Title:Antitumoral Potential of Artepillin C, a Compound Derived from Brazilian Propolis,
against Breast Cancer Cell Lines
Volume: 24
Issue: 2
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*Vania Ramos Sela da Silva
Affiliation:
- Department of Clinical Analysis and Biomedicine, Universidade Estadual de Maringá (UEM), Maringá, Paraná, Brazil
Keywords:
Artepillin C, propolis, natural products, breast cancer cells, cytotoxicity, antitumor effect.
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.
