About: The metabolic fate of ivermectin in host (Ovis aries) and parasite (Haemonchus contortus)

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About: The metabolic fate of ivermectin in host (Ovis aries) and parasite (Haemonchus contortus) Goto Sponge NotDistinct Permalink

An Entity of Type : http://linked.opendata.cz/ontology/domain/vavai/Vysledek, within Data Space : linked.opendata.cz associated with source document(s)

Attributes	Values
rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
rdfs:seeAlso	http://journals.cambridge.org/action/displayFulltext?type=6&fid=8838267&jid=PAR&aid=8838266
Description	Ivermectin (IVE), one of the most important anthelmintics, is often used in the treatment of haemonchosis in ruminants. The objective of our work was (1) to find and identify phase I and II metabolites of IVE formed by the Barber's pole worm (Haemonchus contortus), and (2) to compare IVE metabolites in helminths with IVE biotransformation in sheep (Ovis aries) as host species. Ultrahigh-performance liquid chromatography/tandem mass spectrometry (UHPLC/MS/MS) was used for this purpose. During in vitro incubations, microsomes (from adult worms or from ovine liver) and a primary culture of ovine hepatocytes were incubated with IVE. In the ex vivo study, living H. contortus adults were incubated in the presence of 1 mu M IVE for 24 h. The results showed that the H. contortus enzymatic system is not able to metabolize IVE. On the other hand, 7 different phase I as well as 9 phase II IVE metabolites were detected in ovine samples using UHPLC/MS/MS analyses. Most of these metabolites have not been described before. Haemonchus contortus is not able to deactivate IVE through biotransformation; therefore, biotransformation does not contribute to the development of IVE-resistance in the Barber's pole worm. Ivermectin (IVE), one of the most important anthelmintics, is often used in the treatment of haemonchosis in ruminants. The objective of our work was (1) to find and identify phase I and II metabolites of IVE formed by the Barber's pole worm (Haemonchus contortus), and (2) to compare IVE metabolites in helminths with IVE biotransformation in sheep (Ovis aries) as host species. Ultrahigh-performance liquid chromatography/tandem mass spectrometry (UHPLC/MS/MS) was used for this purpose. During in vitro incubations, microsomes (from adult worms or from ovine liver) and a primary culture of ovine hepatocytes were incubated with IVE. In the ex vivo study, living H. contortus adults were incubated in the presence of 1 mu M IVE for 24 h. The results showed that the H. contortus enzymatic system is not able to metabolize IVE. On the other hand, 7 different phase I as well as 9 phase II IVE metabolites were detected in ovine samples using UHPLC/MS/MS analyses. Most of these metabolites have not been described before. Haemonchus contortus is not able to deactivate IVE through biotransformation; therefore, biotransformation does not contribute to the development of IVE-resistance in the Barber's pole worm. (en)
Title	The metabolic fate of ivermectin in host (Ovis aries) and parasite (Haemonchus contortus) The metabolic fate of ivermectin in host (Ovis aries) and parasite (Haemonchus contortus) (en)
skos:prefLabel	The metabolic fate of ivermectin in host (Ovis aries) and parasite (Haemonchus contortus) The metabolic fate of ivermectin in host (Ovis aries) and parasite (Haemonchus contortus) (en)
skos:notation	RIV/00216208:11160/13:10144279!RIV14-GA0-11160___
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
http://linked.open...vai/riv/dodaniDat	2014
http://linked.open...aciTvurceVysledku	Skálová, Lenka Lamka, Jiří Szotáková, Barbora Vokřál, Ivan Bártíková, Hana Stuchlíková, Lucie
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	87457
http://linked.open...ai/riv/idVysledku	RIV/00216208:11160/13:10144279
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	UHPLC/MS/MS; biotransformation; Haemonchus contortus; ivermectin (en)
http://linked.open.../riv/klicoveSlovo	Haemonchus contortus UHPLC/MS/MS ivermectin biotransformation
http://linked.open...odStatuVydavatele	US - Spojené státy americké
http://linked.open...ontrolniKodProRIV	[0CBC5D3DB3B7]
http://linked.open...i/riv/nazevZdroje	Parasitology
http://linked.open...in/vavai/riv/obor	CE
http://linked.open...ichTvurcuVysledku	6 (xsd:int)
http://linked.open...cetTvurcuVysledku	9 (xsd:int)
http://linked.open...vavai/riv/projekt	Drug-resistance development in helminths - possible mechanisms and defense
http://linked.open...UplatneniVysledku	2013
http://linked.open...v/svazekPeriodika	140
http://linked.open...iv/tvurceVysledku	Holčapek, Michal Lamka, Jiří Skálová, Lenka Jirásko, Robert Szotáková, Barbora Bártíková, Hana Vokřál, Ivan Jedličková, Veronika Stuchlíková, Lucie
http://linked.open...ain/vavai/riv/wos	000315341200010
issn	0031-1820
number of pages	7 (xsd:int)
http://bibframe.org/vocab/doi	10.1017/S0031182012001680
http://localhost/t...ganizacniJednotka	11160

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