title: Malathion, carbofuran and paraquat inhibit Bungarus sindanus (krait) venom acetylcholinesterase and human serum butyrylcholinesterase in vitro.
abstract: Carbofuran and malathion, well known pesticides, and paraquat, a world widely used herbicide, were tested on acetylcholinesterase (AChE) from Bungarus sindanus venom and butyrylcholinesterase (BChE) from human serum. The calculated IC(50 )values for inhibition of venom enzyme by malathion, carbofuran and paraquat were 2.5, 0.14, and 0.16 microM, respectively. The values for inhibition of serum butyrylcholinesterase (BChE) were 3.5, 0.09 and 0.18 microM, respectively. Analysis of kinetic data indicated that the inhibition caused by malathion, carbofuran and paraquat was mixed for venom AChE. For BChE from human serum, the inhibition caused by malathion and paraquat was mixed and for carbofuran it was uncompetitive. The present results suggest a commercial paraquat preparation (a popular herbicide) inhibits cholinesterases with similar or higher potency than classical pesticide inhibitors. Furthermore, this inhibition was observed both in human serum and snake venom, a newly studied source of AChE.
authors.affiliation: Departmento de Química, Centro de Ciências Naturais e Exatas, Universidade Federal de Santa Maria, Santa Maria, RS, Brazil.
authors.forename: Mushtaq
authors.initials: M
authors.lastname: Ahmed
authors.forename: João Batista T
authors.initials: JB
authors.lastname: Rocha
authors.forename: Cinthia M
authors.initials: CM
authors.lastname: Mazzanti
authors.forename: André L B
authors.initials: AL
authors.lastname: Morsch
authors.forename: Denise
authors.initials: D
authors.lastname: Cargnelutti
authors.forename: Maísa
authors.initials: M
authors.lastname: Corrêa
authors.forename: Vânia
authors.initials: V
authors.lastname: Loro
authors.forename: Vera Maria
authors.initials: VM
authors.lastname: Morsch
authors.forename: Maria R C
authors.initials: MR
authors.lastname: Schetinger
mesh_terms: D000110:Acetylcholinesterase / Q000737:chemistry / Q000187:drug effects*; D000328:Adult; D000818:Animals; D017838:Bungarus; D002091:Butyrylcholinesterase / Q000737:chemistry / Q000187:drug effects*; D002235:Carbofuran / Q000494:pharmacology; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D006540:Herbicides / Q000494:pharmacology; D006801:Humans; D007306:Insecticides / Q000494:pharmacology; D007700:Kinetics; D008294:Malathion / Q000494:pharmacology; D010269:Paraquat / Q000494:pharmacology; D044967:Serum / Q000201:enzymology*; D012910:Snake Venoms / Q000201:enzymology*
chemical_list: D002800:Cholinesterase Inhibitors; D006540:Herbicides; D007306:Insecticides; D012910:Snake Venoms; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase; D010269:Paraquat; D002235:Carbofuran; D008294:Malathion