Inhibition effects of quinones on aldose reductase: Antidiabetic properties

被引:62
作者
Demir, Yeliz [1 ,2 ]
Ozaslan, Muhammet Serhat [1 ,2 ]
Duran, Hatice Esra [1 ]
Kufrevioglu, Omer Irfan [1 ]
Beydemir, Sukru [3 ]
机构
[1] Ataturk Univ, Fac Sci, Dept Chem, TR-25240 Erzurum, Turkey
[2] Ardahan Univ, Nihat Delibalta Gole Vocat High Sch, Dept Pharm Serv, TR-75700 Ardahan, Turkey
[3] Anadolu Univ, Fac Pharm, Dept Biochem, TR-26470 Eskisehir, Turkey
关键词
Aldose reductase; Inhibition; Quinones; Purification; Diabetes; DERIVATIVES;
D O I
10.1016/j.etap.2019.103195
中图分类号
X [环境科学、安全科学];
学科分类号
08 ; 0830 ;
摘要
Diabetes mellitus is a chronic metabolic disease characterized by abnormal glucose metabolism. Aldose reductase (AR) is the first enzyme in the polyol pathway and converts glucose to sorbitol. It plays a vital role as a glucose reducing agent and is involved in the pathophysiology of diabetic complications. In this study, we purified AR from sheep kidney with a specific activity of 2.00 EU/mg protein and 133.33- fold purification After the purification of the AR enzyme, sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) was performed and the molecular weight of the enzyme was found approximately as 38 kDa. The inhibition effects of eight quinones were studied against AR. The quinones were potent inhibitors of AR with K-i values in the range of 0.07-20.04 mu M. Anthraquinone showed the best potential inhibitory effects against AR. All compounds exhibited noncompetitive inhibition against AR. These compounds may be selective inhibitors of this enzyme. AR inhibition is an essential strategy for the attenuation and prevention of diabetic complications.
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页数:6
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