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PPARγ transcription effect on naturally occurring O-prenyl cinnamaldehydes and cinnamyl alcohol derivatives

    Salvatore Genovese

    Department of Pharmacy, University “Gabriele d'Annunzio” of Chieti-Pescara, Via dei Vestini 31, Chieti Scalo, 66100, Italy

    ,
    Francesco Epifano

    *Author for correspondence: Tel.: +39 087 1355 4654;

    E-mail Address: francesco.epifano@unich.it

    Department of Pharmacy, University “Gabriele d'Annunzio” of Chieti-Pescara, Via dei Vestini 31, Chieti Scalo, 66100, Italy

    ,
    Judith M Rollinger

    Department of Pharmacognosy, University of Wien, Althanstrasse 14, Wien, A-1090, Austria

    &
    Serena Fiorito

    Department of Pharmacy, University “Gabriele d'Annunzio” of Chieti-Pescara, Via dei Vestini 31, Chieti Scalo, 66100, Italy

    Published Online:https://doi.org/10.4155/fmc-2021-0054

    Background: PPARγ is known to be a key regulator of metabolism and storage of lipids and glucose and to be implicated in the pathology of severe syndromes like obesity, diabetes, atherosclerosis and cancer. Methods: As a continuation of the authors' studies on oxyprenylated secondary metabolites as effective PPARγ agonists, the authors describe herein the chemical synthesis of natural O-prenyl cinnamaldehydes and cinnamyl alcohols and preliminary data on their in vitro effects on PPARγ transcription. Results: Among the panel of eight compounds tested, three – namely, (2E)-3-(4-((E)3,7-dimethylocta-2,6-dienyloxy)-3-methoxyphenyl)acrylaldehyde, (2E)-3-(4-((E)3,7-dimethylocta-2,6-dienyloxy)-3-methoxyphenyl)prop-2-en-1-ol and boropinal A – exerted activity in a dose-dependent manner. Conclusion:O-prenyl cinnamaldehydes and cinnamyl alcohols have the potential to effectively interact with PPARγ receptor.

    Papers of special note have been highlighted as: • of interest; •• of considerable interest

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