pathogen Acinetobacter baumannii, with a
Dichloromethane extracts of both stem bark and root showed growth inhibition of 67.1871.59%, but it had no synergistic effect in
antimicrobial activities against Gram-positive (Bacillus subtilis, Sta- the presence of the antibiotic novobiocin (Phatthalung et al., 2012).
phylococcus aureus) and Gram-negative (Pseudomonas aeruginosa) These results provide comprehensive insight into the tradi-
bacteria and fungus, such as Candida albicans in the disc diffusion tional uses of this plant for the treatment of wound healing,
assay. Among the compounds that have been isolated from these dysentery, bronchitis and gynecological inflammation.
extracts, lapachol (57) and chrysin (2) showed potent antibacterial
and antifungal activities (Ali et al., 1998). The ethanolic and aqueous 3.2. Anti-inflammatory activity
root bark extracts exhibited significant antibacterial and antifungal
activities (Vinod and Kamlesh, 2009). The CH2Cl2 extracts of stem bark and root exhibited significant
The EtOH extract (EE) of stem bark exhibited significant anti- anti-inflammatory activity. Among the isolated compounds from
bacterial activity against Escherichia coli, Klebsiella spp., Proteus spp., the root, lapachol (57) showed strong activity against soya
Pseudomonas aeruginosa and Staphylococcus aureus, with inhibition 5-lipoxygenase that was almost equivalent to that of the positive
zones of 20, 15, 18, 18 and 20 mm, respectively. In contrast, the EE of control fisetin (IC50, 0.97 μg/ml). This anti-inflammatory effect of
60
59
R R R S R R
67 68
R R 62
Z
61 69
S R S
70
S S R Phenylethanoids
R R
63 64
71
72
73
R S S R R R S R
65 66
Fig. 2. (continued)
e Cyclohexylethanoids g Steroids
74 86
75 87
76 88
77
78
89
h Stilbenoids
80
79 81
82
f Triterpenoids
E
O 90
E
O 91
83
84 E O 92 94
85 93
Fig. 2. (continued)
Others Others
95 95
96 96
p 97 p 97
98 98
99 104 99 104
100 105 100 105
101 106 101 106
102 102
103 103
107 107
108 108
110 110
111 111
109 109
Fig. 2. (continued) Fig. 2. (continued)
the root extract was mainly due to the lapachol content (Ali et al., anti-inflammatory activity at 5 h. It could be possible that the extract
1998). inhibited the release of a PGE2-like pro-inflammatory mediator
Among the tested aqueous and alcoholic extracts of the stem bark, (Upaganlawar et al., 2009). The anti-inflammatory activities of petro-
the aqueous extract showed significant in vitro anti-inflammatory leum ether, ethyl acetate and methanol extracts of stem bark during
activity by reducing ( 64%) the release of myeloperoxidase from rat the LPS-induced release of pro-inflammatory mediators in human
peritoneal leukocytes (Laupattarakasem et al., 2003). monocytes was assayed by ELISA and EIA kits using hydrocortisone as a
The anti-inflammatory activity of the aqueous extract of stem bark standard reference. The EtOAc extract was found to be more effective.
was also evaluated in a carrageenan-induced rat paw edema model This EtOAc extract showed a potent NF-kB inhibitory effect on phorbol
using diclofenac sodium as the standard drug. Among the tested doses myristate acetate (PMA)-induced-activation of NF-kB in HeLa cells by
of 150 and 300 mg/kg bw, the higher dose demonstrated a maximum the luciferase assay. The phytochemicals baicalein, oroxylin A, chrysin
and lapachol, which are present in this extract, might have been Petroleum ether (hot and cold) and CHCl3 (hot and cold) extracts of
responsible for this effect (Siriwatanametanon et al., 2010). the stem bark showed cytotoxicity against MDA-MB-231 and WRL-68
Aqueous decoction (14 ml/kg p.o. for 5 d) of both stem bark and cells in the XTT assay. All of the extracts, particularly the petroleum
root bark produced anti-inflammatory activity by reducing paw ether hot extract (PEH), exhibited significantly (Po0.05) higher
edema by 26.30 and 22.70%, respectively, after 3 h of carrageenan cytotoxicity in MDA-MB-231 cells. PEH induced apoptosis in estrogen
induction in the rat hind paw. The decoction was prepared by mixing receptor (ER)-negative MDA-MB-231 cells, and it also exhibited anti-
1 part of bark powder with 16 parts of water and reducing the metastatic potential in the tumor cell migration inhibition assay. This
volume to 1/8th by boiling and filtering through a clean cloth (Doshi extract could be used to alleviate ER-negative breast cancer progres-
et al., 2012). sion in advanced stages of malignancy (Naveen Kumar et al., 2012).
The dichloromethane extract of the stem bark showed strong Both methanolic and aqueous extracts of the stem bark were cytotoxic
anti-inflammatory activity by inhibiting TNF-α-induced NF-kB acti- against MDA-MB-435S, Hep3B and PC-3 cells and induced apoptosis of
vation in HEK-293 cells. Among the isolated chemicals from the DCM cancer cells (Rajkumar et al., 2011). The EtOAc extract of the stem bark
and EtOAc extracts of the stem bark, Oroxylin A, hispidulin, chrysin in the brine shrimp lethality bioassay exhibited promising in vivo
and baicalein showed significant NF-kB inhibitory activities (Tran cytotoxic effects that were comparable to those of the standard drug
et al., 2014). vincristine sulfate (LC50 ¼0.419 μg/ml) (Asaduzzaman et al., 2011).
The anti-inflammatory activities of petroleum ether, chloroform These findings suggested a traditional use for Oroxylum indicum in
and ethyl acetate extracts at 300 mg/kg bw p.o. and of n-butanol the treatment of cancer and jaundice.
extract at 100 and 300 mg/kg bw p.o. from root bark against
carrageenan-induced paw edema and cotton pellet-induced granu- 3.5. Anti-ulcer activity
loma formation in rats were evaluated. Pretreatment with n-butanol
extract showed significant (Po0.05) anti-inflammatory activity by The 50% alcoholic extract (300 mg/kg bw) of the root bark and its
