An In Vitro Larval Immersion Microassay for Identifying and Characterizing Candidate Acaricides
An In Vitro Larval Immersion Microassay for Identifying and Characterizing Candidate Acaricides
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用于识别和表征候选杀螨剂的体外幼虫浸入微量测定法
DOI：
10.1603/0022-2585-41.6.1034
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发表时间：
2004
影响因子：
2.1
通讯作者：
Jesus A. Gutierrez
中科院分区：
文献类型：
--
作者：
W. Hunter White;Philip R. Plummer;Connie J. Kemper;Robert J. Miller;Ronald B. Davey;David H. Kemp;S. Hughes;Charles K. Smith;Jesus A. Gutierrez
我们优化了一种幼虫浸泡微测定法（LIM），该方法具有卓越的灵敏度，适应多种配方的灵活性，以及快速筛选多种化合物的强大能力，并且对评估的测试品要求最少。对有机磷、拟除虫菊酯、吡唑、氨基甲酸酯、大环内酯和甲脒等化学物质的代表性成分进行了剂量反应研究。时间响应试验表明，氯菊酯对美洲斑蝽的杀灭速度最快，氟虫腈对美洲斑蝽的杀灭速度最慢。多种蜱的药敏谱比较表明，美洲蜱是预测复合药效的有效模型。LIM适用于从中小型化合物或天然产物文库中识别和表征活性分子，它可以是一个有用的工具来确定分子的优先级，以进一步在动物模型中进行体内测试。
Abstract We have optimized a larval immersion microassay (LIM) that offers superior sensitivity, flexibility to accommodate multiple formulations, and a robust capability for rapidly screening many compounds with a minimal requirement of test article for evaluation. Dose–response studies were conducted for representative members from the organophosphate, pyrethroid, pyrazole, carbamate, macrocyclic lactone, and formamidine chemistries against Amblyomma americanum (L.). Time–response experiments revealed that permethrin was the most rapid acting, whereas fipronil had the slowest speed-of-kill against A. americanum. Comparison of drug susceptibility profiles between multiple ixodid ticks suggests that A. americanum is an effective model for predicting compound potency against Boophilus spp. in this bioassay. The LIM is suitable for the identification and characterization of active molecules from small- and medium-sized compound or natural product libraries, and it can be a useful tool to prioritize molecules for further in vivo testing in animal models.