Ibrahim Jantan
Universiti Kebangsaan Malaysia, Faculty of Pharmacy, Faculty Member
Arachidonic acid and its metabolites have generated high level of interest among researchers due to their vital role in inflammation. The inhibition of enzymes involved in arachidonic acid metabolism has been considered as synergistic... more
Arachidonic acid and its metabolites have generated high level of interest among researchers due to their vital role in inflammation. The inhibition of enzymes involved in arachidonic acid metabolism has been considered as synergistic anti-inflammatory effect. A series of novel α,β-unsaturated carbonyl based compounds were synthesized and evaluated for their inhibitory activity on secretory phospholipase A₂ (sPLA₂), cyclooxygenases (COX), soybean lipoxygenase (LOX) in addition to proinflammatory cytokines comprising IL-6 and TNF-α. Six α,β-unsaturated carbonyl based compounds (2, 3, 4, 12, 13 and 14) exhibited strong inhibition of sPLA₂ activity, with IC₅₀ values in the range of 2.19-8.76 μM. Nine compounds 1-4 and 10-14 displayed inhibition of COX-1 with IC₅₀ values ranging from 0.37 to 1.77 μM (lower than that of reference compound), whereas compounds 2, 10, 13 and 14 strongly inhibited the COX-2. The compounds 10-14 exhibited strong inhibitory activity against LOX enzyme. All compounds were evaluated for the inhibitory activities against LPS-induced TNF-α and IL-6 release in the macrophages. On the basis of screening results, five active compounds 3, 4, 12, 13 and 14 were found strong inhibitors of TNF-α and IL-6 release in a dose-dependent manner. Molecular docking experiments were performed to clarify the molecular aspects of the observed COX and LOX inhibitory activities of the investigated compounds. Present findings increases the possibility that these α,β-unsaturated carbonyl based compounds might serve as beneficial starting point for the design and development of improved anti-inflammatory agents.
Research Interests: Biochemistry, Chemistry, Organic Chemistry, Macrophages, Medicine, and 15 moreCell line, Mice, Curcumin, Animals, Enzyme, lipoxygenase (LOX) inhibitors, Soybeans, Bioorganic and medicinal Chemistry, Structure activity Relationship, Protein Binding, Arachidonic Acid, Interleukin, binding sites, Pharmacology and pharmaceutical sciences, and lipoxygenase
Research Interests:
ABSTRACT Chalcones are the principal precursors for the biosynthesis of flavonoids and isoflavonoids. A three carbon α, β-unsaturated carbonyl system constitutes chalcones. Chalcones are the condensation products of aromatic aldehyde with... more
ABSTRACT Chalcones are the principal precursors for the biosynthesis of flavonoids and isoflavonoids. A three carbon α, β-unsaturated carbonyl system constitutes chalcones. Chalcones are the condensation products of aromatic aldehyde with acetophenones in attendance of catalyst. They go through an assortment of chemical reactions and are found advantageous in synthesis of pyrazoline, isoxazole and a variety of heterocyclic compounds. In synthesizing a range of therapeutic compounds, chalcones impart key role. They have showed worth mentioning therapeutic efficacy for the treatment of various diseases. Chalcone based derivatives have gained heed since they own simple structures, and diverse pharmacological actions. A lot of methods and schemes have been reported for the synthesis of these compounds. Amongst all, Aldol condensation and Claisen-Schmidt condensation still grasp high up position. Other distinguished techniques include Suzuki reaction, Witting reaction, Friedel-Crafts acylation with cinnamoyl chloride, Photo-Fries rearrangement of phenyl cinnamates etc. These inventive techniques utilize various catalysts and reagents including SOCl2 natural phosphate, lithium nitrate, amino grafted zeolites, zinc oxide, water, Na2CO3, PEG400, silicasulfuric acid, ZrCl4 and ionic liquid etc. The development of better techniques for the synthesis of α, β- unsaturated carbonyl compounds is still in high demand. In brief, we have explained the methods and catalysts used in the synthesis of chalcones along with their biological activities in a review form to provide information for the development of new-fangled processes targeting better yield, less reaction time and least side effects with utmost pharmacological properties.
