Abstract
We report here a new class of compounds, quinoline derivatives, as potential inhibitors of in vitro bovine serum albumin-methylglyoxal glycation. Among compounds 1-19, compound 14 was found to be the most active analog with IC50 of 282.98 +/- 8.4 mu M. Compounds 12 (IC50 = 661.78 +/- 8.7 mu M) and 15 (IC50 = 629.43 +/- 7.85 7 mu M) were also identified as modest inhibitors, in comparison to the standard inhibitor, rutin (IC50 = 294.50 +/- 1.5 mu M). When evaluated for antioxidant activity through in vitro DPPH radical scavenging assay, compounds 3 (IC50 = 2.19 +/- 0.27 mu M), 6 (IC50 = 7.35 +/- 2.27 mu M), 11 (IC50 = 8.96 +/- 0.56 mu M), and 12 (IC50 = 10.11 +/- 2.03 mu M), and 15 (IC50 = 7.01 +/- 3.87 mu M) were found to be more active than the standard i.e. gallic acid (IC50 = 23.34 +/- 0.43 mu M). These compounds were also evaluated for cytotoxicity against rat fibroblast cell line (3T3 cell line). All compounds were found to be non-toxic in cellular model. This study identifies quinoline derivatives as a new class of inhibitors of protein glycation in vitro, along with antioxidant and non-toxic nature. These properties make them interesting leads for further studies as potential anti-diabetic agents.