Evidence-Based Complementary and Alternative Medicine, 2015
The antibacterial and cytotoxic effects of metabolites isolated from an antibacterial extract of ... more The antibacterial and cytotoxic effects of metabolites isolated from an antibacterial extract of Flourensia oolepis were evaluated. Bioguided fractionation led to five flavonoids, identified as 2',4'-dihydroxychalcone (1), isoliquiritigenin (2), pinocembrin (3), 7-hydroxyflavanone (4), and 7,4'-dihydroxy-3'-methoxyflavanone (5). Compound 1 showed the highest antibacterial effect, with minimum inhibitory concentration (MIC) values ranging from 31 to 62 and 62 to 250 μg/mL, against Gram-positive and Gram-negative bacteria, respectively. On further assays, the cytotoxic effect of compounds 1-5 was determined by MTT assay on acute lymphoblastic leukemia (ALL) and chronic myeloid leukemia (CML) cell lines including their multidrug resistant (MDR) phenotypes. Compound 1 induced a remarkable cytotoxic activity toward ALL cells (IC50 = 6.6-9.9 μM) and a lower effect against CML cells (IC50 = 27.5-30.0 μM). Flow cytometry was used to analyze cell cycle distribution and cell death by PI-labeled cells and by Annexin V/PI staining, respectively. Upon treatment, 1 induced cell cycle arrest in the G2/M phase accompanied by a strong induction of apoptosis. These results describe for the first time the antibacterial metabolites of F. oolepis extract, with 1 being the most effective. This chalcone also emerges as a selective cytotoxic agent against sensitive and resistant leukemic cells, highlighting its potential as a lead compound.
ABSTRACT Industrial Crops and Products j o u r n a l h o m e p a g e : w w w . e l s e v i e r . ... more ABSTRACT Industrial Crops and Products j o u r n a l h o m e p a g e : w w w . e l s e v i e r . c o m / l o c a t e / i n d c r o p Insecticidal toxicity of Eucalyptus cinerea essential oil and 1,8-cineole against Musca domestica and possible uses according to the metabolic response of flies a b s t r a c t In a fumigant assay, Musca domestica adults treated with Eucalyptus cinerea EO [LC 50 = 5.5 mg/dm 3 ; majority component by SPME–GC: 1,8-cineole (88.5%), ␣-pinene (2%), ␣-terpineol (9%)], died within 15 min or less. The terpenes absorbed by the flies and their metabolites, analyzed using SPME fiber, were 1,8-cineole (LC 50 = 3.3 mg/dm 3), ␣-pinene (LC 50 = 11.5 mg/dm 3), ␣-terpineol (LC 50 = 36.8 mg/dm 3) and a new component 2,3-dehydro-1,8-cineole, in proportions of 74%, 0.1%, 24.7% and 1.2% respectively. 2,3-Dehydro-1,8-cineole and ␣-terpineol were formed by oxidation of 1,8-cineole mediated by cytochrome P450, as demonstrated by a fumigation assay on flies previously treated with piperonyl butoxide, a P450 inhibitor, which showed an increase in toxicity of the EO and 1,8-cineole, supporting its participation in the formation of metabolites. We also demonstrated that 1,8-cineole acts as a P450 inhibitor-like compound, improving the toxicity of other xenobiotics such as deltamethrin.
International Pesticide Product Registration Requirements, 1999
Federal regulatory requirements for pesticides in Argentina are under the supervision of SENASA (... more Federal regulatory requirements for pesticides in Argentina are under the supervision of SENASA (The Official Argentinean Institution for the health and quality control of crops, vegetables and livestock derivatives). CEPROCOR (Center of Excellence on Products and ...
Several terpenoids and clerod-14-ene-3alpha, 4beta,13xi-triol (1), the main compound of V. tucuma... more Several terpenoids and clerod-14-ene-3alpha, 4beta,13xi-triol (1), the main compound of V. tucumanensis, were isolated and bioassayed. The clerodane 1 showed higher antifeedant activity than other related compounds. Structure-activity relationships are also discussed.
Treatment of 0-3-(but-3-enyIoxy)benzene (1) with anions -SPh, PPhz and - PO(0Et)z in ammonia, ace... more Treatment of 0-3-(but-3-enyIoxy)benzene (1) with anions -SPh, PPhz and - PO(0Et)z in ammonia, acetonitrile or dimethyl sulphoxide gives both direct substitution and cyclized products. The formation of the latter confirms the intermediacy of the 0-3-(but-3-enyIoxy) ...
