Table Info

Table 2.

Cytotoxic effect of the dimeric peptides against colon cancer cells and non-cancer cells (cells were treated for 2 h at 37°C)

Code	Sequence	IC₅₀ (μM)				Selectivity index			Haemolysis (%)
Code	Sequence	HT-29	Caco-2	HEK 293	Fibroblasts	SI¹	SI²	SI³	Haemolysis (%)
²⁶[F]	(RRWQWRFKKLG)₂-K-Ahx	12	18*	22	34	2.8	1.8	> 5.1	6
1	(^dRRWQWRFKKLG)₂-K-Ahx	> 59	45	nd	nd	nd	nd	nd	nd
2	(Orn-RWQWRFKKLG)₂-K-Ahx	18	38	25	20	1.1	1.4	> 3.3	3
3	(R-Orn-WQWRFKKLG)₂-K-Ahx	30	12	41	17	0.6	1.4	> 2.0	5
4	(RRWQW-Orn-FKKLG)₂-K-Ahx	49	10	> 61	> 61	> 1.2	> 1.2	> 1.2	5
5	(^dR-Orn-WQWRFKKLG)₂-K-Ahx	20	11	14	9	0.5	0.7	> 3.1	5
6	(^dRRWQW-Orn-FKKLG)₂-K-Ahx	35	16	25	23	0.7	0.7	> 1.7	7
7	(Ahx-RRWQWRFKKLG)₂-K-Ahx	19	25	19	29	1.5	1.0	> 3.0	5
8	(Biotin-Ahx-RRWQWRFKKLG)₂-K-Ahx	17	20	16	49	2.9	0.9	> 2.9	6
9	(CH₃CO-Ahx-RRWQWRFKKLG)₂-K-Ahx	24	nd	nd	19	0.8	nd	> 2.3	9

SI of peptides is described as the ratio IC₅₀ non-cancer cells/IC₅₀ cancer cells. ${S I}^{1} = \frac{{I C}_{50 F i b r o b l a s t}}{{I C}_{50 H T - 29}}$ ; ${S I}^{2} = \frac{{I C}_{50 H E K 293}}{{I C}_{50 H T - 29}}$ ; ${S I}^{3} = \frac{{I C}_{50 R B C}}{{I C}_{50 H T - 29}}$ . Haemolysis (%) is reported at peptide concentration of 200 μg/mL. nd is not determined. *: IC₅₀ for peptide ²⁶[F] in Caco-2 cells was previously reported [15]. RBC: red blood cells; SI: selectivity index

Supplementary materials

The supplementary figures and table for this article are available at: https://www.explorationpub.com/uploads/Article/file/100891_sup_1.pdf.

Declarations

Author contributions

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.

Conflicts of interest

The authors declare that they have no conflicts of interest.

Ethical approval

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.

Consent to participate

Informed consent to participate in the study was obtained from all participants.

Consent to publication

Not applicable.

Availability of data and materials

The raw data supporting the conclusions of this manuscript will be made available by the authors, without undue reservation, to any qualified researcher.

Funding

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.

Copyright

Publisher’s note

Open Exploration maintains a neutral stance on jurisdictional claims in published institutional affiliations and maps. All opinions expressed in this article are the personal views of the author(s) and do not represent the stance of the editorial team or the publisher.

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