Research Interests:
Hyperpigmentation in human skin and enzymatic browning in fruits, which are caused by tyrosinase enzyme, are not desirable. Investigations in the discovery of tyrosinase enzyme inhibitors and search for improved cytotoxic agents continue... more
Hyperpigmentation in human skin and enzymatic browning in fruits, which are caused by tyrosinase enzyme, are not desirable. Investigations in the discovery of tyrosinase enzyme inhibitors and search for improved cytotoxic agents continue to be an important line in drug discovery and development. In present work, a new series of 30 compounds bearing α,β-unsaturated carbonyl moiety was designed and synthesized following curcumin as model. All compounds were evaluated for their effects on human cancer cell lines and mushroom tyrosinase enzyme. Moreover, the structure-activity relationships of these compounds are also explained. Molecular modeling studies of these new compounds were carried out to explore interactions with tyrosinase enzyme. Synthetic curcumin-like compounds (2a-b) were identified as potent anticancer agents with 81-82% cytotoxicity. Five of these newly synthesized compounds (1a, 8a-b, 10a-b) emerged to be the potent inhibitors of mushroom tyrosinase, providing further insight into designing compounds useful in fields of food, health, and agriculture.
Research Interests:
Research Interests:
Research Interests:
Neurodegeneration, a complex disease state, comprises several pathways that contribute to cell death. Conventional approach of targeting only one of these pathways has not been proven to be entirely successful, and has demanded a... more
Neurodegeneration, a complex disease state, comprises several pathways that contribute to cell death. Conventional approach of targeting only one of these pathways has not been proven to be entirely successful, and has demanded a hypothetical change as to how researchers design and develop new drugs. In this study, effects of a series of α, β-unsaturated carbonyl-based tetralone derivatives against Alzheimer's disease (AD) were investigated. Moreover, their activity towards amyloid β-induced cytotoxicity was also studied. Six compounds including 3f, 3o, 3u, 3ae, 3af and 3ag were discovered to be most protective against Aβ-induced neuronal cell death in PC12 cells. The findings of in vitro experiment revealed that most of these compounds exhibited potent inhibitory activity against MAO-B, AChE and self-induced Aβ1-42 aggregation. The compound 3f exhibited best AChE (IC50 = 0.045±0.02 μM) inhibitory potential in addition to potent inhibition of MAO-B (IC50 = 0.88±0.12 μM). Furthermore, compound 3f disassembled the Aβ fibrils produced by self-induced Aβ aggregation by 78.2±4.8%. Collectively, these findings suggest that some compounds from this series have potential to be promising multifunctional agents for AD treatment. This article is protected by copyright. All rights reserved.
Research Interests: Chemistry, Cytotoxicity, Neurodegeneration, Medicine, In Vitro, and 13 moreAnimals, Ic, Acetylcholinesterase, Programmed cell death, Cholinesterase inhibitors, Liquid Chromatography / Electrospray Ionization Mass Spectrometry, Rats, Alzheimer Disease, Biochemistry and cell biology, Neuroprotective Agents, Butyrylcholinesterase, proton magnetic resonance spectroscopy, and Monoamine oxidase inhibitors
Inhibitory effects on... more
Inhibitory effects on neutrophils' chemotaxis, phagocytosis and production of reactive oxygen species (ROS) are among the important targets in developing anti-inflammatory agents and immunosuppressants. Eight series of chalcone derivatives including five newly synthesized series were assessed for their inhibitory effects on chemotaxis, phagocytosis and ROS production in human polymorphonuclear neutrophils (PMNs). Inhibition of PMNs' chemotaxis and phagocytosis abilities were investigated using the Boyden chamber technique and the Phagotest kit, respectively, while ROS production was evaluated using luminol- and lucigenin-based chemiluminescence assay. The new derivatives (4d and 8d), which contain 4-methylaminoethanol functional group were active in all the assays performed. It was also observed that some of the compounds were active in inhibiting chemotaxis while others suppressed phagocytosis and ROS production. The information obtained gave new insight into chalcone derivatives with the potential to be developed as immunomodulators.
Research Interests:
A novel series of 1,3‐diphenyl‐2‐propen‐1‐one (chalcone) derivatives was synthesized by a simple, eco‐friendly, and efficient Claisen–Schmidt condensation reaction and used as precursors for the synthesis of new pyrazoline derivatives.... more
A novel series of 1,3‐diphenyl‐2‐propen‐1‐one (chalcone) derivatives was synthesized by a simple, eco‐friendly, and efficient Claisen–Schmidt condensation reaction and used as precursors for the synthesis of new pyrazoline derivatives. All the synthesized compounds were screened for anti‐inflammatory related activities such as inhibition of phospholipase A2 (PLA2), cyclooxygenases (COX‐1 and COX‐2), IL‐6, and TNF‐α. The results of the above studies show that the compounds synthesized are effective inhibitors of above pro‐inflammatory enzymes and cytokines. Overall, the results of the studies reveal that the pyrazolines with chlorophenyl substitution (1b–6b) seem to be important for inhibition of enzymes and cytokines. Molecular docking experiments were performed to clarify the molecular aspects of the observed COX‐inhibitory activities of the investigated compounds.
