Increased therapeutic effect of nanotized silibinin against glycation and diabetes: An in vitro and in silico-based approach

The global prevalence of diabetes has increased sharply, with the number of cases expected to rise from 424.9 million in 2017 to 628.6 million by 2045. Flavonoids are plant derived molecules with well-established antioxidant potential in addition to other therapeutic properties. Silibinin is a naturally occurring flavonoid with antioxidant and antidiabetic properties. However, its rapid metabolism and low bioavailability limit its therapeutic effects. In this study, we have synthesized the nanoformulation of silibinin and compared its antiglycating and antidiabetic potential with the soluble form. The inhibitory effect was tested on carbohydrate-hydrolyzing enzymes as well as glycation of human serum albumin (HSA). The structural and biochemical changes in HSA were assessed by spectroscopic analyses and different assays. The nanoforms were found to be better inhibitors of α-amylase and α-glucosidase compared to the bulk forms. Glycation of HSA in the presence of nano-silibinin resulted in the formation of lower level of early and advanced glycation products. This was also confirmed by spectroscopic studies and by estimating protein oxidation and free lysine residues. Molecular docking studies further supported the experimental outcomes. These results indicate that the nano form has significantly stronger antidiabetic and antiglycating effects than the bulk form. Nano-silibinin could therefore be recommended as a dietary supplement for diabetics to help control glycation and other associated complications. [Display omitted] •The antioxidant power of silibinin gets enhanced after nanotization.•Silibinin and its nano formulation exhibited anti-diabetic and antiglycating activities in a dose-dependent manner.•The nanoform of silibinin acts as a better antidiabetic and antiglycating agent compared to its bulk form.•Nano silibinin may therefore, be a better alternative for controlling hyperglycemia and diabetes related complications.