Abstract
Linear, dimeric, tetrameric, and cyclic peptides derived from lactoferricin B, containing the RRWQWR motif, were designed, synthesized, purified, and characterized using RP-HPLC chromatography and MALDI-TOF mass spectrometry. The antibacterial activity of the designed peptides against E. coli (ATCC 11775 and 25922) and their cytotoxic effect against MDA-MB-468 and MDA-MB-231 breast cancer cell lines were evaluated. Dimeric and tetrameric peptides showed higher antibacterial activity in both bacteria strains than linear peptides. The dimeric peptide (RRWQWR)2K-Ahx exhibited the highest antibacterial activity against the tested bacterial strains. Furthermore, the peptides with high antibacterial activity exhibited significant cytotoxic effect against the tested breast cancer cell lines. This cytotoxic effect was fast and dependent on the peptide concentration. The tetrameric molecule containing RRWQWR motif has an optimal cytotoxic effect at a concentration of 22 µM. The evaluated dimeric and tetrameric peptides could be considered as candidates for developing new therapeutic agents against breast cancer. Polyvalence of linear sequences could be considered as a novel and versatile strategy for obtaining molecules with high anticancer activity.
Highlights
According to the World Health Organization (WHO), breast cancer is the most frequent cancer, impacting over 1.5 million women each year, and it causes the greatest number of cancer-related deaths among women
The aim of this study was to establish if the polyvalence or molecular restriction of LfcinB-derived peptides increases its antibacterial activity and/or cytotoxic effect in breast cancer cell lines
It was found that the tetrameric peptide LfcinB (20–25)4 exhibited high cytotoxicity against both tested breast cancer cell lines, and that it is dependent on peptide concentration (Figure 3A)
Summary
According to the World Health Organization (WHO), breast cancer is the most frequent cancer, impacting over 1.5 million women each year, and it causes the greatest number of cancer-related deaths among women. Antimicrobial peptides (AMPs) exhibit a cytotoxic effect on cancer cell lines and antimicrobial activity because of the electrostatic interaction between the amino acid side chain and the negative charge of the membrane surface [5,6]. LfcinB contains aromatic amino acids, such as tryptophan and phenylalanine, and basic residues (arginine and lysine) that confer amphipathic properties [9,16] These positively-charged residues interact electrostatically with the negative charges of the bacterial cell wall lipopolysaccharide (LPS), allowing the peptide to approach the bacterial membrane [9,16]. Tetrameric and dimeric peptides containing the minimal motif have the greatest cytotoxic effect against both MDA-MB-468 and MDA-MB-231 breast cancer cell lines. This activity was fast and dependent on peptide concentration
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