Engineering Research Center of Biopolymer Functional Materials of Yunnan, Yunnan Minzu University, Kunming 650500, China.
Yunnan Rural Leader College, Yunnan Agricultural University, Heilongtan, Kunming 650201, China.
Molecules. 2018 Feb 23;23(2):497. doi: 10.3390/molecules23020497.
BF-30 is a single chain polypeptide of an N-segment with an α-helix from cathelicidin gene encoding, and it contains 30 amino acid residues, with a relative molecular mass and isoelectric point of 3637.54 and 11.79, respectively. Cathelicidin-BF-30 was entrapped in four-arm star-shaped poly(ethylene glycol-b-dl-lactic acid-co-glycolic acid) block copolymers (4-arm-PEG-PLGA) by a double-emulsion solvent-evaporation method. Three release phases of cathelicidin-BF-30loaded 4-arm-PEG-PLGA microspheres were observed, including an initial burst-release phase, followed by a lag phase with minimal drug release and finally a secondary zero-order release phase. The delivery system released BF-30 over more than 15 days in vitro. Furthermore, the material for preparing the microspheres has good biocompatibility and biodegradability. Additionally, based on the drug resistance of food pathogenic bacteria, the antibacterial effects of BF-30 on (), () and () as well as the stability of the in vitro release of the BF-30-loded microspheres were studied. The α-helix secondary structure and antibacterial activity of released BF-30 were retained and compared with native peptide. These BF-30 loaded microspheres presented <10% hemolysis and no toxicity for HEK293T cells even at the highest tested concentration (150 μg/mL), indicating that they are hemocompatible and a promising delivery and protection system for BF-30 peptide.
BF-30 是一种由 cathelicidin 基因编码的 N 段单链多肽，含有 30 个氨基酸残基，相对分子质量和等电点分别为 3637.54 和 11.79。通过双乳液溶剂蒸发法，将 cathelicidin-BF-30 包封在四臂星形聚（乙二醇-b-丙交酯-co-乙交酯）嵌段共聚物（4 臂-PEG-PLGA）中。载 cathelicidin-BF-30 的 4 臂-PEG-PLGA 微球观察到三个释放相，包括初始突释相、随后药物释放最小的迟滞相和最终的二次零级释放相。该递药系统在体外可超过 15 天释放 BF-30。此外，该微球制备材料具有良好的生物相容性和可降解性。此外，基于食源性病原体的耐药性，研究了 BF-30 对（）、（）和（）的抗菌作用以及载 BF-30 微球体外释放的稳定性。释放的 BF-30 保留了α-螺旋二级结构和抗菌活性，并与天然肽进行了比较。这些载 BF-30 的微球的溶血率<10%，即使在最高测试浓度（150μg/mL）下对 HEK293T 细胞也没有毒性，表明它们具有血液相容性，是 BF-30 肽的一种有前途的递药和保护系统。
