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Polyene macrolide antibiotic cytotoxicity and membrane permeability alterations I. Comparative effects of four classes of polyene macrolides on mammalian cells

The relationship between polyene macrolide‐induced early membrane damage and cytotoxicity in B1 (hamster), B82 (mouse), and RAG (mouse) cells has been investigated. Filipin (FIL) induced the greatest immediate damage, as monitored by 51Cr release, followed by mediocidin (MED), amphotericin B‐deoxycholate (Fungizone®) (FZ) and pimaricin (PIM). For long term effect, PIM was the least toxic followed by MED, FZ, and FIL as indicated by 24‐hour survival, 72‐hour viability, and growth rate of cells. In evaluating polyene macrolide‐induced permeability alterations and cytotoxicity two types of interactions with mammalian cells were found: (1) cell toxicity at polyene macrolide levels not eliciting immediate membrane permeability changes; and (2) immediate membrane damage without long range toxicity.