Research and Development Division, Greenvention Biotech Pvt. Ltd., Uruli-Kanchan, Pune, 412202, Maharashtra, India.
National Institute of Traditional Medicine, Indian Council of Medical Research (ICMR), Department of Health Research (Government of India), Nehru Nagar, Belagavi, 590010, Karnataka, India.
Curr Pharm Biotechnol. 2023;24(8):927-945. doi: 10.2174/1389201023666220506104219.
Diabetes is a growing health concern worldwide because it affects people of all age groups and increases the risk of other diseases such as renal impairment and neural and cardiovascular disorders. Oral hypoglycemic drugs mainly control diabetes; however, their associated side effects limit their use in patients with other complications. PTP1B is a viable drug target to explore new antidiabetic drugs. PTP1B acts as a negative regulator of the insulin-signaling pathway, and therefore, PTP1B inhibitors display antihyperglycemic activity. Several classes of compounds from natural and synthetic sources act as PTP1B inhibitors. Fungi are comprehensive in their diversity and recognized as a valuable source for therapeutically active molecules. In recent years, researchers have reported diverse classes of fungal secondary metabolites as potent PTP1B inhibitors. Some metabolites such as 6-O-methylalaternin, fumosorinone A, nordivaricatic acid, and the divarinyl divarate showed good activity and can be taken forward as a lead to develop novel PTP1B inhibitors and antidiabetic drugs. Therefore, the present review focuses on the fungal metabolites identified in the last five years possessing PTP1B inhibitory activity. A total of 128 metabolites are reviewed. Their fungal species and source, chemical structure, and activity in terms of IC are highlighted.
糖尿病是一个在全球范围内日益严重的健康问题，因为它影响所有年龄段的人群，并增加了其他疾病的风险，如肾功能损害、神经和心血管疾病。口服降糖药主要用于控制糖尿病；然而，它们相关的副作用限制了它们在有其他并发症的患者中的使用。PTP1B 是一个有前途的药物靶点，可以用来探索新的抗糖尿病药物。PTP1B 作为胰岛素信号通路的负调节剂，因此，PTP1B 抑制剂具有抗高血糖活性。来自天然和合成来源的几类化合物作为 PTP1B 抑制剂。真菌在多样性方面非常全面，被认为是治疗活性分子的有价值来源。近年来，研究人员已经报道了多种真菌次级代谢产物作为有效的 PTP1B 抑制剂。一些代谢物，如 6-O-甲基阿尔特林、呋塞米酮 A、诺地瓦酸和二烯基二酯，表现出良好的活性，可以作为开发新型 PTP1B 抑制剂和抗糖尿病药物的先导化合物。因此，本综述重点介绍了过去五年中鉴定出的具有 PTP1B 抑制活性的真菌代谢物。共综述了 128 种代谢物。它们的真菌种类和来源、化学结构以及在 IC 方面的活性都被强调了。
