金银花对大鼠体内CYP3A酶活性及基因表达的影响  

The In Vivo Effect of Lonicera japonica Thunb on the CYP3A Enzyme Activity and Gene Expression in Rats

作　　者：涂碎萍 黄丹[1] 黄慧[1] 吴丹[1] 巫传玲[1] 代晶[1] Tu Suiping;Huang Dan;Huang Hui;Wu Dan;Dai Jing(School of Pharmacy, Chengdu Medical College, Chengdu 610083, China)

机构地区：[1]成都医学院药学院,成都610083

出　　处：《成都医学院学报》2020年第2期204-207,231,共5页Journal of Chengdu Medical College

基　　金：四川省教育厅重点科研项目(No:15ZA0263);四川养老与老年健康协同创新中心自然科学研究项目(YLZBZ1512);省级大学生创新创业训练计划项目(No:201513705038)。

摘　　要：目的考察金银花提取物对大鼠体内CYP3A酶活性和基因表达的影响。方法将SD大鼠随机分为5组,分别为空白组(生理盐水)、金银花提取物组低剂量(5 g/(kg·day))、中剂量(10 g/(kg·day))、高剂量(20 g/(kg·day))灌胃10 d,地塞米松组(50 mg/(kg·day))腹腔注射5 d后处死大鼠,取肝组织或制备肝微粒体。以HPLC法测定大鼠肝微粒体内CYP3A底物睾酮代谢速率,考察金银花提取物对CYP3A酶活性的影响。采用实时荧光定量PCR技术测定大鼠肝脏中CYP3A1和CYP3A2酶mRNA的表达量,分析金银花对CYP3A酶基因表达水平的影响。结果与空白组相比,地塞米松组中睾酮在大鼠肝微粒体内的代谢速率明显增加(P<0.01),大鼠肝脏中CYP3A1和CYP3A2酶mRNA表达量明显增多(P<0.01);而金银花各给药组的酶活性和mRNA表达量差异无统计学意义(P>0.05)。结论金银花长期给药后,对大鼠体内CYP3A酶无明显影响。Objective To investigate the in vivo effect of the Lonicera japonica Thunb extract on the CYP3A activity and gene expression in rats.Methods The SD rats were randomly divided into 5 groups including the blank group treated with saline,Lonicera japonica Thunb extract groups treated with the low dose of 5g/kg each day,medium dose of 10g/kg each day and high dose of 20g/kg each day,and dexamethasone group treated with 50mg/kg each day.After 5 days of intraperitoneal injection,the rats were sacrificed and the liver tissues were taken or the liver microsomes were prepared.The testosterone metabolism rate of the CYP3A substrate in the rats'liver microsomes was determined by the HPLC method to investigate the effect of Lonicera japonica Thunb extract on the CYP3A enzyme activity,and the mRNA expression levels of CYP3A1 and CYP3A2 were determined by real-time quantitative PCR to investigate the effect of Lonicera japonica Thunb extract on the expression levels.Results Compared with the blank group,the testosterone metabolism rate in the rats'liver microsomes was significantly increased(P<0.01)and the mRNA expression levels of CYP3A1 and CYP3A2 in the rats'liver were significantly increased(P<0.01)in the dexamethasone group.However,there were no significant differences in the enzyme activity and mRNA expression between the Lonicera japonica Thunb extract groups.Conclusion There is no significant effect on the CYP3A enzyme in rats after a long-term administration with Lonicera japonica Thunb.

关 键 词：金银花 细胞色素P450-3A酶 酶活性 基因 

分 类 号：R285.5[医药卫生—中药学]