中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
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
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
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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.

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来源:生态环境研究中心

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