AIM:To investigate the chemical constituents of the stems,leaves and roots of Euphorbia hirta,and to test for the cytotoxic and antimicrobial potentials of the major constituents of the plant.METHODS: The compounds we...AIM:To investigate the chemical constituents of the stems,leaves and roots of Euphorbia hirta,and to test for the cytotoxic and antimicrobial potentials of the major constituents of the plant.METHODS: The compounds were isolated by silica gel chromatography and their structures were elucidated by NMR spectroscopy.The cytotoxicity tests were conducted using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) assay,while the antimicrobial tests employed the agar well method.RESULTS: The air-dried stems of E.hirta afforded taraxerone 1,a mixture of 25-hydroperoxycycloart-23-en-3-ol(2a) and 24-hydroperoxycycloart-25-en-3-ol(2b)(sample 2) in a 2:1 ratio,and another mixture of cycloartenol(3a),lupeol(3b),-amyrin(3c) and-amyrin(3d)(sample 3) in a 0.5:4:1:1 ratio.The air-dried leaves of E.hirta yielded sample 2 in a 3:2 ratio,sample 3 in a 2:3:1:1 ratio,phytol and phytyl fatty acid ester,while the roots afforded sample 2 in a 2:1 ratio,sample 3 in a 2:1:1:1 ratio,a mixture of cycloartenyl fatty acid ester 4a,lupeol fatty acid ester 4b,-amyrin fatty acid ester 4c and-amyrin fatty acid ester 4d(sample 4) in a 3:2:1:1 ratio,linoleic acid,-sitosterol and squalene.Compound 1 from the stems,sample 2 from the leaves,and sample 3 from the stems were assessed for cytotoxicity against a human cancer cell line,colon carcinoma(HCT 116).Sample 2 showed good activity with an IC50 value of 4.8 g·mL 1,while 1 and sample 3 were inactive against HCT 116.Sample 2 was further tested for cytotoxicity against non-small cell lung adenocarcinoma(A549).It showed good activity against this cell line with an IC50 value of 4.5 g·mL 1.Antimicrobial assays were conducted on 1 and sample 2.Results of the study indicated that 1 was active against the bacteria: Pseudomonas aeruginosa and Staphylococcus aureus,but was inactive against Escherichia coli and Bacillus subtilis.Sample 2 was active against the bacteria: Pseudomonas aeruginosa,Staphylococcus aureus and Escherichia coli and fungi: Candida albicans and Trichophyton mentagrophytes.It was inactive against Bacillus subtilis and Aspergillus niger.CONCLUSIONS: The triterpenes: 2a,2b,3a,3b,3c and 3d were obtained from the stems,roots and leaves of E.hirta.Taraxerol(1) was only isolated from the stems,the leaves yielded phytol and phytyl fatty acid esters,while the roots afforded 4a-4d,linoleic acid,-sitosterol,and squalene.Triterpene 1 and sample 2 were found to exhibit antimicrobial activities.Thus,these compounds are some of the active principles of E.hirta which is used in wound healing and the treatment of boils.The cytotoxic properties of sample 2 imply that triterpenes 2a and 2b contribute to the anticancer activity of E.hirta.展开更多
AIM: To screen for the antibacterial activity of ent-kaurenoic acid (1) from the dichloromethane extract of Smallanthus sonchifolius leaves against Staphylococcus aureus, Staphylococcus epidermidis, Bacillus subtilis,...AIM: To screen for the antibacterial activity of ent-kaurenoic acid (1) from the dichloromethane extract of Smallanthus sonchifolius leaves against Staphylococcus aureus, Staphylococcus epidermidis, Bacillus subtilis, Escherichia coli, Enterobacter aerogenes, Klebsiella pneumoniae, and Pseudomonas aeruginosa, and for its antifungal activity against Candida albicans, Trichophyton rubrum, and Epidermophyton floccosum. METHODS: Compound 1 was isolated by silica gel chromatography and its structure was elucidated by NMR spectroscopy. For assaying the antibacterial and antifungal activities of 1, the disk diffusion method was used, while the minimum inhibitory concentrations (MICs) were determined by the broth dilution method. RESULTS: With the disk diffusion method, 1 was found to be active against all the Gram-positive organisms tested (S. aureus, S. epidermidis, B. subtilis) at the lowest concentration of 1 000 μg·mL-1, while it was active against the fungus T. rubrum at 10 000 μg·mL-1. No inhibitory activity was observed against C. albicans, E. floccosum and all the Gram-negative test strains. The activity indices (AI) of 1 were noted to be highest against S. aureus and lowest against T. rubrum. Statistically significant differences were found between