Possible role of Mg2+ ion in the reaction of organophosphate (dichlorvos) with serine

Shetab-Boushehri, Seyed Vahid; Shetab-Boushehri, Seyed Farid; Abdollahi, Mohammad

doi:10.1016/j.jmhi.2012.05.001

Cited by 6 publications

(20 citation statements)

References 22 publications

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“…Dichlorvos is being used to control pests on the farms and in the house [20]. Self-poisoning from organophosphate pesticide use is an important clinical problem in developing world [5]. Atropine and oximes, the common antidotes being used in managing organophosphate insecticide poisoning, are not effective in some cases [7].…”

Section: Resultsmentioning

confidence: 99%

“…Dichlorvos strongly binds to acetyl cholinesterase (AChE) molecules to form AChE-OP complex. This phosphorylation causes inactivation of the enzyme [5], accumulation of acetylcholine and subsequent over-activation of cholinergic receptors [6]. Reactivation of AChE can be hastened by nucleophilic reagents [7].…”

Section: This Study Investigated Possible Use Of Gentamicin and Magnementioning

confidence: 99%

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Gentamicin and magnesium chloride normalizes cholinesterase and ATPase activities in rats acutely exposed to dichlorvos (DDVP) pesticide

Ajilore¹,

Adewuyi²,

Oluwadairo³

2018

Ukr.Biochem.J.

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Section: Resultsmentioning

confidence: 99%

Section: This Study Investigated Possible Use Of Gentamicin and Magnementioning

confidence: 99%

Gentamicin and magnesium chloride normalizes cholinesterase and ATPase activities in rats acutely exposed to dichlorvos (DDVP) pesticide

Ajilore¹,

Adewuyi²,

Oluwadairo³

2018

Ukr.Biochem.J.

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“…butyrylcholinesterase [BuChE]) cholinesterases (ChEs) by a nucleophilic reaction in which the associative two-step additionelimination reaction with the serine hydroxyl group at their active sites results in phosphorylated and inactivated enzymes. 1,2 AChE is primarily found in nervous tissue and erythrocytes; erythrocytic ChE activity more accurately reflects nervous tissue AChE activity than BuChE, which is primarily produced in the liver and appears in plasma, with its activity varying with a number of disorders including liver disease. 3,4 The irreversible inactivation of ChEs by the dealkylation of the OP moiety of the OP-ChE complex is known as ageing, in which the phosphorusoxygen bond of the OP-ChE complex strengthens.…”

mentioning

confidence: 99%

“…5 After ageing occurs, even oximes are ineffective in reactivating the enzyme, and the only means of restoring ChE activity is via the lengthy process of synthesizing a new AChE enzyme. 2 At present, two main antidotes exist for the treatment of OP poisoning: atropine and oximes, particularly pralidoxime (2-PAM) in the latter group. 2 However, oximes are not always useful in the management of OP poisoning.…”

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In Vitro Cysteine Reactivates Organophosphate Insecticide Dichlorvos-Inhibited Human Cholinesterases

Mohammadi

Jalilian

Karimi

et al. 2017

SQUMJ

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Objectives: Organophosphate (OP) pesticides inhibit both red blood cell (RBC) and plasma cholinesterases (ChEs). Oximes, especially pralidoxime (2-PAM), are widely used as antidotes to treat OP poisoning. In addition, N-acetylcysteine (NAC) is sometimes used as an adjuvant antidote. The current study aimed to assess the feasibility of using NAC as a single therapeutic agent for OP poisoning in comparison to in vitro 2-PAM. Methods: This study was carried out at the Razi Drug Research Center of Iran University of Medical Sciences, Tehran, Iran, between April and September 2014. A total of 22 healthy human subjects were recruited and 8 mL citrated blood samples were drawn from each subject. Dichlorvos-inhibited blood samples were separately exposed to low and high doses (final concentrations of 300 and 600 μmol.L-1 , respectively) of 2-PAM, NAC and cysteine. Plasma and RBCs were then separated by centrifugation and their ChE activity was measured using spectrophotometry. Results: Although cysteine-and not NAC-increased the ChE activity of both plasma and RBCs over those of dichlorvos, it did not increase them over those of a high dose of 2-PAM. Conclusion: These results suggest that the direct reactions of 2-PAM and cysteine with dichlorvos and the reactivation of phosphorylated ChEs occurr via an associative stepwise addition-elimination process. High therapeutic blood concentrations of cysteine are needed for the elevation of ChE activity in plasma and RBCs; however, both this agent and NAC may still be effective in the reactivation of plasma and RBC ChEs.

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Effects of magnesium chloride on in vitro cholinesterase and ATPase poisoning by organophosphate (chlorpyrifos)

Ajilore

Alli

Oluwadairo

2018

Pharmacology Res & Perspec

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The present study investigated possible benefits of magnesium ion (as MgCl2) in organophosphorus poisoning targeting its ability to interact with substrates and membrane enzymes. Blood samples collected from volunteered healthy adult by venepuncture into anticoagulant test tubes containing EDTA were separated into plasma and red blood cell and divided into three groups namely: normal, pesticide only (0.25‐2.0 mmol/L chlorpyrifos) and pesticide (0.25‐2.0 mmol/L chlorpyrifos) + 0.1 mol/L MgCl2. Acetylcholinesterase, Na+/K+ ATPase and Ca2+ ATPase activities were evaluated. Results showed that Chlorpyrifos significantly (P < .05) reduced the levels of cholinesterase both in plasma and on red blood cells. Red blood cells Na+/K+ ATPase and Ca2+ ATPase were also significantly (P < .05) reduced by chlorpyrifos while MgCl2 counteracted effects of chlorpyrifos with significant (P < .05) increase in the levels of cholinesterase, Na+/K+ ATPase and Ca2+ ATPase. We concluded that MgCl2 neutralized effects of chlorpyrifos by promoting normal ATPase activities and inhibiting release of acetylcholine from cell.

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Possible role of Mg2+ ion in the reaction of organophosphate (dichlorvos) with serine

Cited by 6 publications

References 22 publications

Gentamicin and magnesium chloride normalizes cholinesterase and ATPase activities in rats acutely exposed to dichlorvos (DDVP) pesticide

Gentamicin and magnesium chloride normalizes cholinesterase and ATPase activities in rats acutely exposed to dichlorvos (DDVP) pesticide

In Vitro Cysteine Reactivates Organophosphate Insecticide Dichlorvos-Inhibited Human Cholinesterases

Effects of magnesium chloride on in vitro cholinesterase and ATPase poisoning by organophosphate (chlorpyrifos)

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