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铜-聚乙二醇-阿米卡星复合物对结核分枝杆菌的结构测定及细胞系研究

Structural measurements and cell line studies of the copper– PEG–Amikacin complex against Mycobacterium tuberculosis.

作者信息

Manning Thomas, Patel Hatel, Wylie Greg, Phillips Dennis, Jarvis Jackie

机构信息

Chemistry, Valdosta State University, Valdosta, GA 31698, United States

出版信息

Bioorg Med Chem Lett. 2015 Dec 15;25(24):5825-30. doi: 10.1016/j.bmcl.2015.08.012.

Abstract

The bacterium responsible for causing tuberculosis is increasing its resistance to antibiotics resulting in new multidrug-resistant Mycobacterium tuberculosis (MDR-TB) and extensively drug-resistant M. tuberculosis (XDR-TB) strains. In this study, several analytical techniques including NMR, FT-ICR, MALDI-MS, and LC–MS are used to study different aspects of the Copper–polyethylene glycol (PEG)–Amikacin complex. The Cu(II) cation and the aggregate formed by PEG serve as a carrier for the antibiotic. Several Cu–PEG–Amikacin complex variations were tested against NIH-NIAID cell lines containing both resistant and nonresistant strains of M. tuberculosis.

摘要

导致结核病的细菌对抗生素的耐药性正在增强,从而产生了新的耐多药结核分枝杆菌(MDR-TB)和广泛耐药结核分枝杆菌(XDR-TB)菌株。在本研究中,使用了包括核磁共振(NMR)、傅里叶变换离子回旋共振(FT-ICR)、基质辅助激光解吸电离质谱(MALDI-MS)和液相色谱-质谱联用(LC-MS)在内的多种分析技术,来研究铜-聚乙二醇(PEG)-阿米卡星复合物的不同方面。铜(II)阳离子和由PEG形成的聚集体作为抗生素的载体。针对含有耐药和非耐药结核分枝杆菌菌株的美国国立卫生研究院-国家过敏和传染病研究所(NIH-NIAID)细胞系,测试了几种铜-PEG-阿米卡星复合物变体。

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