Manning Thomas, Mikula Rachel, Lee Hilary, Calvin Aaron, Darrah Jarrett, Wylie Greg, Phillips Dennis, Bythell Benjamin J
Chemistry, Valdosta State University, Valdosta, GA 31698, United States.
Chemistry, Valdosta State University, Valdosta, GA 31698, United States.
Bioorg Med Chem Lett. 2014 Feb 1;24(3):976-82. doi: 10.1016/j.bmcl.2013.12.053. Epub 2013 Dec 28.
In recent years, the bacterium responsible for tuberculosis has been increasing its resistance to antibiotics resulting in new multidrug resistant Mycobacterium tuberculosis (MR-TB) and extensively drug-resistant tuberculosis (XDR-TB). In this study we use several analytical techniques including NMR, FT-ICR, TOF-MS, LC-MS and UV/Vis to study the copper-capreomycin complex. The copper (II) cation is used as a carrier for the antibiotic capreomycin. Once this structure was studied using NMR, FT-ICR, and MALDI-TOF-MS, the NIH-NIAID tuberculosis cell line for several Tb strains (including antibiotic resistant strains) were tested against up to seven variations of the copper-capreomycin complex. Different variations of copper improved the efficacy of capreomycin against Tb up to 250 fold against drug resistant strains of Tb.
近年来，导致结核病的细菌对抗生素的耐药性不断增强，从而产生了新型多重耐药结核分枝杆菌（MR-TB）和广泛耐药结核病（XDR-TB）。在本研究中，我们使用了多种分析技术，包括核磁共振（NMR）、傅里叶变换离子回旋共振（FT-ICR）、飞行时间质谱（TOF-MS）、液相色谱-质谱联用（LC-MS）和紫外/可见光谱（UV/Vis）来研究铜卷曲霉素复合物。铜（II）阳离子用作抗生素卷曲霉素的载体。一旦使用核磁共振、傅里叶变换离子回旋共振和基质辅助激光解吸电离飞行时间质谱（MALDI-TOF-MS）对该结构进行了研究，就针对几种结核菌株（包括耐药菌株）的美国国立卫生研究院-美国国立过敏和传染病研究所结核病细胞系对多达七种铜卷曲霉素复合物变体进行了测试。不同的铜变体使卷曲霉素对结核耐药菌株的疗效提高了250倍。
