西红花酸对大鼠血浆胆固醇的调节作用及其机制研究  

Hypocholesterolemic effect of crocetin on serum cholesterol in rats and the mechanism

作　　者：赵博华[1] 钱之玉[1] 陈真[1] 盛亮[1] 杨丽娜[1] 闫俊岭[1] 

机构地区：[1]中国药科大学药理教研室,南京210009

出　　处：《中国新药杂志》2009年第14期1347-1351,共5页Chinese Journal of New Drugs

摘　　要：目的:探讨西红花酸对高胆固醇血症大鼠血浆胆固醇的影响及其机制。方法:建立大鼠高胆固醇血症模型,观察西红花酸对胆固醇吸收、合成、转化等方面的影响。同时,建立细胞模型,考察西红花酸对内源性胆固醇合成的影响。结果:西红花酸能降低血浆总胆固醇(TC)和低密度脂蛋白胆固醇(LDL-C)浓度,升高高密度脂蛋白胆固醇(HDL-C)浓度及卵磷脂胆固醇酯酰转移酶(LCAT)、7α-羟化酶(CYP7A1)活性及mRNA表达,降低HMG-COA还原酶(HMG-CoAR)活性及mRNA表达;增加胆汁酸排泄。体外试验显示,西红花酸可抑制内源性胆固醇的合成。结论:西红花酸能降低大鼠血浆胆固醇水平,其机制可能是抑制内源性胆固醇合成及促进胆固醇向胆汁酸转化及排泄。Objective： To study the hypocholesterolemic mechanism of crocetin in rats with diet-induced hypercholesteremia. Methods： The hypercholesteremia was induced by feeding rats with high-cholesterol diet. The effect of crocetin on the levels of serum cholesterol, cholesterol absorption in jejunum, bile acid metabolism, and cholesterol excretion in feces were determined. The activity and mRNA levels of HMGCoAR（3-hydroxy-3 methylglutaryl coenzyme A reductase） , LCAT（ lecithin cholesterol acyhransferase）, 7α-hydroxylase （CYP7A1） were inspected. The effects of the crocetin on endogenous cholesterol biosynthesis in HepG2 cells were also tested. Re- sults ： Croeetin significantly reduced the level of serum TC （ total cholesterol） , LDL-C （ low-density lipoprotein cholesterol）, and increased HDL-C （high-density lipoprotein cholesterol） in hypercholesteremic rats. The activities and mRNA level of LCAT and 7α-hydroxylase were significantly higher, but the activity and expression of HMGCoAR were lower in crocetin group than in control group. Crocetin increased the content of bile acids in bile and feces, but had no effect on the secretion of bile, cholesterol absorption in jejunum and cholesterol excretion in feces. Crocetin inhibited hepatic cholesterol biosynthesis in vitro. Conclusion： The hypocholesterolemic activity of crocetin may be due to its inhibition of endogenous cholesterol biosynthesis and acceleration of cholesterol conversion to bile acids.

关 键 词：西红花酸 高胆固醇血症 HMG-COA还原酶 卵磷脂胆固醇酯酰转移酶 7Α-羟化酶 

分 类 号：R965.1[医药卫生—药理学] R975.5[医药卫生—药学]