Structure-activity relationships, kinetics, selectivity, and mechanistic studies of synthetic hydraphile channels in bacterial and mammalian cells

W. Matthew Leevy, Seth T. Gammon, Tatiana Levchenko, David D. Daranciang, Oscar Murillo, Vladimir Torchilin, David Piwnica-Worms, James E. Huettner, George W. Gokel

Research output: Contribution to journalArticle

26 Scopus citations

Abstract

Hydraphile compounds are shown to be cytotoxic to Gram-negative and Gram-positive bacteria, yeast, and mammalian cells. Their cellular toxicity compares favorably with other synthetic ionophores and rivals that potency of natural antibiotics. The effects of structural variations on toxicity are described. The effects of these variations correlate well with previous studies of ion transport in liposomes. Whole cell patch clamping with mammalian cells confirms a channel mechanism in living cells suggesting that this family may comprise novel and flexible pharmacological agents.

Original languageEnglish
Pages (from-to)3544-3550
Number of pages7
JournalOrganic and Biomolecular Chemistry
Volume3
Issue number19
DOIs
StatePublished - Oct 7 2005

Fingerprint Dive into the research topics of 'Structure-activity relationships, kinetics, selectivity, and mechanistic studies of synthetic hydraphile channels in bacterial and mammalian cells'. Together they form a unique fingerprint.

  • Cite this

    Leevy, W. M., Gammon, S. T., Levchenko, T., Daranciang, D. D., Murillo, O., Torchilin, V., Piwnica-Worms, D., Huettner, J. E., & Gokel, G. W. (2005). Structure-activity relationships, kinetics, selectivity, and mechanistic studies of synthetic hydraphile channels in bacterial and mammalian cells. Organic and Biomolecular Chemistry, 3(19), 3544-3550. https://doi.org/10.1039/b508157b