reducing edema formation at 3 h when compared with the control petroleum ether and n-butanol fractions (100 and 300 mg/kg bw)
group in the carrageenan-induced paw edema model. In the cotton demonstrated significant inhibition of gastric lesions caused by
pellet model, butanol extract at a dose of 100 mg/kg bw inhibited ethanol-induced gastric mucosal damage in rats. The results were
granuloma formation by 52%, which is comparable to the 59% comparable with those of the standard reference drug omiprazole.
inhibition provided by treatment with the standard reference diclo- Both of these active fractions at a dose of 100 mg/kg bw showed
fenac sodium (5 mg/kg). The baicalein (1) present in the butanol significant reduction of the ulcer index in a pylorus-ligated ulcer
extract might have been responsible for this inflammatory activity of (PLU) model in rats. Both the petroleum ether and butanol fractions
the extract (Zaveri and Jain, 2010). contained baicalein (1) as a major chemical constituent. These active
All of these results supported the traditional use of the plant in fractions were found to exhibit significant antioxidant activities.
rheumatic pain and other inflammatory diseases. These antioxidant activities of the fractions might have been related
to gastric cytoprotection (Khandhar et al., 2006).
3.3. Anti-arthritic activity The hexane and acetone extracts of the stem bark showed mild to
moderate gastroprotective activity in pylorus ligation-induced ulcera-
The CHCl3, EtOAc and n-BuOH extracts of the root bark (300 mg/kg tion (PLU), cold-restraint-induced ulceration (CRU), ethanol-induced
bw) exhibited anti-arthritic activity in Freund’s complete adjuvant- ulceration (ERU) and aspirin-induced ulceration (AIU) models in rats
induced arthritis in rats. The anti-arthritic activity of the extracts (Table 3). Some pure compounds isolated from these extracts showed
followed the order EtOAc4CHCl3 4n-BuOH, with an inhibition of the different degrees of gastroprotective potentials. Among them, chrysin
paw volume of 67.69, 64.61 and 58.46%, respectively. Hematological (2) displayed better activity in PLU and CRU models; dihydrooroxylin
parameters such as RBC counts and hemoglobin content demon- A-7-O-methyl glucuronide (43) and 5,20 -dihydroxy-7,60 -dimethoxyfla-
strated a significant increase, while there was a significant decrease in vone-20 -O-glucoside (39) also showed significant activity in all four of
the total WBC count and ESR in all of the groups of animals that were the tested models (Table 3) (Hari Babu et al., 2010; Madhusudana Rao
pretreated with the extracts. Biochemical components such as catalase et al., 2010). These results justified the traditional use of the bark and
and glutathione showed a significant increase, while lipid peroxidase root of the plant for the treatment of gastric ulcers and mouth cancer.
(LPO) and cathepsin D decreased significantly in EtOAc extract-pret-
reated rats in comparison to the other extracts (Karnati et al., 2013). 3.6. Radioprotective activity
3.4. Anticancer/anti-tumor activity Among the tested doses (20–600 μg/ml) of a 60% EtOH extract of
the fruits, 200 μg/ml was most effective in protecting pBR322 DNA
The methanolic fruit extract also caused in vitro proliferation of HL- against radiation-induced damage, reducing damage caused by
60 cells (Table 3) (Roy et al., 2007). The flavonoid baicalein (1) was 5 and 10 Gy gamma (γ)-radiation by 79.72 and 71.84%, respectively.
found to be an active compound in the methanolic fruit extract. It The 60% EtOH extract (1–2 g/kg bw) of the fruits showed a
showed significant cytotoxicity against HL-60 cells and induced the significant in vivo protective effect against DNA damage due to
apoptosis of tumor cells at a higher dose (Table 3) (Roy et al., 2007). radiation in rat bone marrow cells in response to gamma (γ) ray
The ethanolic extract of the stem bark exhibited significant in vitro (1, 3 and 5 Gy) irradiation of rats as observed by a reduction of the
cytotoxicity against tumor cells, HL-60, CEM, HCT-8 and B-16 in the tail DNA and tail lengths of comets in the comet assay. The higher
MTT assay (Costa-Lotufo et al., 2005). Baicalein isolated from the stem extract dose provided more effective results (Thokchom et al., 2014).
bark also exhibited potent antitumorgenic effects on colorectal carci-
noma CT-26 cells by inhibiting proliferation and migration ( 70%). 3.7. Immunostimulant activity
This cell migration effect was less pronounced with breast cancer
MDA-MB-231 cells. Baicalein (1) also blocked the furin-mediated The n-butanol fraction of the root bark exhibited immunostimulant
cleavage of pro-h-VEGF-C proteins in CT-26 tumor cells more effi- activity in rats, as indicated by an increase in the humoral and
ciently than the other isolated flavonoids, oroxylin A (3) and chrysin delayed-type hypersensitivity (DTH) response to sheep red blood cells
(2). Baicalein is a major flavonoid constituent of both stem bark and (SRBC). Histopathological analysis of serum antioxidant enzymes and
fruits of the plant, and it may represent a new molecule for further lymphoid tissues revealed reductions of GSH and MDA, elevations of
exploration as a potential herbal antitumor agent (Lalou et al., 2013). SOD and CAT levels and an increase in cellularity, namely, T-lymp-
hocytes and sinusoids. In a triple antigen-mediated immunological cholesterol, protein, urea and creatinine levels in the extract-treated
edema model, the extent of edema in extract-treated rats was greater group of rats. The MeOH extract demonstrated a more significant
compared to that in control rats. These results confirmed the enh- antidiabetic effect compared to the aqueous extract (Kaldate et al.,
anced DTH reactions in response to drug treatment. All of these 2011).
