Lassiter T L, Padilla S, Mortensen S R, Chanda S M, Moser V C, Barone S
Curriculum in Toxicology, University of North Carolina, Chapel Hill, North Carolina, USA.
Toxicol Appl Pharmacol. 1998 Sep;152(1):56-65. doi: 10.1006/taap.1998.8514.
Previous studies have shown that, in general, young, postnatal animals are more sensitive than adults to the toxic effects of anticholinesterase (antiChE) pesticides. Paradoxically, often fetal brain cholinesterase (ChE) is less inhibited than maternal brain after gestational exposure to an antiChE, presumably due to placental and fetal detoxification of the antiChE. The present investigation was designed to study selected toxicokinetic and toxicodynamic factors surrounding the toxicity of chlorpyrifos (CPF; [O,O'-diethyl O-3,5,6-trichloro-2-pyridyl] phosphorothionate) in pregnant rats dosed repeatedly or singly during late gestation. Dams were dosed daily (po) with CPF in corn oil (0 or 7 mg/kg) on gestational days (GD) 14 to 18. Animals were euthanized at 2 to 120 h after the last dose and tissues were collected for enzyme analysis. Using this dosing regimen, we found that (1) the time of maximal ChE inhibition was the same (i.e., 5-10 h after dosing) for both maternal and fetal brain, (2) the degree of fetal brain ChE inhibition was 4.7 times less than maternal brain inhibition, and (3) the detoxification potential (i.e., carboxylesterase and chlorpyrifos-oxonase) of the fetal tissues was very low compared to the maternal tissues. A separate group of experiments showed that if pregnant dams received only one oral dose of 7 or 10 mg/kg CPF on GD18, the degree of ChE inhibition in the fetal brain was comparable to the maternal brain ChE inhibition. Taking into consideration the net increase (more than fourfold) in fetal brain ChE activity from GD14 to 18 in control animals, and the fact that maternal brain ChE was inhibited more than fetal brain ChE only in a repeated-dosing regimen, we conclude that the fetus is not genuinely protected from the toxic effects of a given dose of CPF. We propose that fetal brain ChE is simply able to recover more fully between each dose as compared to maternal brain ChE, giving the illusion that the fetal compartment is less affected than the maternal compartment.
先前的研究表明,一般来说,幼年的产后动物比成年动物对抗胆碱酯酶(antiChE)农药的毒性作用更敏感。矛盾的是,在孕期接触antiChE后,胎儿脑胆碱酯酶(ChE)的受抑制程度通常低于母体脑,这可能是由于antiChE在胎盘和胎儿中的解毒作用。本研究旨在探讨妊娠晚期反复或单次给予毒死蜱(CPF;[O,O'-二乙基O-3,5,6-三氯-2-吡啶基]硫代磷酸酯)毒性相关的特定毒代动力学和毒效动力学因素。在妊娠第14至18天,母鼠每天经口给予玉米油中的CPF(0或7mg/kg)。在最后一次给药后2至120小时对动物实施安乐死,并收集组织进行酶分析。采用这种给药方案,我们发现:(1)母体和胎儿脑ChE抑制的最大时间相同(即给药后5 - 10小时);(2)胎儿脑ChE的抑制程度比母体脑抑制程度低4.7倍;(3)与母体组织相比胎儿组织的解毒潜力(即羧酸酯酶和毒死蜱氧化酶)非常低。另一组实验表明,如果妊娠母鼠在妊娠第18天仅口服一剂7或10mg/kg的CPF,胎儿脑中ChE的抑制程度与母体脑ChE的抑制程度相当。考虑到对照动物中胎儿脑ChE活性从妊娠第14天到第18天净增加(超过四倍),以及仅在重复给药方案中母体脑ChE比胎儿脑ChE受抑制更严重这一事实,我们得出结论,胎儿并未真正免受给定剂量CPF的毒性影响。我们提出,与母体脑ChE相比,胎儿脑ChE在每次给药之间能够更完全地恢复,从而造成胎儿部分比母体部分受影响更小的假象。