Role of two efflux proteins, ABCB1 and ABCG2 in blood-brain barrier transport of bromocriptine in a murine model of MPTP-induced dopaminergic degeneration

Purpose: MPTP-induced dopaminergic degeneration is an experimental model commonly used to explore Parkinson’s disease. Cerebral drug transport by ABC transporters in MPTP models has never been reported. Methods: We have investigated the transport of bromocriptine through the blood-brain barrier (BBB...

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Main Author: Milane, Aline (author)
Other Authors: Vautier, Sarah (author), Fernandez, Christine (author), Chacun, Helene (author), Lacomble, Luccette (author), Farinotti, Robert (author)
Format: article
Published: 2009
Online Access:http://hdl.handle.net/10725/4500
http://dx.doi.org/10.18433/J3B596
http://libraries.lau.edu.lb/research/laur/terms-of-use/articles.php
https://ejournals.library.ualberta.ca/index.php/JPPS/article/view/1521
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_version_ 1864513463688101888
author Milane, Aline
author2 Vautier, Sarah
Fernandez, Christine
Chacun, Helene
Lacomble, Luccette
Farinotti, Robert
author2_role author
author
author
author
author
author_facet Milane, Aline
Vautier, Sarah
Fernandez, Christine
Chacun, Helene
Lacomble, Luccette
Farinotti, Robert
author_role author
dc.creator.none.fl_str_mv Milane, Aline
Vautier, Sarah
Fernandez, Christine
Chacun, Helene
Lacomble, Luccette
Farinotti, Robert
dc.date.none.fl_str_mv 2009
2016-10-04T10:29:07Z
2016-10-04T10:29:07Z
2016-10-04
dc.identifier.none.fl_str_mv 1482-1826
http://hdl.handle.net/10725/4500
http://dx.doi.org/10.18433/J3B596
Vautier, S., Milane, A., Fernandez, C., Chacun, H., Lacomblez, L., & Farinotti, R. (2009). Role of two efflux proteins, ABCB1 and ABCG2 in blood-brain barrier transport of bromocriptine in a murine model of MPTP-induced dopaminergic degeneration. Journal of Pharmacy & Pharmaceutical Sciences, 12(2), 199-208.
http://libraries.lau.edu.lb/research/laur/terms-of-use/articles.php
https://ejournals.library.ualberta.ca/index.php/JPPS/article/view/1521
dc.language.none.fl_str_mv en
dc.relation.none.fl_str_mv Journal of Pharmacy and Pharmaceutical Sciences
dc.rights.*.fl_str_mv info:eu-repo/semantics/openAccess
dc.title.none.fl_str_mv Role of two efflux proteins, ABCB1 and ABCG2 in blood-brain barrier transport of bromocriptine in a murine model of MPTP-induced dopaminergic degeneration
dc.type.none.fl_str_mv Article
info:eu-repo/semantics/publishedVersion
info:eu-repo/semantics/article
description Purpose: MPTP-induced dopaminergic degeneration is an experimental model commonly used to explore Parkinson’s disease. Cerebral drug transport by ABC transporters in MPTP models has never been reported. Methods: We have investigated the transport of bromocriptine through the blood-brain barrier (BBB) in a MPTP model to understand the influence of the dopaminergic degeneration on ABCB1 and ABCG2. Results: We have shown that in MPTP treated mice, bromocriptine is widely distributed to brain (2.3-fold versus control, p<0.001) suggesting either disruption of BBB or alteration of active efflux of the drug. The investigation of BBB did not evidence a modification of permeability. Studies of ABCB1 and ABCG2 activity showed that MPTP intoxication did not alter their functionality. Conversely, ABCG2 expression studied on brain capillaries from MPTP-treated mice was decreased (1.3-fold, p<0.05) and ABCB1 expression increased (1.43-fold, p<0.05) as an off-setting of brain transport. Conclusions: These data demonstrate that MPTP intoxication does not alter BBB permeability. However, bromocriptine brain distribution is increased in MPTP animals. Hence, MPTP may interact with another transport mechanism such as uptake and/or other efflux transporters. Inflammation and Parkinson’s-like lesions induced by MPTP intoxication could lead to modification of drug pharmacokinetics and have clinical consequences, such as neurotoxicity.
eu_rights_str_mv openAccess
format article
id LAURepo_3bb45486302b7fc495f284a44f7e4156
identifier_str_mv 1482-1826
Vautier, S., Milane, A., Fernandez, C., Chacun, H., Lacomblez, L., & Farinotti, R. (2009). Role of two efflux proteins, ABCB1 and ABCG2 in blood-brain barrier transport of bromocriptine in a murine model of MPTP-induced dopaminergic degeneration. Journal of Pharmacy & Pharmaceutical Sciences, 12(2), 199-208.