the mean inhibition zones (IZ) of 1 and the standard drugs (ofloxacin and clotrimazole). The results of the broth dilution MIC determination revealed that 1 exhibited moderate activity against S. aureus and S. epidermidis with MIC values of 125 μg·mL-1 and 250 μg·mL-1, respectively; and weak activity against B. subtilis with a MIC of 1 000 μg·mL-1. The growth of T. rubrum in the MIC assay was not inhibited at the highest tested concentration of 1 (10 000 μg·mL-1). CONCLUSION: The minimum bactericidal concentration (MBC) indicated that the bactericidal activities of 1 occurred at concentrations higher than its growth inhibitory concentrations. Furthermore, the MBC: MIC ratio of 2 : 1 clearly demonstrated the in vitro bactericidal effect of 1 against S. aureus and S. epidermidis.展开更多
AIM:To investigate the chemical constituents of Glinus oppositifolius.METHODS:The compounds were isolated by silica gel chromatography.The structure of the new triterpene was elucidated by extensive 1D and 2D NMR spec...AIM:To investigate the chemical constituents of Glinus oppositifolius.METHODS:The compounds were isolated by silica gel chromatography.The structure of the new triterpene was elucidated by extensive 1D and 2D NMR spectroscopy.RESULTS:The dichloromethane extract of the air-dried leaves of Glinus oppositifolius afforded a new triterpene,oppositifolone(1),spinasterol(2),squalene(3) and lutein(4).The structure of 1 was elucidated by NMR spectroscopy,while 2-4 were identified by comparison of their 13C NMR data with those reported in the literature.CONCLUSION:A new triterpene was isolated from G.oppositifolius.展开更多
基金supported by the grant from the De La Salle University Science Foundation
文摘AIM:To investigate the chemical constituents of the stems,leaves and roots of Euphorbia hirta,and to test for the cytotoxic and antimicrobial potentials of the major constituents of the plant.METHODS: The compounds were isolated by silica gel chromatography and their structures were elucidated by NMR spectroscopy.The cytotoxicity tests were conducted using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) assay,while the antimicrobial tests employed the agar well method.RESULTS: The air-dried stems of E.hirta afforded taraxerone 1,a mixture of 25-hydroperoxycycloart-23-en-3-ol(2a) and 24-hydroperoxycycloart-25-en-3-ol(2b)(sample 2) in a 2:1 ratio,and another mixture of cycloartenol(3a),lupeol(3b),-amyrin(3c) and-amyrin(3d)(sample 3) in a 0.5:4:1:1 ratio.The air-dried leaves of E.hirta yielded sample 2 in a 3:2 ratio,sample 3 in a 2:3:1:1 ratio,phytol and phytyl fatty acid ester,while the roots afforded sample 2 in a 2:1 ratio,sample 3 in a 2:1:1:1 ratio,a mixture of cycloartenyl fatty acid ester 4a,lupeol fatty acid ester 4b,-amyrin fatty acid ester 4c and-amyrin fatty acid ester 4d(sample 4) in a 3:2:1:1 ratio,linoleic acid,-sitosterol and squalene.Compound 1 from the stems,sample 2 from the leaves,and sample 3 from the stems were assessed for cytotoxicity against a human cancer cell line,colon carcinoma(HCT 116).Sample 2 showed good activity with an IC50 value of 4.8 g·mL 1,while 1 and sample 3 were inactive against HCT 116.Sample 2 was further tested for cytotoxicity against non-small cell lung adenocarcinoma(A549).It showed good activity against this cell line with an IC50 value of 4.5 g·mL 1.Antimicrobial assays were conducted on 1 and sample 2.Results of the study indicated that 1 was active against the bacteria: Pseudomonas aeruginosa and Staphylococcus aureus,but was inactive against Escherichia coli and Bacillus subtilis.Sample 2 was active against the bacteria: Pseudomonas aeruginosa,Staphylococcus aureus and Escherichia coli and fungi: Candida albicans and Trichophyton mentagrophytes.It was inactive against Bacillus subtilis and Aspergillus niger.CONCLUSIONS: The triterpenes: 2a,2b,3a,3b,3c and 3d were obtained from the stems,roots and leaves of E.hirta.Taraxerol(1) was only isolated from the stems,the leaves yielded phytol and phytyl fatty acid esters,while the roots afforded 4a-4d,linoleic acid,-sitosterol,and squalene.Triterpene 1 and sample 2 were found to exhibit antimicrobial activities.Thus,these compounds are some of the active principles of E.hirta which is used in wound healing and the treatment of boils.The cytotoxic properties of sample 2 imply that triterpenes 2a and 2b contribute to the anticancer activity of E.hirta.