Extracts from fruits and leaves of Melia azedarach were tested for repellent and insecticidal pro... more Extracts from fruits and leaves of Melia azedarach were tested for repellent and insecticidal properties against eggs and nymphs of Triatoma infestans, the vector of Chagas disease. Unripe fruit extract was highly repellent for first and fourth instar nymphs. Ripe fruit had a weaker effect while leaves were ineffective. No effects on egg hatching, nymph survival or development time were
Evidence-Based Complementary and Alternative Medicine, 2015
The antibacterial and cytotoxic effects of metabolites isolated from an antibacterial extract of ... more The antibacterial and cytotoxic effects of metabolites isolated from an antibacterial extract of Flourensia oolepis were evaluated. Bioguided fractionation led to five flavonoids, identified as 2',4'-dihydroxychalcone (1), isoliquiritigenin (2), pinocembrin (3), 7-hydroxyflavanone (4), and 7,4'-dihydroxy-3'-methoxyflavanone (5). Compound 1 showed the highest antibacterial effect, with minimum inhibitory concentration (MIC) values ranging from 31 to 62 and 62 to 250 μg/mL, against Gram-positive and Gram-negative bacteria, respectively. On further assays, the cytotoxic effect of compounds 1-5 was determined by MTT assay on acute lymphoblastic leukemia (ALL) and chronic myeloid leukemia (CML) cell lines including their multidrug resistant (MDR) phenotypes. Compound 1 induced a remarkable cytotoxic activity toward ALL cells (IC50 = 6.6-9.9 μM) and a lower effect against CML cells (IC50 = 27.5-30.0 μM). Flow cytometry was used to analyze cell cycle distribution and cell death by PI-labeled cells and by Annexin V/PI staining, respectively. Upon treatment, 1 induced cell cycle arrest in the G2/M phase accompanied by a strong induction of apoptosis. These results describe for the first time the antibacterial metabolites of F. oolepis extract, with 1 being the most effective. This chalcone also emerges as a selective cytotoxic agent against sensitive and resistant leukemic cells, highlighting its potential as a lead compound.
ABSTRACT Industrial Crops and Products j o u r n a l h o m e p a g e : w w w . e l s e v i e r . ... more ABSTRACT Industrial Crops and Products j o u r n a l h o m e p a g e : w w w . e l s e v i e r . c o m / l o c a t e / i n d c r o p Insecticidal toxicity of Eucalyptus cinerea essential oil and 1,8-cineole against Musca domestica and possible uses according to the metabolic response of flies a b s t r a c t In a fumigant assay, Musca domestica adults treated with Eucalyptus cinerea EO [LC 50 = 5.5 mg/dm 3 ; majority component by SPME–GC: 1,8-cineole (88.5%), ␣-pinene (2%), ␣-terpineol (9%)], died within 15 min or less. The terpenes absorbed by the flies and their metabolites, analyzed using SPME fiber, were 1,8-cineole (LC 50 = 3.3 mg/dm 3), ␣-pinene (LC 50 = 11.5 mg/dm 3), ␣-terpineol (LC 50 = 36.8 mg/dm 3) and a new component 2,3-dehydro-1,8-cineole, in proportions of 74%, 0.1%, 24.7% and 1.2% respectively. 2,3-Dehydro-1,8-cineole and ␣-terpineol were formed by oxidation of 1,8-cineole mediated by cytochrome P450, as demonstrated by a fumigation assay on flies previously treated with piperonyl butoxide, a P450 inhibitor, which showed an increase in toxicity of the EO and 1,8-cineole, supporting its participation in the formation of metabolites. We also demonstrated that 1,8-cineole acts as a P450 inhibitor-like compound, improving the toxicity of other xenobiotics such as deltamethrin.
International Pesticide Product Registration Requirements, 1999
Federal regulatory requirements for pesticides in Argentina are under the supervision of SENASA (... more Federal regulatory requirements for pesticides in Argentina are under the supervision of SENASA (The Official Argentinean Institution for the health and quality control of crops, vegetables and livestock derivatives). CEPROCOR (Center of Excellence on Products and ...
Several terpenoids and clerod-14-ene-3alpha, 4beta,13xi-triol (1), the main compound of V. tucuma... more Several terpenoids and clerod-14-ene-3alpha, 4beta,13xi-triol (1), the main compound of V. tucumanensis, were isolated and bioassayed. The clerodane 1 showed higher antifeedant activity than other related compounds. Structure-activity relationships are also discussed.
Treatment of 0-3-(but-3-enyIoxy)benzene (1) with anions -SPh, PPhz and - PO(0Et)z in ammonia, ace... more Treatment of 0-3-(but-3-enyIoxy)benzene (1) with anions -SPh, PPhz and - PO(0Et)z in ammonia, acetonitrile or dimethyl sulphoxide gives both direct substitution and cyclized products. The formation of the latter confirms the intermediacy of the 0-3-(but-3-enyIoxy) ...
Extracts from fruits and leaves of Melia azedarach were tested for repellent and insecticidal pro... more Extracts from fruits and leaves of Melia azedarach were tested for repellent and insecticidal properties against eggs and nymphs of Triatoma infestans, the vector of Chagas disease. Unripe fruit extract was highly repellent for first and fourth instar nymphs. Ripe fruit had a weaker effect while leaves were ineffective. No effects on egg hatching, nymph survival or development time were
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