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Antineoplastic agents, 88. Pimelea prostrata.

G R Pettit, J C Zou, A Goswami

    Journal of Natural Products
    |July 1, 1983
    PubMed
    Summary
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    Two compounds from Pimelea prostrata, simplexin and Pimelea factor P2, show potent anti-cancer activity. These natural products effectively inhibit the growth of murine P-388 lymphocytic leukemia cells in vitro and in vivo.

    Area of Science:

    • Phytochemistry
    • Natural Products Chemistry
    • Cancer Research

    Background:

    • Pimelea prostrata, a plant native to New Zealand, is explored for its potential medicinal properties.
    • The search for novel anti-cancer agents from natural sources is ongoing.
    • Murine P-388 lymphocytic leukemia serves as a standard model for evaluating anti-cancer drug efficacy.

    Purpose of the Study:

    • To investigate the aerial parts of Pimelea prostrata for compounds with cytotoxic activity against murine P-388 lymphocytic leukemia.
    • To isolate and identify the active compounds responsible for growth inhibition.
    • To characterize the chemical structures of the isolated compounds.

    Main Methods:

    • Extraction and isolation of compounds from Pimelea prostrata.

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  • In vitro cytotoxicity assays using the murine P-388 lymphocytic leukemia cell line.
  • In vivo anti-leukemia efficacy studies in a murine model.
  • Structural elucidation using 1H-NMR, 13C-NMR, and mass spectrometry.

    • Main Results:

    • Simplexin and Pimelea factor P2 were isolated and identified as the primary active compounds.
    • Both compounds demonstrated significant inhibition of P-388 lymphocytic leukemia cell growth in vitro, with ED50 values of 5 x 10(-3) and 8 x 10(-4) µg/ml, respectively.
    • Pimelea factor P2 also exhibited anti-leukemia activity in vivo, showing a T/C value of 132 at 20 µg/kg.

    Conclusions:

    • Pimelea prostrata is a valuable source of natural compounds with potent anti-leukemia activity.
    • Simplexin and Pimelea factor P2 represent promising lead compounds for further development in cancer therapy.
    • The structural characterization confirms the identity of these bioactive molecules.