Objective:To isolate,purify,and characterize gossypol from the fruits of Thespesia populnea(L)Sol.ex Correa,test its antidermatophytic activity,identify its targets on the dermatophyte,and confirm the binding of gossy...Objective:To isolate,purify,and characterize gossypol from the fruits of Thespesia populnea(L)Sol.ex Correa,test its antidermatophytic activity,identify its targets on the dermatophyte,and confirm the binding of gossypol with the fungal target by molecular docking study.Methods:Gossypol from Thespesia populnea was characterized by high performance liquid chromatography,liquid chromatographmass spectrometry,Fourier transform infrared spectroscopy,and nuclear magnetic resonance.The anti-dermatophytic activity of gossypol was tested against four different dermatophytes,viz.Trichophyton mentagrophytes,Trichophyton rubrum,Microsporum canis,and Microsporum gypseum.Trichophyton mentagrophytes was selected for further studies.The inhibitory mode of action of gossypol on Trichophyton mentagrophytes was determined by analyzing the modulation of gene expression in various pathways of the dermatophyte.Results:Gossypol inhibited all the dermatophytes.The minimum inhibitory concentrations were 12.5μg/mL for Trichophyton mentagrophytes and Microsporum canis and 25μg/mL for Trichophyton rubrum and Microsporum gypseum.The minimum fungicidal concentrations were 50μg/mL for Trichophyton mentagrophytes,100μg/mL for Microsporum canis and Trichophyton rubrum,and 200μg/mL for Microsporum gypseum.Gossypol inhibited the mRNA expression of metalloprotease(MEP4)and isocitrate lyase(ICL).The binding of gossypol with the enzymes was confirmed by molecular docking studies.The best docking poses were found and the low binding energies were recorded with the two target enzymes.Conclusions:Gossypol is a potential antifungal agent and can be further explored as an anti-dermatophytic drug.展开更多
[Objectives]To establish a quality standard method for detecting rutin in leaves of Thespesia populnea.[Methods]The leaves of T.populnea as a reagent,the rutin in the leaves of T.populnea was extracted by alcohol extr...[Objectives]To establish a quality standard method for detecting rutin in leaves of Thespesia populnea.[Methods]The leaves of T.populnea as a reagent,the rutin in the leaves of T.populnea was extracted by alcohol extraction,and quantitatively analyzed by high performance liquid chromatography(HPLC).[Results]In the range of 0.21-3.36μg,the peak area A of rutin in the leaves of T.populnea had a good linear relationship with its injection volume m.A=1561.6 m-6.893,and the correlation coefficient r=1.0000.The method was applied to the determination of rutin ethyl acetate extract in the leaves of T.populnea,the average recovery rate was 101.75%,and the RSD was 1.32%.[Conclusions]This method is simple and feasible,the results are accurate,the repeatability is good,and the separation effect is good.It is expected to provide a scientific idea for the determination of rutin in the leaves of T.populnea.展开更多
Objective:To evaluate antidiarrheal activity of the fractions of aqueous extract from stem barks of Thespesia populnea（Malvaceae）.Methods:From the aqueous extract three fractions namely ethyl acetate fraction（EAF）...Objective:To evaluate antidiarrheal activity of the fractions of aqueous extract from stem barks of Thespesia populnea（Malvaceae）.Methods:From the aqueous extract three fractions namely ethyl acetate fraction（EAF）,methanolic fraction（MF） and residue fraction（RF） were made and stuthed for antidiarrheal activity.Antidiarrheal activity of the fractions were evaluated in castor oil induced diarrhea,prostaglandin E<sub>2</sub>（PG-E<sub>2</sub>） induced diarrhea and charcoal meal test as in vivo models and the most potent fraction was further evaluated with in vitro models to determine the possible antimotility effect.Results:In castor oil induced diarrhea model,the RF（10,25,50 and 100 mg/kg,po.） and MF（100 mg/kg,po.） has significantly reduced the cumulative wet faecal mass,where as the EAF have not shown any significant antidiarrheal activity,RF was found to be more potent than MF.Based on these results and percentage yield,only RF was evaluated in PGE<sub>2</sub> induced enteropooling and charcoal meal test.RF（10,25 and 50 mg/kg） had shown significant inhibition of PG-E<sub>2</sub> induced secretions（antisecretory） and decreased the movement of charcoal in charcoal meal test indicating its antimotility activity.Furthermore,RF has showed significant inhibition of acetylcholine,histamine and BaCl<sub>2</sub> induced contractions on rat colon,guinea pig ileum and rabbit jejunum with EC<sub>50</sub> values of 241.7,303.1 and 286.1μg/mL,respectively indicating the antimotility effect of RF.The phytochemical analysis of RF showed presence of gums and mucilages and the possible mechanism may be the combination inhibition of elevated prostaglandin biosynthesis and reduced propulsive movement of the intestine.Conclusions: RF possesses good antidiarrheal activity comparing with other two fractions and the possible mechanism thought to be associated with combination of antisecretory and antimolity.展开更多