findings suggested that the extract enhanced both humoral and cell- The 50% aqueous-ethanolic extract of the stem bark showed a
mediated immune responses in rats (Zaveri et al., 2006). significant, strong in vitro antidiabetic effect by inhibiting the acti-
The stem bark and root bark powder exhibited significant vities of α-glucosidase, bovine serum albumin (BSA) glycation, and
humoral and cell-mediated immune responses in broiler chicks. insulin-sensitive potential in GLUT-4 translocation studies in mature
The effect of root bark was better than that of stem bark, and it was 3T3-L1 adipocyte cells. The in vitro anti-diabetic findings were
comparable to that of the reference drug levamisole (10 mg/kg bw). further confirmed by the in vivo effect observed in STZ-induced
The humoral response of the birds was measured by monitoring the diabetic rats by administration of the extract for 28 d and analysis of
antibody status of the birds against Ranikhet disease (also known as its glucose-lowering capacity, normalized antioxidant status (AGTS
Newcastle disease, ND) virus in the mean hemagglutination inhibi- and FRAP assay), reduction of liver biomarker enzymes, total choles-
tion (MHI) test after vaccination of the birds with ND virus on the terol and HDL levels and restoration of glycated hemoglobin protein
7th and 28th d. Cell-mediated immune responses were studied as well as enhanced insulin sensitivity (Po0.01) in response to
after sensitization of the chicks with 2,4-dinitrofluorobenzene GLUT-4 translocation in skeletal muscles. Baicalein (1), chrysin (2)
(DNFB) at a dose of 0.25 ml (10 mg/ml) on the 28th d at 0, 6, 24, and baicalin (5) were the major flavonoids present in the extract
48 and 72 h. The cell-mediated immune response was assayed by (Singh and Kakkar, 2013).
measuring the mean skin thickness (MST) of the birds (Kumari Oroxylin A (3) isolated from the stem bark exhibited an antidia-
et al., 2011). betic effect in vitro by inhibiting adipogenesis, increasing lipolysis
and inducing apoptosis in mature 3T3-L1 cells. Oroxylin A (10 μM)
3.8. Anti-diarrheal activity suppressed intracellular lipid accumulation by 42% in maturing pre-
adipocytes. It served as an antagonist of PPAR-γ by decreasing its
A medium polarity fraction of butanol extract of the root nuclear translocation and inducing apoptosis via the mRNA expres-
exhibited significant in vivo antidiarrheal activity in castor oil and sion of FAS, LPL and adiponectin secretion. In mature adipocytes,
magnesium sulfate-induced diarrhea models in mice. At the higher oroxylin A at a concentration of 40 μM decreased cell viability to 30%
dose, the fraction protected 50% of the mice against diarrhea in a of the control. These findings suggested that oroxylin A may have
castor oil-induced diarrhea model and reduced the total number of exerted an anti-obesity effect by affecting the life-cycle of adipocytes
feces and wet feces in a magnesium sulfate-induced model in a at critical points of differentiation and maturity. It demonstrated a
comparable manner to that of the positive control loperamide. The superior anti-obesity effect than that of morin, kaempferol and
in vitro study using isolated rabbit ileum to assess acetyl chlorine- naringenin (Singh and Kakkar, 2014).
induced contractions in the presence of Tyrode’s solution revealed
an inhibitory effect on contraction. Such contractions were not 3.10. Anti-gout activity
observed in presence of the antagonist verapamil (blocker of L-type
Ca2 þ channels). These results indicated that the extract directly The methanolic extract of the seeds collected from Foshan, China
inhibited intestinal mobility involving modification of L-type Ca2 þ exhibited significant anti-gout activity in an in vitro xanthine oxi-
channels (Joshi et al., 2012). The MeOH extract of the stem bark also dase (XO) inhibition assay using column-switching liquid chroma-
showed significant in vivo anti-diarrheal activity by reducing the tography with a diode array detection system. Allopurinol was used
number of stools and prolonging the onset of diarrheal episodes as a primary XO inhibitor. Among the chemical constituents of the
(61.0773.67 min) in a castor oil-induced diarrhea model in mice. MeOH extract, baicalein demonstrated stronger activity than allo-
The result was comparable to that of the standard drug loperamide purinol (IC50, 258.3 μM), while baicalin and oroxins A and B showed
(66.67 μg/kg bw), which resulted in a 40.58% inhibition of stool and weaker activities (Li et al., 2014).
onset of diarrheal episodes (60.071.58 min) (Asaduzzaman et al.,
2011). These results supported the indigenous use of this plant for 3.11. Anthelminthic activity
the treatment of diarrhea in patients with inflammatory bowel
disease. The anthelminthic activity of the plant extract was compared to
that of the de-worming agent ivermectin (2 10 1g/ml) (Downing,
3.9. Antidiabetic activity 2000).
The aqueous and ethanolic extracts of the roots were effective for 3.12. Hepatoprotective activity
the reduction of elevated serum glucose levels in alloxan-induced
diabetic rats. Treatment with aqueous and ethanolic extracts in The hepatoprotective activities of petroleum ether, chloroform
alloxan-induced diabetic rats at a dose of 500 mg/kg bw for 21 d and methanolic extracts of the stem bark were also evaluated against
reduced serum glucose by 50.92 and 49.59%, respectively. The serum CCl4-induced liver damage in mice using silymarin as positive
triglyceride level was not significantly reduced in response to the control. The results indicated that the methanolic extract at a dose
EtOH extract alone. Both of these aqueous and ethanolic extracts of 500 mg/kg bw showed significant hepatoprotective activity, which
were also effective in reducing the levels of glucose, triglycerides and was comparable to that of silymarin (25 mg/kg bw) (Tripathy et al.,
