研究某些吲哚化合物对谷胱甘肽 S-转移酶的潜在影响

IF 2.3 4区 生物学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY Biochemistry (Moscow) Pub Date : 2024-04-08 DOI:10.1134/S0006297924030131
Muhammet Serhat Özaslan
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引用次数: 0

摘要

摘要谷胱甘肽 S-转移酶(GST)属于多功能解毒同工酶超家族,在细胞信号传导中发挥着重要作用。它们能通过共价结合同类分子,防止活性亲电化合物对人体造成伤害。除治疗干预外,GST 还可单独或联合用于癌症检测或诊断。近年来,吲哚因其结构特性和生物活性(如抗结核、抗溃疡、抗氧化和抗糖尿病)以及新抗癌剂的开发而变得非常重要。目前的研究调查了一些具有 3-甲醛结构的吲哚对 GST 酶活性的影响。研究考察了不同浓度的吲哚对体外 GST 活性的影响。这些化合物的 IC50 值介于 0.042 至 1.570 mM 之间,Ki 值介于 0.018 ± 0.01 至 1.110 ± 0.15 mM 之间。在所研究的吲哚类化合物中,6-甲基吲哚-3-甲醛(1b)的抑制作用最强。由于本研究中使用的吲哚衍生物对 GST 活性有影响,因此可在进一步的药理学研究中对其进行评估。
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Investigation of Potential Effects of Some Indole Compounds on the Glutathione S-Transferase Enzyme

Glutathione S-transferases (GSTs) belong to the superfamily of multifunctional detoxification isoenzymes with an important role in cellular signaling. They can prevent reactive electrophilic compounds from harming the body by covalently binding identical type of moleculs to each other. GSTs can be used alone or in combination for cancer detection or diagnosis, in addition to therapeutic interventions. In recent years, indoles have become important due to their structural properties and biological activities such as antitubercular, antiulcer, anti-oxidant, and antidiabetic, as well as for the development of new anticancer agents. The current research investigated effects of some indoles with 3-carboxaldehyde structure on the GST enzyme activity. Impacts of various concentrations of indoles on the in vitro GST activity were examined. While IC50 values for the compounds ranged from 0.042 to 1.570 mM, Ki values changed between 0.018 ± 0.01 and 1.110 ± 0.15 mM. 6-Methylindole-3-carboxaldehyde (1b) exhibited the highest inhibitory effect among the indoles examined. Indole derivatives used in the study can be evaluated in further pharmacological studies due to their effects on GST activity.

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来源期刊
Biochemistry (Moscow)
Biochemistry (Moscow) 生物-生化与分子生物学
CiteScore
4.70
自引率
3.60%
发文量
139
审稿时长
2 months
期刊介绍: Biochemistry (Moscow) is the journal that includes research papers in all fields of biochemistry as well as biochemical aspects of molecular biology, bioorganic chemistry, microbiology, immunology, physiology, and biomedical sciences. Coverage also extends to new experimental methods in biochemistry, theoretical contributions of biochemical importance, reviews of contemporary biochemical topics, and mini-reviews (News in Biochemistry).
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