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水鼠管理——抗凝血灭鼠剂的立体化学能否减轻与其使用相关的生态毒性问题?

Water vole management - Could anticoagulant rodenticides stereochemistry mitigate the ecotoxicity issues associated to their use?

机构信息

USC 1233 RS2GP, INRAE, VetAgro Sup, University of Lyon, F-69280 Marcy l'Etoile, France.

USC 1233 RS2GP, INRAE, VetAgro Sup, University of Lyon, F-69280 Marcy l'Etoile, France.

出版信息

Environ Toxicol Pharmacol. 2021 Jan;81:103536. doi: 10.1016/j.etap.2020.103536. Epub 2020 Oct 29.

DOI:10.1016/j.etap.2020.103536
PMID:33130091
Abstract

Cyclic water vole population explosions can be controlled in some European countries with anticoagulant rodenticides leading sometimes to wildlife poisonings due to the toxin's tissue persistence. Here, we analyzed the pharmacokinetics of rodenticide residues in voles and we explored potential ways of improving the mass application of these agents based on the concept of stereoisomers. We demonstrated the dramatic persistence of bromadiolone in vole tissues with a hepatic half-life of about 10-30 days, while the tissue persistence of chlorophacinone is rather short with a hepatic half-life of about one day. The dramatic persistence of bromadiolone is due to the trans-isomer group (the major compound in bromadiolone), while the cis-isomer group has a short half-life. Because of resistance to chlorophacinone, the cis-bromadiolone isomers may constitute an excellent compromise between efficacy and ecotoxicological risk to control voles. A mathematical model is proposed to favor the development of baits mixed with cis-isomer groups.

摘要

周期性水鼠种群爆发在一些欧洲国家可以通过抗凝血灭鼠剂得到控制,但有时由于毒素在组织中的持久性,会导致野生动物中毒。在这里,我们分析了灭鼠剂在水鼠体内的药代动力学,并基于立体异构体的概念探索了改善这些药剂大量应用的潜在方法。我们证明了溴敌隆在肝半衰期约为 10-30 天的水鼠组织中具有明显的持久性,而氯鼠酮的组织持久性相当短,肝半衰期约为一天。溴敌隆的显著持久性归因于反式异构体组(溴敌隆中的主要化合物),而顺式异构体组的半衰期较短。由于对氯鼠酮的抗性,顺式溴敌隆异构体可能是控制水鼠的功效和生态毒理学风险之间的一个极好的折衷方案。提出了一个数学模型来促进混合顺式异构体组的诱饵的开发。

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