Preclinical safety assessment in rats after dermal exposure to acetylcarvacrol, a potential acaricide against the brown dog tick.

Q1 Environmental Science
Toxicology Reports Pub Date : 2024-11-26 eCollection Date: 2024-12-01 DOI:10.1016/j.toxrep.2024.101834
Graziela Hermínia Andrade Mendonça, Aline Chaves Reis, Isaac Filipe Moreira Konig, Gabriela Pereira Brito, José Henrique Silva Rodrigues, Camila Souza de Oliveira Guimarães, Vitor Luís Tenório Mati, Rafael Neodini Remedio
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Abstract

Carvacrol, a phenolic monoterpene found in essential oils of plants of the Lamiaceae family, emerges as an alternative acaricide of plant origin. Its acetylation was proposed to obtain a derivative compound with a better pharmacological profile and lower toxicity to non-target organisms. The present study aimed to assess the preclinical safety of acetylcarvacrol after dermal application in Wistar rats, through the examination of hematological and biochemical parameters, as well as histopathological analysis of the skin, liver and kidney. For this, twenty rats were distributed into four groups with five animals each. Three groups received treatment with different concentrations of the substance (26, 52, and 104 µL/mL) based on the lethal concentration for Rhipicephalus sanguineus ticks, and one group (Control) received only the vehicle. Acetylcarvacrol was applied daily to a trichotomized skin area for 21 days. No changes in hematological parameters were observed. Regarding biochemical analysis, a slight increase in urea and alanine transaminase levels was noted. No significant changes were observed in the kidney and liver, although the rats had developed cumulative irritant contact dermatitis at the application site, as corroborated by the histopathological analysis of the skin. In general, the results showed that the dermal application of acetylcarvacrol in the experimental conditions described here is safe. However, it can cause signs of mild systemic toxicity and skin irritation at high concentrations, suggesting that this product should be used in lower therapeutic doses and that the development of less aggressive formulations, including the combination with other acaricides, is desirable.

对大鼠皮肤接触乙酰香芹酚(一种潜在的棕色狗蜱杀螨剂)后的临床前安全性进行评估。
香芹酚(Carvacrol)是一种存在于Lamiaceae家族植物精油中的酚类单萜,是一种植物源的替代性杀螨剂。它的乙酰化是为了获得一种具有更好药理特征和对非靶生物毒性较低的衍生物。本研究旨在通过对Wistar大鼠的血液学和生化指标的检查,以及皮肤、肝脏和肾脏的组织病理学分析,评估乙酰香芹醇真皮应用后的临床前安全性。为此,将20只大鼠分成四组,每组5只。三组根据血根头蜱致死浓度分别给予不同浓度的物质(26、52和104 µL/mL)处理,另一组(对照组)仅给予载药。每日将乙酰香芹酚涂抹于三分皮肤区域,持续21天。血液学参数未见变化。在生化分析方面,尿素和丙氨酸转氨酶水平略有升高。肾脏和肝脏没有观察到明显的变化,尽管大鼠在应用部位出现了累积性刺激性接触性皮炎,皮肤的组织病理学分析证实了这一点。总的来说,结果表明,在实验条件下,乙酰香芹酚的皮肤应用是安全的。然而,高浓度时可引起轻度全身毒性和皮肤刺激的迹象,这表明该产品应以较低的治疗剂量使用,并应开发不那么具有攻击性的配方,包括与其他杀螨剂联合使用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Toxicology Reports
Toxicology Reports Environmental Science-Health, Toxicology and Mutagenesis
CiteScore
7.60
自引率
0.00%
发文量
228
审稿时长
11 weeks
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