First unequivocal identification of the critical acyl radicals from the anti- tuberculosis drug isoniazid and its hydrazide analogs by complementary applications of ESR spin-trapping and HPLC/MS methods
文献类型:期刊论文
作者 | Qin, Li; Huang, Chun-Hua; Mao, Li; Shao, Bo; Zhu, Ben-Zhan |
刊名 | FREE RADICAL BIOLOGY AND MEDICINE
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出版日期 | 2020-07 |
卷号 | 154页码:1-8 |
关键词 | Isoniazid Hydrazides Carbon-centered acyl radicals ESR spin-trapping/HPLC/MS N-tert-butyl-alpha-phenylnitrone (PBN) NAD(+) adducts |
ISSN号 | 0891-5849 |
英文摘要 | The carbon-centered isonicotinic acyl radical of isoniazid (INH), a widely-used frontline anti-tuberculosis drug, has been considered to play a critical role in inhibiting Mycobacterium tuberculosis, but not fully identified. Here we show that this radical intermediate can be unequivocally characterized by complementary applications of ESR spin-trapping and HPLC/MS methods by employing N-tert-butyl-alpha-phenylnitrone (PBN) as the suitable spin-trapping agent, which can form the most stable radical adduct. More importantly, for the first time, analogous carbon-centered acyl radicals and their respective NAD(+) adducts have also been detected and identified from its two isomers (nicotinic acid hydrazide and 2-pyridinecarbohydrazide) and benzhydrazide which are structurally related to INH, but not by 2-chloroisonicotinohydrazide. This study represents the first unequivocal identification of the carbon-centered acyl radicals of INH and other hydrazide analogs by both ESR spin-trapping and HPLC/MS methods, which may have broad biomedical and toxicological significance for future research for more efficient hydrazide anti-tuberculosis drugs. |
源URL | [http://ir.rcees.ac.cn/handle/311016/44691] ![]() |
专题 | 生态环境研究中心_环境化学与生态毒理学国家重点实验室 |
推荐引用方式 GB/T 7714 | Qin, Li,Huang, Chun-Hua,Mao, Li,et al. First unequivocal identification of the critical acyl radicals from the anti- tuberculosis drug isoniazid and its hydrazide analogs by complementary applications of ESR spin-trapping and HPLC/MS methods[J]. FREE RADICAL BIOLOGY AND MEDICINE,2020,154:1-8. |
APA | Qin, Li,Huang, Chun-Hua,Mao, Li,Shao, Bo,&Zhu, Ben-Zhan.(2020).First unequivocal identification of the critical acyl radicals from the anti- tuberculosis drug isoniazid and its hydrazide analogs by complementary applications of ESR spin-trapping and HPLC/MS methods.FREE RADICAL BIOLOGY AND MEDICINE,154,1-8. |
MLA | Qin, Li,et al."First unequivocal identification of the critical acyl radicals from the anti- tuberculosis drug isoniazid and its hydrazide analogs by complementary applications of ESR spin-trapping and HPLC/MS methods".FREE RADICAL BIOLOGY AND MEDICINE 154(2020):1-8. |
入库方式: OAI收割
来源:生态环境研究中心
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