Research Interests:
Research Interests:
There is a crucial need to develop new effective drugs for Alzheimer's disease (AD) as the currently available AD treatments provide only momentary and incomplete symptomatic relief. Amongst natural products, curcumin, a major... more
There is a crucial need to develop new effective drugs for Alzheimer's disease (AD) as the currently available AD treatments provide only momentary and incomplete symptomatic relief. Amongst natural products, curcumin, a major constituent of turmeric, has been intensively investigated for its neuroprotective effect against β-amyloid (Aβ)-induced toxicity in cultured neuronal cells. The ability of curcumin to attach to Aβ peptide and prevent its accumulation is attributed to its three structural characteristics such as the presence of two aromatic end groups and their co-planarity, the length and rigidity of the linker region and the substitution conformation of these aromatics. However, curcumin failed to reach adequate brain levels after oral absorption in AD clinical trials due to its low water solubility and poor oral bioavailability. A number of new curcumin analogs that mimic the active site of the compound along with analogs that mimic the curcumin anti-amyloid effect combined with anticholinesterase effect have been developed to enhance the bioavailability, pharmacokinetics, water solubility, stability at physiological conditions and delivery of curcumin. In this article, we have summarized all reported synthetic analogs of curcumin showing effects on β-amyloid and discussed their potential as therapeutic and diagnostic agents for AD.
Research Interests:
Research Interests:
A series of new α,β-unsaturated carbonyl-based cyclohexanone derivatives was synthesized by simple condensation method and all compounds were characterized by using various spectroscopic techniques. New compounds were evaluated for their... more
A series of new α,β-unsaturated carbonyl-based cyclohexanone derivatives was synthesized by simple condensation method and all compounds were characterized by using various spectroscopic techniques. New compounds were evaluated for their effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). These compounds were also screened for in vitro cytotoxicity and for inhibitory activity for self-induced Aβ1-42 aggregation. The effect of these compounds against amyloid β-induced cytotoxicity was also investigated. The findings of in vitro experiment revealed that most of these compounds exhibited potent inhibitory activity against AChE and self-induced Aβ1-42 aggregation. The compound 3o exhibited best AChE (IC50=0.037μM) inhibitory potential. Furthermore, compound 3o disassembled the Aβ fibrils produced by self-induced Aβ aggregation by 76.6%. Compounds containing N-methyl-4-piperidone linker, showed high acetylcholinesterase and self-induced Aβ aggregation inhibitory activities as compared to reference drug donepezil. The pre-treatment of cells with synthetic compounds protected them against Aβ-induced cell death by up to 92%. Collectively, these findings suggest that some compounds from this series have potential to be promising multifunctional agents for AD treatment and our study suggest the cyclohexanone derivatives as promising new inhibitors for AChE and BuChE, potentially useful to treat neurodegenerative diseases.
Research Interests: Chemistry, Organic Chemistry, Cytotoxicity, Medicine, Humans, and 13 moreAnimals, Acetylcholinesterase, Drug Design, Cholinesterase inhibitors, Rats, Bioorganic and medicinal Chemistry, Alzheimer Disease, Cell Survival, Neuroprotective Agents, Butyrylcholinesterase, Protein aggregates, Aché, and Pharmacology and pharmaceutical sciences
Research Interests:
Research Interests:
Research Interests:
Research Interests:
Research Interests:
Background Immunomodulatory effects of Tinospora crispa have been investigated due to its traditional use to treat several inflammatory disorders associated to the immune system. The present study reports the underlying mechanisms... more
Background Immunomodulatory effects of Tinospora crispa have been investigated due to its traditional use to treat several inflammatory disorders associated to the immune system. The present study reports the underlying mechanisms involved in the stimulation of 80% ethanol extract of T. crispa stems on pro-inflammatory mediators release in lipopolysaccharide (LPS)-primed U937 human macrophages via MyD88-dependent pathways. Methods Release of interleukin (IL)-1β and tumor necrosis factor (TNF)-α, and production of prostaglandin E2 (PGE2) were determined by using enzyme-linked immunosorbent assay (ELISA). Immunoblot technique was executed to determine the activation of MAPKs molecules, NF-κB, PI3K-Akt and cyclooxygenase-2 (COX-2) protein. Determination of pro-inflammatory cytokines and COX-2 relative gene expression levels was by performing the real-time quantitative reverse transcription polymerase chain reaction (qRT-PCR). A reversed-phase HPLC method was developed and validated to ...
