Intracellular alkalinization induced by amphotericin B derivatives in HL-60 leukemia cells.

The effects on intra- and extracellular pH of two polyenic derivatives of amphotericin B, N-fructosyl amphotericin B and N-fructosyl amphotericin B methyl-ester, were tested on HL-60 promyelocytic leukemia cells. Both derivatives raised the internal pH and reduced the external pH in weakly buffered medium. These results support the idea that both derivatives induce outward proton movement from the cell to the external solution. In this respect, the non-esterified derivative proved to be more powerful that the esterified one. Under the present conditions, there was little or no regulation of pH in HL-60 cells, which exhibited an almost constant pH gradient between the external and internal pH (acid inside relative to outside). This deficiency in pH homeostasis might be due to the immature state of the HL-60 cells.