Kristofco Lauren A, Du Bowen, Chambliss C Kevin, Berninger Jason P, Brooks Bryan W
Department of Environmental Science, Waco, Texas, USA.
AAPS J. 2015 Jan;17(1):175-83. doi: 10.1208/s12248-014-9677-5. Epub 2014 Oct 18.
Pharmaceuticals and other contaminants of emerging concern present unique challenges to environmental risk assessment and management. Fortunately, mammalian pharmacology and toxicology safety data are more readily available for pharmaceuticals than other environmental contaminants. Identifying approaches to read-across such pharmaceutical safety information to non-target species represents a major research need to assess environmental hazards. Here, we tested a biological read-across hypothesis from emergency medicine with common aquatic invertebrate and vertebrate models. In mammals, the antihistamine diphenhydramine (DPH) confers protection from poisoning by acetylcholinesterase inhibition because DPH blocks the acetylcholine receptor. We employed standardized toxicity methods to examine individual and mixture toxicity of DPH and the acetylcholinesterase inhibitor diazinon (DZN) in Daphnia magna (an invertebrate) and Danio rerio (zebrafish, a vertebrate). Though the standardized Fish Embryo Toxicity method evaluates early life stage toxicity of zebrafish (0-3 days post fertilization, dpf), we further evaluated DPH, DZN, and their equipotent mixture during three development stages (0-3, 3-6, 7-10 dpf) in zebrafish embryos. Independent action and concentration addition mixture models and fish plasma modeling were used to assist interpretation of mixture toxicity experiments. Though our primary hypothesis was not confirmed in acute studies with Daphnia magna, DPH conferred a protective effect for acute DZN toxicity to zebrafish when DPH plasma levels were expected to be greater than mammalian therapeutic, but lower than acutely lethal, internal doses. We further observed that timing of developmental exposure influenced the magnitude of DZN and DPH toxicity to zebrafish, which suggests that future zebrafish toxicity studies with pharmaceuticals and pesticides should examine exposure during developmental stages.
新型药物及其他受到关注的污染物给环境风险评估与管理带来了独特挑战。幸运的是,与其他环境污染物相比,有关药物的哺乳动物药理学和毒理学安全数据更容易获取。确定将此类药物安全信息外推至非目标物种的方法是评估环境危害的一项重大研究需求。在此,我们用常见的水生无脊椎动物和脊椎动物模型检验了来自急诊医学的生物外推假说。在哺乳动物中,抗组胺药苯海拉明(DPH)可防止因乙酰胆碱酯酶抑制而中毒,因为DPH会阻断乙酰胆碱受体。我们采用标准化毒性方法,研究了DPH和乙酰胆碱酯酶抑制剂二嗪农(DZN)对大型溞(一种无脊椎动物)和斑马鱼(一种脊椎动物)的单一及混合毒性。尽管标准化的鱼类胚胎毒性方法评估斑马鱼的早期生命阶段毒性(受精后0 - 3天,dpf),但我们进一步评估了DPH、DZN及其等效混合物在斑马鱼胚胎的三个发育阶段(0 - 3、3 - 6、7 - 10 dpf)的情况。使用独立作用和浓度相加混合物模型以及鱼血浆模型来辅助解释混合物毒性实验。尽管我们的主要假说在大型溞的急性研究中未得到证实,但当DPH血浆水平预计高于哺乳动物治疗剂量但低于急性致死内部剂量时,DPH对斑马鱼急性DZN毒性具有保护作用。我们还进一步观察到发育暴露的时间会影响DZN和DPH对斑马鱼毒性的程度,这表明未来针对药物和农药的斑马鱼毒性研究应考察发育阶段的暴露情况。