Human ABCB1 confers cells resistance to cytotoxic guanidine alkaloids from Pterogyne nitens

dc.contributorUniversidade Estadual Paulista (UNESP)
dc.creatorSatake, Kazuhiro
dc.creatorTsukamoto, Megumi
dc.creatorMitani, Yuji
dc.creatorRegasini, Luis Octavio
dc.creatorBolzani, Vanderlan da Silva
dc.creatorEfferth, Thomas
dc.creatorNakagawa, Hiroshi
dc.date2015-10-21T20:24:10Z
dc.date2016-10-25T21:08:24Z
dc.date2015-10-21T20:24:10Z
dc.date2016-10-25T21:08:24Z
dc.date2015-01-01
dc.date.accessioned2017-04-06T09:07:07Z
dc.date.available2017-04-06T09:07:07Z
dc.identifierBio-medical Materials And Engineering. Amsterdam: Ios Press, v. 25, n. 3, p. 249-256, 2015.
dc.identifier0959-2989
dc.identifierhttp://hdl.handle.net/11449/129119
dc.identifierhttp://acervodigital.unesp.br/handle/11449/129119
dc.identifierhttp://dx.doi.org/10.3233/BME-151282
dc.identifierWOS:000356538400003
dc.identifierhttp://content.iospress.com/articles/bio-medical-materials-and-engineering/bme1282
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/939674
dc.descriptionMultidrug resistance (MDR) caused by human ABCB1 (P-glycoprotein/MDR1) is one of the major obstacles in chemotherapy. To understand the mechanism of MDR by ABCB1 and circumvent the MDR, in the present study, we established human ABCB1-expressing cells (Flp-In-293/ABCB1 cells) and examined the cytotoxic effects of four guanidine alkaloids from Pterogyne nitens (galegine, nitensidine A, pterogynidine and pterogynine) using Flp-In-293/Mock and Flp-In-293/ABCB1 cells. The activity of ABCB1 in Flp-In-293/ABCB1 cells were confirmed by typical substrates for ABCB1 (taxol and vinblastine) in MTT assay. Flp-In-293/ABCB1 cells were also resistant to the four guanidine alkaloids as well as taxol and vinblastine compared to Flp-In-293/Mock cells although the four guanidine alkaloids exhibited cytotoxicity against the two Flp-In-293 cells. Furthermore, the four guanidine alkaloids were also found to stimulate the ATPase activity of ABCB1 in ATPase assays. These results suggest that ABCB1 can confer the resistance to the cytotoxic guanidine alkaloids by transporting them.
dc.descriptionFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.languageeng
dc.publisherIos Press
dc.relationBio-medical Materials And Engineering
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectABCB1
dc.subjectP-glycoprotein
dc.subjectATP-binding cassette (ABC) transporter
dc.subjectGuanidine alkaloids
dc.titleHuman ABCB1 confers cells resistance to cytotoxic guanidine alkaloids from Pterogyne nitens
dc.typeOtro


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