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Coadministration of kla peptide with HPRP-A1 to enhance anticancer activity
Wenjing Hao1,2, Cuihua Hu3,4, Yibing Huang1,2
1Key Laboratory for Molecular Enzymology and Engineering of the Ministry of Education, Jilin University, Changchun, China.
Abstract:
The apoptosis-inducing peptide kla (KLAKLAK)2 possesses the ability to disrupt mitochondrial membranes and induce cancer cell apoptosis, but this peptide has a poor eukaryotic cell-penetrating potential. Thus, it requires the assistance of other peptides for effective translocation at micromolar concentrations. In this study, breast and lung cancer cells were treated by kla peptide co-administrated with membrane-active anticancer peptide HPRP-A1. HPRP-A1 assisted kla to enter cancer cells and localized on mitochondrial membranes to result in cytochrome C releasing and mitochondrial depolarization which ultimately induced apoptosis.The apoptosis rate was up to 65%and 45% on MCF-7 and A549 cell lines, respectively, induced by HPRP-A1 coadministration with kla group. The breast cancer model was constructed in mice, and the anticancer peptides were injected to observe the changes in cancer volume, andimmunohistochemical analysis was performed on the tissues and organs after the drug was administered. Both the weight and volume of tumor tissue were remarkable lower in HPRP-A1 with kla group compared with thosepeptidealonggroups. The results showed that the combined drug group effectively inhibited the growth of cancer and did not cause toxic damage to normal tissues, as well as exhibited significantly improvement on peptide anticancer activity in vitro and in vivo.
Insights
The anticancer peptide HPRP-A1 enhances the cell penetration of the apoptosis-inducing peptide KLAKLAK2, leading to effective cancer cell death and reduced tumor growth in vivo without significant toxicity.
Area of Science:
- Biochemistry
- Molecular Biology
- Cancer Research
Background:
- The apoptosis-inducing peptide KLAKLAK2 effectively disrupts mitochondrial membranes but has limited cell penetration.
- Co-administration with cell-penetrating peptides is necessary for KLAKLAK2's translocation and efficacy.
Purpose of the Study:
- To evaluate the synergistic anticancer effects of KLAKLAK2 combined with HPRP-A1.
- To assess the in vitro and in vivo efficacy and safety of this peptide combination.
Main Methods:
- Treatment of breast (MCF-7) and lung (A549) cancer cell lines with KLAKLAK2 and HPRP-A1.
- Induction of apoptosis by monitoring cytochrome C release and mitochondrial depolarization.
- Establishment of a mouse breast cancer model to assess tumor growth inhibition and perform immunohistochemical analysis.
Main Results:
- HPRP-A1 facilitated KLAKLAK2 entry into cancer cells, targeting mitochondrial membranes.
- Significant apoptosis rates (up to 65% in MCF-7, 45% in A549) were observed with the combination therapy.
- Combined treatment markedly reduced tumor weight and volume in vivo with no observed toxic damage to normal tissues.
Conclusions:
- HPRP-A1 significantly enhances the anticancer activity of KLAKLAK2 by improving its cell penetration and mitochondrial targeting.
- The combination of KLAKLAK2 and HPRP-A1 demonstrates potent in vitro and in vivo anticancer efficacy with a favorable safety profile.
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