Out of multiple therapeutic targets, DPP-IV is the lead target for the treatment of the 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 inhibitor were found to be resveratrol, luteolin, apigenin and flavone having activity in nanomolar range. Standard drugs like sitagliptin, saxagliptin, diprotin A have complex structures as compared to these phenolic compounds. Flavonoids and phenolic compounds have their added advantages in being present in the many functional foods and carry antioxidant properties also. So, the scientists working on the new chemical entity hunting for the type 2 diabetes treatment can explore these natural sources for lead generation.