Palikov V A, Terekhov S S, Palikova Yu A, Khokhlova O N, Kazakov V A, Dyachenko I A, Panteleev S V, Mokrushina Yu A, Knorre V D, Shamborant O G, Smirnov I V, Gabibov A G
Branch of the Institute of Bioorganic Chemistry, Academicians M.M. Shemyakin and Yu.A. Ovchinnikova RAS, Nauki Ave., 6, Pushchino, Moscow region, 142290, Russia.
Institute of Bioorganic Chemistry, Academicians M.M. Shemyakin and Yu.A. Ovchinnikova RAS, Miklukho-Maklaya Str., 16/10, Moscow, 117997, Russia.
Acta Naturae. 2018 Oct-Dec;10(4):125-128.
The development of antidotes to organophosphate poisons is an important aspect of modern pharmacology. Recombinant acetylcholinesterase and butyrylcholinesterase are effective DNA-encoded acceptors of organophosphate poisons and, in particular, pesticides. Here, we present the results of a study on the effectiveness of recombinant butyrylcholinesterase (BChE) in modeling organophosphate poisoning caused by oral administration of paraoxon at a dose of 2 mg / kg. The study showed a high activity of BChE as a protective agent for subchronic anticholinesterase poisoning in an model. The administration of BChE in a dose of 20 mg / kg allows one to avoid mortality, and also contributed to rapid recovery after model poisoning.
有机磷酸酯类毒物解毒剂的研发是现代药理学的一个重要方面。重组乙酰胆碱酯酶和丁酰胆碱酯酶是有机磷酸酯类毒物特别是农药的有效DNA编码受体。在此,我们展示了一项关于重组丁酰胆碱酯酶(BChE)对口服2 mg / kg对氧磷所致有机磷酸酯中毒建模有效性的研究结果。该研究表明,在动物模型中,BChE作为亚慢性抗胆碱酯酶中毒的保护剂具有高活性。给予20 mg / kg剂量的BChE可避免死亡,且有助于模型中毒后快速恢复。