total cholesterol in dexamethasone-induced insulin resistance in rats. 2011). The aqueous methanolic extract of the stem bark (100 mg/kg,
Continuous treatment of aqueous and ethanolic extracts with a dose p.o.) exhibited significant hepatoprotective activity by protecting
of 500 mg/kg for 10 d in dexamethasone-induced rats reduced the hepatic tissues against acetaminophen (1000 mg/kg, p.o.)-induced
serum glucose levels by 17.63 and 16.02%, respectively (Tamboli et al., liver injury in rats after 24 h by reducing ALT and AST levels by
2011). These results justified, to some extent, the traditional use of approximately 50% compared to the control group of rats (Bharali
the plant in the treatment of diabetes. et al., 2014).
The MeOH and aqueous extracts of the leaves induced an The hepatoprotective activity of petroleum ether, chloroform,
antidiabetic effect in alloxan (120 mg/kg bw, i.p.)-induced diabetic ethanol and aqueous extracts of the leaves against CCl4-induced
rats by normalizing the SGOT, SGPT, SALP, serum triglyceride, total liver injury in rats was also evaluated. All of the extracts showed
significant protection against hepatic injury by normalizing the erythrocytes and in ABTS radical scavenging assays (Palasuwan
levels of the serum marker enzymes SGOT, SGPT and ALP. The et al., 2005).
ethanol extract demonstrated better protection compared to the Yan et al. (2011) isolated several flavonoids from the aqueous
other extracts. All of the extracts exhibited significant antioxidant ethanolic extract of the seeds and evaluated their antioxidant acti-
activities by scavenging DPPH, nitric oxide, superoxide and hydroxyl vities using DPPH and ORAC assays (Table 3). Among the isolated
radicals. The hepatoprotective effect of these extracts might have flavonoids, scutellarein-7-O-gentiobioside (28) and scutellarein-7-O-
been due to the scavenging of free radicals and the induction of glucoside (27) were the strongest antioxidants, demonstrating even
microsomal enzymes via the inhibition of lipid peroxidation caused stronger activity than the reference compound quercetin. A com-
by CCl4 (Tenpe et al., 2009). parative study of antioxidant activities indicated that the hydroxyl
The 50% EtOH, petroleum ether and n-BuOH extracts of the root group at the C-6 position improved antioxidant activity and glyco-
bark exhibited significant hepatoprotective activity in rats with sylation of 7-OH greatly reduced activity. The antioxidant activities of
CCl4-induced toxicity by increasing lipid peroxidase (LPO) and the tested flavonoids differed in the two assays, which might have
decreasing antioxidant enzymes levels of SOD, CAT and GSH. been due to the different mechanisms involved in these assays: hyd-
Maximum protection was observed with n-BuOH extract at a dose rogen atom versus electron transfer in the ORAC and DPPH assays,
of 300 mg/kg. The significant antioxidant activity of the extracts respectively. Oxidative stress plays a key role in respiratory diseases.
was responsible for the hepatoprotective activity. Baicalein (1), a The presence of antioxidant flavonoids in seeds might confirm the
major constituent of the BuOH extract, was responsible for the traditional use of seeds in the treatment of respiratory diseases.
increased hepatoprotective activity of this extract (Niedworok
et al., 1999; Zaveri and Jain, 2009). 3.14. Nephroprotective activity
The aqueous extract of the root bark exhibited hepatoprotective
activity in paracetamol-induced liver injury in rats in a dose The nephroprotective activity of the ethanolic extract of the
dependent manner. The extract at a dose of 400 mg/kg bw showed roots was evaluated against cisplatin-induced renal injury in rats.
significant hepatoprotective activity by reducing serum enzyme The administration of the extract to rats injured renaly by treatment
levels and total bilirubin content similarly to that of the standard with cisplatin (6 mg/kg bw, i.p.)- significantly restored to normal
drug silymarin (25 mg/kg bw) (Sastry et al., 2011). levels all of the parameters assessed, such as blood urine nitrogen
These pharmacological studies validated the traditional use of (BUN), serum creatinine, urinary total proteins and LPO. Histo-
the plant for the treatment of jaundice. pathological studies substantiated the results. The higher dose was
more effective (Sreedevi et al., 2011a). The administration of
isolated chrysin (20 and 40 mg/kg from roots) in rats with cisplatin
3.13. Antioxidant activity (6 mg/kg)-induced toxicity demonstrated a significant attenuation
of nephrotoxicity by lowering BUN and LPO levels and increasing
The in vitro antioxidant activity of petroleum ether (PE), chloro- the creatinine clearance level. The higher dose was more effective
form (CE), ethanolic (EE) and aqueous extracts (WE) of the leaves (Sreedevi et al., 2011b). This nephroprotective activity of the root
was evaluated in DPPH, nitric oxide, hydroxyl radical and Fe þ 3- extracts justified to some extent the indigenous use of roots for the
reducing power assays. Among these extracts, EE showed better treatment pf urinary disorders by the tribal people of the Chittor
antioxidant activity in all of the assays. In the hydroxyl radical district of Andhra Pradesh, India (Sreedevi et al., 2011a).
scavenging assay, vitamin E served as the positive control. The IC50
values for vitamin E, EE, WE, PE and CE were 12.34, 16.44, 20.53, 3.15. Analgesic activity
23.31 and 24.57 μg/ml, respectively. In the reducing power assay,
BHT was used as the standard. The reducing power of the standard The butanol extract of the root bark exhibited significant ana-
and the extracts were in the following order: BHT4EE4WE4- lgesic effects in vivo in both the tail flick and acetic acid-induced
