Evaluation of the inhibitory effect of abamectin on mammalian butyrylcholinesterase: Enzyme kinetic and molecular docking studies

Abstract

Abamectin, a blend of the natural avermectins B and B, 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 (IC = 10.6 μM; K = 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.

Comparative toxicity of abamectin and nano-derived form on land snail, Helix aspersa in attributing to cytotoxicity and biochemical alterations

“…On the other hand, exposure to high doses of it led to cholinergic-like neurotoxic effects. In fact, use of experimental and computational studies proved evidence that, ABM is a potent (IC50=10.6 µM) inhibitor of horse serum butyryl cholinesterase (BuChE) and interacted 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 [52].…”

Morphological, Histological Changes and Acetyl Cholinesterase Activity in Chicken Embryos After Exposure to Abamectin Insecticide

“…Alhifi (2018) observed a decrease in the percentage inhibition of Ach E to 40.6% and 69% in brain tissue of chick embryo Gallus gallus treated with mixed insecticide (dimethoate 30% + methidathion 40%) at dose 4, 8 ppm, respectively. Pesticides interfere with physiological chemical processes and leading to morphological changes (Teralı et al, 2018;Uggini et al, 2012;Legradi et al, 2018;Hernandez et al, 2020).…”

“…Figure1: showing chemical structure of Abamectin: Abamectin as structure consists of natural avermectins B1a and B1b. B1a compounds of ethyl group while B1b has a methyl group attached in the ring (Teralı et al 2018).…”