Objective To compare the difference of transformation profile and transformation rate of tecomin by using two in vitro liver metabolism models. Methods Liver microsomes and liver S9 fraction models were employed to transform tecomin. HPLC was used to determine the contents of tecomin and its metabolites at the detecting wavelength of 254 nm. The gradient elution (0–6 min, 5％–40％ A; 6–9 min, 40％–50％ A; 9–11 min, 50％–5％ A) was carried out by using mobile phase of acetonitrile (A) - 1％ acetic acid (B) at a flow rate of 1 mL/min. Results Both models could transform tecomin into veratric acid; however, the metabolites obtained with liver S9 were more than those obtained with liver microsomes, and the transformation rate of the former was higher than that of the latter. Conclusion The liver S9 fraction can more efficiently transform esters than liver microsomes.%目的 比较2种体外肝代谢模型转化藜芦酸葡萄糖酯的转化样式和转化率差异.方法 通过大鼠肝微粒体和肝S9体外转化模型对藜芦酸葡萄糖酯进行生物转化,采用HPLC检测转化底物及产物的含量,检测波长254 nm,流动相为乙腈(A)-1％乙酸溶液(B),梯度洗脱(0～6 min,5％～40％A;6～9 min,40％～50％A;9～11 min,50％～5％A),流速1.0 mL/min.结果 2种模型均可将藜芦酸葡萄糖酯转化为藜芦酸,但应用肝S9模型得到的代谢产物多于肝微粒体模型,且肝S9模型对酯类的转化率高于肝微粒体模型.结论 肝S9模型对酯类的转化能力高于肝微粒体模型.
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