Abstract
Quercetin and coumarin, two naturally occurring phytochemicals of plant origin, are known to regulate hyperglycemia and oxidative stress. The present study was designed to evaluate the inhibitory activity of quercetin and coumarin on dipeptidyl peptidase-IV (DPP-IV) and their antioxidant potential. DPP-IV inhibition assays were performed, and evaluated IC50 values of diprotin A, quercetin, coumarin, and sitagliptin were found to be 0.653, 4.02, 54.83, and 5.49 nmol/mL, respectively. Furthermore, in silico studies such as the drug-likeliness and docking efficiency of quercetin and coumarin to the DPP-IV protein were performed; the ex vivo antiperoxidative potential of quercetin and coumarin were also evaluated. The results of the present study showed that the DPP-IV inhibitory potential of quercetin was slightly higher than that of sitagliptin. Virtual docking revealed the tight binding of quercetin with DPP-IV protein. Quercetin and coumarin reduced oxidative stress in vitro and ex vivo systems. We report for the first time that both compounds inhibited the DPP-IV along with antioxidant activity and thus may be use as function food ingredients in the prevention of diabetes.
Highlights
Type 2 diabetes mellitus (T2DM) is a rapidly growing metabolic disorder with multiple etiologies leading to chronic hyperglycemia and insulin resistance [1]
Comparative analysis of the structural components of quercetin and coumarin revealed that the functional groups of both phytochemicals interacted with the agonist binding site of the dipeptidyl peptidase-IV (DPP-IV) enzyme
Based on the results of this study, we concluded that bioactive compounds from plants have the potential to act as DPP-IV inhibitors, leading to glucose homeostasis, and can be used in the development of novel therapeutic strategies for the treatment of diabetes
Summary
Type 2 diabetes mellitus (T2DM) is a rapidly growing metabolic disorder with multiple etiologies leading to chronic hyperglycemia and insulin resistance [1]. The current treatment regimen for T2DM includes several oral hypoglycemic agents (sulfonylureas, biguanides, troglitazone, α-glucosidase inhibitors, thiazolidinediones, and secretagogues) and direct insulin therapy [2,3] These treatments fail to achieve rigorous metabolic control in more than 50% of T2DM cases, necessitating the search for novel antidiabetic agents that mimic or enhance the properties of insulin, as well as protect against diabetic complications. These therapies pose various side effects such as obesity, insulin resistance, hypoglycemia, atherosclerosis, and hormonal imbalance [4]. Quercetin has been reported to exert a protective effect against beta-cell damage, by ameliorating hyperglycemia, hyperlipidemia, and insulin resistance in diabetic rats [12]
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