Evaluation of the intestinal absorption mechanism of casearin X in Caco-2 cells with Modified carboxylesterase activity

dc.accessRightsAnonymous
dc.audienceScience
dc.contributor.authorMoreira da Silva, Rodrigo
dc.contributor.authorVerjee, Sheela
dc.contributor.authorDe Gaitani, Cristiane Masetto
dc.contributor.authorMoraes de Oliveira, Anderson Rodrigo
dc.contributor.authorPires Bueno, Paula Carolina
dc.contributor.authorCavalheiro, Alberto José
dc.contributor.authorPeporine Lopes, Norberto
dc.contributor.authorButterweck, Veronika
dc.date.accessioned2016-11-09T10:58:10Z
dc.date.available2016-11-09T10:58:10Z
dc.date.issued2016
dc.description.abstractThe clerodane diterpene casearin X (1)​, isolated from the leaves of Casearia sylvestris, is a potential new drug candidate due to its potent in vitro cytotoxic activity. In this work, the intestinal absorption mechanism of 1 was evaluated using Caco-​2 cells with and without active carboxylesterases (CES)​. An LC-​MS method was developed and validated for the quantification of 1. The estn. of permeability coeffs. was possible only under CES-​inhibited conditions in which 1 is able to cross the Caco-​2 cell monolayer. The mechanism is probably by active transport, with no significant efflux, but with a high retention of the compd. inside the cells. The enzymic hydrolysis assay demonstrates the susceptibility of 1 to first-​pass metab. as substrate for specific CES expressed in human intestine.
dc.identifier.doi10.1021/acs.jnatprod.5b01139
dc.identifier.issn0163-3864
dc.identifier.issn1520-6025
dc.identifier.urihttp://hdl.handle.net/11654/23426
dc.issue4
dc.language.isoenen_US
dc.publisherAmerican Chemical Societyen_US
dc.relation.ispartofJournal of Natural Productsen_US
dc.titleEvaluation of the intestinal absorption mechanism of casearin X in Caco-2 cells with Modified carboxylesterase activity
dc.type01A - Beitrag in wissenschaftlicher Zeitschrift
dc.volume79
dspace.entity.typePublication
fhnw.InventedHereYes
fhnw.IsStudentsWorkno
fhnw.PublishedSwitzerlandNo
fhnw.ReviewTypeAnonymous ex ante peer review of a complete publication
fhnw.affiliation.hochschuleHochschule für Life Sciencesde_CH
fhnw.affiliation.institutInstitut für Medizintechnik und Medizininformatikde_CH
fhnw.pagination1084-1090
fhnw.publicationOnlineJa
fhnw.publicationStatePublished
relation.isAuthorOfPublication169478d0-7102-45a6-9427-1d60caa2e5cf
relation.isAuthorOfPublication.latestForDiscovery169478d0-7102-45a6-9427-1d60caa2e5cf
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