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

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 ß-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.

Brown propolis-metabolomic innovative approach to determine compounds capable of killing Staphylococcus aureus biofilm and Trichomonas vaginalis.

Propolis, a resin produced by bees, is widely used in industrial products, including food, cosmetics, supplements, and pharmaceuticals. Extracts (ethanolic and hydroethanolic) and fractions, yielded by accelerated solvent extraction methodology, were obtained from different samples of Brazilian brown propolis (BBP). They were evaluated for antioxidant capacity, antibacterial, antibiofilm, and anti-Trichomonas vaginalis activities. The metabolomics profiling was determined by LC-DAD-MS and an innovative application of statistical analyses (univariate and chemometrics) was applied to correlate chemical compounds with biological activities. Eighty-six compounds were identified, including phenylpropanoic acids, flavonoids, chlorogenic acids, and prenylated phenylpropanoic acids. Propolis-fractions killed about 93% of Staphylococcus aureus in biofilm (at concentration of 125 µg/mL), showed activity against T. vaginalis with MIC at 400 µg/mL and significative antioxidant capacity (IC50 2.32-3.80 µg/mL). Propolis extracts and fractions did not show antibacterial and antibiofilm activities against Pseudomonas aeruginosa. The prenylated phenylpropanoic acids positively correlated with both the antibiofilm (S. aureus) and anti-T. vaginalis activities, such as the metabolites artepillin C, drupanin, and baccharin.