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Anti-Cancer Agents in Medicinal Chemistry

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ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

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Research Article

Antitumoral Potential of Artepillin C, a Compound Derived from Brazilian Propolis, against Breast Cancer Cell Lines

Author(s): Lyvia Eloiza de Freitas Meirelles, Analine Rosa Barquez de Assis Carvalho, Gabrielle Marconi Zago Ferreira Damke, Raquel Pantarotto Souza, Edilson Damke, Patrícia de Souza Bonfim-Mendonça, Djaceli Sampaio de Oliveira Dembogurski, Denise Brentan da Silva, Marcia Edilaine Lopes Consolaro* and Vania Ramos Sela da Silva

Volume 24, Issue 2, 2024

Published on: 08 November, 2023

Page: [117 - 124] Pages: 8

DOI: 10.2174/0118715206270534231103074433

Price: $65

Abstract

Background: Breast cancer is the most commonly diagnosed cancer among women worldwide with limited treatment options. Artepillin C (3,5-diprenyl-4-hydroxycinnamic acid) is one of the main constituents of Brazilian propolis presenting different activities, including antitumoral effects against various types of cancer.

Objective: We evaluated the antitumoral potential and mechanisms of action of artepillin C against two distinct human breast cancer cell lines, MCF-7 and MDA-MB-231, to explore a new therapeutic candidate.

Methods: Cell viability was assessed by MTT assay and the long-term cytotoxicity was performed by clonogenic assay. The morphological changes were observed by light microscopy, analysis of cell death pathway by Annexin V FITC/propidium iodide (PI), lactate dehydrogenase (LDH) by colorimetry, DNA fragmentation by agarose gel and senescence by β-galactosidase. Detection of total reactive oxygen species (ROS) by fluorescence microscopy and determination of mitochondrial transmembrane potential by flow cytometry were also performed.

Results: Artepillin C presented a strong and dose-time-dependent cytotoxic effect on MCF-7 and MDA-MB-231 cell lines, with cytotoxicity more evident in MCF-7. In both cancer cell lines, the clonogenic potential was significantly reduced and the morphology of the cells was changed. The treatment also induced death by necrosis and late apoptosis in MCF-7 and MDA-MB-231 and induced cell senescence in MCF-7. Also, artepillin C increased total ROS in both cancer cells and decreased mitochondrial membrane potential in MDA-MB-231 cells.

Conclusion: Artepillin C presented antitumoral potential in two human breast cancer cell lines, MCF-7, and MDA-MB-231, suggesting a new promising option for the treatment and/or chemopreventive strategy for breast cancer.

Keywords: Artepillin C, propolis, natural products, breast cancer cells, cytotoxicity, antitumor effect.

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Graphical Abstract

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