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 µM. Compounds 12 (IC50 = 661.78 ± 8.7 µM) and 15 (IC50 = 629.43 ± 7.85 7 µM) were also identified
as modest inhibitors, in comparison to the standard inhibitor, rutin (IC50 = 294.50 ± 1.5 µM). When evaluated for antioxidant
activity through in vitro DPPH radical scavenging assay, compounds 3 (IC50 = 2.19 ± 0.27 µM), 6 (IC50 = 7.35 ±
2.27 µM), 11 (IC50 = 8.96 ± 0.56 µM), and 12 (IC50 = 10.11 ± 2.03 µM), and 15 (IC50 = 7.01 ± 3.87 µM) were found to be
more active than the standard i.e. gallic acid (IC50 = 23.34 ± 0.43 µM). 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.
Advanced glycation end products (AGEs), antioxidant, diabetes, glycation inhibitors, quinoline, reactive oxygen
H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan.