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槲皮素的抗糖尿病潜力:潜在机制

The Antidiabetic Potential of Quercetin: Underlying Mechanisms.

作者信息

Eid Hoda M, Haddad Pierre S

机构信息

Natural Health Products and Metabolic Diseases Laboratory, Department of Pharmacology, Universite de Montreal, Montreal, QC, Canada.

Department of Pharmacology, Universite de Montreal. P.O. Box 6128, Station Centre- Ville, Montreal, Quebec, H3C 3J7, Canada.

出版信息

Curr Med Chem. 2017;24(4):355-364. doi: 10.2174/0929867323666160909153707.

Abstract

The dramatic increase in modern lifestyle diseases such as cancer, cardiovascular diseases and diabetes has renewed researchers' interest to explore nature as a source of novel therapeutic agents. Flavonoids are a large group of polyphenols that are widely present in the human diet. They have shown promising therapeutic activities against a wide variety of ailments. One of the most widely distributed and most extensively studied flavonoid is the flavonol quercetin. Its powerful antioxidant and anti-inflammatory activities are well documented and are thought to play a role in treating and protecting against diseases including diabetes, cancer, neurodegenerative and cardiovascular diseases. The purpose of this review is to shed light on quercetin therapeutic potential as an antidiabetic agent. Quercetin was reported to interact with many molecular targets in small intestine, pancreas, skeletal muscle, adipose tissue and liver to control whole-body glucose homeostasis. Mechanisms of action of quercetin are pleiotropic and involve the inhibition of intestinal glucose absorption, insulin secretory and insulin-sensitizing activities as well as improved glucose utilization in peripheral tissues. Initial studies suggested poor bioavailability of quercetin. However, recent reports have shown that quercetin was detected in the plasma after food or supplements consumption and has a long half-life in human body. Despite the wealth of in vitro and in vivo results supporting the antidiabetic potential of quercetin, its efficacy in diabetic human subjects is yet to be explored.

摘要

癌症、心血管疾病和糖尿病等现代生活方式疾病的急剧增加,重新激发了研究人员探索大自然作为新型治疗药物来源的兴趣。黄酮类化合物是一大类多酚,广泛存在于人类饮食中。它们已显示出对多种疾病具有有前景的治疗活性。分布最广、研究最深入的黄酮类化合物之一是黄酮醇槲皮素。其强大的抗氧化和抗炎活性已有充分记录,并被认为在治疗和预防包括糖尿病、癌症、神经退行性疾病和心血管疾病在内的疾病中发挥作用。本综述的目的是阐明槲皮素作为抗糖尿病药物的治疗潜力。据报道,槲皮素与小肠、胰腺、骨骼肌、脂肪组织和肝脏中的许多分子靶点相互作用,以控制全身葡萄糖稳态。槲皮素的作用机制是多效性的,包括抑制肠道葡萄糖吸收、胰岛素分泌和胰岛素增敏活性,以及改善外周组织中的葡萄糖利用。初步研究表明槲皮素的生物利用度较差。然而,最近的报告显示,食用食物或补充剂后在血浆中检测到了槲皮素,并且它在人体中的半衰期很长。尽管有大量体外和体内研究结果支持槲皮素的抗糖尿病潜力,但其在糖尿病患者中的疗效仍有待探索。

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