Centre of Advanced Studies, Faculty of Military Health Sciences, University of Defence, Hradec Kralove, Czech Republic.
J Enzyme Inhib Med Chem. 2011 Feb;26(1):93-7. doi: 10.3109/14756361003733613. Epub 2010 Jun 22.
These experiments were performed on a rat model. The rats were divided into eight groups and consequently exposed to either a saline solution (control), atropine or a combination of atropine and tabun. The reactivation efficacy of the oximes was estimated on the rats exposed to tabun, atropine and a reactivator of AChE. The oximes HI-6, obidoxime, trimedoxime, K203 and KR-22836 were used as representative compounds of commonly available and new AChE reactivators. Besides the positive effect of the administered reactivators on blood AChE activity, the sizable modulation of low molecular weight antioxidant (LMWA) levels was also determined. The LMWA levels in the the animals treated with the oxime reactivators were decreased in comparison with the animals treated by atropine alone. It was found that the levels of LMWA returned to the level found in the control animals when either trimedoxime, K203 or KR-22836 were administered. The principle of oxime reactivator function and a novel insight into AChE activity regulation and oxidative stress is discussed.
这些实验是在大鼠模型上进行的。大鼠被分为八组，分别暴露于生理盐水（对照）、阿托品或阿托品和塔崩的混合物中。肟类化合物在暴露于塔崩、阿托品和 AChE 重激活剂的大鼠中的重激活效果进行了评估。HI-6、obidoxime、trimedoxime、K203 和 KR-22836 被用作常用和新型 AChE 重激活剂的代表性化合物。除了给予的重激活剂对血液 AChE 活性的积极影响外，还确定了低分子量抗氧化剂 (LMWA) 水平的明显调节。与单独用阿托品治疗的动物相比，用肟类重激活剂治疗的动物的 LMWA 水平降低。当给予 trimedoxime、K203 或 KR-22836 时，发现 LMWA 水平恢复到对照动物中的水平。讨论了肟类重激活剂的作用原理以及 AChE 活性调节和氧化应激的新见解。
