title: Antiglycation activity of quinoline derivatives- a new therapeutic class for the management of type 2 diabetes complications.
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.
authors.forename: Bilquees
authors.initials: B
authors.lastname: Bano
authors.forename: Sanaullah
authors.initials: S
authors.lastname: Abbasi
authors.forename: Jalaluddin A J
authors.initials: JA
authors.lastname: Khan
authors.forename: Shafqat
authors.initials: S
authors.lastname: Hussain
authors.forename: Saima
authors.initials: S
authors.lastname: Rasheed
authors.forename: Shahnaz
authors.initials: S
authors.lastname: Perveen
authors.forename: Khalid Mohammed
authors.initials: KM
authors.lastname: Khan
authors.affiliation: H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan. khalid.khan@iccs.edu.
authors.forename: M Iqbal
authors.initials: MI
authors.lastname: Choudhary
mesh_terms: D000818:Animals; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001713:Biphenyl Compounds / Q000037:antagonists & inhibitors; D002417:Cattle; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy; D017127:Glycation End Products, Advanced; D006031:Glycosylation / Q000187:drug effects; D006146:Guanidines / Q000494:pharmacology; D007004:Hypoglycemic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D051379:Mice; D041681:NIH 3T3 Cells; D010851:Picrates / Q000037:antagonists & inhibitors; D011765:Pyruvaldehyde / Q000037:antagonists & inhibitors / Q000737:chemistry; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D017382:Reactive Oxygen Species / Q000037:antagonists & inhibitors; D012431:Rutin / Q000494:pharmacology; D012545:Schiff Bases / Q000737:chemistry; D012710:Serum Albumin, Bovine / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D000975:Antioxidants; D001713:Biphenyl Compounds; D017127:Glycation End Products, Advanced; D006146:Guanidines; D007004:Hypoglycemic Agents; D010851:Picrates; D011804:Quinolines; D017382:Reactive Oxygen Species; D012545:Schiff Bases; D012710:Serum Albumin, Bovine; D012431:Rutin; D011765:Pyruvaldehyde; C004931:1,1-diphenyl-2-picrylhydrazyl; C004479:pimagedine