Quistad_2006_Toxicol.Sci_91_166

Reference

Title : Each lipase has a unique sensitivity profile for organophosphorus inhibitors - Quistad_2006_Toxicol.Sci_91_166
Author(s) : Quistad GB , Liang SN , Fisher KJ , Nomura DK , Casida JE
Ref : Toxicol Sci , 91 :166 , 2006
Abstract : Lipases sensitive to organophosphorus (OP) inhibitors play critical roles in cell regulation, nutrition, and disease, but little is known on the toxicological aspects in mammals. To help fill this gap, six lipases or lipase-like proteins are assayed for OP sensitivity in vitro under standard conditions (25 degrees C, 15 min incubation). Postheparin serum lipase, lipoprotein lipase (LPL) (two sources), pancreatic lipase, monoacylglycerol (MAG) lipase, cholesterol esterase, and KIAA1363 are considered with 32 OP pesticides and related compounds. Postheparin lipolytic activity in rat serum is inhibited by 14 OPs, including chlorpyrifos oxon (IC50 50-97 nM). LPL (bovine milk and Pseudomonas) generally is less inhibited by the insecticides or activated oxons, but the milk enzyme is very sensitive to six fluorophosphonates and benzodioxaphosphorin oxides (IC50 7-20 nM). Porcine pancreatic lipase is very sensitive to dioctyl 4-nitrophenyl phosphate (IC50 8 nM), MAG lipase of mouse brain to O-4-nitrophenyl methyldodecylphosphinate (IC50 0.6 nM), and cholesterol esterase (bovine pancreas) to all of the classes of OPs tested (IC50 < 10 nM for 17 compounds). KIAA1363 is sensitive to numerous OPs, including two O-4-nitrophenyl compounds (IC50 3-4 nM). In an overview, inhibition of 28 serine hydrolases (including lipases) by eight OPs (chlorpyrifos oxon, diazoxon, paraoxon, dichlorvos, and four nonpesticides) showed that brain acetylcholinesterase is usually less sensitive than butyrylcholinesterase, liver esterase, cholesterol esterase, and KIAA1363. In general, each lipase (like each serine hydrolase) has a different spectrum of OP sensitivity, and individual OPs have unique ranking of potency for inhibition of serine hydrolases.
ESTHER : Quistad_2006_Toxicol.Sci_91_166
PubMedSearch : Quistad_2006_Toxicol.Sci_91_166
PubMedID: 16449251

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Citations formats

Quistad GB, Liang SN, Fisher KJ, Nomura DK, Casida JE (2006)
Each lipase has a unique sensitivity profile for organophosphorus inhibitors
Toxicol Sci 91 :166

Quistad GB, Liang SN, Fisher KJ, Nomura DK, Casida JE (2006)
Toxicol Sci 91 :166