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Antileukemic principles isolated from euphorbiaceae plants.

S M Kupchan, I Uchida, A R Branfman

    Science (New York, N.Y.)
    |February 23, 1976
    PubMed
    Summary

    Plant extracts from Euphorbia esula and Croton tiglium demonstrated significant antileukemic effects against P-388 lymphocytic leukemia in mice. Researchers identified ingenol 3,20-dibenzoate and phorbol 12-tiglate 13-decanoate as key active compounds.

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    Area of Science:

    • Pharmacology
    • Natural Product Chemistry
    • Oncology

    Background:

    • The Euphorbiaceae family, including Euphorbia esula and Croton tiglium, has a history of use in traditional medicine for cancer treatment.
    • P-388 lymphocytic leukemia in mice is a standard model for evaluating potential anticancer agents.

    Purpose of the Study:

    • To investigate the antileukemic activity of Euphorbia esula L. and Croton tiglium L. extracts.
    • To isolate and characterize the active compounds responsible for the observed antileukemic effects.

    Main Methods:

    • Systematic fractionation of plant extracts.
    • Bioassay-guided isolation of active components.
    • Chemical characterization of isolated compounds using spectroscopic methods.

    Main Results:

    • Both Euphorbia esula L. and Croton tiglium L. extracts exhibited significant antileukemic activity against P-388 lymphocytic leukemia.
    • A novel diterpenoid diester, ingenol 3,20-dibenzoate, was identified as a major active component from Euphorbia esula L.
    • Phorbol 12-tiglate 13-decanoate was characterized as an active principle from Croton oil.

    Conclusions:

    • Euphorbia esula L. and Croton tiglium L. possess potent antileukemic properties.
    • Ingenol 3,20-dibenzoate and phorbol 12-tiglate 13-decanoate are key bioactive diterpenoids with potential for further development as anticancer agents.