Wed, 22 Nov 2017

In Vitro Aldose Reductase Inhibitory Activity of Some 2,4-Thiazolidinedione Derivatives

Gül A. İŞBİLEN1, Meltem CEYLAN-ÜNLÜSOY1, Mutlu SARIKAYA1, Oya BOZDAĞ-DÜNDAR1*, Net DAŞ-EVCİMEN1

1. Faculty of Pharmacy, Ankara University, Ankara, Turkey


ABSTRACT

Aldose reductase (ALR2; AR; EC 1.1.1.21) is the first enzyme of the polyol pathway, which reduces glucose to sorbitol, in the presence of NADPH. The pathway is completed by sorbitol dehydrogenase, which catalyzes the NAD-linked oxidation of sorbitol to fructose. Synthesis and accumulation of sorbitol in cells due to increased aldose reductase activity is one of the main causes of diabetic complications. The aim of our study is to determine the potential inhibitory effect of some 2, 4-TZD derivatives on aldose reductase enzyme activity. Aldose reductase enzyme is isolated from bovine lenses and the activity of the enzyme is determined by spectrophotometric method. In our study 13 thiazolidinedione (TZD) derivatives which are containing benzyl and phenacyl groups were studied. Maximum inhibitory activity was found with 2,4- TZD-N-unsubstituted compound (86 %).  Compound 13, unsubstituted compound which was showed the maximum inhibitory activity, will be the key formula of our future studies.

Keywords: Aldose reductase, polyol pathway, 2,4- thiazolidinedione derivatives


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