Import and efflux of flubendazole in Haemonchus contortus strains susceptible and resistant to anthelmintics

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11160%2F12%3A10124809" target="_blank" >RIV/00216208:11160/12:10124809 - isvavai.cz</a>

Výsledek na webu

<a href="http://www.sciencedirect.com/science/article/pii/S0304401712000805" target="_blank" >http://www.sciencedirect.com/science/article/pii/S0304401712000805</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.vetpar.2012.02.008" target="_blank" >10.1016/j.vetpar.2012.02.008</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Import and efflux of flubendazole in Haemonchus contortus strains susceptible and resistant to anthelmintics

Popis výsledku v původním jazyce

Drug entry into the body of a helminth is a key factor in the efficacy of anthelmintics. The present project was designed to study the ex vivo uptake and efflux of the benzimidazole anthelmintic flubendazole (FLU) in four strains of H. contortus: the ISEstrain (fully susceptible to anthelmintics), the ISE-S strain (resistant to ivermectin), the BR strain (resistant to benzimidazoles) and the WR strain (multi-resistant). The transport of FLU between dead and living nematodes was also compared as well asthe effect of verapamil, an inhibitor of the main efflux ABCB1 transporter (P-glycoprotein), on FLU accumulation in nematodes. The obtained results showed that FLU is able to effectively enter H. contortus adults due to high FLU lipophilicity. Passive diffusion is probably the only mechanism in both FLU import and efflux from nematodes. No differences in FLU transport were found among four H. contortus strains with different sensitivity to anthelmintics. No active FLU efflux from H. con

Název v anglickém jazyce

Import and efflux of flubendazole in Haemonchus contortus strains susceptible and resistant to anthelmintics

Popis výsledku anglicky

Drug entry into the body of a helminth is a key factor in the efficacy of anthelmintics. The present project was designed to study the ex vivo uptake and efflux of the benzimidazole anthelmintic flubendazole (FLU) in four strains of H. contortus: the ISEstrain (fully susceptible to anthelmintics), the ISE-S strain (resistant to ivermectin), the BR strain (resistant to benzimidazoles) and the WR strain (multi-resistant). The transport of FLU between dead and living nematodes was also compared as well asthe effect of verapamil, an inhibitor of the main efflux ABCB1 transporter (P-glycoprotein), on FLU accumulation in nematodes. The obtained results showed that FLU is able to effectively enter H. contortus adults due to high FLU lipophilicity. Passive diffusion is probably the only mechanism in both FLU import and efflux from nematodes. No differences in FLU transport were found among four H. contortus strains with different sensitivity to anthelmintics. No active FLU efflux from H. con

Druh

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

CEP obor

CE - Biochemie

OECD FORD obor

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Projekt

<a href="/cs/project/GAP502%2F10%2F0217" target="_blank" >GAP502/10/0217: Vývoj lékové rezistence u helmintů - možné mechanismy a obrana</a><br>

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>S - Specificky vyzkum na vysokych skolach<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2012

Kód důvěrnosti údajů

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

Název periodika

Veterinary Parasitology

ISSN

0304-4017

e-ISSN

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Svazek periodika

187

Číslo periodika v rámci svazku

3-4

Stát vydavatele periodika

NL - Nizozemsko

Počet stran výsledku

7

Strana od-do

473-479

Kód UT WoS článku

000307323700017

EID výsledku v databázi Scopus

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