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The effect of brimonidine and proparacaine on metabolic enzymes: Glucose-6-phosphate dehydrogenase, 6-phosphogluconate dehydrogenase, and glutathione reductase
Biotechnology and Applied Biochemistry ( IF 2.8 ) Pub Date : 2021-01-13 , DOI: 10.1002/bab.2107
Büşra Çalışkan 1 , Arzu Öztürk Kesebir 2 , Yeliz Demir 3 , İlknur Akyol Salman 1
Affiliation  

Oxidative stress is to upregulate the pentose phosphate pathway (PPP). The PPP consists of two functional branches, glucose-6-phosphate dehydrogenase (G6PD) and 6-phosphogluconaste dehydrogenase (6PGD). Glutathione reductase (GR) has a significant role in catalyzing an oxidized glutathione form into a reduced form. The purpose of this study is to investigate the effects of brimonidine and proparacaine on the activity of 6PGD, G6PD, and GR enzymes purified from human erythrocytes. Brimonidine displayed considerable inhibition profile against G6PD with IC50 value and KI constant of 29.93 ± 3.56 and 48.46 ± 0.66 μM, respectively. On the other hand, proparacaine had no inhibitory effect against G6PD. KI values were found to be 66.06 ± 0.78 and 811.50 ± 11.13 μM for brimonidine and proparacaine, respectively, for 6PGD. KI values were found to be 144.10 ± 2.01 and 1,654.00 ± 26.29 μM for brimonidine and proparacaine, respectively, for GR. Herein, also in silico molecular docking studies were performed between drugs and enzymes.

中文翻译:

溴莫尼定和丙美卡因对代谢酶的影响:6-磷酸葡萄糖脱氢酶、6-磷酸葡萄糖酸脱氢酶和谷胱甘肽还原酶

氧化应激是上调戊糖磷酸途径(PPP)。PPP 由两个功能分支组成,即 6-磷酸葡萄糖脱氢酶 (G6PD) 和 6-磷酸葡萄糖酸脱氢酶 (6PGD)。谷胱甘肽还原酶 (GR) 在将氧化的谷胱甘肽形式催化为还原形式方面具有重要作用。本研究的目的是研究溴莫尼定和丙美卡因对从人红细胞中纯化的 6PGD、G6PD 和 GR 酶活性的影响。Brimonidine 对 G6PD 表现出相当大的抑制作用,IC 50值和K I常数分别为 29.93 ± 3.56 和 48.46 ± 0.66 μM。另一方面,丙美卡因对 G6PD 没有抑制作用。_对于 6PGD,溴莫尼定和丙美卡因的值分别为 66.06 ± 0.78 和 811.50 ± 11.13 μM。对于 GR,溴莫尼定和丙美卡因的K I值分别为 144.10 ± 2.01 和 1,654.00 ± 26.29 μM。在此,还在药物和酶之间进行了计算机分子对接研究。
更新日期:2021-01-13
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