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Tuning the anticancer activity of a novel pro-apoptotic peptide using gold nanoparticle platforms
Mohammad Akrami1, Saeed Balalaie2, Saman Hosseinkhani3,4
1Department of Pharmaceutical Biomaterials and Medical Biomaterials Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.
Abstract:
Pro-apoptotic peptides induce intrinsic apoptosis pathway in cancer cells. However, poor cellular penetration of the peptides is often associated with limited therapeutic efficacy. In this report, a series of peptide-gold nanoparticle platforms were developed to evaluate the anticancer activity of a novel alpha-lipoic acid-peptide conjugate, LA-WKRAKLAK, with respect to size and shape of nanoparticles. Gold nanoparticles (AuNPs) were found to enhance cell internalization as well as anticancer activity of the peptide conjugates. The smaller nanospheres showed a higher cytotoxicity, morphological change and cellular uptake compared to larger nanospheres and nanorods, whereas nanorods showed more hemolytic activity compared to nanospheres. The findings suggested that the anticancer and biological effects of the peptides induced by intrinsic apoptotic pathway were tuned by peptide-functionalized gold nanoparticles (P-AuNPs) as a function of their size and shape.
Insights
Novel peptide-gold nanoparticle platforms enhance cancer cell death. Smaller nanospheres show superior anticancer activity and cellular uptake compared to larger nanoparticles and nanorods.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Cancer Research
Background:
- Pro-apoptotic peptides trigger cancer cell death via the intrinsic apoptosis pathway.
- Limited therapeutic efficacy of peptides is often due to poor cellular penetration.
- Alpha-lipoic acid-peptide conjugates offer potential for cancer therapy.
Purpose of the Study:
- To develop and evaluate peptide-gold nanoparticle (P-AuNP) platforms for enhanced anticancer activity.
- To investigate the influence of nanoparticle size and shape on the efficacy of a novel alpha-lipoic acid-peptide conjugate (LA-WKRAKLAK).
- To assess the impact of P-AuNPs on cancer cell internalization, cytotoxicity, and hemolytic activity.
Main Methods:
- Synthesis of gold nanoparticles (AuNPs) with varying sizes (nanospheres) and shapes (nanorods).
- Conjugation of a novel alpha-lipoic acid-peptide (LA-WKRAKLAK) to AuNPs.
- Evaluation of cellular uptake, cytotoxicity, morphological changes, and hemolytic activity of peptide conjugates and P-AuNPs in cancer cells.
- Comparison of the effects of smaller nanospheres, larger nanospheres, and nanorods.
Main Results:
- Gold nanoparticles (AuNPs) significantly enhanced cell internalization and anticancer activity of peptide conjugates.
- Smaller nanospheres exhibited higher cytotoxicity, induced more significant morphological changes, and demonstrated greater cellular uptake than larger nanospheres and nanorods.
- Nanorods displayed higher hemolytic activity compared to nanospheres.
- The anticancer effects were mediated through the intrinsic apoptosis pathway.
Conclusions:
- Peptide-functionalized gold nanoparticles (P-AuNPs) can effectively enhance the anticancer properties of pro-apoptotic peptides.
- Nanoparticle size and shape are critical factors in tuning the anticancer efficacy and biological effects of P-AuNPs.
- Smaller nanospheres represent a promising platform for improving peptide-based cancer therapy due to enhanced cellular uptake and cytotoxicity.
