title: Enhanced Peptide delivery into cells by using the synergistic effects of a cell-penetrating Peptide and a chemical drug to alter cell permeability.
abstract: Cell-penetrating peptides (CPPs) are short, often hydrophilic peptides that can deliver many kinds of molecules into cells and that are likely to serve as a useful tool of future biotherapeutics. However, CPPs application is limited because of insufficient transduction efficiency and unpredictable cellular localization. Here, we investigated the enhancement of 1,2-benzisothiazolin-3-one (BIT) on the uptake of a synthetic fluorescent TAT and a TAT-conjugated green fluorescent protein (GFP) or pro-apoptotic peptide KLA and evaluated its toxicity in various cell lines. Our results showed that BIT pretreatment can enhance the penetration efficiency of TAT and its fusion peptide. In addition, the fluorescence of the peptide conjugate at effective doses was well-distributed in the intracellular of different cell lines without membrane perforation or detectable cytotoxicity. The internalization of the peptides was serum-dependent and temperature-independent. These findings imply that BIT may serve as a newly found delivery enhancer that is suitable for improving the penetration of CPPs.
authors.forename: Jie-Lan
authors.initials: JL
authors.lastname: Ma
authors.forename: Hu
authors.initials: H
authors.lastname: Wang
authors.forename: Yan-Lin
authors.initials: YL
authors.lastname: Wang
authors.affiliation: §Chongqing Engineering Technology Research Centre of Veterinary Drug, College of Pharmaceutical Sciences, Southwest University, 2 Tiansheng Road, Beibei District, Chongqing 400715, China.
authors.forename: Yong-Huang
authors.initials: YH
authors.lastname: Luo
authors.forename: Chang-Bai
authors.initials: CB
authors.lastname: Liu
mesh_terms: D015153:Blotting, Western; D002460:Cell Line; D002463:Cell Membrane Permeability / Q000187:drug effects; D057846:Cell-Penetrating Peptides / Q000378:metabolism*; D005434:Flow Cytometry; D006461:Hemolysis / Q000187:drug effects; D056945:Hep G2 Cells; D006801:Humans; D020287:In Situ Nick-End Labeling
chemical_list: D057846:Cell-Penetrating Peptides
keywords: 1,2-benzisothiazolin-3-one (BIT); GFP; TAT; cell-penetrating peptides (CPPs); internalization