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香芹酚、百里香酚、丁香酚及其乙酰化衍生物对微小牛蜱(蜱螨目:硬蜱科)杀螨活性的体外评估

In vitro assessment of the acaricidal activity of carvacrol, thymol, eugenol and their acetylated derivatives on Rhipicephalus microplus (Acari: Ixodidae).

作者信息

Novato Tatiane, Gomes Geovany Amorim, Zeringóta Viviane, Franco Cristiane Teixeira, de Oliveira Débora Ramos, Melo Diego, de Carvalho Mário Geraldo, Daemon Erik, de Oliveira Monteiro Caio Márcio

机构信息

Programa de Pós-graduação em Ciências Veterinárias, Universidade Federal Rural do Rio de Janeiro (UFRRJ), 23.890-000, Seropédica, RJ, Brazil.

Centro de Ciências Exatas e Tecnologia, Universidade Estadual Vale do Acaraú, 62040-730, Sobral, Ceará, Brazil.

出版信息

Vet Parasitol. 2018 Aug 30;260:1-4. doi: 10.1016/j.vetpar.2018.07.009. Epub 2018 Jul 18.

Abstract

This study reports the comparative evaluation of the activity of carvacrol, thymol, eugenol and their respective acetylated derivatives (carvacrol acetate, thymol acetate and eugenol acetate) on Rhipicephalus microplus, to verify the possible influence of the acetate group. The acetylated derivatives were prepared from reactions of the phenolic compounds with acetic anhydride/pyridine. The formation of the products was confirmed by analysis of hydrogen and carbon-13 nuclear magnetic resonance (H and C NMR) spectra. The larval packet test was used to evaluate the acaricidal activity, with concentrations of 0.312, 0.625, 1.25, 2.5, 5.0, 7.5, 10.0 and 15.0 mg/mL. Thymol and carvacrol resulted in 100% mortality starting at the concentration of 2.5 mg/mL, while the same was observed for carvacrol acetate starting at the concentration of 5.0 mg/mL. For the other treatments, 100% mortality was only achieved in the groups treated with the highest concentration (15.0 mg/mL). The LC and LC values (mg/mL) of carvacrol acetate (2.49, 4.21), thymol acetate (2.97, 8.52) and eugenol acetate (4.25, 13.10) were higher than those for the corresponding precursor molecules carvacrol (0.83, 2.02), thymol (1.26, 2.21) and eugenol (2.77, 5.35). The acetylation process did not enhance the activity of these substances on unengorged larvae of R. microplus, since the precursor substances (carvacrol, thymol and eugenol) had greater efficacy.

摘要

本研究报告了香芹酚、百里香酚、丁香酚及其各自的乙酰化衍生物(乙酸香芹酯、乙酸百里香酯和乙酸丁香酯)对微小牛蜱的活性比较评估,以验证乙酰基的可能影响。乙酰化衍生物由酚类化合物与乙酸酐/吡啶反应制备。通过氢和碳-13核磁共振(H和C NMR)光谱分析确认产物的形成。采用幼虫包囊试验评估杀螨活性,浓度为0.312、0.625、1.25、2.5、5.0、7.5、10.0和15.0毫克/毫升。百里香酚和香芹酚从2.5毫克/毫升的浓度开始导致100%的死亡率,而乙酸香芹酯从5.0毫克/毫升的浓度开始也观察到相同情况。对于其他处理,仅在最高浓度(15.0毫克/毫升)处理的组中实现了100%的死亡率。乙酸香芹酯(2.49,4.21)、乙酸百里香酯(2.97,8.52)和乙酸丁香酯(4.25,13.10)的LC和LC值(毫克/毫升)高于相应的前体分子香芹酚(0.83,2.02)、百里香酚(1.26,2.21)和丁香酚(2.77,5.35)。乙酰化过程并未增强这些物质对微小牛蜱未饱食幼虫的活性,因为前体物质(香芹酚、百里香酚和丁香酚)具有更高的效力。

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