In Vivo Evaluation of Cholinesterase Activity, Oxidative Stress Markers, Cyto- and Genotoxicity of K048 Oxime - a Promising Antidote against Organophosphate Poisoning

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00179906%3A_____%2F14%3A10272061" target="_blank" >RIV/00179906:_____/14:10272061 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/62690094:18470/14:50002291

Výsledek na webu

<a href="http://dx.doi.org/10.1111/bcpt.12158" target="_blank" >http://dx.doi.org/10.1111/bcpt.12158</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1111/bcpt.12158" target="_blank" >10.1111/bcpt.12158</a>

Jazyk výsledku

angličtina

Název v původním jazyce

In Vivo Evaluation of Cholinesterase Activity, Oxidative Stress Markers, Cyto- and Genotoxicity of K048 Oxime - a Promising Antidote against Organophosphate Poisoning

Popis výsledku v původním jazyce

K048 is a member of K-oximes, a new oxime class that has recently been confirmed effective against poisoning by the nerve agent tabun and several pesticides. The toxicity profile of the K048 oxime has not been fully characterized and its optimal therapeutic dose has not yet been established. Earlier studies report excellent results with K048 in reactivating tabun-phosphorylated AChE and in the therapy of tabun-poisoned mice. It possesses a low acute toxicity and exerts an acceptable toxicity profile onisolated human peripheral blood lymphocytes in vitro. Intraperitoneal administration of K048 in rats resulted in an LD50 of 238.3mg/kg. In this in vivo study, we investigated cholinesterase (ChE) activity and oxidative stress marker levels (lipid peroxidation and superoxide dismutase activity) in the plasma of exposed rats after administering the compound at 25% of its LD50. Lymphocyte viability was evaluated using an acridine orange/ethidium bromide in situ fluorescent assay. The levels

Název v anglickém jazyce

In Vivo Evaluation of Cholinesterase Activity, Oxidative Stress Markers, Cyto- and Genotoxicity of K048 Oxime - a Promising Antidote against Organophosphate Poisoning

Popis výsledku anglicky

K048 is a member of K-oximes, a new oxime class that has recently been confirmed effective against poisoning by the nerve agent tabun and several pesticides. The toxicity profile of the K048 oxime has not been fully characterized and its optimal therapeutic dose has not yet been established. Earlier studies report excellent results with K048 in reactivating tabun-phosphorylated AChE and in the therapy of tabun-poisoned mice. It possesses a low acute toxicity and exerts an acceptable toxicity profile onisolated human peripheral blood lymphocytes in vitro. Intraperitoneal administration of K048 in rats resulted in an LD50 of 238.3mg/kg. In this in vivo study, we investigated cholinesterase (ChE) activity and oxidative stress marker levels (lipid peroxidation and superoxide dismutase activity) in the plasma of exposed rats after administering the compound at 25% of its LD50. Lymphocyte viability was evaluated using an acridine orange/ethidium bromide in situ fluorescent assay. The levels

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

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Projekt

<a href="/cs/project/LH13009" target="_blank" >LH13009: Výzkum modifikovaných reaktivátorů cholinesteras pro léčbu intoxikací organofosforovými pesticidy</a><br>

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2014

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Basic and Clinical Pharmacology and Toxicology

ISSN

1742-7835

e-ISSN

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Svazek periodika

114

Číslo periodika v rámci svazku

4

Stát vydavatele periodika

DK - Dánské království

Počet stran výsledku

8

Strana od-do

344-351

Kód UT WoS článku

000332208300008

EID výsledku v databázi Scopus

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