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Title: (-)-Epigallocatechin 3-Gallate Synthetic Analogues Inhibit Fatty Acid Synthase and Show Anticancer Activity in Triple Negative Breast Cancer.
Author: Crous-Masó, Joan
Palomeras, Sonia
Relat Pardo, Joana
Camó, Cristina
Martínez Garza, Úrsula
Planas, Marta
Feliu, Lidia
Puig i Miquel, Teresa
Keywords: Apoptosi
Síntesi orgànica
Organic synthesis
Issue Date: 11-May-2018
Publisher: MDPI
Abstract: (􀀀)-Epigallocatechin 3-gallate (EGCG) is a natural polyphenol from green tea with reported anticancer activity and capacity to inhibit the lipogenic enzyme fatty acid synthase (FASN), which is overexpressed in several human carcinomas. To improve the pharmacological profile of EGCG, we previously developed a family of EGCG derivatives and the lead compounds G28, G37 and G56 were characterized in HER2-positive breast cancer cells overexpressing FASN. Here, diesters G28, G37 and G56 and two G28 derivatives, monoesters M1 and M2, were synthesized and assessed in vitro for their cytotoxic, FASN inhibition and apoptotic activities in MDA-MB-231 triple-negative breast cancer (TNBC) cells. All compounds displayed moderate to high cytotoxicity and significantly blocked FASN activity, monoesters M1 and M2 being more potent inhibitors than diesters. Interestingly, G28, M1, and M2 also diminished FASN protein expression levels, but only monoesters M1 and M2 induced apoptosis. Our results indicate that FASN inhibition by such polyphenolic compounds could be a new strategy in TNBC treatment, and highlight the potential anticancer activities of monoesters. Thus, G28, G37, G56, and most importantly M1 and M2, are anticancer candidates (alone or in combination) to be further characterized in vitro and in vivo.
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It is part of: Molecules, 2018, vol. 23, num. 5, p. 1160
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ISSN: 1420-3049
Appears in Collections:Articles publicats en revistes (Institut de Recerca en Nutrició i Seguretat Alimentària (INSA·UB))
Articles publicats en revistes (Nutrició, Ciències de l'Alimentació i Gastronomia)

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