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目的研究健脾和胃方对大鼠肝微粒体细胞色素P450同工酶3A1(CYP3A1)活性的作用。方法 25只大鼠随机分为5组:空白对照组(生理盐水1 mL·kg-1·d-1,14 d)、地塞米松组(100 mg·kg-1·d-1,3 d)和健脾和胃方高、中、低剂量组(7.146,3.573,1.786 mg·kg-1·d-1,14 d),每组5只,灌胃给予相应的药物。采用高效液相色谱-紫外检测法,以睾酮为探针,测定睾酮经大鼠肝微粒体温孵后转化的代谢产物6β-羟基睾酮(6β-OHT)的生成速率,以评价各组CYP3A1酶活性。结果空白对照组、地塞米松组和健脾和胃方高、中、低剂量组6β-OHT的生成速率分别为(7.29±0.66)、(27.46±2.35)、(3.51±0.48)、(4.90±1.18)、(6.52±1.23)nmol·mg-1·min-1,健脾和胃方高、中、低剂量组6β-OHT的生成速率与地塞米松组均有显著性差异(P<0.05)。高、中剂量组与空白对照组有显著性差异(P<0.05),低剂量组与空白对照组无显著性差异(P>0.05)。结论本实验结果表明健脾和胃方对大鼠肝药酶CYP3A1酶活性无诱导作用,健脾和胃方的高、中剂量组能使大鼠肝药酶CYP3A1酶活性下降。
Objective To investigate the effect of Jianpi Hewei on the activity of cytochrome P450 isoenzyme 3A1 (CYP3A1) in rat liver microsomes. Methods Twenty-five rats were randomly divided into 5 groups: control group (1 mL · kg-1 · d-1 for 14 days), dexamethasone group (100 mg · kg-1 · d-1, ) And spleen and stomach high, medium and low dose groups (7.146,3.573,1.786 mg · kg-1 · d-1,14 d), each group of five, the corresponding drug given by gavage. The production rate of 6β-hydroxytestosterone (6β-OHT), a metabolite of testosterone which was transformed by incubation with rat liver microsomes, was measured by high performance liquid chromatography-ultraviolet detection with testosterone as a probe to evaluate the activity of CYP3A1 . Results The formation rates of 6β-OHT in the blank control group, dexamethasone group, and spleen and stomach recipe groups were (7.29 ± 0.66), (27.46 ± 2.35), (3.51 ± 0.48) and (4.90 ± 1.18) and (6.52 ± 1.23) nmol · mg-1 · min-1 respectively, there was a significant difference in the rate of 6β-OHT between dexamethasone group and dexamethasone group (P < 0.05). There was a significant difference between the high dose group and the middle dose group and the blank control group (P <0.05), but there was no significant difference between the low dose group and the blank control group (P> 0.05). Conclusion The experimental results show that the spleen and stomach on rat liver enzyme CYP3A1 enzyme activity was not induced by the high and medium doses of Jianpi and Weifang can rat liver enzyme CYP3A1 enzyme activity decreased.