Studies on the Metabolism and Hepatotoxicity of Coumarin in the Baboon

rat urine was 3-hydroxypropylmercapturic acid and not one of two possible isomers of this mercapturic acid (see Table 1). Acrolein is a reactive compound, which probably has a short life within the organism, thereby making it difficult to obtain direct evidence of its formation in an intact animal. Evidence is presented here, however, that administration of acrolein to rats leads to the excretion of 3-hydroxypropylmercapturic acid in the urine, and that in man and the rat excretion of this latter compound follows the administration of cyclophosphamide (see Scheme 1). Although they do not provide proof, these findings are consistent with a belief that acrolein is a metabolite of cyclophosphamide in man, and they lend added interest to the suggestion of Alarcon & Meienhofer (1971) that the therapeutic effects of cyclophosphamide may be related to the metabolic formation of acrolein.