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The contribution of plukenetione A to the anti-tumoral activity of Cuban propolis.

Abstract

Increasing efforts are directed toward finding applications for natural products and their derivatives in the treatment of human diseases. Among such products, propolis, a resinous substance produced by honey bees from various plant sources, has been found to be a promising source of potential therapeutics. In the present work, we aimed at studying the perspective of Cuban propolis as a source of possible anti-cancer agents. We found an anti-metastatic effect in mice and considerable cytotoxicity without cross-resistance in both wild-type and chemoresistant human tumor cell lines. Plukenetione A--identified for the first time in Cuban propolis--induced G0/G1 arrest and DNA fragmentation in colon carcinoma cells. Furthermore, the activities of both topoisomerase I and DNA polymerase were inhibited, while the expression of topoisomerase II-beta, EGF receptor, and multidrug resistance-related protein genes was found repressed. We assume that plukenetione A contributes to the anti-tumoral effect of Cuban propolis mainly by targeting topoisomerase I as well as DNA polymerase.

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  • Authors+Show Affiliations

    ,

    Division of Clinical Pharmacology, Ruhr-University of Bochum, Universitaetsstr. 150, D-44801 Bochum, Germany. david.diaz-carballo@rub.de

    , , ,

    Source

    Bioorganic & medicinal chemistry 16:22 2008 Nov 15 pg 9635-43

    MeSH

    Animals
    Antineoplastic Agents
    Cell Cycle
    Cell Proliferation
    Chromatography, High Pressure Liquid
    Cuba
    DNA Damage
    DNA Polymerase III
    DNA Topoisomerases, Type I
    Female
    G1 Phase
    Gene Expression Profiling
    Humans
    Inhibitory Concentration 50
    Mice
    Polycyclic Compounds
    Propolis
    Resting Phase, Cell Cycle
    Topoisomerase I Inhibitors
    Tumor Cells, Cultured

    Pub Type(s)

    Journal Article
    Research Support, Non-U.S. Gov't

    Language

    eng

    PubMed ID

    18951805

    Citation

    Díaz-Carballo, David, et al. "The Contribution of Plukenetione a to the Anti-tumoral Activity of Cuban Propolis." Bioorganic & Medicinal Chemistry, vol. 16, no. 22, 2008, pp. 9635-43.
    Díaz-Carballo D, Malak S, Bardenheuer W, et al. The contribution of plukenetione A to the anti-tumoral activity of Cuban propolis. Bioorg Med Chem. 2008;16(22):9635-43.
    Díaz-Carballo, D., Malak, S., Bardenheuer, W., Freistuehler, M., & Peter Reusch, H. (2008). The contribution of plukenetione A to the anti-tumoral activity of Cuban propolis. Bioorganic & Medicinal Chemistry, 16(22), pp. 9635-43. doi:10.1016/j.bmc.2008.10.019.
    Díaz-Carballo D, et al. The Contribution of Plukenetione a to the Anti-tumoral Activity of Cuban Propolis. Bioorg Med Chem. 2008 Nov 15;16(22):9635-43. PubMed PMID: 18951805.
    * Article titles in AMA citation format should be in sentence-case
    TY - JOUR T1 - The contribution of plukenetione A to the anti-tumoral activity of Cuban propolis. AU - Díaz-Carballo,David, AU - Malak,Sascha, AU - Bardenheuer,Walter, AU - Freistuehler,Michael, AU - Peter Reusch,H, Y1 - 2008/10/11/ PY - 2008/06/24/received PY - 2008/10/07/revised PY - 2008/10/08/accepted PY - 2008/10/28/pubmed PY - 2009/1/17/medline PY - 2008/10/28/entrez SP - 9635 EP - 43 JF - Bioorganic & medicinal chemistry JO - Bioorg. Med. Chem. VL - 16 IS - 22 N2 - Increasing efforts are directed toward finding applications for natural products and their derivatives in the treatment of human diseases. Among such products, propolis, a resinous substance produced by honey bees from various plant sources, has been found to be a promising source of potential therapeutics. In the present work, we aimed at studying the perspective of Cuban propolis as a source of possible anti-cancer agents. We found an anti-metastatic effect in mice and considerable cytotoxicity without cross-resistance in both wild-type and chemoresistant human tumor cell lines. Plukenetione A--identified for the first time in Cuban propolis--induced G0/G1 arrest and DNA fragmentation in colon carcinoma cells. Furthermore, the activities of both topoisomerase I and DNA polymerase were inhibited, while the expression of topoisomerase II-beta, EGF receptor, and multidrug resistance-related protein genes was found repressed. We assume that plukenetione A contributes to the anti-tumoral effect of Cuban propolis mainly by targeting topoisomerase I as well as DNA polymerase. SN - 1464-3391 UR - https://www.unboundmedicine.com/medline/citation/18951805/The_contribution_of_plukenetione_A_to_the_anti_tumoral_activity_of_Cuban_propolis_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0968-0896(08)00971-1 DB - PRIME DP - Unbound Medicine ER -