文摘AIM: To screen for the antibacterial activity of ent-kaurenoic acid (1) from the dichloromethane extract of Smallanthus sonchifolius leaves against Staphylococcus aureus, Staphylococcus epidermidis, Bacillus subtilis, Escherichia coli, Enterobacter aerogenes, Klebsiella pneumoniae, and Pseudomonas aeruginosa, and for its antifungal activity against Candida albicans, Trichophyton rubrum, and Epidermophyton floccosum. METHODS: Compound 1 was isolated by silica gel chromatography and its structure was elucidated by NMR spectroscopy. For assaying the antibacterial and antifungal activities of 1, the disk diffusion method was used, while the minimum inhibitory concentrations (MICs) were determined by the broth dilution method. RESULTS: With the disk diffusion method, 1 was found to be active against all the Gram-positive organisms tested (S. aureus, S. epidermidis, B. subtilis) at the lowest concentration of 1 000 μg·mL-1, while it was active against the fungus T. rubrum at 10 000 μg·mL-1. No inhibitory activity was observed against C. albicans, E. floccosum and all the Gram-negative test strains. The activity indices (AI) of 1 were noted to be highest against S. aureus and lowest against T. rubrum. Statistically significant differences were found between the mean inhibition zones (IZ) of 1 and the standard drugs (ofloxacin and clotrimazole). The results of the broth dilution MIC determination revealed that 1 exhibited moderate activity against S. aureus and S. epidermidis with MIC values of 125 μg·mL-1 and 250 μg·mL-1, respectively; and weak activity against B. subtilis with a MIC of 1 000 μg·mL-1. The growth of T. rubrum in the MIC assay was not inhibited at the highest tested concentration of 1 (10 000 μg·mL-1). CONCLUSION: The minimum bactericidal concentration (MBC) indicated that the bactericidal activities of 1 occurred at concentrations higher than its growth inhibitory concentrations. Furthermore, the MBC: MIC ratio of 2 : 1 clearly demonstrated the in vitro bactericidal effect of 1 against S. aureus and S. epidermidis.
基金supported by the grant fromthe Accelerated Science and Technology Human Resource Development Program of the Department of Science and Technology of the Philippinesthe Department of Environment and Natural Resources of the Philippines for the permit(Wildlife Gratuitous Permit No.2011-01)to collect the sample
基金supported by Science Foundation of De La Salle University
文摘AIM:To investigate the chemical constituents of Glinus oppositifolius.METHODS:The compounds were isolated by silica gel chromatography.The structure of the new triterpene was elucidated by extensive 1D and 2D NMR spectroscopy.RESULTS:The dichloromethane extract of the air-dried leaves of Glinus oppositifolius afforded a new triterpene,oppositifolone(1),spinasterol(2),squalene(3) and lutein(4).The structure of 1 was elucidated by NMR spectroscopy,while 2-4 were identified by comparison of their 13C NMR data with those reported in the literature.CONCLUSION:A new triterpene was isolated from G.oppositifolius.
