蒙古黄芪中黄酮类成分在大鼠肝微粒体的体外代谢

Metabolism of Flavonoid Constituents in Astrgalus membranaceus( Fisch. ) Bge. var.mongholicus( Bge. ) Hsiao in Rat Liver Microsomes

目的考察蒙古黄芪中黄酮类有效成分在大鼠肝微粒体的降解速度及降解途径。方法将黄芪药材提取液与大鼠肝微粒体进行体外共孵育。采用高效液相色谱法测定三种黄酮类成分毛蕊异黄酮苷、毛蕊异黄酮及芒柄花素的剩余含量。结果三种黄酮类成分的代谢率分别为22.64%,31.18%和55.42%,一级降解速度常数分别为0.267 h-1(r=0.992),0.386 h-1(r=0.991)和0.826 h-1(r=0.996)。结论三种黄酮类成分经大鼠肝微粒体代谢,呈表观一级线性消除,毛蕊异黄酮苷被水解生成毛蕊异黄酮。

Objective To investigate the metabolism mechanism and the degradation rate of flavonoid constituents in Astrgalus membranaceus （ Fisch. ）Bge. var. mongholicus （Bge.）Hsiao in rat liver microsomes. Methods The extract of Astrgalus membra- naceus（ Fisch. ） Bge. var. mongholicus（ Bge. ） Hsiao were incubated with rat liver microsomes at 37℃. The residual of calycosin - 7 - O - β - D - glucoside, calycosin and formononetin were determined by HPLC - UV detection. Results The metabolic rates of calycosin - 7 - O - β - D - glucoside, calycosin and formononetin in rat liver microsomes were 22.64%, 31. 18% and 55.42%, respectively. And the first - order degradation rate constants were 0. 267 h-1 （ r = 0. 992）, 0. 386 h-1（ r = 0. 991 ） and 0. 826 h - 1 （ r = 0. 996）, respectively. Conclusion Three flavonoid constituents were metabolism by rat liver microsomes and their degradation followed first - order rate. Calycosin - 7 - O - β - D - glucoside was degradated to calycosin.