PE4CE. In the DPPH radical scavenging assay, ascorbic acid (ASC) writing response models in rats. In the tail flick method, the extract
was used as the standard. The antioxidant efficacy of the ethanolic significantly prolonged the tail flick reaction time in rats. In the acetic
extract (EE) was comparable to that of ASC, demonstrating IC50 acid-induced writhing response method, the extract at the tested
values of 16.6 and 18.8 μg/ml, respectively. In the superoxide radical dose significantly reduced the amount of writhing by 75.93% com-
scavenging assay, curcumin served as the positive control and pared to the positive control aspirin (87.05% reduction) in 30 min
showed an IC50 value of 3.32 μg/ml. In the nitric oxide radical (Zaveri and Jain, 2010). The MeOH extract of the stem bark demon-
scavenging assay, rutin was used as the standard reference and had strated a considerable analgesic effect in vivo (Po0.05) in the acetic
an IC50 value of 18.38 μg/ml. The antioxidant activity of the acid-induced writhing test in Swiss albino mice (Asaduzzaman et al.,
ethanolic extract (IC50, 21.64 μg/ml) was comparable to that of 2011). This analgesic effect supported the indigenous use of the plant
rutin. The antioxidant activities of the leaf extracts might have been for the treatment of headache.
due to the presence of flavonoids and other phenolics. This anti-
oxidant efficacy of the leaf extracts partially justified its traditional 3.16. Anticolitis activity
use in rheumatic pain (Tenpe et al., 2009).
The antioxidant activity of petroleum ether, ethyl acetate and The aqueous extract of the root bark exhibited a significant anti-
methanol extracts of the stem bark was evaluated in DPPH and colitis effect in DNBS-induced colonic inflammation and injury in
lipid-peroxidation assays. In the DPPH assay, ethyl acetate extract rats. The colonic inflammation and injury induced by dinitroben-
demonstrated the highest radical scavenging activity with an IC50 zene sulfonic acid (DNBS) was reduced significantly by the extract
value of 0.73 μg/ml, which was comparable to that of the positive in a dose-dependent manner. The rats were treated with the extract
control trolox (IC50, 0.31 μg/ml). In the lipid-peroxidation assay, (400 mg/kg bw, p.o.) for 7 d prior to induction of colitis (DNBS,
both the ethyl acetate and methanolic extracts demonstrated 25 mg/rat) and then for another 4 d. The results demonstrated a
potent inhibition of lipid-peroxidation (IC50, 0.08 and 1.05 μg/ml, significant reduction of colonic mucosal damage, as evidenced by a
respectively) that was comparable to that of the standard refer- reduction of the gross area of damage, gain in colon and spleen
ence quercetin (IC50, 0.13 μg/ml) (Siriwatanametanon et al., 2010). weights and the reduction of MPO release and MDA, GSH and nitric
The aqueous extract of the seeds exhibited strong in vitro oxide levels (Joshi et al., 2011). These findings justified the tradi-
antioxidant activity by inhibiting Heinz body formation in tional use of the plant in the treatment of bowel disease problems.
3.17. Antimutagenic activity 4. Toxicity studies
The methanolic extract of the fruits exhibited significant anti- Several research groups have evaluated the acute oral toxicity of
mutagenic activity against the food-derived mutagen Trp-P-1 using extracts of Oroxylum indicum in rat models. When aqueous extract
the Ames pre-incubation method. Baicalein, the major constituent of the root bark is fed to overnight-fasted Wistar rats at doses
of the MeOH extract, demonstrated anti-mutagenic activity in a ranging from 175 to 5000 mg/kg bw, no mortality was observed
dose-dependent manner (Nakahara et al., 2001). This result sug- (Joshi et al., 2011). The feeding of both aqueous and ethanolic
gested that the consumption of Oroxylum indicum fruits in a veg- extracts of the roots at a dose of 5 g/kg bw in overnight-fasted rats
etarian diet would be beneficial for overcoming the mutagenic did not result in any behavioral changes (Tamboli et al., 2011). Oral
effects of heterocyclic amines. These findings confirmed the bene- administration of a fraction of the butanol extract of the root bark at
ficial effects of the consumption of fresh flowers, young shoots and graded doses of 175 mg–2000 mg/kg bw in rats for 14 days did not
stem bark as a side dish in Java (Rasadah, 2001). cause any mortality or behavioral changes (Joshi et al., 2012). Oral
administration of aqueous and ethanolic extracts of Oroxylum
indicum stem bark at graded doses of 5 mg–3000 mg/kg bw in rats
3.18. Wound-healing activity for a period of 72 h did not produce any behavioral changes or
mortality (Tripathy et al., 2011).
The methanolic extract of the root bark exhibited wound-healing In the long-term toxicity test, normal and diabetic rats received
activity in partial thickness burn wounds in mice. Among the two methanolic and aqueous extracts of the leaves orally at a dose of
tested ointment doses containing 1% and 2.5% methanolic extract, 300 mg/kg bw for 28 consecutive days, and no signs of toxicity were
the latter dose was effective in wound healing after treatment for observed in the biochemical blood test or in hematological parameters
20 d based on an improvement in the wound contraction rate, epit- (Kaldate et al., 2011). Similarly, oral administration of a 50% aqueous
helization time and hydroxyproline content. Silver sulfadiazine and ethanol extract of the stem bark at a dose of 250 mg/kg bw for 28 days
chlorhexidine gluconate cream was used as the standard drug for in normal and diabetic rats did not affect the hematological and
comparison (Singh et al., 2011). clinical parameters, suggesting that the extract was safe (Singh and
Kakkar, 2013). In another experiment, a 60% ethanol extract of the
