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Statements

Subject Item
n2:RIV%2F00216208%3A11160%2F12%3A10124809%21RIV13-MSM-11160___
rdf:type
skos:Concept n15:Vysledek
rdfs:seeAlso
http://www.sciencedirect.com/science/article/pii/S0304401712000805
dcterms: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.
dcterms: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
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
skos:notation
RIV/00216208:11160/12:10124809!RIV13-MSM-11160___
n15:predkladatel
n16:orjk%3A11160
n3:aktivita
n11:S n11:P n11:I
n3:aktivity
I, P(GAP502/10/0217), S
n3:cisloPeriodika
3-4
n3:dodaniDat
n12:2013
n3:domaciTvurceVysledku
n4:9958185 n4:6736327 n4:2442256 n4:8004188 n4:2231395 n4:5934141 n4:2270455
n3:druhVysledku
n8:J
n3:duvernostUdaju
n17:S
n3:entitaPredkladatele
n10:predkladatel
n3:idSjednocenehoVysledku
140865
n3:idVysledku
RIV/00216208:11160/12:10124809
n3:jazykVysledku
n21:eng
n3:klicovaSlova
Resistance; Helminths; Nematoda; Strain-differences; Drug transport
n3:klicoveSlovo
n13:Drug%20transport n13:Helminths n13:Strain-differences n13:Nematoda n13:Resistance
n3:kodStatuVydavatele
NL - Nizozemsko
n3:kontrolniKodProRIV
[44C7B907C794]
n3:nazevZdroje
Veterinary Parasitology
n3:obor
n6:CE
n3:pocetDomacichTvurcuVysledku
7
n3:pocetTvurcuVysledku
8
n3:projekt
n5:GAP502%2F10%2F0217
n3:rokUplatneniVysledku
n12:2012
n3:svazekPeriodika
187
n3:tvurceVysledku
Skálová, Lenka Kubíček, Vladimír Bártíková, Hana Szotáková, Barbora Vokřál, Ivan Lamka, Jiří Várady, Marián Prchal, Lukáš
n3:wos
000307323700017
s:issn
0304-4017
s:numberOfPages
7
n18:doi
10.1016/j.vetpar.2012.02.008
n20:organizacniJednotka
11160