黄芪甲苷的生物样品稳定性考察及在大鼠体外肠菌中代谢-中国中药杂志.docVIP

黄芪甲苷在大鼠体外肠菌中代谢转化 孙桂霞1,1, 苗培培1, 杨晓燕1, 苗青1, 李静2, 薛宝娟1，苏谨1，张玉杰* (1.北京中医药大学 中药学院，北京 100102；2.北京积水潭医院 中药房，北京 100035) [摘要] 明确黄芪甲苷(AST)稳定性体外肠菌代谢产物及代谢途径。采用体外的方法对AST人工胃液人工液肝匀浆大鼠离体肠道菌群中的代谢产物进行探讨HPLC法测定AST在生物样本中的含量AST在生物样本中的。采用TLC、HPLCLC-MS/MS相结合的分析手段，鉴定代谢产物。结果AST在及肝脏均较稳定，代谢；AST肠道菌群的代谢是通过脱糖基逐级进行的。首先，失去3位木糖基转化成次生代谢产物环黄芪醇-6-O-β-D-吡喃葡萄糖(CMG)。然后，失去6位葡萄糖基得到极性更小的皂苷元环黄芪醇(CAG)。AST在体内主要在肠道代谢，发生糖基水解作用即肠道菌群的水解作用是AST代谢的主要原因。[关键词] 黄芪甲苷；稳定性；体外；肠菌代谢；代谢产物；代谢途径 Stability Study in biological samples and Metabolites Analysis of Astragaloside Ⅳ in rat intestinal bacteria in vitro SUN Gui-xia1, ZHAO Yuan-yuan1, MIAO Pei-pei1, YANG Xiao-yan1, MIAO Qing1, LI Jing2, XUE Bao-juan1, SU Jin1, ZHANG Yu-jie1* School of Chinese Pharmacy，Beijing University of Chinese Medicine，Beijing 100102，China；2．TCM Dispensary，Beijing JiShuiTan Hospital, Beijing 100035，China） [Abstract] To figure out the and intestinal bacteria metabolites of rats in vitro of Astragaloside Ⅳ(AST). This article explored the stability of AST in the artificial gastric juice、in the artificial intestinal juice and in rat liver homogenate and the metabolism in rat intestinal in vitro. HPLC was used to calculate the remaining rate of AST in biological samples by measuring the content of AST, while metabolites were determined by combining the methods of TLC、HPLC and C-MS/MS. It turned out that AST was stable in the artificial gastric juice、in the artificial intestinal juice and in rat liver, that is to say, difficultly metabolized . Also, the metabolic pathway of AST was stepped by deglycosylation. Firstly, AST was converted to its secondary etabolites(6-O-β-D-glucopyranosyl- cycloastragenol,CMG) by removal of xylose moiety at C-3 ,then transformed into cycloastragenol (CAG) after hydrolytic removal of the glucose moiety at C-6. All the results suggested that the metabolism of AST in vivo occurs mainly in the intestinal by hydrolysis of glycosyl. In conclusion, hydrolysis of intestinal flora is the main reason that AST metabolizes.