Aromatase (CYP19) inhibition by biflavonoids obtained from the branches of Garcinia gardneriana (Clusiaceae).

Zeitschrift Für Naturforschung. C, a Journal of Biosciences
Angelica Maria Recalde-GilAmélia Henriques

Abstract

Overexpression of aromatase in breast cancer cells may substantially influence its progression and maintenance. In this sense, the inhibition of aromatase is a key target for the treatment of breast cancer in postmenopausal women. Although several flavonoids had already demonstrated the capacity of inhibiting aromatase activity, the role of biflavonoids as aromatase inhibitors is poorly studied. In this work, the biflavonoids isolated from Garcinia gardneriana, morelloflavone (1), Gb-2a (2) and Gb-2a-7-O-glucose (3) were submitted to in vitro assay to evaluate the aromatase modulatory effect. As results, it was demonstrated that all biflavonoids were able to inhibit the enzyme, with IC50 values ranging from 1.35 to 7.67 μM. This demonstrates that biflavonoids are an important source of scaffolds for the development of new aromatase inhibitors, focusing on the development of new anticancer agents.

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Citations

Oct 7, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Bruna Larissa Spontoni do Espirito SantoPaulo Roberto Haidamus de Oliveira Bastos
Dec 2, 2020·European Journal of Medicinal Chemistry·Ankur Kumar TanwarVikas Jaitak
Mar 6, 2021·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·José C J M D S Menezes, Marc F Diederich
Sep 30, 2021·Natural Products and Bioprospecting·Christian Bailly, Gérard Vergoten

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