Research Interests:
BackgroundZingiber zerumbetrhizome and its bioactive metabolites have previously been reported to exhibit innumerable pharmacological properties particularly anti-inflammatory activities. In the present study, the 80% ethanol extract,... more
BackgroundZingiber zerumbetrhizome and its bioactive metabolites have previously been reported to exhibit innumerable pharmacological properties particularly anti-inflammatory activities. In the present study, the 80% ethanol extract, essential oil and zerumbone ofZ. zerumbetrhizomes were explored for their in vitro immunosuppressive properties on chemotaxis, CD11b/CD18 expression, phagocytosis and chemiluminescence of isolated human polymorphonuclear neutrophils (PMNs).MethodsThe extract was analyzed quantitatively by performing a validated reversed phase high performance liquid chromatography (RP-HPLC). Zerumbone was isolated by chromatographic technique while the essential oil was acquired through hydro-distillation of the rhizomes and further analyzed by gas chromatography (GC) and GC-MS. Chemotaxis assay was assessed by using a 24-well cell migration assay kit, while CD18 integrin expression and phagocytic engulfment were measured using flow cytometry. The reactive oxygen speci...
Research Interests:
Research Interests:
Research Interests:
This review summarises the recent efforts to engineer macromolecular prodrugs (MPDs) based on polysaccharidal materials. Polysaccharidal materials are of utmost importance to design and develop MPDs of non-steroidal anti-inflammatory... more
This review summarises the recent efforts to engineer macromolecular prodrugs (MPDs) based on polysaccharidal materials. Polysaccharidal materials are of utmost importance to design and develop MPDs of non-steroidal anti-inflammatory drugs, antibiotics, anti-viral and anti-cancer drugs, etc. Covalent drug loading capabilities of the polysaccharidal materials are thoroughly discussed. In order to successfully transform drugs into prodrugs using polysaccharidal materials, present review details different syntheses strategies which are being applied to design pharmaceutically viable MPDs. Herein, we also reported the collection of polysaccharidal materials which are being widely spun in to MPDs of several classes of drugs and their applications. Merits and demerits of polysaccharide biomaterials for MPDs are critically discussed. Cellulose ether derivatives are newly introduced materials attracting the vigil eye of researchers working in MPD design for potential therapeutic applications. Special emphasis will be given to amphiphilic materials, i.e. MPDs, which self-assemble at solvent interfaces into nanorods, nanoparticles (NPs), nanowires, etc. Furthermore, the stability of MPDs at elevated conditions of temperature is discussed to gain information about their storage properties. We highlighted thrust areas in polysaccharidal materials-based research and development of MPDs.
Research Interests:
Plant-derived immunomodulators and anti-cancer agents have attracted a lot of interest from natural product scientists for their efficacy and safety and their significant contribution towards understanding targeted drug action and drug... more
Plant-derived immunomodulators and anti-cancer agents have attracted a lot of interest from natural product scientists for their efficacy and safety and their significant contribution towards understanding targeted drug action and drug delivery mechanisms. Zerumbone, the main constituent of Zingiber zerumbet rhizomes, has been investigated for its wide-spectrum role in treating multitargeted diseases. The rhizomes have been used as food flavoring agents in various cuisines and in herbal medicine. Many in vivo and in vitro studies have provided evidence of zerumbone as a potent immunomodulator as well as a potential anti-cancer agent. This review is an interesting compilation of all those significant outcomes from investigations carried out to date to explore the immunomodulatory and anticancer properties of zerumbone. The ultimate objective of this comprehensive review is to provide updated information and a critical assessment on zerumbone including its chemistry and immunomodulati...
