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苯并呋喃-双吲哚衍生物的混合物:具有良好降脂活性的新型原型物。

Hybrid benzofuran-bisindole derivatives: new prototypes with promising anti-hyperlipidemic activities.

机构信息

Medicinal and Process Chemistry Division, CSIR - Central Drug Research Institute, Lucknow 226 001, Uttar Pradesh, India.

出版信息

Eur J Med Chem. 2013 Oct;68:38-46. doi: 10.1016/j.ejmech.2013.07.009. Epub 2013 Jul 30.

Abstract

A series of different benzofuran-bisindole hybrids were synthesized and evaluated in vitro for their antioxidant and in vivo for antidyslipidemic activity in triton WR-1339 induced hyperlipidemic rats. Among the series, compounds 4a, 4c, 4h and 4j showed significant decrease in plasma levels of total cholesterol (TC), phospholipids (PL) and triglycerides (TG) followed by increase in post heparin lipolytic activity (PHLA). In addition, the active hybrids possessed moderate antioxidant properties and increased the plasma lecithin cholesterol acyltransferase (LCAT) activity, which plays a key role in lipoprotein metabolism contributing to an increased level of HDL-C in serum. These results indicate that these hybrids constitute novel prototypes for the management of dyslipidemia.

摘要

一系列不同的苯并呋喃-双吲哚杂合体被合成,并在体外评估其抗氧化活性,在 Triton WR-1339 诱导的高血脂大鼠体内评估其抗高血脂活性。在这一系列中,化合物 4a、4c、4h 和 4j 显示出显著降低血浆总胆固醇 (TC)、磷脂 (PL) 和甘油三酯 (TG) 的水平,随后增加肝素后脂解活性 (PHLA)。此外,活性杂合体具有中等的抗氧化性能,并增加了血浆卵磷脂胆固醇酰基转移酶 (LCAT) 的活性,LCAT 在脂蛋白代谢中起着关键作用,有助于增加血清中 HDL-C 的水平。这些结果表明,这些杂合体构成了用于治疗高血脂症的新型原型。

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