Synthesis, in silico, in vitro and in vivo studies of novel natural-based arylidenes curcumin as potential glycohydrolase digestive enzymes inhibitors

Diabetes is one of the most common metabolic diseases in humans and the use of herbal medicines is of great clinical importance to inhibit carbohydrate-hydrolyzing enzymes and reduce blood glucose levels in diabetic patients. Inhibition of glycosidase activity is an effective way to treat and prevent diabetes. Therefore, in this study, curcumin-based benzaldehyde derivatives were synthesized and used as influential agents in the treatment of diabetes with inhibitory properties against two carbohydrate-hydrolyzing enzymes alpha-glucosidase (alpha-Glu) and alpha-amylase (alpha-Amy) as significant therapeutic targets for reducing postprandial hyperglycemia. Overall, the findings showed that due to the specific inhibitory activity against alpha-Glu in comparison with alpha-Amy, as well as more stability and antioxidant activity than curcumin, C5 and C8 derivatives are potentially important anti-diabetic drugs, not only to decrease glycemic index but also to limit the activity of the main production pathways of reactive oxygen species (ROS) in diabetic patients.

Automated summary

Diabetes, a common metabolic disease, can be treated by herbal medicines that inhibit carbohydrate-hydrolyzing enzymes and reduce blood glucose levels. In this study, curcumin-based benzaldehyde derivatives were synthesized as influential agents in diabetes treatment, inhibiting alpha-glucosidase and alpha-amylase to reduce postprandial hyperglycemia. The C5 and C8 derivatives showed specific inhibitory activity against alpha-glucosidase, as well as stability and antioxidant activity, making them potentially important anti-diabetic drugs to decrease glycemic index and limit reactive oxygen species production in diabetic patients.