Monoterpenes as potential tools to improve the activity of synthetic anthelmintics: pharmacological screening of their effects on drug metabolism and intestinal accumulation

Autores
Miró, María Victoria; Costa Junior, Livio M.; Alvarez, Luis Ignacio; Lanusse, Carlos Edmundo; Virkel, Guillermo Leon; Lifschitz, Adrian Luis
Año de publicación
2021
Idioma
inglés
Tipo de recurso
documento de conferencia
Estado
versión publicada
Descripción
The search for novel alternatives to control gastrointestinal nematodes in ruminants is relevant considering the increasing of anthelmintic resistance. The use of monoterpenes may contribute to improving parasite control by enhancing the effectiveness of existing synthetic anthelmintic drugs. The work described here evaluated in vitro the effects of monoterpenes on the processes of drug metabolism and intestinal accumulation and additionally, the anthelmintic activity of the best ?candidate?. In Trial 1 the internal accumulation of Rhodamine- 123 (Rho123), a P-glycoprotein substrate, was studied in cattle ileum in the presence or absence of carvone (CNE), geraniol (GNL), citral (CTL), anethole (ANT), carvacrol (CVC) and thymol (TML). The effect of CNE, GNL and CTL on flavin-containing monooxygenase (FMO) and cytochrome P450 (CYP) dependent metabolism was assessed in sheep liver microsomes measuring specific enzyme activities. Among the monoterpenes tested, only the presence of CNE and GNL increased the accumulation of Rho123 by 73 % and 44 % respectively (P<0.05). CNE, GNL and CIT reduced the CYP-dependent metabolism between 29.5 and 91 % (P<0.05) and the FMO dependent metabolism between 46 and 84 % (P<0.05). Additionally, in a separate experiment (Trial 2), the anthelmintic activity of the best monoterpene ?candidate? was evaluated in lambs. Six lambs artificially infected with 2000 Haemonchus contortus larvae each were treated with CNE (the best candidate from Trial 1) at 100 mg/kg orally, four times every 24 h. The fecal eggs count (FEC) reduction was measured at 7, 14 and 21 days post-administration of the first dose of CNE. The FEC reduction after the in vivo administration of CNE to infected lambs was 85 % (7 d), 88 % (14 d) and 82 (21 d). Integrated in-vitro-in vivo assays are critical for the design of successful alternative parasite control strategies based on the use of bioactive phytochemicals.
Fil: Miró, María Victoria. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil. Centro de Investigación Veterinaria de Tandil. Universidad Nacional del Centro de la Provincia de Buenos Aires. Centro de Investigación Veterinaria de Tandil. Provincia de Buenos Aires. Gobernación. Comision de Investigaciones Científicas. Centro de Investigación Veterinaria de Tandil; Argentina
Fil: Costa Junior, Livio M.. Universidade Federal do Maranhao; Brasil
Fil: Alvarez, Luis Ignacio. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil. Centro de Investigación Veterinaria de Tandil. Universidad Nacional del Centro de la Provincia de Buenos Aires. Centro de Investigación Veterinaria de Tandil. Provincia de Buenos Aires. Gobernación. Comision de Investigaciones Científicas. Centro de Investigación Veterinaria de Tandil; Argentina
Fil: Lanusse, Carlos Edmundo. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil. Centro de Investigación Veterinaria de Tandil. Universidad Nacional del Centro de la Provincia de Buenos Aires. Centro de Investigación Veterinaria de Tandil. Provincia de Buenos Aires. Gobernación. Comision de Investigaciones Científicas. Centro de Investigación Veterinaria de Tandil; Argentina
Fil: Virkel, Guillermo Leon. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil. Centro de Investigación Veterinaria de Tandil. Universidad Nacional del Centro de la Provincia de Buenos Aires. Centro de Investigación Veterinaria de Tandil. Provincia de Buenos Aires. Gobernación. Comision de Investigaciones Científicas. Centro de Investigación Veterinaria de Tandil; Argentina
