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目的:研究半夏泻心汤及不同配伍组对大鼠肝微粒体CYP450亚型酶的影响,从肝脏代谢角度评价半夏泻心汤组方的合理性。方法:将大鼠随机分为全方组、辛开组、苦降组、甘补组及空白对照组,分别灌胃水煎液,运用肝微粒体体外温孵法,对探针底物进行孵育,并结合超高效液相检测方法,测定各探针底物代谢产物的含量,计算代谢速率,以反映各给药组的肝微粒体CYP2C6,CYP2E1,CYP3A1/2亚型酶活性。结果:与空白组相比,全方组,苦降组对各亚型酶均起抑制作用(P<0.01);辛开组对CYP2C6有抑制作用(P<0.01),而对CYP2E1和CYP3A1/2无显著抑制作用;甘补组对CYP2C6和CYP2E1亚型起抑制作用(P<0.01),而对CYP3A1/2无抑制作用。结论:全方对大鼠肝微粒体CYP450酶起抑制作用,比较各配伍组间差异,苦降组抑制作用较其他配伍组显著。
Objective: To study the effect of Banxiaxiexin Decoction and different compatibility groups on CYP450 isoforms of rat liver microsomes, and to evaluate the rationality of Banxiaxiexin Decoction prescription from the aspect of liver metabolism. Methods: The rats were randomly divided into the whole group, Xinkai group, bitterness group, Ganxu group and blank control group, respectively, gavage of decoction, the use of liver microsomal in vitro incubation method, the probe substrate Incubated and combined with ultra-high performance liquid phase detection method, the content of each probe substrate metabolites was determined, and the metabolic rate was calculated to reflect the activity of CYP2C6, CYP2E1 and CYP3A1 / 2 subtypes of liver microsomes in each administration group. Results: Compared with the blank control group, all the three groups had the same inhibitory effect on CYP2C6 (P <0.01), while CYP2E1 and CYP3A1 / 2 had no significant inhibitory effect; Ganbu group had inhibitory effect on CYP2C6 and CYP2E1 subtypes (P <0.01), but had no inhibitory effect on CYP3A1 / 2. CONCLUSION: All prescriptions can inhibit the activity of CYP450 in rat liver microsome. Comparing the differences among the compatibility groups, the inhibitory effect of bitter suppository is more significant than that of other compatibility groups.