Exploration of Drug Science

Table 1. Peptides derived from RWQWRWQWR (¹R⁵R⁹R) sequence containing D-aminoacids. Characterization by RP-HPLC and ESI-QTOF MS, and cytotoxic effect against breast cancer cells and non-cancerous fibroblast primary cell culture

Code	Sequence	RP-HPLC		ESI-MS (M^a)		IC₅₀, µg/mL (µM)
Code	Sequence	t_R (min)	Purity (%)	Theoretical	Exp.	MCF-7	Fibroblasts
¹R⁵R⁹R	RWQWRWQWR	6.3	92	1,485.75	1,485.88	120 (81)	> 200 (135)*
1	^dRWQWRWQWR	5.9	99	1,485.76	1,485.77	> 200 (135)*	> 200 (135)*
2	R^dWQWRWQWR	6.7	94	1,485.76	1,485.77	> 200 (135)*	> 200 (135)*
3	RW^dQWRWQWR	5.9	99	1,485.76	1,485.76	> 200 (135)*	> 200 (135)*
4	RWQ^dWRWQWR	6.5	95	1,485.76	1,485.77	> 200 (135)*	> 200 (135)*
5	RWQW^dRWQWR	5.9	95	1,485.76	1,485.77	> 200 (135)*	> 200 (135)*
6	RWQWR^dWQWR	6.1	89	1,485.76	1,485.77	> 200 (135)*	> 200 (135)*
7	RWQWRW^dQWR	6.1	100	1,485.76	1,485.77	> 200 (135)*	> 200 (135)*
8	RWQWRWQ^dWR	6.3	98	1,485.76	1,485.77	> 200 (135)*	> 200 (135)*
9	RWQWRWQW^dR	6.3	99	1,485.76	1,485.77	> 200 (135)*	> 200 (135)*
10	^dRWQW^dRWQW^dR	5.4	94	1,485.76	1,485.77	> 200 (135)*	> 200 (135)*
11	R^dWQ^dWR^dWQ^dWR	6.5	99	1,485.76	1,485.77	> 200 (135)*	> 200 (135)*
12	RW^dQWRW^dQWR	5.6	99	1,485.76	1,485.77	> 200 (135)*	> 200 (135)*
13	^dR^dW^dQ^dW^dR^dW^dQ^dW^dR	6.4	90	1,485.76	1,485.77	> 200 (135)*	> 200 (135)*

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^dR, ^dW, ^dQ indicate the position of D-Arg, D-Trp and D-Gln, respectively. *: IC₅₀ could not be reached at the evaluated concentrations; ESI-MS: electrospray ionization mass spectrometry; IC₅₀: half maximal inhibitory concentration; M^a: corresponds to monoisotopic mass; RP-HPLC: reversed-phase high-performance liquid chromatography; t_R: retention time

Supplementary materials

The supplementary figures for this article are available at: https://www.explorationpub.com/uploads/Article/file/100852_sup_1.pdf.

Declarations

Author contributions

ABC: Conceptualization, Software, Validation, Formal analysis, Investigation, Data curation, Writing—original draft. DCA: Validation, Formal analysis, Investigation, Data curation. YVC: Validation, Formal analysis, Investigation. CPG: Conceptualization, Project administration, Funding acquisition, Resources. AUP and JLM: Conceptualization, Methodology, Data curation, Supervision, Resources. ZRM: Conceptualization, Resources, Supervision, Writing—review & editing, Project administration, Funding acquisition, Resources. JGC: Conceptualization, Resources, Supervision, Writing—original draft, Writing—review & editing, Project administration, Funding acquisition, Resources. All authors read and approved the submitted version.

Conflicts of interest

The authors declare that they have no conflicts of interest.

Ethical approval

All the experiments were carried out in compliance with the guidelines and standards of Resolution 08430 of 1993 of the Colombian Ministry of Health and Law 84 of 27 December 1989 and were governed by the principles and standards for the care and use of animals, decreed by the institutional Ethics Committee from Science Faculty (Act 03-2018) of the National University of Colombia.

Consent to participate

Not applicable.

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 funded by COLCIENCIAS grant number [RC No. 706-2018]. Project: “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”. Code [110180762973]. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.

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