Fil: Lifschitz, Adrian Luis. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil. Centro de Investigación Veterinaria de Tandil. Universidad Nacional del Centro de la Provincia de Buenos Aires. Centro de Investigación Veterinaria de Tandil. Provincia de Buenos Aires. Gobernación. Comision de Investigaciones Científicas. Centro de Investigación Veterinaria de Tandil; Argentina
28th International Conference of the World Association for the Advancement of Veterinary Parasitology
Dublin
Irlanda
World Association for the Advancement of Veterinary Parasitology
University College of Dublin
Materia
MONOTERPENES
ANTHELMINTICS
METABOLISM
ACCUMULATION
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/156969
Acceder
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network_name_str CONICET Digital (CONICET)
spelling Monoterpenes as potential tools to improve the activity of synthetic anthelmintics: pharmacological screening of their effects on drug metabolism and intestinal accumulationMiró, María VictoriaCosta Junior, Livio M.Alvarez, Luis IgnacioLanusse, Carlos EdmundoVirkel, Guillermo LeonLifschitz, Adrian LuisMONOTERPENESANTHELMINTICSMETABOLISMACCUMULATIONhttps://purl.org/becyt/ford/4.3https://purl.org/becyt/ford/4The search for novel alternatives to control gastrointestinal nematodes in ruminants is relevant considering the increasing of anthelmintic resistance. The use of monoterpenes may contribute to improving parasite control by enhancing the effectiveness of existing synthetic anthelmintic drugs. The work described here evaluated in vitro the effects of monoterpenes on the processes of drug metabolism and intestinal accumulation and additionally, the anthelmintic activity of the best ?candidate?. In Trial 1 the internal accumulation of Rhodamine- 123 (Rho123), a P-glycoprotein substrate, was studied in cattle ileum in the presence or absence of carvone (CNE), geraniol (GNL), citral (CTL), anethole (ANT), carvacrol (CVC) and thymol (TML). The effect of CNE, GNL and CTL on flavin-containing monooxygenase (FMO) and cytochrome P450 (CYP) dependent metabolism was assessed in sheep liver microsomes measuring specific enzyme activities. Among the monoterpenes tested, only the presence of CNE and GNL increased the accumulation of Rho123 by 73 % and 44 % respectively (P<0.05). CNE, GNL and CIT reduced the CYP-dependent metabolism between 29.5 and 91 % (P<0.05) and the FMO dependent metabolism between 46 and 84 % (P<0.05). Additionally, in a separate experiment (Trial 2), the anthelmintic activity of the best monoterpene ?candidate? was evaluated in lambs. Six lambs artificially infected with 2000 Haemonchus contortus larvae each were treated with CNE (the best candidate from Trial 1) at 100 mg/kg orally, four times every 24 h. The fecal eggs count (FEC) reduction was measured at 7, 14 and 21 days post-administration of the first dose of CNE. The FEC reduction after the in vivo administration of CNE to infected lambs was 85 % (7 d), 88 % (14 d) and 82 (21 d). Integrated in-vitro-in vivo assays are critical for the design of successful alternative parasite control strategies based on the use of bioactive phytochemicals.Fil: Miró, María Victoria. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil. Centro de Investigación Veterinaria de Tandil. Universidad Nacional del Centro de la Provincia de Buenos Aires. Centro de Investigación Veterinaria de Tandil. Provincia de Buenos Aires. Gobernación. Comision de Investigaciones Científicas. Centro de Investigación Veterinaria de Tandil; ArgentinaFil: Costa Junior, Livio M.. Universidade Federal do Maranhao; BrasilFil: Alvarez, Luis Ignacio. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil. Centro de Investigación Veterinaria de Tandil. Universidad Nacional del Centro de la Provincia de Buenos Aires. Centro de Investigación Veterinaria de Tandil. Provincia de Buenos Aires. Gobernación. Comision de Investigaciones Científicas. Centro de Investigación Veterinaria de Tandil; ArgentinaFil: Lanusse, Carlos Edmundo. