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Acetylation, deacetylation and acyltransfer.

C M King, I B Glowinski

    Environmental Health Perspectives
    |March 1, 1983
    PubMed
    Summary
    This summary is machine-generated.

    N-substituted aromatic compounds undergo metabolic transformations, including N-acetylation and N,O-acyltransfer, influencing their biological effects. Enzyme specificity determines whether these processes activate or deactivate compounds, impacting their carcinogenic potential.

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    Area of Science:

    • Biochemistry
    • Pharmacology
    • Toxicology

    Background:

    • N-substituted aromatic compounds are metabolized to N-acetylated derivatives.
    • These derivatives undergo further transformations like hydrolysis and N,O-acyltransfer.
    • These processes can modulate biological responses, potentially leading to adverse effects or metabolic activation.

    Purpose of the Study:

    • To investigate the enzymatic transformations of N-substituted aromatic compounds.
    • To understand the role of N-acetyltransferase and N,O-acyltransferase in metabolic activation.
    • To explore the influence of these metabolic pathways on the carcinogenic process.

    Main Methods:

    • Enzyme assays involving N-acetyltransferase and N,O-acyltransferase.
    • Incubation of various species' enzymes with N-substituted aromatic compounds and their derivatives.

    Related Experiment Videos

  • Analysis of metabolite formation and nucleic acid adducts.

    • Main Results:

    • N-acetyltransferase and N,O-acyltransferase can activate arylhydroxamic acids via N,O-acyltransfer in rabbits and rats.
    • Cytosolic enzymes are organotriphosphate ester-resistant and activate arylhydroxamic acids by O-acetylation.
    • Microsomal enzymes are organotriphosphate ester-sensitive deacylases and do not activate certain substrates.

    Conclusions:

    • Metabolic activation of N-substituted aromatic compounds by N,O-acyltransfer occurs during both acetylation and deacylation.
    • Enzyme specificity plays a crucial role in determining the activation or deactivation of these compounds.
    • The carcinogenic implications of N,O-acyltransfer-mediated activation are under ongoing investigation.