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[Genotoxic and mutagenic activity of antineoplastic anthracyclines and their aglycones: study in two test-systems]

S V Vasil'eva, E V Makhova, O V Efremenkova

    Genetika
    |February 1, 1996
    PubMed

    Insights

    Natural anthracycline monosaccharides like daunorubicin and doxorubicin show strong mutagenic activity. Their genotoxicity is linked to DNA intercalation via a saccharide amino group, a mechanism explored in bacterial tests.

    Area of Science:

    • Molecular Biology
    • Genetics
    • Pharmacology

    Background:

    • Anthracyclines are potent antitumor agents.
    • Their genotoxicity is a significant concern.
    • The role of the saccharide amino group in DNA interaction was hypothesized.

    Purpose of the Study:

    • To assess the mutagenic and genotoxic activities of natural anthracycline monosaccharides.
    • To investigate the role of the saccharide amino group in anthracycline genotoxicity.
    • To compare activities of intact compounds with their hydrolysis products (aglycones).

    Main Methods:

    • Ames tests (mutagenicity) using Salmonella typhimurium strains TA98 and TA100.
    • SOS chromotest (genotoxicity).
    • Evaluation of anthracycline monosaccharides, their aglycones, aclacynomycin A, and aclavinone.

    Main Results:

    • Anthracycline monosaccharides (daunorubicin, doxorubicin, carminomycin) exhibited strong mutagenicity.
    • Aglycones showed moderate mutagenicity, indicating the amino group is not solely responsible.
    • Aclacynomycin A was not mutagenic; S9 fraction increased aclavinone mutagenicity.

    Conclusions:

    • The saccharide amino group facilitates DNA intercalation, contributing to genotoxicity.
    • Mutagenicity can occur via intercalation or ionic interactions, depending on the compound's structure.
    • Anthracycline genotoxicity is mediated by inducing the SOS-repair process in bacterial cells.

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