槲皮素在糖尿病模型大鼠肝脏甲基化代谢的研究  

Hepatic methylation of quercetin in diabetes mellitus rats

作　　者：石荣[1] 马越鸣[1] 方圆圆[1] 吴家胜[1] 钟杰[1] 

机构地区：[1]上海中医药大学中药药代动力学实验室,上海201203

出　　处：《中药药理与临床》2011年第5期34-38,共5页Pharmacology and Clinics of Chinese Materia Medica

基　　金：上海市教育委员会科研项目(08cz033);上海高校创新团队建设项目;上海市博士点基金(2011)

摘　　要：目的:考察糖尿病模型大鼠体内槲皮素甲基化代谢的变化情况。方法:采用高脂高糖饮食+链脲佐菌素(STZ)诱导的糖尿病大鼠肝匀浆,研究槲皮素甲基化代谢特征及酶动力学,并与正常大鼠比较观察糖尿病状态下甲基化代谢的差异。结果:槲皮素(浓度2.6～165.5μM)在大鼠肝匀浆中甲基化代谢酶动力学符合Michaelis-Menten方程。槲皮素在正常和糖尿病大鼠肝匀浆的甲基化代谢的酶动力学参数米氏常数(Km)分别为12.4±2.6、12.0±0.7μM,最大反应速度(Vmax)分别为440.4±27.5、307.9±5.1pmol/min/mg,内在代谢清除率(CLint)分别为35.4、25.7 ml/min/mg。与正常大鼠相比,糖尿病大鼠肝匀浆中槲皮素甲基化代谢物的Vmax和CLint降低。结论:糖尿病状态降低了槲皮素甲基化代谢,可能会减慢槲皮素在体内的消除过程。Objective： To investigate hepatic methylation of quercetin in diabetes mellitus rats.Methods： Quercetin was metabolized in vitro by liver homogenate in normal and streptozotocin induced diabetic rats.The substrate concentration vs time curve and enzyme kinetic parameters（Km,Vmax and Clint） of quercetin were estimated using liver homogenate.The differences of hepatic methylation of quercetin between normal and diabetes mellitus group were tested by T-test.Results： The kinetics of methylated quercetin formation by liver homogenate at 2.6-165.5 μM exhibited characteristics of typical Michaelis-Menten kinetics.Km values of methylated quercetin formation in normal and diabetic rats were 12.4 ±2.6,12.0 ±0.7μM,respectively.Vmax were 440.4 ±27.5,307.9±5.1 pmol/min/mg,respectively.Clint values were 35.4,25.7 ml/min/mg,respectively.Compared with normal rats,Vmax and Clint values were significantly reduced in diabetic rats（P〈0.05）.Conclusion： Methylation of quercetin was significantly decreased and the elimination of quercetin was slowed in diabetic status.

关 键 词：槲皮素 糖尿病 甲基化代谢 大鼠肝匀浆 

分 类 号：R285[医药卫生—中药学]