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil. Centro de Investigación Veterinaria de Tandil. Universidad Nacional del Centro de la Provincia de Buenos Aires. Centro de Investigación Veterinaria de Tandil. Provincia de Buenos Aires. Gobernación. Comision de Investigaciones Científicas. Centro de Investigación Veterinaria de Tandil; ArgentinaFil: Virkel, Guillermo Leon. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil. Centro de Investigación Veterinaria de Tandil. Universidad Nacional del Centro de la Provincia de Buenos Aires. Centro de Investigación Veterinaria de Tandil. Provincia de Buenos Aires. Gobernación. Comision de Investigaciones Científicas. Centro de Investigación Veterinaria de Tandil; ArgentinaFil: Lifschitz, Adrian Luis. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil. Centro de Investigación Veterinaria de Tandil. Universidad Nacional del Centro de la Provincia de Buenos Aires. Centro de Investigación Veterinaria de Tandil. Provincia de Buenos Aires. Gobernación. Comision de Investigaciones Científicas. Centro de Investigación Veterinaria de Tandil; Argentina28th International Conference of the World Association for the Advancement of Veterinary ParasitologyDublinIrlandaWorld Association for the Advancement of Veterinary ParasitologyUniversity College of DublinWorld Association for the Advancement of Veterinary Parasitology2021info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/conferenceObjectConferenciaBookhttp://purl.org/coar/resource_type/c_5794info:ar-repo/semantics/documentoDeConferenciaapplication/pdfapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/156969Monoterpenes as potential tools to improve the activity of synthetic anthelmintics: pharmacological screening of their effects on drug metabolism and intestinal accumulation; 28th International Conference of the World Association for the Advancement of Veterinary Parasitology; Dublin; Irlanda; 2021; 1-2CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/http://www.waavp2021.com/info:eu-repo/semantics/altIdentifier/url/http://www.waavp2021.com/wp-content/uploads/2021/08/WAAVP-2021-Abstract-book-22.07.21-FINAL.pdfInternacionalinfo:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-03T09:55:50Zoai:ri.conicet.gov.ar:11336/156969instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-09-03 09:55:50.504CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Monoterpenes as potential tools to improve the activity of synthetic anthelmintics: pharmacological screening of their effects on drug metabolism and intestinal accumulation
title Monoterpenes as potential tools to improve the activity of synthetic anthelmintics: pharmacological screening of their effects on drug metabolism and intestinal accumulation
spellingShingle Monoterpenes as potential tools to improve the activity of synthetic anthelmintics: pharmacological screening of their effects on drug metabolism and intestinal accumulation
Miró, María Victoria
MONOTERPENES
ANTHELMINTICS
METABOLISM
ACCUMULATION
title_short Monoterpenes as potential tools to improve the activity of synthetic anthelmintics: pharmacological screening of their effects on drug metabolism and intestinal accumulation
title_full Monoterpenes as potential tools to improve the activity of synthetic anthelmintics: pharmacological screening of their effects on drug metabolism and intestinal accumulation
title_fullStr Monoterpenes as potential tools to improve the activity of synthetic anthelmintics: pharmacological screening of their effects on drug metabolism and intestinal accumulation
title_full_unstemmed Monoterpenes as potential tools to improve the activity of synthetic anthelmintics: pharmacological screening of their effects on drug metabolism and intestinal accumulation
title_sort Monoterpenes as potential tools to improve the activity of synthetic anthelmintics: pharmacological screening of their effects on drug metabolism and intestinal accumulation
dc.creator.none.fl_str_mv Miró, María Victoria
Costa Junior, Livio M.
