Eleven 1-(1H-1,2,4-triazole)-2-(2,4-diflurophenyl)-3-(N-methyl-N-substituted benzylamino)-2-propanols were designed and synthesized, on the basis of the crystal structure of P450 cytochrome 14α-sterol demethylase(CYP...Eleven 1-(1H-1,2,4-triazole)-2-(2,4-diflurophenyl)-3-(N-methyl-N-substituted benzylamino)-2-propanols were designed and synthesized, on the basis of the crystal structure of P450 cytochrome 14α-sterol demethylase(CYP51) and the docking results of inhibitors to the active site of the enzyme. All title compounds were first by reported. Results of preliminary biological tests showed that most of title compounds exhibited activity against the seven common pathogenic fungi. Compound 11 showed best antifungal activity with broad antifungal spectrum and proved to be more active against Cryptococcus neoformans, Candida albicans, Microsporum lanosum and Trichophyton rubrum than ketoconazole. Compounds 3, 10 and 4 also had high activities.展开更多
The polyphenol content,antioxidant and antimicrobial activities of the extracts obtained by classical, ultrasonic and Soxhlet extractions from dry aerial parts of two Artemisia species(Artemisia vulgaris and Artemisia...The polyphenol content,antioxidant and antimicrobial activities of the extracts obtained by classical, ultrasonic and Soxhlet extractions from dry aerial parts of two Artemisia species(Artemisia vulgaris and Artemisia campestris)were compared.Ultrasound positively affected the yield of extractive substance and the kinetics of extraction,but the extract obtained by the classical extraction showed the highest antioxidant activities and contained higher total contents of phenolic compounds and flavonoids than the extracts obtained by two other extraction techniques.Both flavonoid aglycones(apigenin,quercetin,quercetin 3,3′-dimethyl ether)and flavonoid glycosides(rutin,hyperoside and kaempferol 3-rhamnoside)were identified by thin layer chromatograph(TLC)analysis in the extracts from both species.A.campestris extracts were richer in quercetin than A.vulgaris and its antimicrobial activity was also better than A.vulgaris.Extracts obtained from both species were found to be more effective on the tested yeasts than bacteria.The kinetics of the total extractive substances,such as phenolic,flavonoids and quercetin extraction,was successfully described by the model of unsteady-state diffusion.展开更多
A novel homoisoflavone typicalvone A （1）, together with two known compounds, n-heneicosane and p-hydroxy benzoic acid, were isolated from Aspidistra typica Baill. The structure of the new compound was elucidated by ...A novel homoisoflavone typicalvone A （1）, together with two known compounds, n-heneicosane and p-hydroxy benzoic acid, were isolated from Aspidistra typica Baill. The structure of the new compound was elucidated by sepctral techniques, viz. 1D, 2D NMR spectra and HR-ESI-MS. Compared with berberine hydrochloride, typicalvone A showed moderate anti-bacterial activities, especially against the Gram-negative Paeudomonas aeruginosa ATCC-9027 and Escherichia coli ATCC-25922, with MBC values of 1000 and 500 μg/mL, respectively. In addition, it exhibited weak inhibitory activities against the tumour cells.展开更多
文摘Eleven 1-(1H-1,2,4-triazole)-2-(2,4-diflurophenyl)-3-(N-methyl-N-substituted benzylamino)-2-propanols were designed and synthesized, on the basis of the crystal structure of P450 cytochrome 14α-sterol demethylase(CYP51) and the docking results of inhibitors to the active site of the enzyme. All title compounds were first by reported. Results of preliminary biological tests showed that most of title compounds exhibited activity against the seven common pathogenic fungi. Compound 11 showed best antifungal activity with broad antifungal spectrum and proved to be more active against Cryptococcus neoformans, Candida albicans, Microsporum lanosum and Trichophyton rubrum than ketoconazole. Compounds 3, 10 and 4 also had high activities.
基金Supported by the Ministry of Science and Environmental Protection,Republic of Serbia(172047)
文摘The polyphenol content,antioxidant and antimicrobial activities of the extracts obtained by classical, ultrasonic and Soxhlet extractions from dry aerial parts of two Artemisia species(Artemisia vulgaris and Artemisia campestris)were compared.Ultrasound positively affected the yield of extractive substance and the kinetics of extraction,but the extract obtained by the classical extraction showed the highest antioxidant activities and contained higher total contents of phenolic compounds and flavonoids than the extracts obtained by two other extraction techniques.Both flavonoid aglycones(apigenin,quercetin,quercetin 3,3′-dimethyl ether)and flavonoid glycosides(rutin,hyperoside and kaempferol 3-rhamnoside)were identified by thin layer chromatograph(TLC)analysis in the extracts from both species.A.campestris extracts were richer in quercetin than A.vulgaris and its antimicrobial activity was also better than A.vulgaris.Extracts obtained from both species were found to be more effective on the tested yeasts than bacteria.The kinetics of the total extractive substances,such as phenolic,flavonoids and quercetin extraction,was successfully described by the model of unsteady-state diffusion.
基金The Project of Department of Science in Sichuan Province(Grant No.14ZA0003)
文摘A novel homoisoflavone typicalvone A （1）, together with two known compounds, n-heneicosane and p-hydroxy benzoic acid, were isolated from Aspidistra typica Baill. The structure of the new compound was elucidated by sepctral techniques, viz. 1D, 2D NMR spectra and HR-ESI-MS. Compared with berberine hydrochloride, typicalvone A showed moderate anti-bacterial activities, especially against the Gram-negative Paeudomonas aeruginosa ATCC-9027 and Escherichia coli ATCC-25922, with MBC values of 1000 and 500 μg/mL, respectively. In addition, it exhibited weak inhibitory activities against the tumour cells.