文摘Objective:To isolate,purify,and characterize gossypol from the fruits of Thespesia populnea(L)Sol.ex Correa,test its antidermatophytic activity,identify its targets on the dermatophyte,and confirm the binding of gossypol with the fungal target by molecular docking study.Methods:Gossypol from Thespesia populnea was characterized by high performance liquid chromatography,liquid chromatographmass spectrometry,Fourier transform infrared spectroscopy,and nuclear magnetic resonance.The anti-dermatophytic activity of gossypol was tested against four different dermatophytes,viz.Trichophyton mentagrophytes,Trichophyton rubrum,Microsporum canis,and Microsporum gypseum.Trichophyton mentagrophytes was selected for further studies.The inhibitory mode of action of gossypol on Trichophyton mentagrophytes was determined by analyzing the modulation of gene expression in various pathways of the dermatophyte.Results:Gossypol inhibited all the dermatophytes.The minimum inhibitory concentrations were 12.5μg/mL for Trichophyton mentagrophytes and Microsporum canis and 25μg/mL for Trichophyton rubrum and Microsporum gypseum.The minimum fungicidal concentrations were 50μg/mL for Trichophyton mentagrophytes,100μg/mL for Microsporum canis and Trichophyton rubrum,and 200μg/mL for Microsporum gypseum.Gossypol inhibited the mRNA expression of metalloprotease(MEP4)and isocitrate lyase(ICL).The binding of gossypol with the enzymes was confirmed by molecular docking studies.The best docking poses were found and the low binding energies were recorded with the two target enzymes.Conclusions:Gossypol is a potential antifungal agent and can be further explored as an anti-dermatophytic drug.
基金Supported by Subproject of Open Program of Key Laboratory of Guangxi Zhuang and Yao Medicine(GXZYKF2019-7)Project of Traditional Chinese Medicine Analysis(First-class Discipline in 2020)(05020044).
文摘[Objectives]To establish a quality standard method for detecting rutin in leaves of Thespesia populnea.[Methods]The leaves of T.populnea as a reagent,the rutin in the leaves of T.populnea was extracted by alcohol extraction,and quantitatively analyzed by high performance liquid chromatography(HPLC).[Results]In the range of 0.21-3.36μg,the peak area A of rutin in the leaves of T.populnea had a good linear relationship with its injection volume m.A=1561.6 m-6.893,and the correlation coefficient r=1.0000.The method was applied to the determination of rutin ethyl acetate extract in the leaves of T.populnea,the average recovery rate was 101.75%,and the RSD was 1.32%.[Conclusions]This method is simple and feasible,the results are accurate,the repeatability is good,and the separation effect is good.It is expected to provide a scientific idea for the determination of rutin in the leaves of T.populnea.
文摘Objective:To evaluate antidiarrheal activity of the fractions of aqueous extract from stem barks of Thespesia populnea（Malvaceae）.Methods:From the aqueous extract three fractions namely ethyl acetate fraction（EAF）,methanolic fraction（MF） and residue fraction（RF） were made and stuthed for antidiarrheal activity.Antidiarrheal activity of the fractions were evaluated in castor oil induced diarrhea,prostaglandin E<sub>2</sub>（PG-E<sub>2</sub>） induced diarrhea and charcoal meal test as in vivo models and the most potent fraction was further evaluated with in vitro models to determine the possible antimotility effect.Results:In castor oil induced diarrhea model,the RF（10,25,50 and 100 mg/kg,po.） and MF（100 mg/kg,po.） has significantly reduced the cumulative wet faecal mass,where as the EAF have not shown any significant antidiarrheal activity,RF was found to be more potent than MF.Based on these results and percentage yield,only RF was evaluated in PGE<sub>2</sub> induced enteropooling and charcoal meal test.RF（10,25 and 50 mg/kg） had shown significant inhibition of PG-E<sub>2</sub> induced secretions（antisecretory） and decreased the movement of charcoal in charcoal meal test indicating its antimotility activity.Furthermore,RF has showed significant inhibition of acetylcholine,histamine and BaCl<sub>2</sub> induced contractions on rat colon,guinea pig ileum and rabbit jejunum with EC<sub>50</sub> values of 241.7,303.1 and 286.1μg/mL,respectively indicating the antimotility effect of RF.The phytochemical analysis of RF showed presence of gums and mucilages and the possible mechanism may be the combination inhibition of elevated prostaglandin biosynthesis and reduced propulsive movement of the intestine.Conclusions: RF possesses good antidiarrheal activity comparing with other two fractions and the possible mechanism thought to be associated with combination of antisecretory and antimolity.
