Background:
Curcumin, as the substantial constituent of the turmeric plant (Curcuma longa), plays a significant role in
the prevention of various diseases, including diabetes. It possesses ideal structure features as enzyme inhibitor, including a flexible
backbone, hydrophobic nature, and several available hydrogen bond (H-bond) donors and acceptors.
Objective:
The present study aimed at synthesizing several novel curcumin derivatives and further evaluation of these compounds
for possible antioxidant and anti-diabetic properties along with inhibitory effect against two carbohydrate-hydrolyzing enzymes,
α-amylase and α-glucosidase, as these enzymes are therapeutic targets for attenuation of postprandial hyperglycemia.
Methods:
Therefore, curcumin-based pyrido[2,3-d]pyrimidine derivatives were synthesized and identified using an instrumental
technique like NMR spectroscopy and then screened for antioxidant and enzyme inhibitory potential. Total antioxidant activity,
reducing power assay and 1,1-diphenyl-2-picrylhydrazyl (DPPH•
) radical scavenging activity were done to appraisal the antioxidant
potential of these compounds in vitro.
Results:
Compounds L6-L9 showed higher antioxidant activity while L4, L9, L12 and especially L8 exhibited the best selectivity
index (lowest α-amylase/α-glucosidase inhibition ratio).
Conclusion:
These antioxidant inhibitors may be potential anti-diabetic drugs, not only to reduce glycemic index but also to limit
the activity of the major reactive oxygen species (ROS) producing pathways.
Characterization, antioxidant activity, and inhibitory effect on pancreatic lipase of extracts from the edible insects Acheta domesticus and Tenebrio molitor