3.19. Proprotein convertase inhibitory activity fruits was administered intra-peritoneally to Albino rats at a dosage of
2.5, 3.0, 3.5, 4.0 and 4.5 g/kg bw, and the animals were maintained
Proprotein convertases (PCs) are also known as Proprotein Con- under constant observation for 30 days. Mortality was recorded every
vertase Subtilisin/Kexins (PCSKs). Structurally, PCSKs are Ca2 þ - 24 h. The LD50 (72 h) was 4.02 g/kg bw, and the maximum tolerated
dependent serine endoproteases that are related to bacterial sub- dose (MTD) was 2.25 g/kg bw (Thokchom et al., 2014).
tilisin and yeast kexin and play major roles in the processing of Therefore, both aqueous and ethanolic extracts of stem bark,
inactive precursor proteins to their bioactive matured proteins that root bark and fruits are safe for oral administration in traditional
are involved in a wide variety of diseases such as cancer and viral and systems.
bacterial infections. Among some PC enzymes, furin is a key member.
Four isolated flavonoids from stem bark, such as baicalein (1),
oroxylin A (3), chrysin (2) and oroxylin A-7-O-glucoside (17), have 5. Clinical trials
shown in vitro PC inhibitory activity against the fluorogenic peptide
substrate Boc-RVRR-MCA (Boc¼tert-butyloxy carbonyl, MCA¼4- To date, no human clinical trials of either crude extract or
methyl coumarin-7-amide). A comparative analysis of the inhibition isolated chemical constituents of Oroxylum indicum have been
against furin and other PC enzymes, PC4, PC5 and PC7 suggested a reported in the literature.
partial selectivity toward PC4 by these flavonoid. These flavonoids
also efficiently blocked the PC4 enzyme-mediated processing of a
fluorogenic peptide derived from the processing site of its substrate 6. Discussion
pro-insulin-growth-factor-1 (ProIGF-1). Among the four tested flavo-
noids (1–3, 17) against furin, oroxylin A, baicalein and chrysin were Historically, Oroxylum indicum (L.) Kurz has been used as an
potent furin inhibitors, with measured competitive inhibition con- important medicinal plant in a number of Asian countries for
stant Ki values of 5.070.04, 26.7570.95 and 34.9170.15 μM, centuries and is frequently used in India and China for the treatment
respectively. This was the first report of the anti-PC activity of of a variety of diseases in the traditional system. For their nutraceu-
flavonoids (Majumdar et al., 2010). This anti-PC activity of flavonoids tical potential, throughout Southeast Asia, there is a high consump-
supports the traditional choice of the plant for the treatment of tion of the cooked flowers, buds and young pods as an esteemed
cancer, bronchitis, and pharyngitis. vegetable (Rasadah, 2001).
The presence of high amounts of crude protein, ash, crude fiber,
carbohydrates (8.45, 4.11, 18.89 and 67.49 g/100 g, respectively)
3.20. Anti-leishmanial activity and total dietary fiber (42.45%) in beko (Oroxylum indicum) pod
flour supports its use as a basic raw material for the development
Baicalein (1) isolated from the stem bark showed anti-leishmanial of new functional food ingredients (Bhat et al., 2014).
activity against camptothecin (CPT)-resistant Leishmania donovani Table 1 shows that most of the important traditional uses of
promastigotes (Das et al., 2006). Baicalein was found to be a potent stem bark and root bark are for the treatment of jaundice, heart
topoisomerase IB inhibitor of the parasite Leishmania donovani, problems, gastric ulcers, diarrhea, dysentery and cancers, seeds for
producing topoisomerase IB-DNA complex and causing apoptosis of respiratory disorders, leaves for enlarged spleen and ulcer, and
the parasite via caspase-independant activation of endonuclease G fruits as anthelmintic and for respiratory diseases. Flavonoids and
(LdEndoG) followed by its translocation from mitochondria to the other phenolics are the major constituents of the different parts of
nucleus to form separate complexes with LdFEN-1 and LdTatD for the plant. The main compounds isolated from stem bark and root
DNA fragmentation (BoseDasgupta et al., 2008). This result sugges- are flavonoids such as baicalein, oroxylin A, chrysin and baicalin,
ted that the plant extract could be useful for the treatment of naphthoquinone-lapachol and the phenolic ellagic acid. Among
leishmaniasis. them, baicalein (1) is most abundant in both stem bark and root
bark (Ali et al., 1998; Dinda et al., 2007). Baicalein (1) is also present standards (MRS) and single reference standard (SRS). The results
as a major constituent of leaves and fruits (Subramanian and Nair, indicated that there were no statistically significant differences by
1972a; Teshima et al., 1996; Yuan et al., 2008). In seeds, baicalin (5) the T-test in the seven bioactive flavonoids, chrysin, baicalein,
and some other glycosides of baicalein and chrysin are present in baicalin, baicalein 7-O-glucoside, chrysin 7-O-glucuronide, chrysin
large quantities (Yan et al., 2011). 7-O-gentiobioside and baicalein 7-O-gentiobioside (P40.05),
The antibacterial and antidiarrheal activities of stem-bark and demonstrating that this method can be applied to other ethnome-
root bark extracts justified the associated traditional claims in the dicinal preparations (Cao et al., 2013). Adulteration of the Indian
treatment of diarrhea and dysentery (Ali et al., 1998; Joshi et al., Ayurvedic preparation: ‘Dasamula’ was detected in the molecular
2012). The hepatoprotective activities of the alcoholic and aqueous identification method via the extraction of the DNA of constituent
extracts of stem bark and root bark support the traditional use of the medicinal plants followed by the polymerase chain reaction-
plant parts in the treatment of jaundice (Zaveri and Jain, 2009; Sastry restriction fragment length polymorphism (PCR-RFLP) technique
