Antiglycation Activity of Quinoline Derivatives- A New Therapeutic Class for the Management of Type 2 Diabetes Complications

Title:Antiglycation Activity of Quinoline Derivatives- A New Therapeutic Class for the Management of Type 2 Diabetes Complications

Volume: 11 Issue: 1

Author(s): Bilquees Bano, Sanaullah Abbasi, Jalaluddin A. J. Khan, Shafqat Hussain, Saima Rasheed, Shahnaz Perveen, Khalid Mohammed Khan and M. Iqbal Choudhary

Affiliation:

Keywords: Advanced glycation end products (AGEs), antioxidant, diabetes, glycation inhibitors, quinoline, reactive oxygen species.

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 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.

Cite this article as:

Bano Bilquees, Abbasi Sanaullah, Khan A. J. Jalaluddin, Hussain Shafqat, Rasheed Saima, Perveen Shahnaz, Khan Mohammed Khalid and Choudhary Iqbal M., Antiglycation Activity of Quinoline Derivatives- A New Therapeutic Class for the Management of Type 2 Diabetes Complications, Medicinal Chemistry 2015; 11 (1) . https://dx.doi.org/10.2174/1573406410666140526151254