Saikosaponins(SSs)are the main active components extracted from Bupleuri Radix(BR)which has been used as an important herbal drug in Asian countries for thousands of years.It has been reported that the intestinal bact...Saikosaponins(SSs)are the main active components extracted from Bupleuri Radix(BR)which has been used as an important herbal drug in Asian countries for thousands of years.It has been reported that the intestinal bacteria plays an important role in the in vivo disposal of oral SSs.Although the deglycosylated derivatives(saikogenins,SGs)of SSs metabolized by the intestinal bacteria are speculated to be the main components absorbed into the blood after oral administration of SSs,no studies have been reported on the characteristics of SGs for their intestinal absorption,and those for SSs are also limited.Therefore,a rapid UHPLC-MS/MS method was developed to investigate and compare the apparent permeability of three common SSs(SSa,SSd,SSb2)and their corresponding SGs(SGF,SGG,SGD)through a bidirectional transport experiment on Caco-2 cell monolayer model.The method was validated according to the latest FDA guidelines and applied to quantify the six analytes in transport medium samples extracted via liquid-liquid extraction(LLE).The apparent permeability coefficient(Papp)determined in this study indicated that the permeability of SGs improved to the moderate class compared to the corresponding parent compounds,predicting a higher in vivo absorption.Moreover,the efflux ratio(ER)value demonstrated an active uptake of SSd and the three SGs,while a passive diffusion of SSa and SSb2.展开更多
AIM: To study the chemical constituents from the roots of Bupleurum bicaule Helm(Apiaceae). METHOD: Silica gel, Sephadex LH-20, MPLC Rp-C18 column chromatography, and HPLC were used for isolation of compounds. The str...AIM: To study the chemical constituents from the roots of Bupleurum bicaule Helm(Apiaceae). METHOD: Silica gel, Sephadex LH-20, MPLC Rp-C18 column chromatography, and HPLC were used for isolation of compounds. The structures were elucidated on the basis of 1D- and 2D-NMR technology and HRESI-MS. Compounds were evaluated in vitro for their inhibitory ability against the proliferation of rat mesangial cells by the MTT method. RESULTS: Twelve compounds were isolated, and their structures were identified on the basis of their spectroscopic and ico-chemical properties as 13, 28-epoxy-olean-11-en-3-one(1), saikogenin E(2), saikogenin G(3), 11α-methoxy-3β, 16β, 23, 28-tetrahydroxyolean-12-ene(4), saikogenin D(5), prosaikogenin F(6), prosaikogenin A(7), prosaikogenin G(8), prosaikogenin D(9), laccaic acid(10), methyl gallate(11), and ethyl gallate(12). Compounds 1, 2, 7, 8, and 10 were observed to have inhibitory activity against mesangial cell proliferationin to different degrees. CONCLUSION: Compound 1, 8, and 10 exhibit significant inhibitory effects on rat mesangial cell proliferation induced by Ang II.展开更多
基金project was financially supported by the National Natural Science Foundation of China(No.81573626)the Open Project Program of Guangxi Key Laboratory of Traditional Chinese Medicine Quality Standards,China(No.201503)+1 种基金the Natural Research Foundation of Jiangsu Province,China(No.BK20161456)the Qing Lan Project of Jiangsu Province,China(2017)。
文摘Saikosaponins(SSs)are the main active components extracted from Bupleuri Radix(BR)which has been used as an important herbal drug in Asian countries for thousands of years.It has been reported that the intestinal bacteria plays an important role in the in vivo disposal of oral SSs.Although the deglycosylated derivatives(saikogenins,SGs)of SSs metabolized by the intestinal bacteria are speculated to be the main components absorbed into the blood after oral administration of SSs,no studies have been reported on the characteristics of SGs for their intestinal absorption,and those for SSs are also limited.Therefore,a rapid UHPLC-MS/MS method was developed to investigate and compare the apparent permeability of three common SSs(SSa,SSd,SSb2)and their corresponding SGs(SGF,SGG,SGD)through a bidirectional transport experiment on Caco-2 cell monolayer model.The method was validated according to the latest FDA guidelines and applied to quantify the six analytes in transport medium samples extracted via liquid-liquid extraction(LLE).The apparent permeability coefficient(Papp)determined in this study indicated that the permeability of SGs improved to the moderate class compared to the corresponding parent compounds,predicting a higher in vivo absorption.Moreover,the efflux ratio(ER)value demonstrated an active uptake of SSd and the three SGs,while a passive diffusion of SSa and SSb2.
基金supported by the Fund of Program for Traditional Chinese Medicine Scientific Research on Public Health Care(No.201107007)
文摘AIM: To study the chemical constituents from the roots of Bupleurum bicaule Helm(Apiaceae). METHOD: Silica gel, Sephadex LH-20, MPLC Rp-C18 column chromatography, and HPLC were used for isolation of compounds. The structures were elucidated on the basis of 1D- and 2D-NMR technology and HRESI-MS. Compounds were evaluated in vitro for their inhibitory ability against the proliferation of rat mesangial cells by the MTT method. RESULTS: Twelve compounds were isolated, and their structures were identified on the basis of their spectroscopic and ico-chemical properties as 13, 28-epoxy-olean-11-en-3-one(1), saikogenin E(2), saikogenin G(3), 11α-methoxy-3β, 16β, 23, 28-tetrahydroxyolean-12-ene(4), saikogenin D(5), prosaikogenin F(6), prosaikogenin A(7), prosaikogenin G(8), prosaikogenin D(9), laccaic acid(10), methyl gallate(11), and ethyl gallate(12). Compounds 1, 2, 7, 8, and 10 were observed to have inhibitory activity against mesangial cell proliferationin to different degrees. CONCLUSION: Compound 1, 8, and 10 exhibit significant inhibitory effects on rat mesangial cell proliferation induced by Ang II.
