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肉桂酸衍生物的杀幼虫活性:探索替代产品控制 L.

Larvicidal Activity of Cinnamic Acid Derivatives: Investigating Alternative Products for L. Control.

机构信息

Post Graduation Program in Natural and Synthetic Bioactive Products, Federal University of Paraíba, João Pessoa 58051-900, Brazil.

Bio-Cheminformatics Research Group and Escuela de Ciencias Físicas y Matemáticas, Universidad de Las Américas, Quito 170125, Ecuador.

出版信息

Molecules. 2020 Dec 24;26(1):61. doi: 10.3390/molecules26010061.

Abstract

The mosquito transmits the virus that causes dengue, yellow fever, Zika and Chikungunya viruses, and in several regions of the planet represents a vector of great clinical importance. In terms of mortality and morbidity, infections caused by are among the most serious arthropod transmitted viral diseases. The present study investigated the larvicidal potential of seventeen cinnamic acid derivatives against fourth stage larvae. The larvicide assays were performed using larval mortality rates to determine lethal concentration (LC). Compounds containing the medium alkyl chains butyl cinnamate () and pentyl cinnamate () presented excellent larvicidal activity with LC values of around 0.21-0.17 mM, respectively. While among the derivatives with aryl substituents, the best LC result was 0.55 mM for benzyl cinnamate (). The tested derivatives were natural compounds and in pharmacology and antiparasitic studies, many have been evaluated using biological models for environmental and toxicological safety. Molecular modeling analyses suggest that the larvicidal activity of these compounds might be due to a multi-target mechanism of action involving inhibition of a carbonic anhydrase (CA), a histone deacetylase (HDAC2), and two sodium-dependent cation-chloride co-transporters (CCC2 e CCC3).

摘要

蚊子传播导致登革热、黄热病、寨卡病毒和基孔肯雅热的病毒,在全球的几个地区,它是一种具有重要临床意义的传播媒介。就死亡率和发病率而言,由引起的感染是最严重的节肢动物传播的病毒性疾病之一。本研究调查了十七种肉桂酸衍生物对第四龄幼虫的杀幼虫潜力。使用幼虫死亡率进行幼虫毒力测定来确定致死浓度 (LC)。含有中链烷基的化合物丁基肉桂酸 () 和戊基肉桂酸 () 表现出优异的杀幼虫活性,LC 值约为 0.21-0.17 mM。而在具有芳基取代基的衍生物中,苄基肉桂酸 () 的最佳 LC 值为 0.55 mM。测试的衍生物是天然化合物,在药理学和寄生虫学研究中,许多化合物已经使用生物模型进行了环境和毒理学安全性评估。分子建模分析表明,这些化合物的杀幼虫活性可能是由于多靶作用机制,涉及抑制碳酸酐酶 (CA)、组蛋白去乙酰化酶 (HDAC2) 和两种钠依赖性阳离子-氯离子共转运体 (CCC2 和 CCC3)。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9edf/7796249/b5ef6054ebf2/molecules-26-00061-sch001.jpg

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