Pyranocoumarins: A new class of anti-hyperglycemic and anti-dyslipidemic agents

被引：142

作者：

Kumar, Atul ^{[1
]}

Maurya, Ram Awatar ^{[1
]}

Sharma, Siddharth ^{[1
]}

Ahmad, Pervez ^{[1
]}

Singh, A. B. ^{[2
]}

Bhatia, Gitika ^{[2
]}

Srivastava, Arvind K. ^{[2
]}

机构：

[1] Cent Drug Res Inst, Med & Proc Chem Div, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India

[2] Cent Drug Res Inst, Div Biochem, Council Sci & Ind Res, Lucknow 226001, Uttar Pradesh, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 22期

关键词：

Pyranocoumarins; Anti-hyperglycemic; Anti-dyslipidemic; PTP; 1B; TYROSINE-PHOSPHATASE; 1B; IN-VITRO; INHIBITORS;

D O I：

10.1016/j.bmcl.2009.09.031

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of pyranocoumarin derivatives were synthesized and evaluated in vivo for their anti-hyperglycemic as well as anti-dyslipidemic activities. Compounds 7a, 7c, 8a, 8b, 8c, 8e and 8f have shown promising anti-hyperglycemic activities in sucrose loaded model (SLM) as well as sucrose challenged streptozotocin induced diabetic rat model (STZ). Compounds 8a and 8b were showing 38.0% and 42.0% blood glucose lowering activity in db/db mice model. In vitro anti-hyperglycemic activity evaluation exhibited that compounds 8a (IC50 = 24.5 mu M) and 8b (IC50 = 36.2 mu M) are potential PTP-1B inhibitors thereby revealing their possible mechanism of anti-diabetic action. Compounds 7a, 7b, 8a, 8b, 8d, 8e and 8f have shown significant anti-dyslipidemic activity in triton induced dyslipidemia in rats. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：6447 / 6451

页数：5

共 17 条

[1] Protein tyrosine phosphatase 1B inhibitors from Morus root bark [J].