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Drug repositioning or repurposing,  i . e . identifying new indications for existing drugs, has gained increasing attention in the recent years. This approach enables the scientists to discover “new targets” for known drugs in a cost and time efficient manner. Glycation, the non-enzymatic reaction of sugars with proteins or nucleic acids to form early glycation (Amadori or fructosamine) products, is a key molecular basis of diabetic complications. Inhibiting the process of non-enzymatic protein glycation is one of the key strategies to prevent glycation-mediated diabetic complications. The present study focuses on the anti-glycation activity of 18 drugs, commonly used for the treatment of gastrointestinal, central nervous system, inflammatory diseases, bacterial infections, and gout. This study was carried out by using two  in-vitro  protein anti-glycation assay models. Results revealed that nimesulide ( 3 ), a non-steroidal anti-inflammatory drug, possesses a good anti-glycation activity in  in-vitro  BSA-MG and BSA-glucose glycation models with IC 50  values of 330.56 ± 2.90, and 145.46 ± 16.35  μ M, respectively. Phloroglucinol dihydrate ( 11 ), a drug used for the treatment of gastrointestinal diseases, showed a weak activity in BSA-MG glycation model (IC 50  = 654.89 ± 2.50  μ M), while it showed a good activity in BSA-glucose assay (IC 50  = 148.23 ± 0.15  μ M). Trimethylphloroglucinol ( 9 ), a drug used for the treatment of pain related to functional disorders of the digestive and biliary tracts, also showed a good antiglycation activity in BSA-MG model (IC 50  = 321.15 ± 1.26  μ M), while it was found to be inactive in  in-vitro  BSA-glucose assay (IC 50  = 12.95% inhibition). These activities of drugs were compared with the anti-glycation activity of the standard, rutin (IC 50  = 294.5 ± 1.50  μ M in BSA-MG glycation model, and IC 50  = 86.94 ± 0.24  μ M in BSA- glucose model). Rest of the drugs exhibited a relatively weak antiglycation activity. This study identifies nimesulide ( 3 ), and phloroglucinol dihydrate ( 11 ) as new inhibitors of  in-vitro  protein glycation for further investigations as potential anti-diabetic agents.

Drug repurposing: In-vitro anti-glycation properties of 18 common drugs