Abstract:

Aldoz reduktase (AR) catalyses sorbitol production from glucose through polyol and is a critical enzyme that causes an abnormal sorbitol aggregation in insulin-independent tissues, causing certain problems such as retinopathy, neuropathy and nefropathy. AR inhibition has been shown to be a suitable approach to reduce these side effects. The current study aims to introduce new AR inhibitors to literature. For this purpose, benzaldehits have been studied as AR inhibitors. The homogenate was first prepared from the livestock kidneys, then inhibition studies were performed. It was found that all the benzaldehite derivatives that were studied inhibited the AR. The inhibitor activity of derivatives 3 and 6, with the values of 0.23 and 1.37 μM IC50, was found to be higher than the standard inhibitor sorbinil. After in vitro inhibition studies, the estimated linking energies and derivatives’ enzyme linking modes were predicted by molecular docking. The compound showed a maximum placement score of 3, -8,61 kcal/mol. As a result, these compounds, especially compound 3, may be the leading molecules for the synthesis of new drug candidate molecules in the treatment or prevention of diabetic complications.

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