Gossypol, a natural polyphenolic compound, induces growth-inhibitory and antiparasitic effects in Taenia taeniaeformis metacestodes in vivo and in vitro. We investigated the uptake and localization of [3H]-gossypol in this parasite. Metacestodes were incubated in 10(-5) M [3H]-gossypol at 37 degrees C. Parasites steadily took up tritium activity over the first 3 h of incubation, after which a plateau was maintained for the duration of the experiment. Tissue: medium radioactivity ratios revealed that intralarval tritium activity matched extralarval activity within 30 min of incubation and continued to increase with time. Reverse-phase high-performance liquid chromatographic (HPLC) analysis confirmed tissue incorporation of tritium activity that manifested as a single radioactive species. Autoradiography localized [3H]-gossypol to the tegument, calcareous corpuscles, and parenchyma over the first 2 h of incubation. By 6 h, parenchymal radioactivity had disappeared. T. taeniaeformis metacestodes rapidly take up and accumulate [3H]-gossypol in vitro. This accumulation is apparently selective for specific sites, which may have implications for gossypol's metacestocidal action.