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温度对滴滴涕及其结构类似物抑制大鼠脑突触体ATP酶的影响。

Effect of temperature on the inhibition of rat brain synaptosomal ATPases by DDT and its structural analogs.

作者信息

Chetty S C, Aldous C N, Desaiah D

出版信息

J Appl Toxicol. 1984 Aug;4(4):194-7. doi: 10.1002/jat.2550040407.

DOI:10.1002/jat.2550040407
PMID:6149241
Abstract

In vitro effects of DDT and its isomers or metabolites were studied on Na+-K+-ATPase and oligomycin-sensitive (OS) Mg++-ATPase activities at 17, 27 and 37 degrees C in rat brain synaptosomes. Dicofol and methoxychlor were found to be more effective inhibitors of Na+-K+-ATPase and OS Mg++-ATPase than DDT, DDD and DDE. Inhibition of OS Mg++-ATPase by the compounds tested (except DDE) was found to be greater at 17 degrees C than at higher temperatures (17 greater than 27 greater than 37 degrees C), suggesting a negative temperature correlation trend Na+-K+-ATPase was less sensitive to these compounds when compared with OS Mg++-ATPase and the inhibition was greater at higher temperatures (37 greater than 27 greater than 17 degrees C), suggesting a positive temperature correlation trend. Other DDT isomers and metabolites showed variable effects on Na+-K+-ATPase and OS Mg++-ATPases. DDD, but not DDE, inhibited both enzyme activities and the inhibition was independent of temperature. No significant differences were observed in the inhibitory potencies of the various DDT, DDD or DDE ring substitutes studied. The present data indicate that DDT, dicofol and methoxychlor were more effective inhibitors of OS Mg++-ATPase than Na+-K+-ATPase and that the inhibition of the former enzyme had a negative temperature dependence, a feature which parallels toxicity results in insects.

摘要

研究了滴滴涕及其异构体或代谢物在17、27和37摄氏度下对大鼠脑突触体中钠钾 - 三磷酸腺苷酶(Na+-K+-ATPase)和寡霉素敏感(OS)的镁离子 - 三磷酸腺苷酶(Mg++-ATPase)活性的体外影响。发现三氯杀螨醇和甲氧滴滴涕比滴滴涕、滴滴滴和滴滴伊对Na+-K+-ATPase和OS Mg++-ATPase的抑制作用更强。所测试的化合物(除滴滴伊外)对OS Mg++-ATPase的抑制作用在17摄氏度时比在较高温度时(17℃>27℃>37℃)更强,表明存在负温度相关趋势;与OS Mg++-ATPase相比,Na+-K+-ATPase对这些化合物不太敏感,且在较高温度时(37℃>27℃>17℃)抑制作用更强,表明存在正温度相关趋势。其他滴滴涕异构体和代谢物对Na+-K+-ATPase和OS Mg++-ATPase表现出不同的影响。滴滴滴(而非滴滴伊)抑制了这两种酶的活性,且抑制作用与温度无关。在所研究的各种滴滴涕、滴滴滴或滴滴伊环取代物的抑制效力方面未观察到显著差异。目前的数据表明,滴滴涕、三氯杀螨醇和甲氧滴滴涕对OS Mg++-ATPase的抑制作用比对Na+-K+-ATPase更有效,且前者酶的抑制具有负温度依赖性,这一特征与昆虫的毒性结果相似。

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