Department of Pharmacology and Cancer Biology, Duke University Medical Center, Durham, Box 3813 DUMC, Duke Univ. Med. Ctr., Durham, NC 27710, USA.
Brain Res. 2010 Feb 26;1316:1-16. doi: 10.1016/j.brainres.2009.12.025. Epub 2009 Dec 21.
Cell-signaling cascades are convergent targets for developmental neurotoxicity of otherwise unrelated agents. We compared organophosphates (chlorpyrifos, diazinon), an organochlorine (dieldrin) and a metal (Ni(2+)) for their effects on neuronotypic PC12 cells, assessing gene transcription involved in the cyclic AMP pathway. Each agent was introduced during neurodifferentiation at a concentration of 30 microM for 24 or 72 h and we assessed 69 genes encoding adenylyl cyclase isoforms and regulators, G-protein alpha-and beta,gamma-subunits, protein kinase A subtypes and the phosphodiesterase family. We found strong concordance among the four agents across all the gene families, with the strongest relationships for the G-proteins, followed by adenylyl cyclase, and lesser concordance for protein kinase A and phosphodiesterase. Superimposed on this pattern, chlorpyrifos and diazinon were surprisingly the least alike, whereas there was strong concordance of dieldrin and Ni(2+) with each other and with each individual organophosphate. Further, the effects of chlorpyrifos differed substantially depending on whether cells were undifferentiated or differentiating. To resolve the disparities between chlorpyrifos and diazinon, we performed analyses in rat brain regions after in vivo neonatal exposures; unlike the in vitro results, there was strong concordance. Our results show that unrelated developmental neurotoxicants can nevertheless produce similar outcomes by targeting cell signaling pathways involved in neurodifferentiation during a critical developmental period of vulnerability. Nevertheless, a full evaluation of concordance between different toxicants requires evaluations of in vitro systems that detect direct effects, as well as in vivo systems that allow for more complex interactions that converge on the same pathway.
细胞信号级联是不同来源的发育神经毒物的共同靶标。我们比较了有机磷(毒死蜱、二嗪农)、有机氯(狄氏剂)和金属(Ni(2+))对神经元型 PC12 细胞的影响,评估了参与环磷酸腺苷途径的基因转录。每种药物在神经分化期间以 30 μM 的浓度引入 24 或 72 小时,我们评估了 69 个基因,这些基因编码腺苷酸环化酶同工型和调节剂、G 蛋白 α、β、γ 亚基、蛋白激酶 A 亚型和磷酸二酯酶家族。我们发现,四种药物在所有基因家族中都具有很强的一致性,其中 G 蛋白的相关性最强,其次是腺苷酸环化酶,而蛋白激酶 A 和磷酸二酯酶的相关性较弱。在这种模式的基础上,毒死蜱和二嗪农出人意料地最不相似,而狄氏剂和 Ni(2+)彼此之间以及与每个有机磷化合物之间都有很强的一致性。此外,氯蜱的作用在细胞未分化或分化时存在显著差异。为了解决氯蜱和二嗪农之间的差异,我们在体内新生暴露后对大鼠脑区进行了分析;与体外结果不同,它们之间有很强的一致性。我们的结果表明,尽管不同的发育神经毒物具有不同的作用机制,但它们可以通过靶向参与神经分化的细胞信号通路,在易损性的关键发育时期产生相似的结果。然而,要全面评估不同毒物之间的一致性,需要评估检测直接作用的体外系统,以及允许更复杂相互作用集中在同一途径的体内系统。