CONVERSION OF AFLATOXICOL TO AFLATOXIN-B1 IN RATS INVIVO AND IN PRIMARY HEPATOCYTE CULTURE

The hepato-metabolic conversion of aflatoxicol to aflatoxin B, was studied by administering [14C]aflatoxicol to the rat iv and to rat primary hepatocyte culture. Aflatoxicol was found to be rapidly metabolized to the parent toxin, aflatoxin B,, both in the rat in vivo and in primary hepatocyte culture. The aflatoxin B1 so-formed was confirmed by thin-layer chromatography, autoradiography and high-pressure liquid chromatography, and that formed in vitro was also confirmed by ultraviolet absorption spectroscopy, and by its mutagenic potency. In comparison to aflatoxin B1, aflatoxicol showed a higher level of distribution to the tissues and a shorter plasma biological half-life. The biological potency of aflatoxicol and the correlation of its formation with species sensitivity to the carcinogenic effect of aflatoxin B, may be due to its ability to undergo oxidation to the parent toxin, aflatoxin B1, allowing further bioactivation. © 1971.