抗坏血酸对人红细胞谷胱甘肽S-转移酶的抑制作用

Q4 Pharmacology, Toxicology and Pharmaceutics

Current Enzyme Inhibition Pub Date : 2023-05-30 DOI:10.2174/1573408019666230530095315

M. - Erat, Yunus Emre Erat, Ayşe Rümeysa Erat

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引用次数: 0

摘要

某些特异性谷胱甘肽S-转移酶同功酶的抑制与癌症患者化疗的疗效有关。我们的目的是确定抗坏血酸是否是谷胱甘肽S-转移酶同工酶抑制剂，抗坏血酸可作为药物和抗氧化食品补充剂。为此，首次从人红细胞中纯化了谷胱甘肽S-转移酶，并研究了抗坏血酸对酶活性的体外影响。然后，进行动力学研究以评估抗坏血酸的抑制潜力，抗坏血酸被确定为该酶的抑制剂。该酶纯化1286倍，产率81%，比活性为18.00U/mg蛋白质。抗坏血酸对谷胱甘肽S-转移酶的体外酶活性的影响被测试，并且被检测为具有10mM IC50值的酶的抑制剂。还测定了该酶的Ki常数和抑制类型。这一发现表明，抗坏血酸可以有效抑制癌症细胞中某些GST同功酶的增加。大量摄入抗坏血酸可以通过增强抗氧化防御系统来预防癌症的形成，另一方面，它可以通过抑制化疗耐药性GST酶来提高癌症治疗的有效性。

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Inhibitory effect of ascorbic acid on glutathione S-transferase from human erythrocytes

Inhibition of certain specific glutathione S-transferase isozymes is associated with the efficacy of chemotherapy in the treatment of cancer patients. We aimed to determine whether ascorbic acid, which can be used as a drug and antioxidant food supplement, is a glutathione S-transferase isozyme inhibitor. For this purpose, glutathione S-transferase was first purified from human erythrocytes and the in vitro effect of ascorbic acid on enzyme activity was investigated. Then, kinetic studies were performed to evaluate the inhibition potential of ascorbic acid, which was determined to be an inhibitor of the enzyme. The enzyme was purified 1286-fold with a yield of 81% and specific activity of 18.00 U/mg protein. The effects of ascorbic acid were tested on the in vitro enzyme activity of glutathione S-transferase and detected to be an inhibitor for the enzyme with 10 mM of IC50 value. Ki constants and inhibition type were also determined for the enzyme. This finding indicates that ascorbic acid can be an effective inhibitor of some GST isoenzymes increased in cancer cells. Abundant ascorbic acid intake may prevent cancer formation by strengthening the antioxidant defense system, on the other hand, it may increase the effectiveness of cancer treatment by inhibiting the chemotherapy-resistant GST enzyme.

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来源期刊

Current Enzyme Inhibition Pharmacology, Toxicology and Pharmaceutics-Drug Discovery

CiteScore

1.30

自引率

0.00%

发文量

期刊介绍： Current Enzyme Inhibition aims to publish all the latest and outstanding developments in enzyme inhibition studies with regards to the mechanisms of inhibitory processes of enzymes, recognition of active sites, and the discovery of agonists and antagonists, leading to the design and development of new drugs of significant therapeutic value. Each issue contains a series of timely, in-depth reviews written by leaders in the field, covering a range of enzymes that can be exploited for drug development. Current Enzyme Inhibition is an essential journal for every pharmaceutical and medicinal chemist who wishes to have up-to-date knowledge about each and every development in the study of enzyme inhibition.