et al., 2011; Tripathy et al., 2011). The acetone extract of the stem bark (Biswas and Biswas, 2013). Pesticide residue analysis of ‘Dasamoola’
exhibited significant gastroprotective activity against various gastric collected from different places in India indicated the presence of α-
ulceration models in Wistar rats, justifying the traditional use of the and γ-isomers of hexachlorocyclohexane as pesticide residues in
stem bark for the treatment of ulcers. The isolated flavonoids from 97.5% of the samples (Rai et al., 2008).
this acetone extract, such as baicalein (1), chrysin (2) and others The pharmacological data described in this review only showed
flavonoids, exhibited significant anti-ulcer activity against gastric a particular activity of the extract of a plant part. Some of the
mucosal lesions induced by ethanol, cold stress, aspirin and pylorus extracts differed from the original ethnomedicinal preparations.
ligation, at a dose of 25 mg/kg bw (Madhusudana Rao et al., 2010; Furthermore, they did not show any safety and quality features of
Hari Babu et al., 2011). Lapachol (57) isolated from the roots exhibited the ethnomedicinal preparations. Thus, additional analytical and
significant anti-inflammatory activity against soya 5-lipoxygenase clinical studies must be conducted to validate the safety and
with an IC50 of 0.79 μg/ml (Ali et al., 1998). Interestingly, flavonoids quality assurance of the ethnomedicinal preparations of this plant.
isolated from the stem bark, such as oroxylin A (3), baicalein (1) and
chrysin (2), exhibited significant antiprotease activity against furin
and other PC enzymes, which have active roles in the growth of 7. Conclusion
cancer and in viral and bacterial infections in the human body
(Majumdar et al., 2010). Baicalein (1) was found to exhibit anti- As described in this review, the promising pharmacological
proliferative activity against cancer HL-60 and CT-26 cells (Roy et al., properties of Oroxylum indicum (L.) Kurz may be recognized fully
2007, Lalou et al., 2013). Baicalein also demonstrated significant following further research of this plant for its commercial devel-
activity against Leishmania donovani (Das et al., 2006). In addition to opment in nutraceutical and pharmaceutical products.
these pharmacological activities, some other interesting biological Although several pharmacological activities of the extracts and
activities of baicalein (Koda et al., 1977; Sekiya and Okuda, 1982; pure isolates have been reported, additional research investigating
Kubo et al., 1984; Qain et al., 1989; Ono et al., 1989; Austin et al., 1992; ethnomedicinal preparations and extracts/isolates are needed for their
Huang et al., 1994; Motoo and Sawabu, 1994; Matsuzaki et al., 1996; application as effective drugs. The most important research gaps are
Gao et al., 1996; So et al., 1997; Nishioka et al., 1998; Wakabayashi, as follows: (i) traditional knowledge of this plant in conditions such as
1999; Inoue and Jackson, 1999; Ikemoto et al., 2000; Nakajima et al., tonsillitis, pharyngitis, bronchitis, leprosy, enlarged spleen, pneumo-
2001; Hsu et al., 2001; Ahn et al., 2001; Kimura et al., 2001; Hong nia, piles and snake bite, among others; (ii) different biological
et al., 2002; Kang et al., 2003; Nakamura et al., 2003; Liu et al., 2003; screenings of the extracts/pure isolates for their application for the
Zhu et al., 2004; Lee et al., 2005; Ma et al., 2005; Gao et al., 2007; treatment of different diseases; (iii) synergistic effects of the different
Chao et al., 2007; Lee et al., 2008; Tu et al., 2008; Li et al., 2009b; Liu extracts/pure isolates to evaluate their ability to enhance the efficiency
et al., 2010; Mu et al., 2011; Lu et al., 2011; Zhang et al., 2012), baicalin of the additive mixture (Williamson, 2001; Wagner, 2011); (iv) exte-
(Baylor et al., 1992; Li et al., 1993, Lin and Shieh, 1996; Kitamura et al., nsive in vivo experiments to validate the existing pharmacological
1998; Li et al., 2000a, 2000b; Chan et al., 2000; Ikezoe et al., 2001; activities; (v) human clinical trials investigating potential bioactive
Chen et al., 2001; Zeng et al., 2007; Zhang et al., 2007; Tarrago et al., extracts/pure isolates; (vi) the mechanisms underlying the drug action
2008; Peng et al., 2009), oroxylin A (Chen et al., 2000; Hu et al., 2006; of bioactive extracts/pure isolates for their effective use by the medical
Yang et al., 2008; Li et al., 2009a; Liu et al., 2009; Lu et al., 2012; Wei practitioners; (vii) rigorous quality control measures and standardiza-
et al., 2013a), chrysin (Walle et al., 2000; Woo et al., 2004; Zhang et tion of the bioactive chemicals/fractions/extracts/ethnomedicinal pre-
al., 2004; Woo et al., 2005; Harris et al., 2006; Fu et al., 2007; parations for their commercial exploitation as nutraceutical and
Pushpavalli et al., 2010), lapachol (Balassino et al., 2005) and acteo- pharmaceutical products in local and international markets; (viii)
side (Koo et al., 2006; Lee et al., 2006) isolated from other plants or biotechnology for the large-scale production of bioactive phytochem-
purchased from pharmaceutical industries have also been reported. icals of this plant.
Thus, these phytochemicals may represent prospective chemicals for Some important future studies of this plant have been requested
the development of new pharmaceutical and nutraceutical products to facilitate its commercial exploitation as a potential source of
for the treatment of various diseases following extensive clinical trials. medicines.
Some antioxidant flavonoids such as scutellarein 7-O-glucoside First, it will be important to contact the local communities and
(27), baicalin (5), baicalein (1) and baicalein 7-O-glucoside (4) ethnomedical practitioners (e.g., Kabiraj, Hakim, among others)
