Agrawal Neetu, Sharma Manisha, Singh Shikha, Goyal Ahsas
Institute of Pharmaceutical Research, GLA University, Mathura, 281406 U.P., India.
Curr Top Med Chem. 2022;22(25):2069-2086. doi: 10.2174/1568026622666220831092855.
Diabetes mellitus (DM) is a critical health issue prevailing in nearly half a billion people worldwide. It is one of the most threatening metabolic diseases. Type 2 DM is caused due to insulin resistance and accounts for 90% of diabetes cases. If it remains untreated, it can lead to major frightening complications and can cause death, which ultimately threatens humankind.
Various oral hypoglycaemic drugs are available today, acting on different targets by adopting different pathways. However, the α-glucosidase inhibitors proved to be a novel and effective strategy to manage T2DM. These inhibitors alleviate postprandial glycemia by aiming to inhibit intestinal α-glucosidase competitively and reversibly, thus delaying carbohydrate digestion and turning down the rate of glucose absorption. Plenty of α-glucosidase inhibitors have been discovered from synthetic routes as well as from natural sources, including plants, fungi, and bacteria.
This article comprises the natural and synthetic α-glucosidase discovered from 2016 to 2021 and can be utilized to discover novel α-glucosidase inhibitors. This review is an endeavor to highlight the progress in the discovery and development of α-glucosidase inhibitors, which could provide an overview to the medicinal chemists for the development of clinically viable drugs using this information.
糖尿病（DM）是一个在全球近5亿人中普遍存在的关键健康问题。它是最具威胁性的代谢疾病之一。2型糖尿病是由胰岛素抵抗引起的，占糖尿病病例的90%。如果不加以治疗，它会导致严重可怕的并发症并可能导致死亡，最终威胁人类。
如今有各种口服降糖药，它们通过不同途径作用于不同靶点。然而，α-葡萄糖苷酶抑制剂被证明是治疗2型糖尿病的一种新颖且有效的策略。这些抑制剂旨在竞争性和可逆性地抑制肠道α-葡萄糖苷酶，从而减轻餐后高血糖，进而延迟碳水化合物消化并降低葡萄糖吸收速率。已经从合成途径以及包括植物、真菌和细菌在内的天然来源中发现了大量α-葡萄糖苷酶抑制剂。
本文涵盖了2016年至2021年发现的天然和合成α-葡萄糖苷酶，可用于发现新型α-葡萄糖苷酶抑制剂。这篇综述旨在突出α-葡萄糖苷酶抑制剂发现和开发方面的进展，可为药物化学家利用这些信息开发临床可行药物提供一个概述。
