葛根芩连汤中葛根和甘草对黄芩有效成分在大鼠肝代谢的影响

目的 研究葛根芩连汤中葛根和甘草对黄芩有效成分黄芩苷、汉黄芩苷、黄芩素、汉黄芩素在大鼠肝微粒体代谢的影响,探讨该复方配伍机制.方法 采用在体诱导-体外肝微粒体温孵方法,分别考察葛根芩连汤中葛根、甘草对黄芩苷、汉黄芩苷、黄芩素、汉黄芩素在大鼠肝微粒体中代谢的影响,利用超高效液相色谱(UPLC)法测定大鼠肝微粒体中黄芩苷、汉黄芩苷、黄芩素、汉黄芩素的量.结果 温孵时间黄芩苷在0～90 min,汉黄芩苷在0～60 min,黄芩素在0～10 min,汉黄芩素在0～40 min呈线性消除.对照组各成分代谢速率大小顺序为:黄芩素＞汉黄芩素＞汉黄芩苷＞黄芩苷.与对照组相比,葛根对汉黄芩苷、黄芩素的代谢具有抑制作用,对黄芩苷及汉黄芩素的代谢具有诱导作用；甘草对汉黄芩素的代谢具抑制作用,对黄芩苷、汉黄芩苷、黄芩素的代谢则呈现诱导作用.结论 黄芩苷、汉黄芩苷、黄芩素、汉黄芩素可以被大鼠肝微粒体代谢,葛根芩连汤中葛根、甘草对黄芩有效成分的代谢过程有影响.

Effects of Puerariae Lobatae Radix and Glycyrrhizae Radix et Rhizomain Gegen Qinlian Decoction on rat liver metabolism of active ingredients in Scutellaria Radix

ObjectiveTo study the effects of Puerariae Lobatae Radix (PLR) and Glycyrrhizae Radix et Rhizoma(GRR) in Gegen Qinlian Decoction (GQD) on the rat liver microsome metabolism of baicalin, wogonoside,baicalein, and wogonin in Scutellariae Radix(SR) and to explore the compatibility mechanism of the constituents. Methods The effects of various medicinal materials in GQD, such as PLR and GRR on the rat liver microsomes metabolic activities of baicalin, wogonoside, baicalein, and wogonin were investigated by in vivoinduced-in vitroliver microsomes incubation method. UPLC method was developed for the determination of baicalin, wogonoside, baicalein,and wogonin in the rat liver microsomes incubation system. ResultsBaicalin, wogonoside, baicalein, and wogonin were linear to be eliminated within 90, 60, 10, and 40 min, respectively. In the control group, the order of metabolic rate for each ingredient was baicalein > wogonin > wogonoside > baicalin. Compared with the control group, PLR showed the metabolic inhibition on wogonoside and baicalein, but the metabolic induction on baicalin and wogonin; GRR showed the metabolic inhibition on wogonin, butthe metablic induction on baicalin, wogonoside, and baicalein. ConclusionBaicalin, wogonoside, baicalein, and wogonin could be metabolizedin rat liver microsomes. PLR and GRR in GQD could affect the metabolic process of the active ingredients in SR.