Drug Design & Discovery Laboratory, School of Medical and Allied Sciences, K.R. Mangalam University, Sohna Road, Gurugram, India.
Curr Protein Pept Sci. 2019;20(12):1218-1225. doi: 10.2174/1389203720666190502154129.
Out of multiple therapeutic targets, DPP-IV is the lead target for the treatment of type 2 diabetes. Natural products have always been available for the possible lead generation against various diseases and disorders. In the present review, we have covered various natural sources which have experimentally validated anti-diabetic activity for type 2 diabetic patients with specific focus on the DPP-IV inhibition. Out of all, the most potent DPP-IV inhibitors were found to be resveratrol, luteolin, apigenin and flavone having activity in nanomolar range. Standard drugs like sitagliptin, saxagliptin, and diprotin A have complex structures as compared to these phenolic compounds. Flavonoids and phenolic compounds have their added advantages in being present in a number of functional foods and carry antioxidant properties as well. So, the scientists working on the new chemical entity hunting for the type 2 diabetes treatment can also explore these natural sources for lead generation.
在多种治疗靶点中,DPP-IV 是治疗 2 型糖尿病的主要靶点。天然产物一直是针对各种疾病和失调产生可能的先导化合物的来源。在本综述中,我们涵盖了各种具有实验验证的抗糖尿病活性的天然来源,特别关注对 DPP-IV 的抑制作用。在所有这些来源中,最有效的 DPP-IV 抑制剂是白藜芦醇、木樨草素、芹菜素和黄酮,其活性在纳摩尔范围内。与这些酚类化合物相比,西他列汀、沙格列汀和二肽基肽酶 4 抑制剂等标准药物具有复杂的结构。类黄酮和酚类化合物具有许多优点,它们存在于许多功能性食品中,并且具有抗氧化特性。因此,从事 2 型糖尿病治疗新药研发的科学家也可以探索这些天然资源来寻找先导化合物。