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Evaluating the In Vitro Activity and Safety of Modified LfcinB Peptides as Potential Colon Anticancer Agents: Cell
Karen J Cárdenas-Martínez1, Andrea C Barragán-Cárdenas1, Manuela de la Rosa-Arbeláez1
1Department of Pharmacy, Department of Biotechnology, Deparment of Chemistry, Universidad Nacional de Colombia, Carrera 45#26-85, Bogotá 111321, Colombia.
Abstract:
Anticancer peptides are increasingly being considered as alternative treatments for cancer due to their potency, selectivity, and low toxicity. Previously, the peptide LfcinB (21-25)Pal showed in vitro anticancer effects against the Caco-2 colon cancer cell line (half-maximal inhibitory concentration (IC50): 86 μM). In this study, we developed modifications to the peptide sequence to increase its anticancer activity. Sequence modifications were made such as the inclusion of amino hexanoic acid (Ahx), N-terminal biotinylation, acetylation, and substitutions of Orn for Arg and/or d-Arg by l-Arg. The molecules were synthesized using manual solid-phase peptide synthesis (SPPS), and their synthetic feasibility (SAScore) ranged from 6.2 to 7.6. The chromatographic purities of the synthesized peptides were greater than 89%. We found that Ahx-RWQWRWQWR and RWQWRWQW-Orn showed activity against both Caco-2 and HT-29 cell lines and decreased IC50 values by approx. 50% in Caco-2 cells (IC50: 40 μM) when compared to the parent peptide RWQWRWQWR. Moreover, the modified peptides demonstrated lower hemolytic effects, with values <10% at 200 μg/mL. Toxicity was assessed using the Galleria mellonella model and the half-maximal lethal dose (LD50) for the best peptides was >100 mg/kg, indicating that their toxicity is classified as moderately toxic or lower. In contrast, cisplatin showed an LD50 of 13 mg/Kg. The designed anticancer peptides presented good in vitro activity and low toxicity, making them promising molecules for future drug development studies.
Insights
Modified anticancer peptides show enhanced efficacy against colon cancer cells with reduced toxicity. These novel peptide analogs offer a promising alternative to traditional chemotherapy agents like cisplatin for future cancer drug development.
Area of Science:
- Biochemistry
- Medicinal Chemistry
- Oncology
Background:
- Anticancer peptides are emerging as potent, selective, and low-toxicity alternatives for cancer therapy.
- The parent peptide LfcinB (21-25)Pal demonstrated preliminary in vitro anticancer effects against Caco-2 colon cancer cells (IC50: 86 μM).
Purpose of the Study:
- To develop modified anticancer peptides with increased anticancer activity and reduced toxicity.
- To evaluate the in vitro and in vivo efficacy and safety of novel peptide analogs.
Main Methods:
- Peptide modifications included amino hexanoic acid (Ahx), N-terminal biotinylation, acetylation, and amino acid substitutions.
- Synthesis was performed using manual solid-phase peptide synthesis (SPPS), followed by purity assessment (>89%).
- In vitro anticancer activity was tested against Caco-2 and HT-29 cell lines, and in vivo toxicity was assessed using the Galleria mellonella model.
Main Results:
- Modified peptides, specifically Ahx-RWQWRWQWR and RWQWRWQW-Orn, exhibited activity against both Caco-2 and HT-29 cells.
- These analogs reduced the IC50 by approximately 50% in Caco-2 cells (IC50: 40 μM) compared to the parent peptide.
- The modified peptides showed low hemolytic effects (<10% at 200 μg/mL) and favorable in vivo toxicity profiles (LD50 >100 mg/kg) in the Galleria mellonella model, contrasting with cisplatin (LD50: 13 mg/Kg).
Conclusions:
- Designed anticancer peptides exhibit significant in vitro anticancer activity and low toxicity.
- These modified peptides represent promising candidates for further investigation in cancer drug development.
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