Oxime-mediated in vitro reactivation kinetic analysis of organophosphates-inhibited human and electric eel acetylcholinesterase
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F62690094%3A18470%2F16%3A50004737" target="_blank" >RIV/62690094:18470/16:50004737 - isvavai.cz</a>
Alternative codes found
RIV/00179906:_____/16:10330362
Result on the web
<a href="http://www.tandfonline.com/doi/abs/10.3109/15376516.2016.1143070?journalCode=itxm20" target="_blank" >http://www.tandfonline.com/doi/abs/10.3109/15376516.2016.1143070?journalCode=itxm20</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.3109/15376516.2016.1143070" target="_blank" >10.3109/15376516.2016.1143070</a>
Alternative languages
Result language
angličtina
Original language name
Oxime-mediated in vitro reactivation kinetic analysis of organophosphates-inhibited human and electric eel acetylcholinesterase
Original language description
Organophosphate (OP)-based pesticides and nerve agents are highly toxic compounds which interrupt the catalytic mechanism of acetylcholinesterase (AChE) by phosphorylating the hydroxyl moiety of serine residue. The inhibited enzyme can be reactivated by the nucleophilic action of oxime reactivators. To analyze the effect of different AChE sources on reactivation efficacy of reactivators, several in vivo studies have carried out using variety of AChE sources like pig, rat and monkey. Investigations on species differences provide a better insight for the development of new reactivators. Hence, present study was mainly targeted on comparative analysis of the reactivation of electric eel and human AChE inhibited by different OP. A series of butene-linked bis-pyridinium mono oximes which vary in functional groups present at the second pyridinium ring have been examined against sarin, VX, tabun and ethyl-paraoxon-poisoned AChE. In case of tabun-inhibited AChEs, tested oximes were better than reference oximes. For VX-poisoned human AChE, reactivator K251 (k(r2);1.51mM(-1)min(-1)) showed good reactivation efficacy with standard oximes. Studies stipulated that butene-linked oximes consisting of different functional moieties are good reactivators and found to have better efficacy to reactivate nerve agent-inhibited human AChE in comparison to eel AChE.
Czech name
—
Czech description
—
Classification
Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
FR - Pharmacology and apothecary chemistry
OECD FORD branch
—
Result continuities
Project
<a href="/en/project/LH13009" target="_blank" >LH13009: The research of modified cholinesterase reactivators for organophosphorus pesticide poisoning treatment</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)
Others
Publication year
2016
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Toxicology mechanisms and methods
ISSN
1537-6516
e-ISSN
—
Volume of the periodical
26
Issue of the periodical within the volume
5
Country of publishing house
US - UNITED STATES
Number of pages
8
Pages from-to
319-326
UT code for WoS article
000380053100002
EID of the result in the Scopus database
—