Membrane Transport Inhibition as Mode of Action of Polyene Antimycotics: Recent Data Supported by Old Ones

Abstract

Recent studies demonstrate that the actual interactions of polyenes with membrane sterols are the basis for their antimycotic toxicity and not, as previously assumed, their potential to form pores. Therefore, sterols must play a vital role in membranes and this function is seriously disturbed once polyenes bind to and/or sequester them. Essential membrane proteins obviously require sterols for their activity. Among the various membrane protein/ergosterol interactions discussed herein, transport proteins of the plasma membrane are most likely the primary target for polyenes. All data available which support this notion are summarized in this review. Even data obtained almost 40 years ago could be useful in guiding future research.

Keywords

• amphotericin B
• nystatin
• natamycin
• sugar and amino acid transport