Abstract

Diabetes mellitus remains a major global health issue, and great attention is directed at natural therapeutics. This systematic review aimed to assess the potential of flavonoids as antidiabetic agents by investigating their inhibitory effects on α-glucosidase and α-amylase, two key enzymes involved in starch digestion. Six scientific databases (PubMed, Virtual Health Library, EMBASE, SCOPUS, Web of Science, and WHO Global Index Medicus) were searched until August 21, 2022, for in vitro studies reporting IC₅₀ values of purified flavonoids on α-amylase and α-glucosidase, along with corresponding data for acarbose as a positive control. A total of 339 eligible articles were analyzed, resulting in the retrieval of 1643 flavonoid structures. These structures were rigorously standardized and curated, yielding 974 unique compounds, among which 177 flavonoids exhibited inhibition of both α-glucosidase and α-amylase are presented. Quality assessment utilizing a modified CONSORT checklist and structure–activity relationship (SAR) analysis were performed, revealing crucial features for the simultaneous inhibition of flavonoids against both enzymes. Moreover, the review also addressed several limitations in the current research landscape and proposed potential solutions. The curated datasets are available online at https://github.com/MedChemUMP/FDIGA.

Graphical Abstract

中文翻译：

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类黄酮作为 α-葡萄糖苷酶和 α-淀粉酶双靶点抑制剂：体外研究的系统评价

摘要

糖尿病仍然是一个主要的全球健康问题，自然疗法受到极大关注。本系统综述旨在通过研究类黄酮对 α-葡萄糖苷酶和 α-淀粉酶（淀粉消化中涉及的两种关键酶）的抑制作用，评估类黄酮作为抗糖尿病药物的潜力。截至 2022 年 8 月 21 日，对六个科学数据库（PubMed、Virtual Health Library、EMBASE、SCOPUS、Web of Science 和 WHO Global Index Medicus）进行了检索，以获取报告纯化黄酮类化合物对 α-淀粉酶和 α- 的 IC ₅₀值的体外研究。葡萄糖苷酶，以及作为阳性对照的阿卡波糖的相应数据。总共分析了 339 篇符合条件的文章，检索到 1643 个黄酮类结构。这些结构经过严格标准化和策划，产生了 974 种独特的化合物，其中 177 种黄酮类化合物表现出对 α-葡萄糖苷酶和 α-淀粉酶的抑制作用。利用修改后的 CONSORT 检查表和构效关系 (SAR) 分析进行质量评估，揭示了类黄酮同时抑制两种酶的关键特征。此外，该评论还解决了当前研究领域的一些局限性，并提出了潜在的解决方案。整理的数据集可在线获取：https://github.com/MedChemUMP/FDIGA。

图形概要