Research Interests:
Phyllanthin found in many Phyllanthus species has various biochemical and pharmacological properties especially on its hepatoprotective effects. However, its effect on the immune system has not been well documented. In the present study,... more
Phyllanthin found in many Phyllanthus species has various biochemical and pharmacological properties especially on its hepatoprotective effects. However, its effect on the immune system has not been well documented. In the present study, phyllanthin isolated from Phyllanthus amarus was investigated for its immunosuppressive effects on various cellular and humoral immune responses in Balb/C mice. Male mice were treated daily at 20, 40 and 100mg/kg of phyllanthin for 14 days by oral gavage. The effects of phyllanthin on cellular immune responses in treated /non treated mice were determined by measuring CD 11b/CD 18 integrin expression, phagocytosis, nitric oxide (NO) production, myeloperoxidase activity (MPO), T and B cells proliferation, lymphocyte phenotyping, serum cytokines production by activated T-cells and delayed type hypersensitivity (DTH). Its effects on humoral immune responses were evaluated by determining the serum levels of lysozyme and ceruloplasmin, and immunoglobulins...
Research Interests: Pharmacology, Complementary and Alternative Medicine, Biology, Cytokines, Inflammation, and 15 moreMedicine, Biological Sciences, Escherichia coli, Animals, Lignans, Male, CHEMICAL SCIENCES, Immune system, Phyllanthus, Erythrocytes, Immunoglobulins, Myeloperoxidase, Hypersensitivity Delayed, Medical and Health Sciences, and Pharmacology and pharmaceutical sciences
Mimosa pudica Linn. (Family: Mimosaceae) is used as an ornamental plant due to its thigmonastic and nyctinastic movements. M. pudica is also used to avoid or cure several disorders like cancer, diabetes, hepatitis, obesity, and urinary... more
Mimosa pudica Linn. (Family: Mimosaceae) is used as an ornamental plant due to its thigmonastic and nyctinastic movements. M. pudica is also used to avoid or cure several disorders like cancer, diabetes, hepatitis, obesity, and urinary infections. M. pudica is famous for its anticancer alkaloid, mimosine, along with several valuable secondary metabolites like tannins, steroids, flavonoids, triterpenes, and glycosylflavones. A wide array of pharmacological properties like antioxidant, antibacterial, antifungal, anti‐inflammatory, hepatoprotective, antinociceptive, anticonvulsant, antidepressant, antidiarrheal, hypolipidemic activities, diuretic, antiparasitic, antimalarial, and hypoglycemic have been attributed to different parts of M. pudica. Glucuronoxylan polysaccharide extruded from seeds of M. pudica is used for drug release formulations due to its high swelling index. This review covers a thorough examination of functional bioactives as well as pharmacological and phytomedicina...
Research Interests:
Psyllium (PS), a water-swellable dietary fiber from seeds of widely distributed plant, Plantago ovata (PO) is esteemed for its medicinal and nutraceutical values. PS has been attributed to its broad range of pharmacological activities... more
Psyllium (PS), a water-swellable dietary fiber from seeds of widely distributed plant, Plantago ovata (PO) is esteemed for its medicinal and nutraceutical values. PS has been attributed to its broad range of pharmacological activities like anti-tumor, anti-inflammatory, anti-diabetic, hypolipidemic, laxative, anti-obesity, anti-diarrheal, anti-amoebic, and anti-nociceptive, and has been employed for sustained/delayed/targeted drug delivery due to its biocompatible and biodegradable nature. Interestingly, PS can be utilized for the absorption of toxic materials from industrial waste and is also used as substituent of gluten in breads for better acceptance. This review focuses upon the utilization of PS in drug delivery systems, medicinal uses, and pharmacological attributes to explore its potential in the nutraceutical industry.
Research Interests:
Current analytical techniques for characterizing solid-state pharmaceuticals include powder x-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, infrared spectroscopy, Raman spectroscopy, electron microscopy... more
Current analytical techniques for characterizing solid-state pharmaceuticals include powder x-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, infrared spectroscopy, Raman spectroscopy, electron microscopy and nuclear magnetic resonance. Powder x-ray diffraction and differential scanning calorimetry are mainstream techniques but they lack spatial resolution. Scanning electron microscopy and micro-Raman spectroscopy provide good chemical and optical characterization but they are not capable of analysing very small nanoparticles. Transmission electron microscopy and nano-thermal analysis can provide explicit characterization of nanoparticles but they are invasive. Nuclear magnetic resonance offers good spatial resolution but its use is mainly limited by poor sensitivity and high costs. In view of the many challenges posed by existing methods, new and novel techniques are being continually researched and developed to cater to the growing number of solid f...
