Slotkin Theodore A, Skavicus Samantha, Seidler Frederic J
Department of Pharmacology & Cancer Biology, Duke University Medical Center, Durham, NC 27710, USA.
Department of Pharmacology & Cancer Biology, Duke University Medical Center, Durham, NC 27710, USA.
Brain Res Bull. 2017 Apr;130:268-273. doi: 10.1016/j.brainresbull.2017.02.004. Epub 2017 Feb 21.
Organophosphate pesticides elicit developmental neurotoxicity through mechanisms over and above their shared property as cholinesterase inhibitors. We compared the consequences of neonatal exposure (postnatal days PN1-4) to diazinon or parathion on development of norepinephrine systems in rat brain, using treatments designed to produce equivalent effects on cholinesterase, straddling the threshold for barely-detectable inhibition. Norepinephrine levels were measured throughout development from the immediate posttreatment period (PN5), to early adolescence (PN30), young adulthood (PN60) and full adulthood (PN100); we assessed multiple brain regions containing all the major noradrenergic synaptic projections. Diazinon elicited a significant overall deficit of norepinephrine, whereas parathion produced a net increase. The effects were not immediately apparent (PN5) but rather emerged over the course of development, indicating that the organophosphate effects represent alteration of the trajectory of development, not just continuance of an initial injury. There were no comparable effects on β-adrenergic receptors, indicating that the presynaptic changes were not an adaptation to an underlying, primary effect on postsynaptic receptor signaling. Because we used the cholinesterase inhibition benchmark, the absolute dose of diazinon was much higher than that of parathion, since the latter is a more potent cholinesterase inhibitor. Our results are consistent with the growing evidence that the various organophosphates can differ in their impact on brain development and that consequently, the cholinesterase benchmark is an inadequate predictor of adverse neurodevelopmental effects.
有机磷酸酯类农药引发发育性神经毒性的机制,不仅仅是作为胆碱酯酶抑制剂所共有的特性。我们比较了新生大鼠(出生后第1 - 4天)接触二嗪农或对硫磷对大鼠脑中去甲肾上腺素系统发育的影响,采用旨在对胆碱酯酶产生等效作用的处理方法,刚好跨越几乎无法检测到抑制作用的阈值。在从处理后即刻(出生后第5天)到青春期早期(出生后第30天)、青年期(出生后第60天)和成年期(出生后第100天)的整个发育过程中测量去甲肾上腺素水平;我们评估了包含所有主要去甲肾上腺素能突触投射的多个脑区。二嗪农引发了去甲肾上腺素的显著总体缺乏,而对硫磷则导致净增加。这些影响在处理后即刻(出生后第5天)并不明显,而是在发育过程中逐渐显现,这表明有机磷酸酯的影响代表了发育轨迹的改变,而不仅仅是初始损伤的持续。对β - 肾上腺素能受体没有类似影响,表明突触前变化并非对突触后受体信号传导潜在的主要影响的一种适应。因为我们使用了胆碱酯酶抑制基准,二嗪农的绝对剂量远高于对硫磷,因为后者是一种更强效的胆碱酯酶抑制剂。我们的结果与越来越多的证据一致,即各种有机磷酸酯对大脑发育的影响可能不同,因此,胆碱酯酶基准不足以预测不良的神经发育影响。