Unbound MEDLINE

A metabolically stable analogue of anandamide, Met-F-AEA, inhibits human thyroid carcinoma cell lines by activation of apoptosis.

Abstract

The active components of Cannabis sativa and their derivatives produce a wide spectrum of effects, some of which may have clinical application. The discovery of specific cannabinoid receptors and a family of endogenous ligands of those receptors has attracted much attention to cannabinoids as agents capable of controlling the decision of cells to survive or die. We analysed the effects exerted by 2-methyl-2'-F-anandamide (Met-F-AEA), a metabolically stable analogue of anandamide, and observed a growth inhibition in cell lines derived from thyroid carcinomas. Growth inhibition was associated with a high level of CB1 receptor expression, suggesting that the cytotoxic effect is due to interaction with the CB1 receptor. This phenomenon was associated with activation of the protein, p53, an increased apoptotic rate, and expression of p21(CIP1/WAF1). This study provides new insights into the mechanism of Met-F-AEA action, and could have significance in providing a basis for the management of thyroid carcinoma.

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  • Publisher Full Text
  • Authors

    Cozzolino R, Calì G, Bifulco M, Laccetti P

    Institution

    Department of Structural and Functional Biology, University of Naples Federico II, 80126 Naples, Italy. cozzolino1@interfree.it

    Source

    Investigational new drugs 28:2 2010 Apr pg 115-23

    MeSH

    Apoptosis
    Arachidonic Acids
    Cell Cycle Proteins
    Cell Line, Tumor
    Cell Nucleus
    Cell Proliferation
    Drug Screening Assays, Antitumor
    Humans
    Molecular Weight
    Piperidines
    Poly(ADP-ribose) Polymerases
    Polyunsaturated Alkamides
    Pyrazoles
    Receptor, Cannabinoid, CB1
    Thyroid Neoplasms
    Tumor Suppressor Protein p53

    Pub Type(s)

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

    Language

    eng

    PubMed ID

    19189054