Soman Neelesh R, Lanza Gregory M, Heuser John M, Schlesinger Paul H, Wickline Samuel A
Department of Biomedical Engineering, Washington University School of Medicine, St. Louis, MI 63110, USA.
Nano Lett. 2008 Apr;8(4):1131-6. doi: 10.1021/nl073290r. Epub 2008 Feb 27.
The therapeutic potential of cytolytic peptides is plagued by nonspecificity and enzymatic degradation. We report the first stable incorporation of melittin (a 26 amino acid amphipathic peptide) into an outer lipid monolayer of perfluorocarbon nanoparticles. Melittin binds avidly to the nanoparticles (dissociation constant approximately 3.27 nM) and retains its pore-forming activity after contact-mediated delivery to model bilayer membrane (liposomes) thereby demonstrating the effectiveness of perfluorocarbon nanoparticles as unique nanocarriers for cytolytic peptides.
溶细胞肽的治疗潜力受到非特异性和酶降解的困扰。我们报道了蜂毒肽(一种由26个氨基酸组成的两亲性肽)首次稳定地掺入全氟化碳纳米颗粒的外层脂质单分子层中。蜂毒肽与纳米颗粒紧密结合(解离常数约为3.27 nM),并在通过接触介导递送至模型双层膜(脂质体)后保留其成孔活性,从而证明全氟化碳纳米颗粒作为溶细胞肽独特纳米载体的有效性。