4.3 Article

Some sulfonamides as aldose reductase inhibitors: therapeutic approach in diabetes

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ARCHIVES OF PHYSIOLOGY AND BIOCHEMISTRY
卷 128, 期 4, 页码 979-984

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TAYLOR & FRANCIS LTD
DOI: 10.1080/13813455.2020.1742166

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Enzyme purification; aldose reductase; oxidative stress; enzyme inhibition; sulfonamides

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In this study, aldose reductase (AR) was purified from sheep kidney and the interactions between some sulfonamides and the enzyme were examined. The results show that sulfonamides effectively inhibit sheep kidney AR and display different inhibition mechanisms.
In this study, aldose reductase (AR) was purified from sheep kidney using chromatographic methods and examined the interactions between some sulfonamides and the enzyme. According to results, sulfonamides display effective inhibitor features for sheep kidney AR with IC50 values in the range of 37.27-87.65 mu M and K(i)s in the range of 25.72 +/- 6.45 to 73.56 +/- 17.49 mu M. The sulfonamides displayed different inhibition mechanisms. It was found that studied all compounds displayed non-competitive inhibition type except for 5-chlorothiophene-2-sulfonamide (1). It showed competitive inhibition. Among these compounds, 2,5-dichlorothiophene-3-sulfonamide compound (2) was showed the most potent AR inhibitor (K-i: 25.72 +/- 6.45). These compounds may be useful in the treatment of diabetic complications.

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