Investigation of Potential Effects of Some Indole Compounds on the Glutathione S-Transferase Enzyme

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Muhammet Serhat Özaslan^a

Department of Pharmacy Services, Nihat Delibalta Göle Vocational High School, Ardahan University, 75700 Ardahan, Turkey

Received August 23, 2023; Revised February 23, 2024; Accepted February 27, 2024

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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, K_i 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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KEY WORDS: purification, glutathione S-transferase, indole, enzyme inhibition

DOI: 10.1134/S0006297924030131

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