健脾和胃方对大鼠肝微粒体CYP3A1酶活性的影响  

Effects of Jianpiheweifang on Enzymic Activity of CYP3A1 in Liver Microsome of Rats

作　　者：梁蔚婷[1,2] 黄红兵[1,2] 刘韬[1,2] 潘莹[1,2] 陈卓佳[1,2] 魏雪[1,2] 林子超[1,2] 陈倩超[1,2] 刘庆[1,2] 

机构地区：[1]中山大学肿瘤防治中心药学部 [2]华南肿瘤学国家重点实验室,肿瘤医学协同创新中心,广东广州510060

出　　处：《今日药学》2014年第7期473-476,480,共5页Pharmacy Today

基　　金：广东省医院药学研究基金资助项目(编号:2013A03)

摘　　要：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 study the effect of Jianpiheweifang on the enzymic activity of liver microsomal cytochrome P450 isoenzyme 3A1 （CYP 3A1） in SD rats.Methods A total of 25 SD rats were randomly divided into 5 groups： blank control group （NS, 1 mL· kg-l · d-1, 14 d）, dexamethasone group （100 mg · kg-1 · d-l）, Jianpiheweifang high-dose, medium-dose and low-dose groups （7.146, 3.573, 1.786 mg ·kg-1·d-1）, with 5 rats in each group. Those groups were given relevant medicine intragastrically. The HPLC-UV method was established and validated to determine the productive velocity of metabolite （6[3-hydroxyl-testosterone, 6β-OHT） of testosterone after incubation of rat liver microsome and to measure the activity of CYP3A1. Results The productive velocities of 6β-OHT in rats of the blank control group, dexamethasone group and Jianpiheweifang high-dose, medium-dose and low-dose groups were （7.29±0.66） , （27.46± 2.35）, （3.51±0.48）, （4.90±1.18） and （6.52±1.23） nmol · mg-1· min-1, respectively. There were significant differences between Jianpiheweifang groups and dexamethasone group （P 〈 0.05 ）. There were significant differences between the high-dose, medium-dose group and the blank control group （P〈0.05） , but there was no significant difference between low-dose group and the blank control group （P〉0.05）.Conclusion Jianpiheweifang had no inducible effect on the enzymic activity of CYP3A1 in rats. The high-dose, medium-dose of Jianpiheweifang can reduce the activity of CYP3A1 in rats.

关 键 词：健脾和胃方 肝微粒体 细胞色素P450 CYP3A1 CYP3A4 酶活性 

分 类 号：R969[医药卫生—药理学]