Research Interests:
Research Interests:
The in vivo immunomodulatory activities of Tinospora crispa have been reported but its molecular mechanisms underlying its immunomodulatory properties remains obscure and the active constituents contributing to the activities have not... more
The in vivo immunomodulatory activities of Tinospora crispa have been reported but its molecular mechanisms underlying its immunomodulatory properties remains obscure and the active constituents contributing to the activities have not been identified. The present study was aimed to investigate the immunomodulatory effects of T. crispa extract (TCE) and its chemical constituents on RAW 264.7 macrophages. Six known compounds including magnoflorine and syringin were isolated by various chromatographic techniques from TCE and their structures were determined spectroscopically. A validated HPLC method was used to quantify magnoflorine and syringin in the extract. The immunomodulatory effects of TCE and its isolated compounds on chemotaxis, phagocytosis, production of inflammatory mediators including reactive oxygen species (ROS), nitric oxide (NO), prostaglandin E2 (PGE2) and pro-inflammatory cytokines which include tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6 and monocyte ...
Research Interests: Chemistry, Cytokines, Macrophages, Medicine, Immunopharmacology, and 14 moreReactive Oxygen Species, Mice, Nitric oxide, Animals, Chemotaxis, Immune system, Plant extracts, Phagocytosis, Tinospora, Tumor necrosis factor-alpha, Phytochemicals, Immunostimulant, Cell Survival, and Pharmacology and pharmaceutical sciences
Previous studies on Labisia pumila var. alata (LPva) have showed that it could inhibit low-density lipoprotein (LDL) oxidation and provide protection on myocardial infarction in rats. We hypothesized that LPva extracts can modulate the... more
Previous studies on Labisia pumila var. alata (LPva) have showed that it could inhibit low-density lipoprotein (LDL) oxidation and provide protection on myocardial infarction in rats. We hypothesized that LPva extracts can modulate the lipid profiles and serum antioxidant status of hypercholesterolemic rats. In the present study, we investigated the effects of aqueous and 80% ethanol extracts of LPva on atherogenic and serum antioxidant parameters as well as changes in abdominal aorta of high-cholesterol diet rats. The major components of the extracts, gallic acid, flavonoids and alkyl resorcinols were analyzed by using a validated reversed phase HPLC method. The rats were induced to hypercholesterolemic status with daily intake of 2% cholesterol for a duration of 8 weeks. Three different doses (100, 200 and 400mg/kg) of the extracts were administered daily on the 4th week onwards. The rats were then sacrificed and the blood was collected via abdominal aorta and serum was separated by centrifugation for biochemical analysis. Part of the aorta tissues were excised immediately for histopathological examination. The serum of LPva treated rats showed significant reduction in serum aspartate aminotransferase (AST), alanine aminotransferase (ALT) and lactate dehydrogenase (LDH) levels and the abdominal aorta showed a significant decrease of atheroma lesions in treated rats. Serum lipid profiles of treated rats showed a decrease in total cholesterol, total triglycerides and low-density lipoprotein (LDL) levels as compared to control group. The atherogenic indices in treated rats were significantly improved along with an increasing level of serum high-density lipoprotein (HDL). The extracts also exhibited significant increase of antioxidant enzymes and decrease of MDA as a product of lipid peroxidation. LPva extracts can reduce the risk of dyslipidemia by improving the serum lipid profiles and modulating serum antioxidants.
Research Interests: Chemistry, Complementary and Alternative Medicine, Plant Biology, Atherosclerosis, Diet, and 15 moreMedicine, Phytomedicine, Antioxidants, Lipids, Animals, Male, Plant extracts, Rats, Lipid Profile, Aspartate Aminotransferases, Primulaceae, Alanine Transaminase, Abdominal Aorta, Aorta Abdominal, and Pharmacology and pharmaceutical sciences
Research Interests:
Research Interests:
Research Interests:
Hsp90 is an ATP-dependent molecular chaperone that assists folding and conformational maturation/maintenance of many proteins. It is a potential cancer drug target because it chaperones oncoproteins. A prokaryotic homolog of Hsp90 (HtpG)... more
Hsp90 is an ATP-dependent molecular chaperone that assists folding and conformational maturation/maintenance of many proteins. It is a potential cancer drug target because it chaperones oncoproteins. A prokaryotic homolog of Hsp90 (HtpG) is essential for thermotolerance in some bacteria and virulence of zoonotic pathogens. To identify a new class of small molecules which target prokaryotic and eukaryotic Hsp90s, we studied the effects of a naturally occurring cyclic sesquiterpene zerumbone, which inhibits proliferation of a wide variety of tumor cells, on the activity of Hsp90. Zerumbone enhanced the ATPase activity of cyanobacterial Hsp90 (Hsp90), yeast Hsp90, and human Hsp90α. It also enhanced the catalytic efficiency of Hsp90 by greatly increasing Mass analysis showed that zerumbone binds to cysteine side chains of Hsp90 covalently. Mutational studies identified 3 cysteine residues (one per each domain of Hsp90) that are involved in the enhancement, suggesting the presence of all...
