Fate of [14C]xanthotoxin (8-methoxypsoralen) in a goat and in bovine ruminal fluid.

A lactating Nubian goat was treated with [14C]xanthotoxin, a photosensitizing psoralen that occurs naturally in some phototoxic range plants, as a single oral dose equivalent to 10.0 mg of xanthotoxin/kg of body weight. The radiochemical was rapidly absorbed, metabolized, and excreted. Although expired air was not monitored for the presence of volatile radiocarbon, the data indicated that greater than 50% of the administered [14C]xanthotoxin was metabolized by cleavage of the O-[14C]methyl moiety, with subsequent loss of the label as, presumably, [14C]CO2. Studies with bovine ruminal fluid in vitro indicated that cleavage of the O-methyl moiety of xanthotoxin could occur rapidly in the rumen. In the goat, nonmetabolized xanthotoxin was not excreted in urine, and of several metabolites in urine extracts, 3 were identified as resulting from opening of the furan or lactone ring. Only about 2% of the dose was recovered in the feces, and this consisted mainly of unmetabolized xanthotoxin. Although appreciable amounts of radiocarbon were secreted into milk, this radiocarbon was not in the form of xanthotoxin or any identifiable metabolites. The radiocarbon in milk likely resulted from the biosynthetic incorporation of [14C]CO2 into normal milk components.