Brassinin and its derivatives as potential anticancer agents

Martina Chripkova, David Drutovic, Martina Pilatova, Jaromir Mikes, Mariana Budovska, Janka Vaskova, Massimo Broggini, Ladislav Mirossay, Jan Mojzis

Research output: Contribution to journalArticle

Abstract

The aim of the study was to investigate the anti-proliferative activity of brassinin and its derivatives on human cancer cell lines. We found that among twenty-one tested compounds, 1- methoxybrassinin exerted the most potent anti-proliferative activity in Caco-2 cells with IC50 8.2 (±1.2)μmoll-1. The flow cytometric analysis revealed a 1-methoxybrassinin-induced increase in the sub-G1 DNA content fraction which is considered to be a marker of apoptotic cell death. Apoptosis was also confirmed by DNA fragmentation assay. Moreover, quantitative real-time PCR showed that 1-methoxybrassinin upregulated the expression of pro-apoptotic Bax and downregulated the expression of anti-apoptotic genes Bcl-2 and Bcl-xL. The compound also increased activity of caspase-3, -7, cleaved PARP and decreased intracellular GSH content. The present study has assessed the in vitro anti-proliferative potential of 1-methoxybrassinin. The results generate a rationale for in vivo efficacy studies with this compound in preclinical cancer models.

Original languageEnglish
Pages (from-to)909-915
Number of pages7
JournalToxicology in Vitro
Volume28
Issue number5
DOIs
Publication statusPublished - 2014

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Keywords

  • Anti-proliferative effect
  • Apoptosis
  • Brassinin
  • Indole phytoalexins

ASJC Scopus subject areas

  • Toxicology
  • Medicine(all)

Cite this

Chripkova, M., Drutovic, D., Pilatova, M., Mikes, J., Budovska, M., Vaskova, J., Broggini, M., Mirossay, L., & Mojzis, J. (2014). Brassinin and its derivatives as potential anticancer agents. Toxicology in Vitro, 28(5), 909-915. https://doi.org/10.1016/j.tiv.2014.04.002