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Synthesis, Cytotoxicity, Antioxidant and Antimicrobial Activity of Indole Based Novel Small Molecules

[ Vol. 18 , Issue. 5 ]

Author(s):

Aslıhan Kurt-Kızıldoğan, Çiğdem Otur, Can Yılmaz, Sevki Arslan, Dogukan Mutlu, Arif Kivrak*, Muheb Algso, Abdussamet Kayhan, Doğan Çetin and Metin Konus*   Pages 461 - 470 ( 10 )

Abstract:


Aims: In this study experiments were carried out to explore antioxidant, antimicrobial, cytotoxic properties of novel indole derivative 1-ethyl-2-phenyl-3-phenylethyl-3-thiophen-2-yl-1Hindole (EPI) together with its effect on glutathione S-transferases (GST) activities in human liver carcinoma (HepG2) cells.

Background: Indoles probably represent one of the most important heterocyclic structures that have been attracting the interest of many scientists in drug discovery.

Objective: The present study was carried out to explore antioxidant, antimicrobial, cytotoxic properties of novel indole derivative 1-ethyl-2-phenyl-3-phenylethyl-3-thiophen-2-yl-1H-indole (EPI) and its effect on glutathione S-transferases (GST) activities in human liver carcinoma (HepG2) cells.

Materials and Methods: Pd-catalyst Sonogashira coupling reactions, MTT Assay, Antioxidant capacity test, Antimicrobial test, GST enzyme activity test.

Results: 1-ethyl-2-phenyl-3-(phenylethynyl)-1H-indole had antioxidant and antimicrobial properties. It displayed significant induction in glutathione S-transferases (GST) enzyme activity in human liver cancer cell lines (HepG2), but cytotoxic effect on all tested cancer cell lines could not be observed.

Conclusion: All of these results showed that 1-ethyl-2-phenyl-3-(phenylethynyl)-1H-indole had antioxidant and antimicrobial properties without cytotoxic effect, which could make it a promising active component with further studies.

Keywords:

Indole, heteroaromatic compounds, antioxidant, cytotoxicity, antimicrobial, small molecules.

Affiliation:

Department of Agricultural Biotechnology, Faculty of Agriculture, Ondokuz Mayıs University, 55139 Samsun, Department of Agricultural Biotechnology, Faculty of Agriculture, Ondokuz Mayıs University, 55139 Samsun, Department of Molecular Biology and Genetics, Faculty of Sciences, Van Yuzuncu Yil University, 65080, Van, Department of Biology, Faculty of Arts and Sciences, Pamukkale University, 20100, Denizli, Department of Biology, Faculty of Arts and Sciences, Pamukkale University, 20100, Denizli, Department of Chemistry, Faculty of Sciences, Van Yuzuncu Yil University, Van, 65080, Department of Chemistry, Faculty of Sciences, Van Yuzuncu Yil University, Van, 65080, Department of Molecular Biology and Genetics, Faculty of Sciences, Van Yuzuncu Yil University, 65080, Van, Department of Molecular Biology and Genetics, Faculty of Sciences, Van Yuzuncu Yil University, 65080, Van, Department of Molecular Biology and Genetics, Faculty of Sciences, Van Yuzuncu Yil University, 65080, Van

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