Division of Toxicology, Office of Applied Research and Safety Assessment, Center for Food Safety and Applied Nutrition, U.S. Food and Drug Administration, Laurel, MD, USA.
Division of Toxicology, Office of Applied Research and Safety Assessment, Center for Food Safety and Applied Nutrition, U.S. Food and Drug Administration, Laurel, MD, USA.
Toxicol Appl Pharmacol. 2024 Nov;492:117108. doi: 10.1016/j.taap.2024.117108. Epub 2024 Sep 23.
The worm Development and Activity Test (wDAT) measures C. elegans developmental milestone acquisition timing and stage-specific spontaneous locomotor activity (SLA). Previously, the wDAT identified developmental delays and SLA level changes in C. elegans with mammalian developmental toxicants arsenic, lead, and mercury. 5-fluorouracil (5FU), cyclophosphamide (CP), hydroxyurea (HU), and ribavirin (RV) are teratogens that also induce growth retardation in developing mammals. In at least some studies on each of these chemicals, fetal weight reductions were seen at mammalian exposures below those that had teratogenic effects, suggesting that screening for developmental delay in a small alternative whole-animal model could act as a general toxicity endpoint to identify chemicals for further testing for more specific adverse developmental outcomes. Consistent with mammalian developmental effects, 5FU, HU, and RV were associated with developmental delays with the wDAT. Exposures associated with developmental delay induced hypoactivity with 5FU and HU, but slight hyperactivity with RV. CP is a prodrug that requires bioactivation by cytochrome P450s for both therapeutic and toxic effects. CP tests as a false negative in several in vitro assays, and it was also a false negative with the wDAT. These results suggest that the wDAT has the potential to identify some developmental toxicants, and that a positive wDAT result with an unknown may warrant further testing in mammals. Further assessment with larger panels of positive and negative controls will help qualify the applicability and utility of this C. elegans wDAT assay within toxicity test batteries or weight of evidence approaches for developmental toxicity assessment.
线虫发育和活动测试 (wDAT) 可测量秀丽隐杆线虫获得发育里程碑的时间和特定阶段的自发运动活动 (SLA)。以前,wDAT 已经在受到哺乳动物发育毒物砷、铅和汞影响的秀丽隐杆线虫中识别出发育迟缓以及 SLA 水平变化。5-氟尿嘧啶 (5FU)、环磷酰胺 (CP)、羟基脲 (HU) 和利巴韦林 (RV) 是致畸剂,也会导致发育中的哺乳动物生长迟缓。在这些化学物质的至少一些研究中,在哺乳动物暴露于低于具有致畸作用的水平时,胎儿体重减轻,这表明在小型替代全动物模型中筛选发育迟缓可以作为一般毒性终点,以识别出需要进一步测试以获得更具体的不良发育结果的化学物质。与哺乳动物发育效应一致,5FU、HU 和 RV 与 wDAT 中的发育迟缓有关。与发育迟缓相关的暴露会导致 5FU 和 HU 引起活动减少,而 RV 则引起轻微的活动增加。CP 是一种前药,需要细胞色素 P450 生物激活才能发挥治疗和毒性作用。CP 在几种体外测定中表现为假阴性,并且在 wDAT 中也是假阴性。这些结果表明,wDAT 有可能识别出一些发育毒物,并且对于未知物的阳性 wDAT 结果可能需要在哺乳动物中进一步测试。进一步使用更大的阳性和阴性对照面板将有助于确定这种秀丽隐杆线虫 wDAT 测定在毒性测试组合或发育毒性评估的证据权重方法中的适用性和实用性。