Larvicidal activity and in silico studies of cinnamic acid derivatives against Aedes aegypti (Diptera: Culicidae)
| Autor: | Edeildo Ferreira da Silva-Júnior, Saraliny Bezerra França, Cristhyan Rychard da Silva Cunha, Maria Ester de Sá Barreto Barros, Daniela S. Anunciação, Dimas J. P. Lima, Luana Carine Barros de Lima |
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| Rok vydání: | 2021 |
| Předmět: |
Clinical Biochemistry
Pharmaceutical Science Aedes aegypti 01 natural sciences Biochemistry Cinnamic acid chemistry.chemical_compound Structure-Activity Relationship Aedes Drug Discovery Cinnamates Animals Molecular Biology Larvicide chemistry.chemical_classification biology Dose-Response Relationship Drug Molecular Structure 010405 organic chemistry fungi Organic Chemistry biology.organism_classification Antimicrobial Acetylcholinesterase In vitro 0104 chemical sciences 010404 medicinal & biomolecular chemistry Enzyme chemistry Larva Molecular Medicine |
| Zdroj: | Bioorganicmedicinal chemistry. 44 |
| ISSN: | 1464-3391 |
| Popis: | Cinnamic acid derivatives (CAD's) represent a great alternative in the search for insecticides against Aedes aegypti mosquitoes since they have antimicrobial and insecticide properties. Ae. aegypti is responsible for transmitting Dengue, Chikungunya, and Zika viruses, among other arboviruses associated with morbimortality, especially in developing countries. In view of this, in vitro analyses of n-substituted cinnamic acids and esters were performed upon 4th instar larvae (L4) of Ae. aegypti, as well as, molecular docking studies to propose a potential biological target towards this mosquitoes species. The larvicide assays proved that n-substituted ethyl cinnamates showed a more pronounced activity than their corresponding acids, in which p-chlorocinnamate (3j) presented a LC50 value of 8.3 µg/mL. Thusly, external morphologic alterations (rigid and elongated body, curved bowel, and translucent or darkened anal papillae) of mosquitoes’ group exposed to compound 3j, were observed by microscopy. In addition, an analytical method was developed for the quantification of the most promising analog by using high-performance liquid chromatography with UV detection (HPLC-UV). Molecular docking studies suggested that the larvicide action is associated with inhibition of acetylcholinesterase (AChE) enzyme. Therefore, expanding the larvicidal study with the cinnamic acid derivatives against the vector Ae. aegypti is important for finding search for more effective larvicides and with lower toxicity, since they have already shown good larvicidal properties against Ae. aegypti. |
| Databáze: | OpenAIRE |
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