This study measured the impact of alisol B 23-acetate and alisol A 24-acetate, the main active ingredients of the traditional Chinese medicine Alismatis rhizoma, on total cholesterol (TC), triglyceride (TG), high density lipoprotein-cholesterol (HDL-C), and low density lipoprotein-cholesterol (LDL-C) levels of hyperlipidemic mice. The binding of alisol B 23-acetate and alisol A 24-acetate to the key enzyme involved in the metabolism of TC, 3-hydroxy-3-methylglutary-coenzyme A (HMG-CoA) reductase, was studied using the reagent kit method and the western blotting technique combined with a molecular simulation technique. According to the results, alisol acetates significantly lower the TC, TG, and LDL-C concentrations of hyperlipidemic mice, while raising HDL-C concentrations. Alisol acetates lower HMG-CoA reductase activity in a dose-dependent fashion, both in vivo and in vitro. Neither of these alisol acetates significantly lower the protein expression of HMG-CoA. This suggests that alisol acetates lower the TC level via inhibiting the activity of HMG-CoA reductase by its prototype drug, which may exhibit an inhibition effect via directly and competitively binding to HMG-CoA. The side chain of the alisol acetate was the steering group via molecular simulation.

中文翻译：

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基于HMG-CoA还原酶的乙酸酯降低胆固醇的作用及其分子机理

这项研究测量了传统中药Alismatis rhizoma的主要活性成分alisol B 23-乙酸酯和alisol A 24-乙酸酯对总胆固醇（TC），甘油三酸酯（TG），高密度脂蛋白胆固醇（HDL- C）和高脂血症小鼠的低密度脂蛋白胆固醇（LDL-C）水平。使用试剂盒方法研究了23乙酸阿里索尔B和24乙酸阿里索尔A与TC代谢的关键酶3-羟基-3-甲基谷氨酸辅酶A（HMG-CoA）还原酶的结合。 Western blotting技术与分子模拟技术相结合。根据结果​​，乙酸阿萨尔醇可显着降低高脂血症小鼠的TC，TG和LDL-C浓度，同时提高HDL-C浓度。体内和体外。这些乙酸阿糖醇酯均不能显着降低HMG-CoA的蛋白表达。这表明乙酸阿里索尔乙酸盐通过其原型药物通过抑制HMG-CoA还原酶的活性而降低了TC水平，这可能通过与HMG-CoA直接和竞争性结合而表现出抑制作用。通过分子模拟，乙酸阿萨洛尔的侧链是控制基团。