TAILIEUCHUNG - In vitro antiproliferative/cytotoxic activity of 2,3ʹ-biindole against various cancer cell lines
2,3’-Biindole (2) was synthesized via bromination of indole (1) with molecular bromine and underwent simultaneous dimerization. Antiproliferative and cytotoxic activity of 2 was investigated in vitro on C6 (rat brain tumor), HeLa (human cervix carcinoma), and HT29 (human colon carcinoma) cells lines by using BrdU cell proliferation ELISA and lactate dehydrogenase (LDH) assays. | Turkish Journal of Biology Turk J Biol (2015) 39: 15-22 © TÜBİTAK doi: Research Article In vitro antiproliferative/cytotoxic activity of 2,3ʹ-biindole against various cancer cell lines 1, 2 3 4 Salih ÖKTEN *, Ramazan ERENLER , Tuğba KUL KÖPRÜLÜ , Şaban TEKİN Department of Primary Education, Division of Science Education, Faculty of Education, Kırıkkale University, Kırıkkale, Turkey 2 Department of Chemistry, Faculty of Arts and Sciences, Gaziosmanpaşa University, Tokat, Turkey 3 Department of Biology, Faculty of Arts and Sciences, Gaziosmanpaşa University, Tokat, Turkey 4 Department of Molecular Biology and Genetics, Faculty of Arts and Sciences, Gaziosmanpaşa University, Tokat, Turkey 1 Received: Accepted: Published Online: Printed: Abstract: 2,3’-Biindole (2) was synthesized via bromination of indole (1) with molecular bromine and underwent simultaneous dimerization. Antiproliferative and cytotoxic activity of 2 was investigated in vitro on C6 (rat brain tumor), HeLa (human cervix carcinoma), and HT29 (human colon carcinoma) cells lines by using BrdU cell proliferation ELISA and lactate dehydrogenase (LDH) assays. In contrast to 5-fluorouracil (5-FU), 2,3’-biindole (2) significantly inhibited proliferation of HeLa and HT29 cell lines. According to LDH assay, the cytotoxicity of compound 2 was low on HT29 cell lines and high on HeLa and C6 cell lines. Moreover, 2 did not cause any DNA laddering on the DNA of tested cells; therefore, it is suggested that the mechanism of action of this compound may not involve apoptosis. In addition, 2 inhibited relaxation of supercoiled plasmid DNA by topoisomerase activity. Results of the present study indicates that biindole (2) may have promising anticancer and antitopoisomerase potential with an unknown mechanism of action. Key words: 2,3’-Biindole, anticancer, cytotoxicity, apoptosis, antitopoisomerase, C6 cell
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