Demir Yeliz, Işık Mesut, Gülçin İlhami, Beydemir Şükrü
Department of Chemistry, Faculty of Sciences, Atatürk University, Erzurum, 25240, Turkey.
Health Services Vocational School, Department of Pharmacy Services, Harran University, Şanlıurfa, 63000, Turkey.
J Biochem Mol Toxicol. 2017 Sep;31(9). doi: 10.1002/jbt.21935. Epub 2017 May 29.
Aldose reductase (AR) is the key enzyme for the polyol pathway and responsible for sorbitol accumulation during the hyperglycemia. The present article focuses on the role of phenol, pyrogallol, hydroquinone, resorcinol, catechol, and phloroglucinol in in vitro inhibition of AR. For this purpose, AR was purified from the sheep kidney with 5.33 EU mg specific activity and 0.64% yield using several chromatographic methods. Various concentrations of the compounds were tested on in vitro AR activity. IC values were found for phenol, pyrogallol, hydroquinone, resorcinol, catechol, and phloroglucinol as 6.5, 1.13, 5.45, 2.21, 1.8, and 2.09 mM, respectively, and their K constant was calculated as 3.45 ± 0.92, 0.96 ± 0.28, 3.07 ± 0.46, 1.59 ± 0.43, 2.5 ± 0.35, and 2.54 ± 0.45 mM, respectively. Pyrogallol showed better inhibitory effect compared to the other compounds. The inhibition mechanisms of all compounds were noncompetitive. In the presents study, in vitro AR inhibition was examined by the phenolic compounds.
醛糖还原酶（AR）是多元醇途径的关键酶，在高血糖期间负责山梨醇的积累。本文重点研究苯酚、连苯三酚、对苯二酚、间苯二酚、儿茶酚和间苯三酚在体外对AR的抑制作用。为此，采用多种色谱方法从羊肾中纯化出比活性为5.33 EU mg、产率为0.64%的AR。对不同浓度的这些化合物进行了体外AR活性测试。发现苯酚、连苯三酚、对苯二酚、间苯二酚、儿茶酚和间苯三酚的IC值分别为6.5、1.13、5.45、2.21、1.8和2.09 mM，其K常数分别计算为3.45±0.92、0.96±0.28、3.07±0.46、1.59±0.43、2.5±0.35和2.54±0.45 mM。与其他化合物相比，连苯三酚显示出更好的抑制效果。所有化合物的抑制机制均为非竞争性。在本研究中，通过酚类化合物检测了体外AR抑制作用。
