大鼠肠内菌对毛冬青皂苷ilexsaponin A<sub>1</sub>的代谢转化

赵钟祥; 李美芬; 林朝展; 熊天琴; 祝晨蔯

大鼠肠内菌对毛冬青皂苷ilexsaponin A₁的代谢转化

广州中医药大学中药学院

基金项目: 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）

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出版历程
- 刊出日期: 2011-08-24

Metabolic transformation of ilexsaponin A₁ by intestinal flora

摘要

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(250 mm×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。
- 毛冬青 /
- 肠内菌群 /
- 代谢 /
- 生物转化
Abstract: A high-performance liquid chromatography method was used to investigate the metabolic transformation characteristics of ilexsaponin A₁ by rat intestinal flora in vitro and in vivo.The HPLC separation was performed on a reversed-phase Kromasil 100-5 C₁₈column (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 flora of rats.In vivo samples including feces and urine samples were collected individually after oral administration of ilexsaponin A₁ to healthy rats.Then the in vivo and in vitro metabolism of ilexsaponin A₁ was investigated using the established HPLC method.The results showed that ilexsaponin A₁ could be metabolized to its aglycone (ilexgenin A) by rat intestinal flora in vitro,and after incubating for 48 h,about 93.12% of ilexsaponin A₁ was metabolized to ilexgenin A.In vivo,ilexsaponin A₁ and its aglycone were found in feces,but not in urine.It was found that ilexsaponin A₁could 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.
- Ilex pubescens Hook et Arn /
- intestinal flora /
- metabolism /
- biotransformation