神经毒剂抑制的丁酰胆碱酯酶可以被氯代吡啶酮肟类化合物有效重激活。
Butyrylcholinesterase inhibited by nerve agents is efficiently reactivated with chlorinated pyridinium oximes.
机构信息
Institute for Medical Research and Occupational Health, Ksaverska cesta 2, HR-10000 Zagreb, Croatia.
Department of Chemistry, Faculty of Science, University of Hradec Kralove, Rokitanskeho 62, 50003 Hradec Kralove, Czech Republic; University Hospital in Hradec Kralove, Biomedical Research Center, Sokolska 581, 50005 Hradec Kralove, Czech Republic.
出版信息
Chem Biol Interact. 2019 Jul 1;307:16-20. doi: 10.1016/j.cbi.2019.04.020. Epub 2019 Apr 18.
Bispyridinium oximes with one (K865, K866, K867) or two (K868, K869, K870) ortho-positioned chlorine moiety, analogous to previously known K027, K048 and K203 oximes, and potent reactivators of human acetylcholinesterase (AChE) inhibited by nerve agents, were tested in the reactivation of human butyrylcholinesterase (BChE) inhibited by sarin, cyclosarin, VX, and tabun. A previously highlighted AChE reactivator, dichlorinated bispyridinium oxime with propyl linker (K868), was tested in more detail for reactivation of four nerve agent-BChE conjugates. Its BChE reactivation potency was showed to be promising when compared to the standard oximes used in medical practice, asoxime (HI-6) and pralidoxime (2-PAM), especially in case of sarin and tabun. This finding could be used in the pseudo-catalytic scavenging of the most nerve agents due to its cumulative capacity to reactivate both AChE and BChE.
具有一个（K865、K866、K867）或两个（K868、K869、K870）邻位氯取代基的双吡啶烷酮肟类似于先前已知的 K027、K048 和 K203 肟，是神经毒剂抑制的人乙酰胆碱酯酶（AChE）的有效重活化剂，对沙林、梭曼、VX 和塔崩抑制的人丁酰胆碱酯酶（BChE）的重活化作用进行了测试。先前突出的 AChE 重活化剂、带有丙基连接基的二氯双吡啶烷酮肟（K868），对四种神经毒剂-BChE 缀合物的重活化作用进行了更详细的测试。与在医学实践中使用的标准肟，如硫酸羟肟酸（HI-6）和氯解磷定（2-PAM）相比，其 BChE 重活化能力具有很大的潜力，特别是在沙林和塔崩的情况下。由于其能够同时重活化 AChE 和 BChE，因此这种发现可用于大多数神经毒剂的假催化清除。
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