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α-葡萄糖苷酶抑制剂的体外和体内筛选综述

A review on the in vitro and in vivo screening of α-glucosidase inhibitors.

作者信息

Pan Guangjuan, Lu Yantong, Wei Zhiying, Li Yaohua, Li Li, Pan Xiaojiao

机构信息

Guangxi University of Chinese Medicine, Nanning, 530200, China.

Guangxi Key Laboratory of Zhuang and Yao Ethnic Medicine, Nanning, 530200, China.

出版信息

Heliyon. 2024 Sep 8;10(18):e37467. doi: 10.1016/j.heliyon.2024.e37467. eCollection 2024 Sep 30.

Abstract

As a global metabolic disease, the control and treatment of diabetes have always been the focus of medical research. α-Glucosidase is a key enzyme in regulating blood glucose levels and has important applications in the treatment of diabetes. This review aims to explore the enzyme activity of α-glucosidase and its inhibition mechanism and evaluate the efficacy and limitations of existing inhibitor screening methods. First, the chemical structure, biological activity, and influencing factors of α-glucosidase on diabetes are discussed in detail. Then, the various methods that have been used to screen α-glucosidase inhibitors in recent years are reviewed, including in vivo animal experiments, in vitro experiments, and virtual molecular docking. The experimental principles, advantages, and limitations of each method and their application in discovering new inhibitors are also discussed. Finally, this review emphasizes the importance of developing efficient and safe α-glucosidase inhibitors, summarizes the advantages and disadvantages of various screening models, and proposes future research directions. This review comprehensively examines the enzyme activity of α-glucosidase and the screening methods for α-glucosidase inhibitors, provides an important perspective in the field of diabetes drug discovery and development, and provides a reference for future research.

摘要

作为一种全球性代谢疾病,糖尿病的控制与治疗一直是医学研究的重点。α-葡萄糖苷酶是调节血糖水平的关键酶,在糖尿病治疗中具有重要应用。本综述旨在探讨α-葡萄糖苷酶的酶活性及其抑制机制,并评估现有抑制剂筛选方法的疗效和局限性。首先,详细讨论了α-葡萄糖苷酶的化学结构、生物学活性以及对糖尿病的影响因素。然后,综述了近年来用于筛选α-葡萄糖苷酶抑制剂的各种方法,包括体内动物实验、体外实验和虚拟分子对接。还讨论了每种方法的实验原理、优点和局限性及其在发现新抑制剂中的应用。最后,本综述强调了开发高效、安全的α-葡萄糖苷酶抑制剂的重要性,总结了各种筛选模型的优缺点,并提出了未来的研究方向。本综述全面考察了α-葡萄糖苷酶的酶活性和α-葡萄糖苷酶抑制剂的筛选方法,为糖尿病药物研发领域提供了重要视角,并为未来研究提供参考。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/43ad/11415703/b45a168067ea/gr1.jpg

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