糖原磷酸化酶抑制剂积雪草酸对糖代谢的影响  

Effects of asiatic acid as a novel glycogen phosphorylase inhibitor on glucose metabolism

作　　者：柳军[1] 毛利飞[1] 尚靖[1] 孙宏斌[2] 张陆勇[1] 

机构地区：[1]中国药科大学新药筛选中心 [2]中国药科大学新药研究中心

出　　处：《中国临床药理学与治疗学》2011年第7期736-739,共4页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：教育部中央高校基本科研业务费专项资金(JKP2009002)

摘　　要：目的:研究积雪草酸(AA)对糖原磷酸化酶的抑制作用及其对HepG2细胞的葡萄糖消耗作用,最后研究其对小鼠糖代谢的影响,初步探讨其降糖机制。方法:体外检测AA对糖原磷酸化酶抑制作用和对HepG2细胞培养基中的葡萄糖消耗水平的影响。体内小鼠实验,采用灌胃AA7 d,以皮下注射肾上腺素造成高血糖模型,并与正常组一起测定静脉血糖和肝糖原含量。结果:AA具有抑制糖原磷酸化酶活性,其IC50为12.1μmol/L,AA能增加HepG2细胞对培养基中葡萄糖的消耗,并且可显著拮抗肾上腺素引起的血糖升高,对抗肾上腺素引起的肝糖原降解。结论:AA具有降血糖作用,机制与其抑制肝糖原分解有关。AIM. To determine the effects of asiatic acid, a novel glycogen phosphorylase inhibitor, on glucose consumption in HepG2 cell and on blood glucose and hepatic glycogen in mice, and study the hypoglycemic mechanism. METHODS： Mice were given intragastrically either vehicle or asiatic acid for 7 days. The model of hyperglycemia in mice was induced by subcutaneous injection of Adrenaline; the fasting plasma glucose and hepatic glycogen of mice were measured. RESULTS：The elevation of blood glucose level caused by Adrenaline was antagonized by asiatic acid significantly. Asiatic acid also increased the hepatic glycogen content in adrenaline-induced hyperglycemia mice. Furthermore, Asiatic acid showed significant effect on glucose consumption in HepG2 cells, and its IC50 of inhibiting glycogen phosphorylase was 12.1 μmol/ L in vivo. CONCLUSION： Asiatic acid presents anti-diabetic effect, the mechanism is probably concerned with inhibiting excessive hepatic glycogen degradation.

关 键 词：积雪草酸 糖原磷酸化酶 肾上腺素 肝 糖原 降血糖 

分 类 号：R965.2[医药卫生—药理学]