Wasp venom peptide improves the proapoptotic activity of alendronate sodium in A549 lung cancer cells
Nabil A Alhakamy1,2,3,4, Solomon Z Okbazghi5, Mohamed A Alfaleh6
1Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia.
Background:
Lung cancer in men and women is considered the leading cause for cancer-related mortality worldwide. Anti-cancer peptides represent a potential untapped reservoir of effective cancer therapy.
Methodology:
Box-Behnken response surface design was applied for formulating Alendronate sodium (ALS)-mastoparan peptide (MP) nanoconjugates using Design-Expert software. The optimization process aimed at minimizing the size of the prepared ALS-MP nanoconjugates. ALS-MP nanoconjugates' particle size, encapsulation efficiency and the release profile were determined. Cytotoxicity, cell cycle, annexin V staining and caspase 3 analyses on A549 cells were carried out for the optimized formula.
Results:
The results revealed that the optimized formula was of 134.91±5.1 nm particle size. The novel ALS-MP demonstrated the lowest IC50 (1.3 ± 0.34 μM) in comparison to ALS-Raw (37.6 ± 1.79 μM). Thus, the results indicated that when optimized ALS-MP nanoconjugate was used, the IC50 of ALS was also reduced by half. Cell cycle analysis demonstrated a significantly higher percentage of cells in the G2-M phase following the treatment with optimized ALS-MP nanoconjugates.
Conclusion:
The optimized ALS-MP formula had significantly improved the parameters related to the cytotoxic activity towards A549 cells, compared to control, MP and ALS-Raw.
Insights
Novel anti-cancer peptides (ACPs) show promise for lung cancer therapy. Researchers developed Alendronate sodium (ALS)-mastoparan peptide (MP) nanoconjugates, significantly enhancing cytotoxic activity against A549 lung cancer cells.
Area of Science:
- Biochemistry
- Nanotechnology
- Oncology
Background:
- Lung cancer is a leading cause of cancer mortality globally.
- Anti-cancer peptides (ACPs) offer a potential therapeutic avenue.
- Developing novel drug delivery systems is crucial for effective cancer treatment.
Purpose of the Study:
- To formulate and optimize Alendronate sodium (ALS)-mastoparan peptide (MP) nanoconjugates.
- To evaluate the cytotoxic activity and cellular effects of the optimized nanoconjugates on A549 lung cancer cells.
- To investigate the potential of ACPs in enhancing anti-cancer drug efficacy.
Main Methods:
- Box-Behnken response surface design was used for nanoconjugate formulation and optimization.
- Particle size, encapsulation efficiency, and release profiles of ALS-MP nanoconjugates were determined.
- Cytotoxicity (IC50), cell cycle, annexin V staining, and caspase 3 analyses were performed on A549 cells.
Main Results:
- The optimized ALS-MP nanoconjugate achieved a particle size of 134.91±5.1 nm.
- The novel ALS-MP demonstrated a significantly lower IC50 (1.3 ± 0.34 μM) compared to ALS-Raw (37.6 ± 1.79 μM).
- Treatment with optimized ALS-MP nanoconjugates increased the percentage of A549 cells in the G2-M phase.
Conclusions:
- The optimized ALS-MP nanoconjugate formula significantly enhanced cytotoxic activity against A549 cells.
- The nanoconjugate formulation improved the anti-cancer efficacy of Alendronate sodium.
- ALS-MP nanoconjugates represent a promising strategy for lung cancer therapy.
