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目的:研究三黄降糖片及其主要成分对羟甲基戊二酸单酰辅酶A(HMG-Co A)还原酶的抑制作用。方法:在反应体系为70 mmol/L磷酸盐缓冲液、200 mmol/L NADPH、5μg HMG-Co A还原酶、2 mmol/L EDTA、2 mmol/L半胱胺、0.06%BSA中,加入浓度1、5、25、125μg/m L的三黄降糖片,三黄降糖片的主要成分大黄的水煎液和HMG-Co A还原酶抑制剂普伐他汀,然后加入37℃预热的HMG-Co A(0.6μg/m L)启动反应,检测在340 nm中反应前后其酶的即时活力、15 min内其酶的活力变化和NAPDH下降率。结果:HMG-Co A还原酶抑制作用强弱为普伐他汀>三黄降糖片>大黄水煎液,三种药物在浓度范围内呈现剂量效应关系。与浓度0μg/m L比较,三种药物在浓度25μg/m L和浓度125μg/m L时的抑制作用显著增强(P<0.05),NADPH下降率显著增加(P<0.05),而浓度为125μg/m L时,抑制作用会随时间延长而有所降低,浓度为25μg/m L时抑制作用变化不大。结论:三黄降糖片及其主要成分对HMG-Co A还原酶有一定的抑制作用,是其降脂的作用机制之一。
Objective: To study the inhibitory effect of Sanhuang Hypoglycemic Tablets and its main constituents on HMG-Co A reductase. Methods: The reaction system consisted of 70 mmol / L phosphate buffer, 200 mmol / L NADPH, 5 μg HMG-Co A reductase, 2 mmol / L EDTA, 2 mmol / L cysteamine and 0.06% BSA. 1.5, 25, 125μg / m L of three Huang Jiang sugar tablets, sanhuang hypoglycemic tablets of the main components rhubarb decoction and HMG-Co A reductase inhibitor pravastatin, and then added 37 ℃ preheated HMG-Co A (0.6μg / mL) started the reaction and detected its immediate activity before and after reaction at 340 nm. The enzyme activity and NAPDH descended within 15 min. Results: The inhibitory effect of HMG-Co A reductase was pravastatin> Sanhuang Jiangtang> rhubarb decoction. The three drugs showed a dose-response relationship in the concentration range. Compared with the concentration of 0μg / m L, the inhibitory effects of the three drugs at the concentration of 25μg / m L and the concentration of 125μg / m L were significantly increased (P <0.05) and the decrease of NADPH was significantly increased (P <0.05) / m L, the inhibition will be reduced with time prolonging, when the concentration of 25μg / m L little change in inhibition. Conclusion: Sanhuang Hypoglycemic Tablets and its main components have certain inhibitory effect on HMG-Co A reductase, which is one of the mechanisms of its lowering lipid.