Alvarez, Luis Ignacio
Lanusse, Carlos Edmundo
Virkel, Guillermo Leon
Lifschitz, Adrian Luis
author Miró, María Victoria
author_facet Miró, María Victoria
Costa Junior, Livio M.
Alvarez, Luis Ignacio
Lanusse, Carlos Edmundo
Virkel, Guillermo Leon
Lifschitz, Adrian Luis
author_role author
author2 Costa Junior, Livio M.
Alvarez, Luis Ignacio
Lanusse, Carlos Edmundo
Virkel, Guillermo Leon
Lifschitz, Adrian Luis
author2_role author
author
author
author
author
dc.subject.none.fl_str_mv MONOTERPENES
ANTHELMINTICS
METABOLISM
ACCUMULATION
topic MONOTERPENES
ANTHELMINTICS
METABOLISM
ACCUMULATION
purl_subject.fl_str_mv https://purl.org/becyt/ford/4.3
https://purl.org/becyt/ford/4
dc.description.none.fl_txt_mv The search for novel alternatives to control gastrointestinal nematodes in ruminants is relevant considering the increasing of anthelmintic resistance. The use of monoterpenes may contribute to improving parasite control by enhancing the effectiveness of existing synthetic anthelmintic drugs. The work described here evaluated in vitro the effects of monoterpenes on the processes of drug metabolism and intestinal accumulation and additionally, the anthelmintic activity of the best ?candidate?. In Trial 1 the internal accumulation of Rhodamine- 123 (Rho123), a P-glycoprotein substrate, was studied in cattle ileum in the presence or absence of carvone (CNE), geraniol (GNL), citral (CTL), anethole (ANT), carvacrol (CVC) and thymol (TML). The effect of CNE, GNL and CTL on flavin-containing monooxygenase (FMO) and cytochrome P450 (CYP) dependent metabolism was assessed in sheep liver microsomes measuring specific enzyme activities. Among the monoterpenes tested, only the presence of CNE and GNL increased the accumulation of Rho123 by 73 % and 44 % respectively (P<0.05). CNE, GNL and CIT reduced the CYP-dependent metabolism between 29.5 and 91 % (P<0.05) and the FMO dependent metabolism between 46 and 84 % (P<0.05). Additionally, in a separate experiment (Trial 2), the anthelmintic activity of the best monoterpene ?candidate? was evaluated in lambs. Six lambs artificially infected with 2000 Haemonchus contortus larvae each were treated with CNE (the best candidate from Trial 1) at 100 mg/kg orally, four times every 24 h. The fecal eggs count (FEC) reduction was measured at 7, 14 and 21 days post-administration of the first dose of CNE. The FEC reduction after the in vivo administration of CNE to infected lambs was 85 % (7 d), 88 % (14 d) and 82 (21 d). Integrated in-vitro-in vivo assays are critical for the design of successful alternative parasite control strategies based on the use of bioactive phytochemicals.
