Antibacterial activity and cytotoxycity of gelatine-conjugated lysine-based peptides

作者:Vincek Maja Kaiser**erger; Mor Amram; Gorgieva Selestina; Kokol Vanja*
来源:Journal of Biomedical Materials Research Part A, 2017, 105(11): 3110-3126.
DOI:10.1002/jbm.a.36164

摘要

The effect of the coupling approach (chemical by using carbodiimide chemistry, and enzymatic by using transglutaminase) of a hydrophilic -poly-L-lysine (PL) and a structurally-hydrophobic oligo-acyl-lysyl (OAK) to a gelatine (GEL) macromolecule, and their antibacterial activity against Gram-negative E. coli and Gram-positive S. aureus bacteria, as well as cytotoxicity to human osteoblast cells was studied as potential macromolecules for biomedical applications. Different spectroscopic (ultraviolet-visible, infrared, fluorescence, and electron paramagnetic resonance) and separation (size-exclusion chromatography and capillary zone electrophoresis) techniques, as well as zeta-potential analysis were performed to confirm the PL/OAK covalent coupling and to determine their amount and orientation of the immobilization. The highest and kinetically the fastest reduction of bacteria (77% against E. coli vs. 82% against S. aureus) was achieved with GEL functionalized with PL/OAK by the chemical grafting-to approach being correlated with conformationally the highly-flexible ?brush-like? orientation linkage of peptides, enable its targeted and rapid interactions with bacteria membrane. The up to 400-fold lower yield of OAKs being immobilized may be related also to its cationic charge and hydrophobic alkyl chain moieties, compared to more hydrophilic PL easily causing random polymerization and self-conjugation. The PL/OAK-functionalized GEL did not induce citotoxicity to osteoblasts, even at approximate to 25-fold higher concentration than bacterial minimum inhibitory (MIC) concentration of PL/OAK.

  • 出版日期2017-11