Key Laboratory for Ultrafine Materials of Ministry of Education, School of Materials Science and Engineering , East China University of Science and Technology , Shanghai , 200237 , China.
Department of Pharmaceutical and Medicinal Chemistry , Royal College of Surgeons in Ireland , St. Stephens Green , Dublin 2 , Ireland.
Biomacromolecules. 2018 Jul 9;19(7):2673-2681. doi: 10.1021/acs.biomac.8b00296. Epub 2018 May 4.
With increasing troubles in bacterial contamination and antibiotic-resistance, new materials possessing both biocompatibility and antimicrobial efficacy are supposed to be developed for future biomedical application. Herein, we demonstrated a chemo-enzymatic ring opening polymerization (ROP) approach for block copolyester, that is, poly(4-benzyl formate piperidine lactone- b-ω-pentadecalactone) (PNPIL- b-PPDL), in a one-pot two-step process. Afterward, cationic poly(4-piperidine lactone- b-ω-pentadecalactone) (PPIL- b-PPDL) with pendent secondary amino groups was obtained via acidic hydrolysis of PNPIL- b-PPDL. The resulting cationic block copolyester exhibited high antibacterial activity against Gram negative E. coli and Gram positive S. aureus, while showed low toxicity toward NIH-3T3 cells. Moreover, the antibacterial property, cytotoxicity and degradation behavior could be tuned simply by variation of PPIL content. Therefore, we anticipate that such cationic block copolymers could potentially be applied as biomaterials for medicine or implants.
随着细菌污染和抗生素耐药性问题的日益增多，人们需要开发出兼具生物相容性和抗菌效果的新材料，用于未来的生物医学应用。在此，我们展示了一种化学-酶催化开环聚合（ROP）方法，用于合成嵌段共聚酯，即聚（4-苄基甲酸哌啶内酯-b-ω-十五内酯）（PNPIL-b-PPDL），采用一步两步法。随后，通过 PNPIL-b-PPDL 的酸性水解，得到了带有侧基仲氨基的阳离子聚（4-哌啶内酯-b-ω-十五内酯）（PPIL-b-PPDL）。所得阳离子嵌段共聚酯对革兰氏阴性大肠杆菌和革兰氏阳性金黄色葡萄球菌表现出高抗菌活性，而对 NIH-3T3 细胞的毒性较低。此外，通过改变 PPIL 的含量，可以简单地调节其抗菌性能、细胞毒性和降解行为。因此，我们预计此类阳离子嵌段共聚物可作为用于医学或植入物的生物材料得到应用。
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