Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.1.1.8 (cholinesterase)
 12,691 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

In 2001, an outbreak of Mediterranean fruit fly in Adelaide was controlled by South Australian Government workers applying organophosphorus insecticides (OPs) to domestic gardens. Residents made claims of adverse effects associated with allegations that worker application practices were poor and led to contamination of homes, residents and pets. The concerns led to a Parliamentary enquiry, the suspension of OP applications for fruit fly control, and the investigation of alternative methods of combating fruit fly in metropolitan Adelaide. The extent of exposure of workers and residents was not estimated. This paper describes a simulated application of the OPs concerned (fenthion and malathion) with measurements of potential exposure through inhalation, dermal contact and deposition of pesticides on surfaces. The data were used as part of a toxicological risk assessment to determine the likely impact of the use of these insecticides. Malathion, used as a 1% suspension in a protein bait mixture, was found to have little potential for airborne exposure, although some workers were found to have up to 0.315 microg/cm(2) malathion deposited on overalls (principally on forearms) and over 500 microg deposited on liner gloves and hats, respectively. Risks to workers and residents were low, with exposures likely to be a small fraction of the acceptable daily intake. Fenthion, used as a 0.05% foliar cover spray, was found between 0.02 and 0.23 mg/m(3) in air 10 m downwind from spray activity and was unlikely to pose a significant risk to residents, since exposures were of short durations of up to 20 min. Personal air samples of spray workers averaged 0.55 mg/m(3) (Workplace Exposure Standard 0.20mg/m(3)). Since workers were usually engaged in spraying for a large proportion of the day, this demonstrates the need for respiratory protective equipment. Maximum deposition of fenthion on workers overalls ranged from 0.06 to over 0.20 microg/cm(2), although little was found on gloves and hats, suggesting workers were skilled in avoiding the plume of overspray. Dialkyl phosphates (metabolites of OP insecticides) were not detected in urine of workers, and there were no changes observed in serum cholinesterase (SChE) enzyme activities 24h following the simulation. These data suggest absorption of OP insecticides by workers was negligible. Deposition on surfaces 5 and 10 m downwind ranged from none detected to 145 microg/cm(2), suggesting that exposure of residents and children in contact with contaminated surfaces (such as garden furniture or play equipment) is possible. Estimates of the potential dermal intake of fenthion by children from contaminated surfaces suggested that risks of acute and chronic effects are slight, since exposures may occur for short periods at intervals of approximately 10 days during fruit fly outbreaks.
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PMID:Worker exposure and a risk assessment of malathion and fenthion used in the control of Mediterranean fruit fly in South Australia. 1691 34

Parkinson's disease (PD) is a complex neurodegenerative disorder with multifactorial pathologies, including progressive loss of dopaminergic (DA) neurons, oxidative stress, mitochondrial dysfunction, and increased monoamine oxidase (MAO) enzyme activity. There are currently only a few agents approved to ameliorate the symptoms of PD; however, no agent is able to reverse the progression of the disease. Due to the multifactorial pathologies, it is necessary to develop multifunctional agents that can affect more than one target involved in the disease pathology. We have designed and synthesized a series of new multifunctional anti-Parkinson's compounds which can protect cerebral granular neurons from 1-methyl-4-phenylpyridinium (MPP+) insult, scavenge free radicals, and inhibit monoamine oxidase (MAO)/cholinesterase (ChE) activities. Among them, MT-20R exhibited the most potent MAO-B inhibition both in vitro and in vivo. We further investigated the neuroprotective effects of MT-20R using a 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced PD mouse model. In vivo, MT-20R alleviated MPTP-induced motor deficits, raised the striatal contents of dopamine and its metabolites, and restored the expression of tyrosine hydroxylase (TH) and the number of TH-positive DA neurons in the substantia nigra. Additionally, MT-20R enhanced the expression of Bcl-2, decreased the expression of Bax and Caspase 3, and activated the AKT/Nrf2/HO-1 signaling pathway. These findings suggest that MT-20R may be a novel therapeutic candidate for treatment of PD.
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PMID:Neuroprotective Effects and Mechanisms of Action of Multifunctional Agents Targeting Free Radicals, Monoamine Oxidase B and Cholinesterase in Parkinson's Disease Model. 2814 26


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