Protein glycation is one of the major causes of diabetic complications while antiglycation therapy is the most important intervention to manage diabetic complications.  Currently, sulfur-containing compounds are under extensive studies due to their vast pharmacological applications particularly, against diabetic mellitus and oxidative stress induced pathological disorders.

Present study is an effort to evaluate various classes of organosulfur compounds to explore promising inhibitors against protein glycation with enhanced antiglycation potential and low toxic effects. A library of organosulfur compounds belonging to different classes was investigated for their potential inhibition against protein glycation in vitro while MTT assay on mouse fibroblast 3T3 cells was used to assess the potential cytotoxicity of most promising antiglycation agents.

On antiglycation assay, eight organosulfur compounds (1-8) exhibited a potent antiglycation activity with IC50 values (<16 µM), as compared to standard antiglycation agent rutin (IC50 = 98.01±2.03 µM). Similarly, compound (9) and compound (10) exhibited good antiglycation potential with IC50 values 591.6±1.53 and 401±1.20 µM, respectively. In this assay compounds (12-18) exhibited moderate antiglycation activity (47-62% inhibition) at 1mM concentration.

On mouse fibroblast 3T3 cells cytotoxicity assay, all the tested compounds were found to be largely non-toxic with IC50 values (72.5-100) µM. In this assay, compound (10) exhibited slight toxic nature with IC50 value 5.00±1.89 as compared cycloheximide which is used as a standard in this assay with IC50 value 0.3 ± 0.089 μM.

Key Words: Organosulfur compounds, diabetic complications, antiglycation agents, cytotoxicity assay