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具有抗糖尿病活性的天然来源的酶抑制剂:综述。

Enzymes inhibitors from natural sources with antidiabetic activity: A review.

机构信息

Department of Pharmacy, COMSATS University, Islamabad, Pakistan.

出版信息

Phytother Res. 2019 Jan;33(1):41-54. doi: 10.1002/ptr.6211. Epub 2018 Nov 11.

DOI:10.1002/ptr.6211
PMID:30417583
Abstract

Natural products have been extensively investigated for antidiabetic therapy. Many of the natural products have direct or indirect effect in diabetes pathways as enzyme inhibitors. The most involved mechanisms are inhibition of intestinal alpha-glucosidase and alpha-amylase, lens aldose reductase, oxidative stress protection, inhibition of formation of advanced glycation end products, inhibition of aldose reductase, lowering plasma glucose levels, altering enzyme activity of hexokinases and glucose-6-phosphate, synthesizing and releasing of insulin, postprandial hyperglycemia inhibition, stimulation of GLUT-4, decreasing activity of G6P, lowering the level of skeletal hexokinases, etc. The following medicinal plants products or extracts showed promising effects as enzyme inhibitors: Abelmoschus moschatus, Alangium salvifolium, Azadirachta indica, Bidens pilosa, Boerhaavia diffusa, Capsicum frutescens, Cassia alata, Eclipta alba, Embellica officinalis, Ficus carica, Gentiana Olivier, Glycyrrhiza glabra, Gymnema sylvestre, Hordeum vulgare, Ipomoea aquatica, Juniperus communis, Mangifera indica, Momordica charantia, Ocimum sanctum, Punica granatum, and Zingiber officinale. Some of the group of phytochemicals isolated with enzyme inhibition activities are Alkaloids, sesquiterpene and saponins, polysaccharides, flavonoids, dietary fibers, ferulic acid, tannins, limonene, and oleuropeoside. This review will provide very useful material to enhance the efficiency of rational antidiabetic drug design.

摘要

天然产物在抗糖尿病治疗中得到了广泛的研究。许多天然产物具有直接或间接的作用,可作为酶抑制剂参与糖尿病途径。最涉及的机制是抑制肠道α-葡萄糖苷酶和α-淀粉酶、晶状体醛糖还原酶、氧化应激保护、抑制晚期糖基化终产物的形成、抑制醛糖还原酶、降低血糖水平、改变己糖激酶和葡萄糖-6-磷酸的酶活性、合成和释放胰岛素、抑制餐后高血糖、刺激 GLUT-4、降低 G6P 活性、降低骨骼肌己糖激酶活性等。以下药用植物产品或提取物作为酶抑制剂表现出有前景的效果:冬葵、冬葵、印楝、鬼针草、田基黄、辣椒、鸡冠花、白背叶、白花蛇舌草、石榴、番石榴、甘草、甜叶菊、贯叶连翘、大麦、水飞蓟、和姜黄。一些具有酶抑制活性的植物化学物质组分为生物碱、倍半萜和皂苷、多糖、类黄酮、膳食纤维、阿魏酸、单宁、柠檬烯和橄榄苦苷。本综述将为提高合理抗糖尿病药物设计的效率提供非常有用的材料。

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