SYNTHESIS AND MUTAGENICITY OF 4-(N-BUTYLNITROSAMINO)-4-HYDROXYBUTYRIC ACID LACTONE, A POSSIBLE ACTIVATED METABOLITE OF THE PROXIMATE BLADDER CARCINOGEN N-BUTYL-N-(3-CARBOXYPROPYL)NITROSAMINE

  • 1 January 1980
    • journal article
    • research article
    • Vol. 40  (1) , 162-165
Abstract
4-(N-Butylnitrosamino)-4-hydroxybutyric acid lactone (BBAL) was synthesized as a possible intermediate produced by metabolic activation of a selective bladder carcinogen, N-butyl-N-(3-carboxypropyl)nitrosamine. BBAL was stable in neutral sodium phosphate buffer (ionic strength, 0.2), with a half-life of more than 30 h at 25.degree.. The mutagenic effects of BBAL were tested with the use of Salmonella typhimurium TA1535 and Escherichia coli B/rWP2-try-, WP2-try-hcr-, and Sd4. The gene-damaging effects were assayed by repair tests with Bacillus subtilis H17 (rec+) and M45 (rec-). BBAL showed potent effects in the mutation and repair tests on all the strains without activation. A possibility is suggested for the metabolic activation of N-butyl-N-(3-carboxypropyl)-nitrosamine to BBAL by .alpha.-hydroxylation at the site of the 3-carboxypropyl chain followed by lactonization in target tissues prior to interaction with macromolecules to lead to carcinogenesis.