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目的研究何首乌主要活性成分在肝L-02细胞中的吸收和代谢。方法将何首乌主要活性成分二苯乙烯苷(TSG)、大黄素(EN)作用于正常人肝L-02细胞,给药0、2、4、6、8、12、24、36、48 h后,分别取上层培养液及细胞裂解液,利用HPLC探究二者的吸收、蓄积及代谢规律,并用LC-MS法进行代谢产物的定性分析。结果 TSG在肝L-02细胞中无明显蓄积,HPLC检测出TSG和一个代谢产物吸收峰,且在8 h后浓度随给药时间延长呈递增趋势,经LC-MS/MS鉴定为二苯乙烯苷葡萄糖醛酸结合物;EN在肝L-02细胞中有部分蓄积,细胞呈黄色,检测出4个EN的代谢产物吸收峰,浓度随时间的延长而增加,经LCMS/MS鉴定为大黄素葡萄糖醛酸的3个同分异构体及大黄素硫酸结合物。结论大黄素较二苯乙烯苷更易被L-02细胞吸收,在L-02细胞中二者的Ⅰ相代谢产物均未被检测到,仅检测到二者的Ⅱ相代谢产物。
Objective To study the absorption and metabolism of the major active components of Polygonum multiflorum Thunb. In liver L-02 cells. Methods The main active components of Polygonum multiflorum were treated with TSG and EN in normal human L-02 cells at 0,2,4,6,8,12,24,36,48 h , The supernatant liquid and cell lysate were taken respectively. The absorption, accumulation and metabolism of the two substances were investigated by HPLC, and the qualitative analysis of metabolites was carried out by LC-MS. Results There was no significant accumulation of TSG in L-02 cells. The absorption peak of TSG and one metabolite was detected by HPLC. The concentration of TSG increased gradually with the prolongation of administration time and was identified as stilbene by LC-MS / MS Glucosidic acid conjugates; EN partially accumulated in liver L-02 cells, the cells were yellow, the absorption peaks of four metabolites of EN were detected, the concentration increased with time, identified as emodin by LCMS / MS Three isomers of glucuronic acid and emodin sulfate conjugates. Conclusion Emodin is more easily absorbed by L-02 cells than stilbene glycoside. The phase I metabolites of L-02 cells are not detected in L-02 cells, and only phase Ⅱ metabolites of L-02 are detected.