The antienzymic activities of 14 organophosphorous compounds, the derivatives of dialkyl thiophosphoric acid, towards the acetylcholinesterase (AChE), butyrylcholinesterase (BuChE) and carboxylesterase (CE) from the spring grain aphid and mammals were investigated. The dependence of inhibitory activity of the compounds on their alkyl radical length was shown to be different for the AchE from the aphid and man. Some less pronounced differences in this dependence were revealed between the BuChEs from the aphid and horse as well as between the CEs from the aphid, mouse and red spider mite. The data give evidence of a distinction in structure of the active surfaces of the enzymes from the aphid and mammals. Some peculiar properties of the aphid cholinesterases are discussed taking account of the results of the present and previous papers.
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Molecules
August 2023
Food Safety Division, ICMR-National Institute of Nutrition, Hyderabad 500007, Telangana, India.
To monitor human exposure to pesticides, experts commonly measure their metabolites in urine, particularly dialkyl phosphates (DAPs), which include diethyl phosphate (DEP), Diethyl thiophosphate (DETP), diethyl dithiophosphate (DEDTP), dimethyl phosphate (DMP), dimethyl thiophosphate (DMTP) and dimethyl dithiophosphate (DMDTP)to monitor the metabolites of organophosphates. These DAP metabolites are a urinary biomarker for assessing pesticide exposure and potential health risks. This study presented a new screening method combining ultrafast liquid chromatography with tandem mass spectrometry (UFLC-MS/MS) to detect six DAP metabolites in human urine.
View Article and Find Full Text PDFPLoS One
October 2014
School of Medicine, Shanghai JiaoTong University, Shanghai, China.
Background: A large amount of organophosphate pesticides (OPs) are used in agriculture in China every year, contributing to exposure of OPs through dietary consumption among the general population. However, the level of exposure to OPs in China is still uncertain.
Objective: To investigate the effect of the exposure to OPs on the neonatal neurodevelopment during pregnancy in Shenyang, China.
Eur J Med Chem
December 2011
Lauras, Gaustadalléen 21, N-0349 Oslo, Norway.
N(6)-Monoalkylated, N(6)-dialkylated and N(6)-acylated (R(P))-adenosine 3',5'-cyclic phosphorothioic acids have been prepared by stereoselective syntheses from cAMP for a study of protein kinase A antagonist activity. The antagonist activity of the parent primary 6-amino cAMP derivative was reduced after N-monoalkylation. No significant activity was detected in the N,N-dialkylated derivative.
View Article and Find Full Text PDFOrg Biomol Chem
July 2011
Institute of Organic Chemistry, University of Vienna, Währingerstrasse 38, A-1090, Wien, Austria.
S-Alkyl O,O-dialkyl thiophosphates are prepared by alkylation of the triethylammonium salt of O,O-diisopropyl thiophosphoric acid. S-Benzyl thiophosphate was metallated at temperatures of ≥-45 °C by trityllithium and LiTMP (lithium 2,2,6,6-tetramethylpiperidide) and S-alkyl thiophosphates only by LiTMP to give dipole-stabilised carbanions which rearrange to α-mercaptophosphonates in yields of up to 45%. Metallation occurs with a high primary kinetic isotope effect (k(H)/k(D) up to ≈50).
View Article and Find Full Text PDFHum Exp Toxicol
March 2012
Centre of Toxicology Sciences and Research, Division of Morphology, Medical School, University of Crete, Voutes, Heraklion, Crete, Greece.
In the present paper, the possibility to use dialkyl phosphate metabolites (DAPs) hair segmental analysis as a biomarker of past acute exposure to organophosphates is examined. Hair samples of four acute poisoning survivors were collected and segmental hair analysis was performed. The total hair samples were divided to 1 cm segments and analysed by gas chromatography-mass spectrometry (GC-MS) for the presence of four DAP metabolites, dimethyl phosphate (DMP), diethyl phosphate (DEP), diethyl thiophosphate (DETP) and diethyl dithiophosphate (DEDTP).
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