Cytotoxic effect of the dimeric peptides 10–13 against colon cancer cells HT-29 (cells were treated for 2 h at 37°C)
| Code | Sequence | IC50 (μM) | Selectivity index | Haemolysis (%) | ||
|---|---|---|---|---|---|---|
| HT-29 | Fibroblasts | SI1 | SI3 | |||
| 10 | (RWQWRWQWR)2-K-Ahx | 34 | 34 | 1.0 | > 1.9 | 2 |
| 11 | (Ahx-RWQWRWQWR)2-K-Ahx | 49 | 19 | 0.4 | > 1.2 | 1 |
| 12 | (RWQWRWQW-Orn)2-K-Ahx | 12 | 4 | 0.3 | > 5.1 | 1 |
| 13 | (CH3CO-RWQWRWQWR)2-K-Ahx | 12 | > 61 | > 5.0 | > 5.0 | 3 |
Haemolysis (%) is reported at peptide concentration of 200 μg/mL.
The supplementary figures and table for this article are available at: https://www.explorationpub.com/uploads/Article/file/100891_sup_1.pdf.
KJCM: Conceptualization, Methodology, Investigation, Formal analysis, Writing—original draft, Visualization, Writing—review & editing. JERC, YVC, and LFOG: Formal analysis, Resources, Writing—original draft. CMPG: Formal analysis, Resources, Writing—original draft. ACBC: Formal analysis, Resources. RFM: Conceptualization, Supervision, Funding acquisition. JELM: Conceptualization, Methodology, Writing—review & editing. ZJRM: Conceptualization, Methodology, Resources, Writing—review & editing, Funding acquisition. JEGC: Conceptualization, Methodology, Formal analysis, Resources, Writing—original draft, Visualization, Funding acquisition. All authors read and approved the submitted version.
The authors declare that they have no conflicts of interest.
For hemolytic activity (code 05-2019) and Irwin test (code 03-2018) were approved by the institutional ethics committee of the National University of Colombia. Zebrafish experiments were approved by the Institutional Committee for Animal Care and Use of the University of the Andes, code 24-01-2020.
Informed consent to participate in the study was obtained from all participants.
Not applicable.
The raw data supporting the conclusions of this manuscript will be made available by the authors, without undue reservation, to any qualified researcher.
This research was conducted with the financial support of MinCiencias with the projects: “Obtención de un prototipo peptídico promisorio para el desarrollo de un medicamento de amplio espectro para el tratamiento del cáncer de colon, cuello uterino y próstata”. Contract RC No. [845-2019]. “Desarrollo de un medicamento contra el cáncer de mama basado en un péptido polivalente derivado de la LfcinB: Estudio de la fase preclínica (fase cero), caracterización fisicoquímica de un lote del fármaco para estudios preclínicos”. RC No. [706-2018]. The funder had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.
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