Synthesis of Esters Containing Cinnamoyl Motif with Potential Larvicide Action: A Computational, Ecotoxicity and in Vitro Cytotoxicity Assessments

An increasing morbidity and mortality rate has been related to arboviruses transmitted by Aedes aegypti. Compounds with cinnamoyl moiety represent an alternative against mosquitos, considering their larvicidal activity. This study aimed to assess the larvicidal activity of cinnamic ester derivates a...

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Published in:Chemistry & biodiversity 2022-11, Vol.19 (11), p.e202200256-n/a
Main Authors: Santos Correia, Paulo Ricardo, Carvalho, Cenira Monteiro, Silva Cunha, Cristhyan Rychard, Silva, Rafael Antonio Santos, Oliveira Lima, Monaly, França, Saraliny Bezerra, Oliveira Barreto, Emiliano, Tonholo, Josealdo, Paz Lima, Dimas José
Format: Article
Language:English
Subjects:
Acetylcholinesterase
Aedes aegypti
Artemia
Bioassays
biological activity
Cell viability
cinnamic derivatives
Computer applications
Cytotoxicity
ecotoxicity
Esters
Germination
Hydrogen bonds
hydrolase
Larvae
Larvicides
medicinal chemistry
Molecular docking
Morbidity
Mosquitoes
Phytotoxicity
Root development
Thorax
Toxicity
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Summary:An increasing morbidity and mortality rate has been related to arboviruses transmitted by Aedes aegypti. Compounds with cinnamoyl moiety represent an alternative against mosquitos, considering their larvicidal activity. This study aimed to assess the larvicidal activity of cinnamic ester derivates against Aedes aegypti larvae, along with evaluating their toxicity effect to assess its safety as a larvicide. Ethyl cinnamate demonstrated larvicidal activity (LC50=48.59 μg/mL). Morphological changes in larvae were detected, as a degenerative response in the thorax. Through molecular docking, the molecular binding mode between 3b, 3c, and acetylcholinesterase showed strong hydrogen bond interactions. Preliminary in vitro cell viability revealed the non‐cytotoxicity of 3c. Ecotoxicity results indicated a sensitivity of Artemia salina to cinnamic esters. The phytotoxicity bioassays show potential for cinnamic compounds to enhance germination and root development. These findings suggest that compound 3c is more suitable as a larvicide since it demonstrated low toxicity.
ISSN:1612-1872
1612-1880
DOI:10.1002/cbdv.202200256