isolated from seeds may be beneficial for the treatment of lung regarding their knowledge concerning the use of plant parts for
inflammation and related respiratory diseases (Kirkham and symptoms of diseases and to determine other plant parts that are
Rahman, 2006; Yan et al., 2011). also used in drug formulations for the treatment of these diseases.
The roots, stem bark and seeds are the most promising parts of Accordingly, the pharmacological activities of the combined extracts
the plant used in formulations used in most Indian Ayurvedic, and their pure isolates must be evaluated. Second, the mechanism
Chinese and Japanese drugs (National Commission of Chinese underlying the activity of the drug must be determined. A lack of
Pharmacopoeia, 2010; Radhika et al., 2011). knowledge regarding the activity of the drug, either the active extract
A quality evaluation of forty samples of semen oroxyli, the or its bioactive pure isolates, results in an inability to apply it
seeds of Oroxylum indicum (¼Mu-Hu-Die) collected from different properly for disease symptoms. Third, the pharmacological activities
places in China, was performed using HPLC with both multireference of the extracts/isolates must be validated in in vivo animal models
and detailed toxicity studies. Fourth, mixing of the active extract of Biswas, K., Biswas, R., 2013. Identification of medicinal plants using PCR-RFLP in
the plant with the extracts of other herbs with similar pharmacolo- Dasamula—an Ayurvedic drug. Journal of Pharmaceutical and Biosciences 1,
94–99.
gical activities followed by an evaluation of the effective dose of the Biswas, K.P., Ghosh, E., 1994. Bharater Bonoushodi, second ed.vol. 3. Calcutta
mixed extract to determine the maximum efficiency and the mini- University, Calcutta p. 858.
mum side effects. Fifth, bioactive phytochemicals could be produced BoseDasgupta, S., Das, B.B., Sengupta, S., Ganguly, A., Roy, A., Dey, S., Tripathi, G.,
by tissue culture of the plant part(s). Sixth, it will be important to Dinda, B., Majumder, H.K., 2008. The caspase-independent algorithm of
programmed cell death in Leishmania induced by baicalein: the role of Ld
conduct clinical trials of traditional medicinal preparations based on Endo G, LdFEN-1 and LdTatD as DNA ‘degradesome’. Cell Death and Differ-
Oroxylum indicum (L.) Kurz and on active extract/fractions/pure entiation 15, 1629–1640.
isolates of the plant. Seventh, the restoration of this plant may be Burkill, I.H., 1966. A Dictionary of Economic Products of Malay Peninsular. vol. 2.
Ministry of Agriculture and Cooperatives, Kuala Lumpur, Malaysia, pp.
achieved by plantation in low-altitude forest lands as well as
1617–1618.
restriction for commercial use as timber or the indiscriminate Chan, F.L., Choi, H.L., Chen, Z.Y., Chan, P.S.F., Huang, Y., 2000. Induction of apoptosis
collection of whole plants for other purposes (RaviKumar et al., in prostate cancer cell lines by a flavonoid, baicalin. Cancer Letters 160,
2000; Jayram and Prasad, 2008). In addition, the geographic and 219–228.
Chao, J.-I., Su, W.-C., Liu, H.-F., 2007. Baicalein induces cancer cell death and
seasonal variability of the levels of phytochemicals and efficiency of proliferation retardation by the inhibition of CDC2 kinase and survivin
the extracts represent areas of further research. associated with opposite role of p38 mitogen-activated protein kinase and
AKT. Molecular Cancer Therapy 6, 3039–3048.
Cao, Y., Yan, R., Yang, L., Guo, J., Liu, H., Zhang, J., Yang, B., Huang, L., 2013. Quality
evaluation of semen oroxyli based on the determination of multiple compo-
Acknowledgements
nents with a single reference standard. Journal of Chromatographic Science 51,
477–484.
The authors thank Prof. P. Metz, Technical University of Dres- Chen, L.-J., Games, D.E., Jones, J., 2003. Isolation and identification of four flavonoids
constituents from the seeds of Oroxylum indicum by high-speed counter-
den, Germany for providing research papers, the Department of
current chromatography. Journal of Chromatography A 988, 95–105.
Science & Technology, New Delhi, India for funding support (Grant Chen, L.J., Song, H., Lan, X.Q., Games, D.E., Sutherland, I.A., 2005. Comparison of
no. DST/SR/S1/OC-75/2009) and the Council of Scientific and high-speed counter-current chromatography instruments for the separation of
Industrial Research, New Delhi, India for a senior research fellow- the extracts of the seeds of Oroxylum indicum. Journal of Chromatography A
1063, 241–245.
ship award to PR for his personal research project (Grant no. 09/ Chen, S., Ruan, Q., Bedner, E., Deptala, A., Wang, X., Hsieh, T.C., Traganos, F.,
714(0013)/2011-EMR-1). Darzynkiewicz, Z., 2001. Effects of the flavonoid baicalin and its metabolite
baicalein on androgen receptor expression, cell cycle progression and apoptosis
of prostate cancer cell lines. Cell Proliferation 34, 293–304.
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Contents lists available at ScienceDirect

Oroxylum indicum (L.) Kurz, an important Asian traditional medicine:

Plant part Traditional use(s) Country Preparation(s) Reference(s)

Plant part Traditional use(s) Country Preparation(s) Reference(s)

Leaf (a) Enlarged spleen India Decoction Drury (2006)

N/S: Not stated.

Phytochemical Chemical constituents Reference(s)

(a) Phytochemicals reported from leaves

Chrysin (2) and chrysin 7-O-diglucoside (13) Chen et al. (2003)

Phytochemical Chemical constituents Reference(s)

2.2. Isoﬂavonoids 2.7. Steroids

2.3. Naphthalenoids 2.8. Stilbenoids

Miscellaneous compounds (95–111) of anthraquinone, pheno-

2.5. Cyclohexylethanoids A number of pharmacological studies have been reported in the

Fig. 2. (continued) Fig. 2. (continued)

3.17. Antimutagenic activity 4. Toxicity studies

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