Evaluation of the intestinal absorption mechanism of casearin X in Caco-2 cells with Modified carboxylesterase activity
dc.accessRights | Anonymous | |
dc.audience | Science | |
dc.contributor.author | Moreira da Silva, Rodrigo | |
dc.contributor.author | Verjee, Sheela | |
dc.contributor.author | De Gaitani, Cristiane Masetto | |
dc.contributor.author | Moraes de Oliveira, Anderson Rodrigo | |
dc.contributor.author | Pires Bueno, Paula Carolina | |
dc.contributor.author | Cavalheiro, Alberto José | |
dc.contributor.author | Peporine Lopes, Norberto | |
dc.contributor.author | Butterweck, Veronika | |
dc.date.accessioned | 2016-11-09T10:58:10Z | |
dc.date.available | 2016-11-09T10:58:10Z | |
dc.date.issued | 2016 | |
dc.description.abstract | The 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.doi | 10.1021/acs.jnatprod.5b01139 | |
dc.identifier.issn | 0163-3864 | |
dc.identifier.issn | 1520-6025 | |
dc.identifier.uri | http://hdl.handle.net/11654/23426 | |
dc.issue | 4 | |
dc.language.iso | en | en_US |
dc.publisher | American Chemical Society | en_US |
dc.relation.ispartof | Journal of Natural Products | en_US |
dc.title | Evaluation of the intestinal absorption mechanism of casearin X in Caco-2 cells with Modified carboxylesterase activity | |
dc.type | 01A - Beitrag in wissenschaftlicher Zeitschrift | |
dc.volume | 79 | |
dspace.entity.type | Publication | |
fhnw.InventedHere | Yes | |
fhnw.IsStudentsWork | no | |
fhnw.PublishedSwitzerland | No | |
fhnw.ReviewType | Anonymous ex ante peer review of a complete publication | |
fhnw.affiliation.hochschule | Hochschule für Life Sciences | de_CH |
fhnw.affiliation.institut | Institut für Medizintechnik und Medizininformatik | de_CH |
fhnw.pagination | 1084-1090 | |
fhnw.publicationOnline | Ja | |
fhnw.publicationState | Published | |
relation.isAuthorOfPublication | 169478d0-7102-45a6-9427-1d60caa2e5cf | |
relation.isAuthorOfPublication.latestForDiscovery | 169478d0-7102-45a6-9427-1d60caa2e5cf |
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