Research Interests:
Zingiber zerumbet (L.) Roscoe ex Sm. (family, Zingiberaceae) is a potent medicinal herb widely known as shampoo ginger and its rhizome is used in numerous ethnomedicinal applications including as antipyretic, anti-inflammatory,... more
Zingiber zerumbet (L.) Roscoe ex Sm. (family, Zingiberaceae) is a potent medicinal herb widely known as shampoo ginger and its rhizome is used in numerous ethnomedicinal applications including as antipyretic, anti-inflammatory, antibacterial, anti-diarrheal, antidiabetics, carminative, and diuretic. The aim of this review was to bring together all of scientific updates on the phytochemistry and pharmacological activities of this herb, including their toxicological studies, and critically analyzed the outcomes to provide directions for future research on the herb as potential source of bioactive metabolites for pharmaceutical and nutraceutical applications. About 60 metabolites, mainly polyphenols, and terpenoids have been isolated and identified. However, most of reported pharmacological studies were based on crude extracts, and only a few of those isolated metabolites, particularly zerumbone has been investigated for biological and pharmacological activities. The bioactive metaboli...
Research Interests:
An autoimmune disease is defined as a clinical syndrome resulted from an instigation of both T cell and B cell or individually, in the absence of any present infection or any sort of distinguishable cause. Clonal deletion of auto reactive... more
An autoimmune disease is defined as a clinical syndrome resulted from an instigation of both T cell and B cell or individually, in the absence of any present infection or any sort of distinguishable cause. Clonal deletion of auto reactive cells remains the central canon of immunology for decades, keeping the role of T cell and B cell aside, which are actually the guards to recognize the entry of foreign body. According to NIH, 23.5 million Americans are all together affected by these diseases. They are rare, but with the exception of RA. Rheumatoid arthritis is chronic and systemic autoimmune response to the multiple joints with unknown ethology, progressive disability, systemic complications, early death and high socioeconomic costs. Its ancient disease with an old history found in North American tribes since 1500 BCE, but its etiology is yet to be explored. Current conventional and biological therapies used for RA are not fulfilling the need of the patients but give only partial r...
Research Interests:
Research Interests:
A series of new α,β-unsaturated carbonyl-based cyclohexanone derivatives was synthesized by simple condensation method and all compounds were characterized by using various spectroscopic techniques. New compounds were evaluated for their... more
A series of new α,β-unsaturated carbonyl-based cyclohexanone derivatives was synthesized by simple condensation method and all compounds were characterized by using various spectroscopic techniques. New compounds were evaluated for their effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). These compounds were also screened for in vitro cytotoxicity and for inhibitory activity for self-induced Aβ1-42 aggregation. The effect of these compounds against amyloid β-induced cytotoxicity was also investigated. The findings of in vitro experiment revealed that most of these compounds exhibited potent inhibitory activity against AChE and self-induced Aβ1-42 aggregation. The compound 3o exhibited best AChE (IC50=0.037μM) inhibitory potential. Furthermore, compound 3o disassembled the Aβ fibrils produced by self-induced Aβ aggregation by 76.6%. Compounds containing N-methyl-4-piperidone linker, showed high acetylcholinesterase and self-induced Aβ aggregation inhibitory act...
Research Interests: Chemistry, Organic Chemistry, Medicine, Humans, Animals, and 12 moreAcetylcholinesterase, Drug Design, Cholinesterase inhibitors, Rats, Bioorganic and medicinal Chemistry, Alzheimer Disease, Cell Survival, Neuroprotective Agents, Butyrylcholinesterase, Protein aggregates, Aché, and Pharmacology and pharmaceutical sciences
Tinospora crispa extract exhibited immunostimulatory effects by promoting nitric oxide production ability, peritoneal macrophage phagocytosis, delayed type hypersensitivity, and enhancing serum immunoglobulins and serum lysozyme levels.
