参芎葡萄糖注射液的丹参组分对小鼠细胞色素P450的影响

目的:考察参芎葡萄糖注射液中的主要组分丹参(Salviae Miltiorrhizae Radix et Rhizoma,SM)水提取物对小鼠细胞色素P450酶(CYPs)主要亚型(CYP1A2,CYP2D22,CYP3A11和CYP2E1)的影响。方法:昆明种雄性小鼠分为5组,分别为正常组,苯巴比妥组,丹参水提取物组(3.9 mg·kg-1·d-1),丹参低、高剂量组(2.6,5.2 mg·kg-1·d-1),连续ig 7 d给药。取各组小鼠的肝脏组织,提取肝脏中RNA以及制备肝微粒体,检测各组小鼠CYP450酶活性,mRNA和蛋白水平的变化。结果:与正常组比较,丹参高剂量组可以显著降低CYP2E1的酶活性,mRNA和蛋白表达的水平(P0.05),丹参对CYP1A2,CYP3A11,CYP2D22没有显著性影响。结论:参芎葡萄糖注射液中的丹参组分可以影响CYP2E1的酶活性,mRNA以及蛋白的表达。

Effect of Salviae Miltiorrhizae Radix et Rhizoma in Shenxiong Glucose Injectionon Cytochrome P450 in Mice

Objective: To investigate the effect of water extracts from the main component Salviae Miltiorrhizae Radix et Rhizoma (SM) in Shenxiong glucose injection on subtypes (CYP1A2, CYP2D22, CYP3A11 and CYP2E1) of mice cytochrome P450(CYP450). Method: Malemice from Kunming were randomly divided into blank group, phenobarbital group, and SM water extract group (3.9 mg·kg^-1·d^-1), and SM low and high-dose groups (2.6, 5.2 mg·kg^-1·d^-1). Then the mice were killed after the animals were administered with medicines by gavageonce daily for consecutively 7 days. Liver RNAs were collected to prepare microsomes, in order to determine the enzyme activities of CYP2E1, CYP2D22, CYP1A2 and CYP3A, and quantitative real-time PCR and Western blot was employed to examine the mRNA and protein expressions of these four CYP450 enzymes in liver tissues of mice. Result: Compared with the normal group, CYP2E1 activity, and mRNA and protein expressions were decreased in the SM high-dose group (P<0.05). SM had no effect on the activities of CYP1A2, CYP3A and CYP2D22. Conclusion: SM in Shenxiong glucose injection has effects on CYP2E1 enzymatic activity, and mRNA and protein expressions.