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Issue 10, 2014
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Identification of BP16 as a non-toxic cell-penetrating peptide with highly efficient drug delivery properties

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Abstract

Antimicrobial peptides are an interesting source of non-cytotoxic drug delivery vectors. Herein, we report on the identification of a new cell-penetrating peptide (KKLFKKILKKL-NH2, BP16) from a set of antimicrobial peptides selected from a library of cecropin-melittin hybrids (CECMEL11) previously designed to be used in plant protection. This set of peptides was screened for their cytotoxicity against breast adenocarcinoma MCF-7, pancreas adenocarcinoma CAPAN-1 and mouse embryonic fibroblast 3T3 cell lines. BP16 resulted to be non-toxic against both malignant and non-malignant cells at concentrations up to 200 μM. We demonstrated by flow cytometry and confocal microscopy that BP16 is mainly internalized in the cells through a clathrin dependent endocytosis and that it efficiently accumulates in the cell cytoplasm. We confirmed that the cell-penetrating properties of BP16 are retained after conjugating it to the breast tumor homing peptide CREKA. Furthermore, we assessed the potential of BP16 as a drug delivery vector by conjugating the anticancer drug chlorambucil to BP16 and to a CREKA-BP16 conjugate. The efficacy of the drug increased between 6 and 9 times when conjugated to BP16 and between 2 and 4.5 times when attached to the CREKA-BP16 derivative. The low toxicity and the excellent cell-penetrating properties clearly suggest that BP16 is a suitable vector for the delivery of therapeutic agents into cells.

Graphical abstract: Identification of BP16 as a non-toxic cell-penetrating peptide with highly efficient drug delivery properties

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Publication details

The article was received on 04 Dec 2013, accepted on 10 Jan 2014 and first published on 10 Jan 2014


Article type: Paper
DOI: 10.1039/C3OB42422G
Author version available: Download Author version (PDF)
Citation: Org. Biomol. Chem., 2014,12, 1652-1663
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    Identification of BP16 as a non-toxic cell-penetrating peptide with highly efficient drug delivery properties

    M. Soler, M. González-Bártulos, D. Soriano-Castell, X. Ribas, M. Costas, F. Tebar, A. Massaguer, L. Feliu and M. Planas, Org. Biomol. Chem., 2014, 12, 1652
    DOI: 10.1039/C3OB42422G

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