language_invalid_str_mv en
network_acronym_str LAURepo
network_name_str Lebanese American University repository
oai_identifier_str oai:laur.lau.edu.lb:10725/4500
publishDate 2009
repository.mail.fl_str_mv
repository.name.fl_str_mv
repository_id_str
spelling Role of two efflux proteins, ABCB1 and ABCG2 in blood-brain barrier transport of bromocriptine in a murine model of MPTP-induced dopaminergic degenerationMilane, AlineVautier, SarahFernandez, ChristineChacun, HeleneLacomble, LuccetteFarinotti, RobertPurpose: MPTP-induced dopaminergic degeneration is an experimental model commonly used to explore Parkinson’s disease. Cerebral drug transport by ABC transporters in MPTP models has never been reported. Methods: We have investigated the transport of bromocriptine through the blood-brain barrier (BBB) in a MPTP model to understand the influence of the dopaminergic degeneration on ABCB1 and ABCG2. Results: We have shown that in MPTP treated mice, bromocriptine is widely distributed to brain (2.3-fold versus control, p<0.001) suggesting either disruption of BBB or alteration of active efflux of the drug. The investigation of BBB did not evidence a modification of permeability. Studies of ABCB1 and ABCG2 activity showed that MPTP intoxication did not alter their functionality. Conversely, ABCG2 expression studied on brain capillaries from MPTP-treated mice was decreased (1.3-fold, p<0.05) and ABCB1 expression increased (1.43-fold, p<0.05) as an off-setting of brain transport. Conclusions: These data demonstrate that MPTP intoxication does not alter BBB permeability. However, bromocriptine brain distribution is increased in MPTP animals. Hence, MPTP may interact with another transport mechanism such as uptake and/or other efflux transporters. Inflammation and Parkinson’s-like lesions induced by MPTP intoxication could lead to modification of drug pharmacokinetics and have clinical consequences, such as neurotoxicity.PublishedN/A2016-10-04T10:29:07Z2016-10-04T10:29:07Z20092016-10-04Articleinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article1482-1826http://hdl.handle.net/10725/4500http://dx.doi.org/10.18433/J3B596Vautier, S., Milane, A., Fernandez, C., Chacun, H., Lacomblez, L., & Farinotti, R. (2009). Role of two efflux proteins, ABCB1 and ABCG2 in blood-brain barrier transport of bromocriptine in a murine model of MPTP-induced dopaminergic degeneration. Journal of Pharmacy & Pharmaceutical Sciences, 12(2), 199-208.http://libraries.lau.edu.lb/research/laur/terms-of-use/articles.phphttps://ejournals.library.ualberta.ca/index.php/JPPS/article/view/1521enJournal of Pharmacy and Pharmaceutical Sciencesinfo:eu-repo/semantics/openAccessoai:laur.lau.edu.lb:10725/45002021-03-19T10:03:18Z
spellingShingle Role of two efflux proteins, ABCB1 and ABCG2 in blood-brain barrier transport of bromocriptine in a murine model of MPTP-induced dopaminergic degeneration
Milane, Aline
status_str publishedVersion
title Role of two efflux proteins, ABCB1 and ABCG2 in blood-brain barrier transport of bromocriptine in a murine model of MPTP-induced dopaminergic degeneration
title_full Role of two efflux proteins, ABCB1 and ABCG2 in blood-brain barrier transport of bromocriptine in a murine model of MPTP-induced dopaminergic degeneration
title_fullStr Role of two efflux proteins, ABCB1 and ABCG2 in blood-brain barrier transport of bromocriptine in a murine model of MPTP-induced dopaminergic degeneration
title_full_unstemmed Role of two efflux proteins, ABCB1 and ABCG2 in blood-brain barrier transport of bromocriptine in a murine model of MPTP-induced dopaminergic degeneration
title_short Role of two efflux proteins, ABCB1 and ABCG2 in blood-brain barrier transport of bromocriptine in a murine model of MPTP-induced dopaminergic degeneration
title_sort Role of two efflux proteins, ABCB1 and ABCG2 in blood-brain barrier transport of bromocriptine in a murine model of MPTP-induced dopaminergic degeneration
url http://hdl.handle.net/10725/4500
http://dx.doi.org/10.18433/J3B596
http://libraries.lau.edu.lb/research/laur/terms-of-use/articles.php
https://ejournals.library.ualberta.ca/index.php/JPPS/article/view/1521