Research and Development Division, Greenvention Biotech Pvt. Ltd., Uruli-Kanchan, Pune-412202, Maharashtra, India.
SGT College of Pharmacy, SGT University, Gurugram-122505 (HR), India.
Recent Pat Biotechnol. 2023;17(1):24-61. doi: 10.2174/1872208316666220512122439.
The enzyme α-glucosidases (EC 3.2.1.20) catalyzes the hydrolysis of α-1,4- glucopyranoside bond in oligosaccharides and disaccharides, and thus plays an essential role in regulating glucose content and the level of postprandial hyperglycemia. The inhibition of α-glucosidases is considered a viable strategy to develop new and effective antidiabetic drugs. Many patents like ZA201905405B; US9073897B2 have been published on α- glucosidase inhibitors. In recent years, several classes of fungal metabolites possessing a varying degree of α-glucosidases inhibitory activity have been reported. The primary chemical classes include xanthone, phenanthrene, terpenoid, coumarin, isocoumarin, naphthalene, piperazine, and polyketides. Few of the identified inhibitors exhibited severalfold better activities than well-known α-glucosidases inhibitor acarbose and can be used as a lead to develop new antidiabetic drugs. The present review highlights the recent development in the identification of α-glucosidases inhibitors from various fungal sources. Their chemical class, structures, and inhibitory activity in terms of IC or MIC are discussed here.
α-葡萄糖苷酶(EC 3.2.1.20)催化寡糖和二糖中α-1,4-葡萄糖苷键的水解,因此在调节葡萄糖含量和餐后高血糖水平方面起着至关重要的作用。抑制α-葡萄糖苷酶被认为是开发新型有效抗糖尿病药物的可行策略。已经发表了许多关于α-葡萄糖苷酶抑制剂的专利,如 ZA201905405B;US9073897B2。近年来,已经报道了几类具有不同程度α-葡萄糖苷酶抑制活性的真菌代谢产物。主要的化学类包括黄烷酮、菲、萜类、香豆素、异香豆素、萘、哌嗪和聚酮。一些已鉴定的抑制剂的活性比著名的α-葡萄糖苷酶抑制剂阿卡波糖高出几倍,可以作为开发新型抗糖尿病药物的先导化合物。本综述重点介绍了从各种真菌来源中鉴定α-葡萄糖苷酶抑制剂的最新进展。讨论了它们的化学类别、结构以及在 IC 或 MIC 方面的抑制活性。