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Biodegradable polycaprolactone metallopolymer–antibiotic bioconjugates containing phenylboronic acid and cobaltocenium for antimicrobial application
Biomaterials Science ( IF 6.6 ) Pub Date : 2021-09-24 , DOI: 10.1039/d1bm00970b
Peng Yang 1 , Yuanyuan Luo 1 , Leman B Kurnaz 1 , Marpe Bam 2 , Xiaoming Yang 2 , Alan W Decho 3 , Mitzi Nagarkatti 2 , Chuanbing Tang 1
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This paper reports antimicrobial metallopolymers containing biodegradable polycaprolactone as the backbone with boronic acid and cobaltocenium as the side chain. While boronic acid promotes interactions with bacterial cells via boronolectin with lipopolysaccharides, cationic cobaltocenium facilitates the unique complexation with anionic β-lactam antibiotics. The synergistic interactions in these metallopolymer–antibiotic bioconjugates were evidenced by re-sensitized efficacy of penicillin-G against four different Gram-negative bacteria (E. coli, P. vulgaris, P. aeruginosa and K. pneumoniae). The degradability of the polyester backbone was validated through tests under physiological pH (7.4) and acidic pH (5.5) or under enzymatic conditions. These metallopolymers exhibited time-dependent uptake and reduction of cobalt metals in different organs of mice via in vivo absorption, distribution, metabolism, and excretion (ADME) tests.

中文翻译:

可生物降解的聚己内酯金属聚合物-抗生素生物共轭物,含有苯基硼酸和二茂钴,用于抗菌应用

本文报道了以可生物降解的聚己内酯为骨架,以硼酸和茂钴为侧链的抗菌金属聚合物。硼酸通过硼凝集素和脂多糖促进与细菌细胞的相互作用,而阳离子钴茂促进与阴离子β-内酰胺抗生素的独特络合。青霉素-G 对四种不同革兰氏阴性菌(大肠杆菌普通假单胞菌铜绿假单胞菌肺炎克雷伯菌)的再致敏功效证明了这些金属聚合物-抗生素生物共轭物的协同相互作用)。通过在生理 pH (7.4) 和酸性 pH (5.5) 或酶促条件下进行测试,验证了聚酯骨架的可降解性。通过体内吸收、分布、代谢和排泄 (ADME) 测试,这些金属聚合物在小鼠的不同器官中表现出对钴金属的时间依赖性吸收和还原。
更新日期:2021-10-01
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