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Metabolic activation of benzo(a)pyrene proceeds by a diol-epoxide

Abstract

CARCINOGENIC polycyclic hydrocarbons such as the widespread environmental contaminant, benzo(a)pyrene (Fig. 1a), undoubtedly require metabolic activitation. Boyland1 proposed that epoxides, whose formation is catalysed by the NADPH-dependent microsomal mono-oxygenases2,3, are the initial products of double-bond oxidation and we have suggested that epoxides are the important reactive metabolites responsible for the biological effects of these carcinogens4.

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SIMS, P., GROVER, P., SWAISLAND, A. et al. Metabolic activation of benzo(a)pyrene proceeds by a diol-epoxide. Nature 252, 326–328 (1974). https://doi.org/10.1038/252326a0

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