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香豆素类化合物作为潜在的抗糖尿病药物。

Coumarins as potential antidiabetic agents.

机构信息

Department of Pharmaceutical Sciences, Institute of Pharmacology, Zhejiang University of Technology, Hangzhou, China.

Section of Endocrinology, School of Medicine, Yale University, New Haven, USA.

出版信息

J Pharm Pharmacol. 2017 Oct;69(10):1253-1264. doi: 10.1111/jphp.12774. Epub 2017 Jul 3.

Abstract

OBJECTIVES

Even with great advances in modern medicine and therapeutic agent development, the search for effective antidiabetic drugs remains challenging. Coumarins are secondary metabolites found widely in nature plants and used mainly in anticoagulation and antithrombotic therapy. Over the past two decades, however, there has been an increasing body of literatures related to the effects of coumarins and their derivatives on diabetes and its complications. This review aimed to focus on research findings concerning the effects of coumarins against diabetes and its complications using in-vitro and in-vivo animal models, and also to discuss cellular and molecular mechanisms underlying these effects.

KEY FINDINGS

The search for new coumarins against diabetes and it complications, either isolated from traditional medicine or chemically synthesized, has been constantly expanding. The cellular and molecular mechanisms involved include protecting pancreatic beta cells from damage, improving abnormal insulin signalling, reducing oxidative stress/inflammation, activating AMP-activated protein kinase (AMPK), inhibiting α-glucosidases and ameliorating diabetic complications.

CONCLUSIONS

The effects and mechanisms of coumarins and their derivatives upon diabetes and its complications are discussed in current review. Further investigations remain to be carried out to develop a promising antidiabetic agent based on coumarin cores.

摘要

目的

即使在现代医学和治疗剂开发方面取得了巨大进展,寻找有效的抗糖尿病药物仍然具有挑战性。香豆素是广泛存在于天然植物中的次生代谢产物,主要用于抗凝和抗血栓治疗。然而,在过去的二十年中,关于香豆素及其衍生物对糖尿病及其并发症的影响的文献越来越多。本综述旨在关注使用体外和体内动物模型研究香豆素对糖尿病及其并发症的作用的研究结果,并讨论这些作用的细胞和分子机制。

主要发现

一直在不断探索从传统医学中分离或化学合成的新型香豆素来治疗糖尿病及其并发症。所涉及的细胞和分子机制包括保护胰岛β细胞免受损伤、改善异常的胰岛素信号传递、减少氧化应激/炎症、激活 AMP 激活的蛋白激酶 (AMPK)、抑制α-葡萄糖苷酶和改善糖尿病并发症。

结论

本综述讨论了香豆素及其衍生物对糖尿病及其并发症的作用和机制。需要进一步研究以开发基于香豆素核心的有前途的抗糖尿病药物。

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