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.