Polymorphonuclear Leukocyte (PMN) Penetration of Macrolides

Abstract

A radioisotopic method was used to determine the penetration of five macrolide antibiotics into human polymorphonuclear leukocytes (PMN). The penetration ratios (that is, of the cellular concentration to the extracellular concentration) of erythromycin, josamycin, rokitamycin, TE-031, and Ru-28965, all macrolides, were very high. Macrolide uptake by PMN was dependent on environmental temperature and cell viability. Also, the accumulation of these antimicrobials was inhibited by sodium cyanide, potassium fluoride, and adenosine. Based on our findings, we consider that macrolide uptake by human PMN is mediated by an active transport system, and more specifically a nucleoside transport system. © 1987, Japanese Society of Chemotherapy. All rights reserved.