白花蛇舌草水提取物对大鼠细胞色素P450 1A2亚型的影响  

Effect of Chinese crude drug hedyotis diffusa willd on the activity of rat CYP 1A2

作　　者：鲍岩岩[1] 刘艳[2] 唐晓波[1] 刘秉义[1] 武正华[1] 朱大岭[1,3] 

机构地区：[1]哈尔滨医科大学药学院 [2]哈尔滨医科大学第二临床医学院临床药物研究所,黑龙江哈尔滨150081 [3]黑龙江省生物医药工程重点实验室

出　　处：《哈尔滨医科大学学报》2007年第1期4-7,共4页Journal of Harbin Medical University

基　　金：国家863课题(2002AA223410);黑龙江省自然科学基金重点项目(ZJY03-8);黑龙江省生物医药工程重点实验室基金(004)

摘　　要：目的观察白花蛇舌草水提取物对大鼠细胞色素P450 1A2亚型(CYP 1A2)的影响。方法实验组(高、中、低剂量组)大鼠分别给予白花蛇舌草水提取物5．84g/kg、8．26g／kg、11．68g/kg,对照组给予生理盐水,用蛋白印迹方法测定大鼠CYP 1A2的蛋白表达。通过高效液相色谱(HPLC)法测定全血中咖啡因的代谢率,研究白花蛇舌草水提取物对大鼠肝脏CYP 1A2的影响;用HPLC法测定非那西丁的代谢率,确定白花蛇舌草水提取物对大鼠肝微粒体CYP 1A2活性的影响。结果蛋白印迹分析结果表明,白花蛇舌草水提取物对CYP 1A2蛋白表达没有影响。给予高、中、低剂量白花蛇草水提物的大鼠咖啡因代谢率分别为(33．62±5．08)％、(32．19±4．87)％、(31．05±4．93)％;对照组大鼠咖啡因代谢率为(30．73±5．40)％,实验组间及与对照组比较均无显著性差异(P>0．05)。肝微粒体体外温孵实验中,实验各剂量组和对照组非那西丁代谢率分别为(3．76±0．83)％、(3．61±0．79)％、(3．84±0．86)％、(3．81±0．82)％,实验组间及与对照组比较均无显著性差异(P>0．05)。结论体内、体外实验结果均表明,白花蛇舌草水提取物对大鼠肝脏CYP 1A2没有抑制作用。Objective To investigate the effect of hedyotis diffusa wind on the activity of rat CYP450 1A2 （CYP 1A2） in vivo and in vitro. Methods The treated rats were given 5.84g/kg, 8.26g/kg, 11.68g/kg of hedyotis diffusa willd while the control rats were given saline. Expression of CYP 1A2 was determined by the method of Western blot. Metabolic rate of caffeine in the whole blood was determined by HPLC to study the effect of hedyotis diffusa wind on the activity of rat liver CYP 1A2;Metabolic rate of phenacetin was determined by HPLC to determine the effect of hedyotis diffusa willd on the activity of rat liver microsome CYP 1A2. Results Western blot analysis indicated that hedyotis diffusa willd had no effect on the activity of rat CYP 1A2.The metabolic rates of caffeine intreated rats were （33.62 ± 5.08） %, （32.19 ± 4.87）% ,and （31.05 ± 4.93 ） % while in control rats was （30.73 ± 5.40） %. There was no significant difference among these groups（ P 〉 0.05）. In rat liver microsomal incubated system, the metabolic rate of phenacetin were（3.76 ± 0.83）%,（3.61 ±0.79）%,and （3.84 ±0.86）% in treated groups and（3.81 ±0.82）% in control group, and there was no significant difference among these groups（ P 〉 0.05）. Conclusion Clinical dose of hedyotis diffusa wind has no inhibitory action on the activity of rat CYP 1A2 in vivo andin vitro.

关 键 词：白花蛇舌草 细胞色素P450 肝微粒体 高效液相色谱 

分 类 号：R-332[医药卫生] R965