Antifungal and cancer cell growth inhibitory activities of 1-(3′,4′,5′-trimethoxyphenyl)-2-nitro-ethylene

Robin Pettit, E. Hamel, P. Verdier-Pinard, Robert Roberson, K. C. Hazen, George Pettit, Laura C. Crews

Research output: Contribution to journalArticle

5 Scopus citations

Abstract

The antifungal and cancer cell growth inhibitory activities of 1-(3′,4′,5′-trimethoxyphenyl)-2-nitro-ethylene (TMPN) were examined. TMPN was fungicidal for the majority of 132 reference strains and clinical isolates tested, including those resistant to fluconazole, ketoconazole, amphotericin B or flucytosine. Minimum fungicidal concentration/minimum inhibitory concentration (MFC/MIC) ratios were ≤2 for 96% of Cryptococcus neoformans clinical isolates and 71% of Candida albicans clinical isolates. TMPN was fungicidal for a variety of other basidiomycetes, endomycetes and hyphomycetes, and its activity was unaffected by alterations in media pH. The frequency of occurrence of fungal spontaneous mutations to resistance was <10-6. Kill-curve analyses confirmed the fungicidal action of TMPN, and demonstrated that killing was concentration- and time-dependent. At sub-MIC exposure to TMPN, C. albicans did not exhibit yeast/hyphae switching. TMPN was slightly cytotoxic for murine and human cancer cell lines (GI50=1-4 μg ml-1), and weakly inhibited mammalian tubulin polymerization (IC50=0.60 μg ml-1).

Original languageEnglish (US)
Pages (from-to)65-74
Number of pages10
JournalMycoses
Volume45
Issue number3-4
DOIs
StatePublished - May 30 2002

Keywords

  • 1-(3′,4′,5′-trimethoxyphenyl)-2-nitro-ethylene
  • Anti-cancer
  • Antifungal
  • Tubulin

ASJC Scopus subject areas

  • Dermatology
  • Infectious Diseases

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