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

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About: Import and efflux of flubendazole in Haemonchus contortus strains susceptible and resistant to anthelmintics Goto Sponge NotDistinct Permalink

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
rdfs:seeAlso	http://www.sciencedirect.com/science/article/pii/S0304401712000805
Description	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 ISE strain (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 as the 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. contortus and no effect of verapamil were observed, indicating that H. contortus cannot protect itself against FLU by the active removal of this anthelmintic from its body. 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 ISE strain (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 as the 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. contortus and no effect of verapamil were observed, indicating that H. contortus cannot protect itself against FLU by the active removal of this anthelmintic from its body. (en)
Title	Import and efflux of flubendazole in Haemonchus contortus strains susceptible and resistant to anthelmintics Import and efflux of flubendazole in Haemonchus contortus strains susceptible and resistant to anthelmintics (en)
skos:prefLabel	Import and efflux of flubendazole in Haemonchus contortus strains susceptible and resistant to anthelmintics Import and efflux of flubendazole in Haemonchus contortus strains susceptible and resistant to anthelmintics (en)
skos:notation	RIV/00216208:11160/12:10124809!RIV13-MSM-11160___
http://linked.open...avai/predkladatel	Farmaceutická fakulta v Hradci Králové
http://linked.open...avai/riv/aktivita	I P S
http://linked.open...avai/riv/aktivity	I, P(GAP502/10/0217), S
http://linked.open...iv/cisloPeriodika	3-4
http://linked.open...vai/riv/dodaniDat	2013
http://linked.open...aciTvurceVysledku	Skálová, Lenka Lamka, Jiří Szotáková, Barbora Vokřál, Ivan Bártíková, Hana Kubíček, Vladimír Prchal, Lukáš
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Univerzita Karlova v Praze / Farmaceutická fakulta v Hradci Králové
http://linked.open...dnocenehoVysledku	140865
http://linked.open...ai/riv/idVysledku	RIV/00216208:11160/12:10124809
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	Resistance; Helminths; Nematoda; Strain-differences; Drug transport (en)
http://linked.open.../riv/klicoveSlovo	Resistance Drug transport Nematoda Strain-differences Helminths
http://linked.open...odStatuVydavatele	NL - Nizozemsko
http://linked.open...ontrolniKodProRIV	[44C7B907C794]
http://linked.open...i/riv/nazevZdroje	Veterinary Parasitology
http://linked.open...in/vavai/riv/obor	CE
http://linked.open...ichTvurcuVysledku	7 (xsd:int)
http://linked.open...cetTvurcuVysledku	8 (xsd:int)
http://linked.open...vavai/riv/projekt	Drug-resistance development in helminths - possible mechanisms and defense
http://linked.open...UplatneniVysledku	2012
http://linked.open...v/svazekPeriodika	187
http://linked.open...iv/tvurceVysledku	Lamka, Jiří Skálová, Lenka Szotáková, Barbora Kubíček, Vladimír Bártíková, Hana Vokřál, Ivan Prchal, Lukáš Várady, Marián
http://linked.open...ain/vavai/riv/wos	000307323700017
issn	0304-4017
number of pages	7 (xsd:int)
http://bibframe.org/vocab/doi	10.1016/j.vetpar.2012.02.008
http://localhost/t...ganizacniJednotka	11160
is http://linked.open...avai/riv/vysledek of	Import and efflux of flubendazole in Haemonchus contortus strains susceptible and resistant to anthelmintics

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