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dc.contributor.authorSurichan, Somchaiyaen
dc.contributor.authorArroo, R. R. J.en
dc.contributor.authorRuparelia, K. C.en
dc.contributor.authorTsatsakis, A. M.en
dc.contributor.authorAndroutsopoulos, V.P.en
dc.date.accessioned2018-03-01T09:26:10Z
dc.date.available2018-03-01T09:26:10Z
dc.date.issued2018-01-31
dc.identifier.citationSurichan, S., Arroo, R.R., Ruparelia, K., Tsatsakis, A.M., Androutsopoulos, V.P. (2018) Nobiletin bioactivation in MDA-MB-468 breast cancer cells by cytochrome P450 CYP1 enzymes. Food and Chemical Toxicology, 113, pp. 228-235.en
dc.identifier.issn0278-6915
dc.identifier.urihttp://hdl.handle.net/2086/15314
dc.descriptionThe file attached to this record is the author's final peer reviewed version. The Publisher's final version can be found by following the DOI linken
dc.description.abstractNobiletin is a fully methoxylated flavone that has demonstrated anticancer activity via multiple modes of action. In the present study, the metabolism and further antiproliferative activity of nobiletin was evaluated in the CYP1 expressing human breast cancer cell line MDA–MB–468 and the normal breast cell line MCF10A. Nobiletin was metabolized in MDA–MB–468 cells to a single-demethylated derivative assigned NP1. This metabolite was absent in MCF10A cells that did not express CYP1 enzymes. Nobiletin exhibited submicromolar IC50 (0.1±0.04 μM) in MDA–MB–468 cells, whereas it was considerably less active in MCF10A cells (40 μM). In the presence of the CYP1 inhibitor acacetin, the conversion of nobiletin to NP1 was significantly reduced in MDA–MB–468 cells. Furthermore, a significant increase was noted in the population of the cells at the G1 phase, following treatment with nobiletin (10 μM) for 24 h compared with the control cells treated with DMSO (0.1%) alone (55.9±0.14 vs. 45.6±1.96), whereas the cell cycle of MCF10A cells was not significantly altered under the same treatment conditions. Taken collectively, the results suggest that nobiletin is selectively bioactivated in MDA–MB–468 breast cancer cells via metabolism by the CYP1 family of enzymes.en
dc.language.isoenen
dc.publisherElsevieren
dc.subjectFlavonoidsen
dc.subjectnobiletinen
dc.subjectCytochrome P450en
dc.subjectAntiproliferationen
dc.subjectcanceren
dc.titleNobiletin bioactivation in MDA-MB-468 breast cancer cells by cytochrome P450 CYP1 enzymes.en
dc.typeArticleen
dc.identifier.doihttps://doi.org/10.1016/j.fct.2018.01.047
dc.peerreviewedYesen
dc.funderPharmaceutical Organization in Thailanden
dc.funderUniversity of Crete ELKE granten
dc.projectidUniversity of Crete ELKE grant KA2590en
dc.cclicenceCC-BY-NCen
dc.date.acceptance2018-01-27en
dc.researchinstituteLeicester Institute for Pharmaceutical Innovation - From Molecules to Practice (LIPI)en


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