大鼠肠内菌对毛冬青皂苷ilexsaponin A_1的代谢转化  

Metabolic transformation of ilexsaponin A_1 by intestinal flora

作　　者：赵钟祥[1] 李美芬[1] 林朝展[1] 熊天琴[1] 祝晨蔯[1] 

机构地区：[1]广州中医药大学中药学院,广州510006

出　　处：《中国药科大学学报》2011年第4期329-332,共4页Journal of China Pharmaceutical University

基　　金：国家自然科学基金资助项目(No.30901954);广东省自然科学基金资助项目(No.9451040701003203);高等学校博士学科点专项科研基金资助项目(No.20094425110008);广州中医药大学创新基金资助项目(No.09CX015)~~

摘　　要：采用HPLC法研究大鼠肠内菌对毛冬青皂苷ilexsaponin A1的代谢作用。研究采用Kromasil 100-5 C18(250mm×4.6 mm)为色谱柱,流动相为乙腈-0.02%三氟乙酸梯度洗脱,流速:1.0 mL/min,柱温:30℃。将ilexsaponin A1加至大鼠肠内菌培养液中,温孵一定时间后,分析体外代谢产物和代谢模式;大鼠灌胃给予ilexsaponin A1,分析尿液和粪便中的代谢产物,同时测定粪便样品中原型物和代谢产物的含量。结果表明,离体培养大鼠肠内菌可代谢ilexsaponin A1,其主要代谢产物为其苷元ilexgenin A,培养48 h后,约93.12%的ilexsaponin A1被转化成ilexgenin A;大鼠在体实验中,尿液未检测到原型物及代谢物,在粪便中可检测到原型物和代谢物苷元ilexgenin A;ilexsaponin A1经口给予后经原物和代谢产物ilexgenin A排除体外的量高达89.85%。研究结果表明:ilexsaponin A1经口给予后大部分经肠内菌群代谢后被排出体外,主要代谢产物为其苷元。A high-performance liquid chromatography method was used to investigate the metabolic transforma-tion characteristics of ilexsaponin A1 by rat intestinal flora in vitro and in vivo.The HPLC separation was per-formed on a reversed-phase Kromasil 100-5 C18 column（250 mm × 4.6 mm） at a temperature of 30 °C and the mobile phase system consists of acetonitrile and trifluoroacetic acid（0.02%） in water using a gradient elution with the flow rate of 1.0 mL/min.In vitro samples were prepared by incubating ilexsaponin A1 with intestinal flo-ra of rats.In vivo samples including feces and urine samples were collected individually after oral administration olized to ilexgenin A.In vivo,ilexsaponin A1 and its aglycone were found in feces,but not in urine.It was foundof ilexsaponin A1 to healthy rats.Then the in vivo and in vitro metabolism of ilexsaponin A1 was investigated usingthe established HPLC method.The results showed that ilexsaponin A1 could be metabolized to its aglycone（ilex-genin A） by rat intestinal flora in vitro,and after incubating for 48 h,about 93.12% of ilexsaponin A1 was metab-that ilexsaponin A1 could be metabolized to its aglycone by intestinal flora in vitro and in vivo,and after oral administration about 89.85% of ilexsaponin A1 was exerceted as its prototype and metabolites.

关 键 词：毛冬青 肠内菌群 代谢 生物转化 

分 类 号：R284[医药卫生—中药学] R969.1[医药卫生—中医学]