Objective To study the influence of total saponins from Panax quinquefolium Linne on the activity of CYP1A2 in rats.Methods Rats were randomly divided into control group,total saponins from Panax quinquefolium Linne groups [50,100 and 200 mg/(kg·d)] and positive control group.After pretreatment for 11 consecutive days,the activity,mRNA expression and protein expression of CYP1A2 were measured.The pharmacokinetic changes of phenacetin (probe substrate of CYP1A2) in pretreatment rats were investigated.Results After pretreatment with total saponins from Panax quinquefolium Linne,the activity,mRNA expression and protein expression of CYP1A2 in rats were improved with dose increasing.The metabolic rate of phenacetin was speeded up.Conclusion Total saponins from Panax quinquefolium Linne might induce the activity of CYP1A2.%目的 考察西洋参总皂苷对大鼠肝微粒体CYP1A2活性的影响.方法 将大鼠随机分为空白对照组(空白组)、西洋参总皂苷低剂量组[低剂量组,50 mg/(kg·d)]、西洋参总皂苷中剂量组[中剂量组,100 mg/(kg·d)]、西洋参总皂苷高剂量组[高剂量组,200 mg/(kg·d)]和β-萘黄酮阳性药对照组[阳性药组,80 mg/(kg·d)],预处理11 d后,观察大鼠肝微粒体CYP1A2酶活性、CYP1A2 mRNA表达和CYP1A2酶蛋白表达情况,研究CYP1A2特异性探针底物非那西丁在预处理大鼠体内的药动学变化.结果 预处理后,大鼠肝微粒体CYP1A2活性、mRNA和蛋白表达随西洋参总皂苷剂量升高有增加趋势,非那西丁在预处理大鼠体内代谢速率加快.结论 西洋参总皂苷对大鼠肝微粒体CYP1A2活性有一定诱导作用.
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