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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.identifier.issn0163-3864
dc.identifier.doi10.1021/acs.jnatprod.5b01139
dc.identifier.urihttp://hdl.handle.net/11654/23426
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.description.urihttp://pubs.acs.org/doi/abs/10.1021/acs.jnatprod.5b01139
dc.language.isoen
dc.relation.ispartofJournal of Natural Products
dc.accessRightsAnonymous
dc.titleEvaluation of the intestinal absorption mechanism of casearin X in Caco-2 cells with Modified carboxylesterase activity
dc.type01 - Zeitschriftenartikel, Journalartikel oder Magazin
dc.volume79
dc.issue4
dc.audienceScience
fhnw.publicationStatePublished
fhnw.ReviewTypeAnonymous ex ante peer review of a complete publication
fhnw.InventedHereYes
fhnw.PublishedSwitzerlandNo
fhnw.pagination1084-1090
fhnw.IsStudentsWorkno
fhnw.publicationOnlineJa


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