Fil: Miró, María Victoria. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil. Centro de Investigación Veterinaria de Tandil. Universidad Nacional del Centro de la Provincia de Buenos Aires. Centro de Investigación Veterinaria de Tandil. Provincia de Buenos Aires. Gobernación. Comision de Investigaciones Científicas. Centro de Investigación Veterinaria de Tandil; Argentina
Fil: Costa Junior, Livio M.. Universidade Federal do Maranhao; Brasil
Fil: Alvarez, Luis Ignacio. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil. Centro de Investigación Veterinaria de Tandil. Universidad Nacional del Centro de la Provincia de Buenos Aires. Centro de Investigación Veterinaria de Tandil. Provincia de Buenos Aires. Gobernación. Comision de Investigaciones Científicas. Centro de Investigación Veterinaria de Tandil; Argentina
Fil: Lanusse, Carlos Edmundo. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil. Centro de Investigación Veterinaria de Tandil. Universidad Nacional del Centro de la Provincia de Buenos Aires. Centro de Investigación Veterinaria de Tandil. Provincia de Buenos Aires. Gobernación. Comision de Investigaciones Científicas. Centro de Investigación Veterinaria de Tandil; Argentina
Fil: Virkel, Guillermo Leon. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil. Centro de Investigación Veterinaria de Tandil. Universidad Nacional del Centro de la Provincia de Buenos Aires. Centro de Investigación Veterinaria de Tandil. Provincia de Buenos Aires. Gobernación. Comision de Investigaciones Científicas. Centro de Investigación Veterinaria de Tandil; Argentina
Fil: Lifschitz, Adrian Luis. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tandil. Centro de Investigación Veterinaria de Tandil. Universidad Nacional del Centro de la Provincia de Buenos Aires. Centro de Investigación Veterinaria de Tandil. Provincia de Buenos Aires. Gobernación. Comision de Investigaciones Científicas. Centro de Investigación Veterinaria de Tandil; Argentina
28th International Conference of the World Association for the Advancement of Veterinary Parasitology
Dublin
Irlanda
World Association for the Advancement of Veterinary Parasitology
University College of Dublin
description The search for novel alternatives to control gastrointestinal nematodes in ruminants is relevant considering the increasing of anthelmintic resistance. The use of monoterpenes may contribute to improving parasite control by enhancing the effectiveness of existing synthetic anthelmintic drugs. The work described here evaluated in vitro the effects of monoterpenes on the processes of drug metabolism and intestinal accumulation and additionally, the anthelmintic activity of the best ?candidate?. In Trial 1 the internal accumulation of Rhodamine- 123 (Rho123), a P-glycoprotein substrate, was studied in cattle ileum in the presence or absence of carvone (CNE), geraniol (GNL), citral (CTL), anethole (ANT), carvacrol (CVC) and thymol (TML). The effect of CNE, GNL and CTL on flavin-containing monooxygenase (FMO) and cytochrome P450 (CYP) dependent metabolism was assessed in sheep liver microsomes measuring specific enzyme activities. Among the monoterpenes tested, only the presence of CNE and GNL increased the accumulation of Rho123 by 73 % and 44 % respectively (P<0.05). CNE, GNL and CIT reduced the CYP-dependent metabolism between 29.5 and 91 % (P<0.05) and the FMO dependent metabolism between 46 and 84 % (P<0.05). Additionally, in a separate experiment (Trial 2), the anthelmintic activity of the best monoterpene ?candidate? was evaluated in lambs. Six lambs artificially infected with 2000 Haemonchus contortus larvae each were treated with CNE (the best candidate from Trial 1) at 100 mg/kg orally, four times every 24 h. The fecal eggs count (FEC) reduction was measured at 7, 14 and 21 days post-administration of the first dose of CNE. The FEC reduction after the in vivo administration of CNE to infected lambs was 85 % (7 d), 88 % (14 d) and 82 (21 d). Integrated in-vitro-in vivo assays are critical for the design of successful alternative parasite control strategies based on the use of bioactive phytochemicals.
publishDate 2021
dc.date.none.fl_str_mv 2021
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dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/156969
Monoterpenes as potential tools to improve the activity of synthetic anthelmintics: pharmacological screening of their effects on drug metabolism and intestinal accumulation; 28th International Conference of the World Association for the Advancement of Veterinary Parasitology; Dublin; Irlanda; 2021; 1-2
CONICET Digital
CONICET
url http://hdl.handle.net/11336/156969
identifier_str_mv Monoterpenes as potential tools to improve the activity of synthetic anthelmintics: pharmacological screening of their effects on drug metabolism and intestinal accumulation; 28th International Conference of the World Association for the Advancement of Veterinary Parasitology; Dublin; Irlanda; 2021; 1-2
CONICET Digital
CONICET
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dc.publisher.none.fl_str_mv World Association for the Advancement of Veterinary Parasitology
publisher.none.fl_str_mv World Association for the Advancement of Veterinary Parasitology
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repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
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