[二氯乙烯基磷酸酯与母鸡和大鼠脑中神经毒性酯酶相互作用的比较研究]
[A comparative study of the interaction of phosphoric acid dichlorovinyl esters with a neurotoxic esterase from the brain of hens and rats].
作者信息
Makhaeva G F, Filonenko I V, Malygin V V
出版信息
Zh Evol Biokhim Fiziol. 1995 Jul-Aug;31(4):396-403.
In order to validate a rodent biochemical model of delayed neurotoxicity of organophosphates (OP) inhibition of rat and hen brain neurotoxic esterase (NTE) by some dichlorovinyl phosphates and phosphonates was studied in vitro and in vivo. It was shown that compounds investigated exhibited the similar inhibitory potency to NTE from both species in vitro, in addition rat and hen NTE showed the same sensitivity to variation of the structure of OP inhibitors. A good correlation was found between pI50 estimated with enzymes from rat and hen trains: r2 = 0.951, n = 18, p < or = 0.05. NTE activities were also measured in rat and hen brains after acute administration of various dosages of potent axonopathic compound dipropyldichlorovinyl phosphate. The results obtained indicate that difference in species susceptibility to neurotoxic action of OP, in particular the absence of ataxia in rats, is not caused by difference in target enzyme sensitivity to axonopathic organophosphates.
为了验证有机磷酸酯（OP）延迟神经毒性的啮齿动物生化模型，研究了一些二氯乙烯基磷酸酯和膦酸酯对大鼠和母鸡脑神经毒性酯酶（NTE）的抑制作用，包括体外和体内研究。结果表明，所研究的化合物在体外对两种动物的NTE表现出相似的抑制效力，此外，大鼠和母鸡的NTE对OP抑制剂结构变化的敏感性相同。用大鼠和母鸡脑中的酶估算的pI50之间发现了良好的相关性：r2 = 0.951，n = 18，p≤0.05。在急性给予各种剂量的强效轴突病化合物二丙基二氯乙烯基磷酸酯后，还测量了大鼠和母鸡脑中的NTE活性。所得结果表明，物种对OP神经毒性作用的易感性差异，特别是大鼠不存在共济失调，不是由靶酶对轴突病性有机磷酸酯的敏感性差异引起的。
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