Evaluation of the inhibitory effect of abamectin on mammalian butyrylcholinesterase: Enzyme kinetic and molecular docking studies.
J Environ Sci Health B
; 53(11): 713-718, 2018.
Article
em En
| MEDLINE
| ID: mdl-29883250
ABSTRACT
Abamectin, a blend of the natural avermectins B1a and B1b, is a widely-used insecticide/miticide with relatively low toxicity to mammals. Exposure to high doses of it, however, leads to cholinergic-like neurotoxic effects. Butyrylcholinesterase, which is best known for its abundant presence in plasma, is a serine hydrolase loosely coupled with the cholinergic system. It protects and supports the neurotransmitter function of its sister enzyme acetylcholinesterase. Here, using experimental and computational studies, we provide evidence demonstrating that abamectin is a potent (IC50 = 10.6 µM; Ki = 2.26 ± 0.35 µM) inhibitor of horse serum butyrylcholinesterase and that it interacts with the enzyme in a reversible, competitive manner predictively to block the mouth of the active-site gorge of the enzyme and to bind to several critical residues that normally bind/hydrolyze choline esters.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Ivermectina
/
Butirilcolinesterase
/
Inibidores da Colinesterase
/
Inseticidas
Limite:
Animals
Idioma:
En
Revista:
J Environ Sci Health B
Ano de publicação:
2018
Tipo de documento:
Article
País de afiliação:
Turquia