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Published on: June 13, 2014
The BR2 peptide associated with 2-aminoethyl dihydrogen phosphate is a formulation with antiproliferative potential
Laertty Garcia de Sousa Cabral1, Henrique Hesse1, Katielle Albuquerque Freire2
1Faculty of Medicine, University of Sao Paulo, FMUSP, Sao Paulo, Brazil; Laboratory of Development and Innovation, Butantan Institute, Sao Paulo, Brazil.
Abstract:
Triple-negative breast cancer is the most aggressive subtype of breast cancer, with worse clinical evolution and tumor-free survival, leading to the need to develop new effective therapies for its control. The present study evaluated the action of tumor-penetrating peptide BR2 associated with 2-aminoethyl dihydrogen phosphate (2-AEH2P) on triple-negative breast tumor cells. Cell viability was evaluated by the MTT colorimetric method, mitochondrial electrical potential, and proteins involved in cell proliferation and death control were evaluated by flow cytometry and structural and morphological analysis by confocal microscopy. The results obtained showed that the peptide BR2 and the association 2-AEH2P + BR2 promoted significant cytotoxicity in tumor lines, compared to 2-AEH2P alone. In addition, the association 2-AEH2P + BR2 promoted tumor cells arrest in the G0/G1 phases. Interestingly, both treatments modulated the expression of markers CD44, CD34, CD24, cyclin D1, and Bcl-2, increased p21, Bax, and released cytochrome c. The association proved to be more effective, providing modulation of proteins involved in cell death and senescence, more pronounced cytotoxicity for tumor cells compared to normal cells, and the reduction of markers related to aggressiveness profile, progression, and tumor metastasis.
Insights
The peptide BR2, combined with 2-aminoethyl dihydrogen phosphate (2-AEH2P), effectively targets triple-negative breast cancer cells. This combination therapy demonstrates significant cytotoxicity and reduces markers associated with tumor progression and metastasis.
Area of Science:
- Oncology
- Biochemistry
- Molecular Biology
Background:
- Triple-negative breast cancer (TNBC) is an aggressive subtype with poor prognosis.
- There is an urgent need for novel therapeutic strategies to control TNBC.
- Tumor-penetrating peptides offer potential for targeted cancer therapy.
Purpose of the Study:
- To evaluate the efficacy of tumor-penetrating peptide BR2 combined with 2-aminoethyl dihydrogen phosphate (2-AEH2P) against triple-negative breast cancer cells.
- To investigate the mechanisms of action, including cytotoxicity, cell cycle arrest, and modulation of cell death pathways.
Main Methods:
- Cell viability assessed using MTT assay.
- Mitochondrial membrane potential and protein expression analyzed by flow cytometry.
- Cellular morphology examined via confocal microscopy.
Main Results:
- The combination of 2-AEH2P + BR2 demonstrated significant cytotoxicity against TNBC cells, surpassing 2-AEH2P alone.
- The 2-AEH2P + BR2 treatment induced G0/G1 cell cycle arrest.
- Both treatments modulated CD44, CD34, CD24, cyclin D1, and Bcl-2 expression, while increasing p21, Bax, and cytochrome c release.
Conclusions:
- The 2-AEH2P + BR2 combination therapy is a promising strategy for TNBC treatment.
- This combination induces cell death and senescence, with enhanced cytotoxicity towards tumor cells over normal cells.
- The treatment effectively reduces markers linked to tumor aggressiveness, progression, and metastasis.
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