Research Interests:
Research Interests:
There is a crucial need to develop new effective drugs for... more
There is a crucial need to develop new effective drugs for Alzheimer's disease (AD) as the currently available AD treatments provide only momentary and incomplete symptomatic relief. Amongst natural products, curcumin, a major constituent of turmeric, has been intensively investigated for its neuroprotective effect against β-amyloid (Aβ)-induced toxicity in cultured neuronal cells. The ability of curcumin to attach to Aβ peptide and prevent its accumulation is attributed to its three structural characteristics such as the presence of two aromatic end groups and their co-planarity, the length and rigidity of the linker region and the substitution conformation of these aromatics. However, curcumin failed to reach adequate brain levels after oral absorption in AD clinical trials due to its low water solubility and poor oral bioavailability. A number of new curcumin analogs that mimic the active site of the compound along with analogs that mimic the curcumin anti-amyloid effect combined with anticholinesterase effect have been developed to enhance the bioavailability, pharmacokinetics, water solubility, stability at physiological conditions and delivery of curcumin. In this article, we have summarized all reported synthetic analogs of curcumin showing effects on β-amyloid and discussed their potential as therapeutic and diagnostic agents for AD.
Research Interests:
Carica papaya and Ocimum basilicum are widely used in traditional medicine around the world but little toxicological information is available on their safety. The aim of this study was to evaluate the acute, subacute and subchronic... more
Carica papaya and Ocimum basilicum are widely used in traditional medicine around the world but little toxicological information is available on their safety. The aim of this study was to evaluate the acute, subacute and subchronic toxicities of the aqueous extracts of the leaves of C. papaya and O. basilicum in Sprague Dawley rats. In the acute study, the rats received a single dose of the C. papaya and O. basilicum extracts orally at 2 and 5 g/kg body weight (bw), respectively, while control rats received water only. For subacute and subchronic studies, repeated doses of the extracts were administered daily for 28 days and 13 weeks, respectively. Each treatment group received C. papaya extract of 0.01, 0.14 and 2 g/kg BW and O. basilicum extract of 0.05, 0.5 and 5 g/kg bw, while control group received water only. Parameters measured were clinical observation, mortality, food and water intake. Rats were sacrificed and hematological, biochemical parameters as well as histopathologic...
Research Interests: Biology and Phagocytosis
ABSTRACT Carica papaya L. is commonly used as food as well as traditional medicine. The different parts of the plant have traditional claims for treatment of various diseases. The increase in use of this plant as traditional medicine has... more
ABSTRACT Carica papaya L. is commonly used as food as well as traditional medicine. The different parts of the plant have traditional claims for treatment of various diseases. The increase in use of this plant as traditional medicine has made it necessary to establish a safety profile of this plant.In order to establish a safety margin, animal toxicity studies are required. The present study was carried out to evaluate the sub chronic toxicity effect of the leaf extract of C.papaya in Sprague Dawley (SD) rats. C.papaya leaf extract was prepared daily by dissolving the freeze dried extract of C.papaya in water and administered orally to SD rats for 13 weeks. The study consisted of three treatment groups at doses of 0.01 g/kg BW, 0.14 g/kg BW and 2 g/kg BW (low, medium, and high dose, respectively) and one control group. Each consisting of 10 rats/sex/group. Clinical observation, mortality, food and water intake were monitored throughout the experimental period. At the end of the experiment, the animals were sacrificed. Hematological and biochemical parameters, relative organ weights and histopathological were evaluated. Findings showed that C.papaya leaf juices did not cause any abnormalities on the clinical observation, changes in body weight, food intake and water intake. Therewere no significant differences observed in thehematology parameters measured. There were significant difference in clinical biochemistry values, such as the LDH, creatinine, total protein and albumin. However, these changes were not associated with histopathological observation. In conclusion, our findings suggest that daily oral administration of rats with C.papaya leaf juicefor 13 weeks did not cause any toxic effect.
Research Interests:
Research Interests:
Objective: Gymnema sylvestre R. Br. is regarded as one of the plants with potent anti diabetic properties and has been classified as endangered due to indiscriminate collection of wild plants for use in pharmaceutical preparations.... more
Objective: Gymnema sylvestre R. Br. is regarded as one of the plants with potent anti diabetic properties and has been classified as endangered due to indiscriminate collection of wild plants for use in pharmaceutical preparations. Methods: The effect of ethanolic ...
Research Interests:
The water decoction of Labisia pumila var. alata is used traditionally in childbirth, as well as for the treatment of flatulence, dysentery, dysmenorrhoea and join pains. This study was carried out to determine the best method and optimum... more
The water decoction of Labisia pumila var. alata is used traditionally in childbirth, as well as for the treatment of flatulence, dysentery, dysmenorrhoea and join pains. This study was carried out to determine the best method and optimum parameters of aqueous ...