Effect of tincture of Crataegus on the LDL-receptor activity of hepatic plasma membrane of rats fed an atherogenic diet
Effect of tincture of Crataegus on the LDL-receptor activity of hepatic plasma membrane of rats fed an atherogenic diet
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DOI：
10.1016/0021-9150(96)05813-3
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发表时间：
1996-06-01
期刊：
影响因子：
5.3
通讯作者：
Devaraj, SN
中科院分区：
文献类型：
--
作者：
Rajendran, S;Deepalakshmi, PD;Devaraj, SN
山楂酊（TCR）是一种由山楂果制成的降胆固醇和抗动脉粥样硬化药物。其主要成分为黄酮类、三萜皂苷类及少量强心胺类化合物。TCR，当同时给予大鼠喂致动脉粥样硬化饮食，显着增加了I-125-LDL的肝质膜，在体外的结合。特异性结合数据的Scatchard分析显示，在TCR处理的影响下，肝膜结合更多数量的I-125-LDL分子，表明LDL受体活性增强。TCR也被证明增加胆汁酸排泄和抑制肝胆固醇合成动脉粥样硬化饮食喂养大鼠。鉴于这些观察结果，TCR的降胆固醇作用似乎是由于肝LDL受体的上调导致血浆胆固醇更多地流入肝脏。TCR还通过增强胆固醇降解为胆汁酸并通过同时抑制胆固醇生物合成来防止胆固醇在肝脏中的积累。TCR的各种成分可以协同作用以产生所观察到的效果。
Tincture of Crataegus, (TCR), is a hypocholesterolemic and antiatherosclerotic drug made from berries of hawthorn, Crataegus oxyacantha. Its main constituents are flavonoids, triterpene saponins and a few cardioactive amines. TCR, when administered simultaneously to rats fed an atherogenic diet, significantly increased the binding of I-125-LDL to the liver plasma membranes, in vitro. Scatchard analysis of the specific binding data revealed that under the influence of TCR treatment the liver membranes bound to a greater number of I-125-LDL molecules indicating an enhancement in the LDL-receptor activity. TCR was also shown to increase bile acid excretion and to depress hepatic cholesterol synthesis in atherogenic diet fed rats. With these observations in view, the hypocholesterolemic action of TCR appears to be due to an upregulation of hepatic LDL-receptors resulting in greater influx of plasma cholesterol into the liver. TCR also prevents the accumulation of cholesterol in the liver by enhancing cholesterol degradation to bile acids and by simultaneously suppressing cholesterol biosynthesis. The various constituents of TCR may act synergistically to bring about the observed effects.