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Discovery of a New Xanthone against Glioma: Synthesis and Development of (Pro)liposome Formulations

2019-01Journal article Open access
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dc.contributor.authorAlves, Ana
dc.contributor.authorCorreia-da-Silva, Marta
dc.contributor.authorNunes, Claúdia
dc.contributor.authorCampos, João
dc.contributor.authorSousa, Emília
dc.contributor.authorSilva, Patrícia
dc.contributor.authorBousbaa, Hassan
dc.contributor.authorRodrigues, Francisca
dc.contributor.authorFerreira, Domingos
dc.contributor.authorCosta, Paulo
dc.contributor.authorPinto, Madalena
dc.date.accessioned2020-10-30T14:57:30Z
dc.date.available2020-10-30T14:57:30Z
dc.date.issued2019-01
dc.description.abstractFollowing our previous work on the antitumor activity of acetylated flavonosides, a new acetylated xanthonoside, 3,6-bis(2,3,4,6-tetra-O-acetyl-β-glucopyranosyl)xanthone (2), was synthesized and discovered as a potent inhibitor of tumor cell growth. The synthesis involved the glycosylation of 3,6-di-hydroxyxanthone (1) with acetobromo-α-d-glucose. Glycosylation with silver carbonate decreased the amount of glucose donor needed, comparative to the biphasic glycosylation. Xanthone 2 showed a potent anti-growth activity, with GI50 < 1 μM, in human cell lines of breast, lung, and glioblastoma cancers. Current treatment for invasive brain glioma is still inadequate and new agents against glioblastoma with high brain permeability are urgently needed. To overcome these issues, xanthone 2 was encapsulated in a liposome. To increase the well-known low stability of these drug carriers, a proliposome formulation was developed using the spray drying method. Both formulations were characterized and compared regarding three months stability and in vitro anti-growth activity. While the proliposome formulation showed significantly higher stability, it was at the expense of losing its biocompatibility as a drug carrier in higher concentrations. More importantly, the new xanthone 2 was still able to inhibit the growth of glioblastoma cells after liposome formulation.pt_PT
dc.description.sponsorshipThis work was partially supported through national funds provided by FCT and European Regional Development Fund (ERDF) through the COMPETE—Programa Operacional Factores de Competitividade (POFC) programme, under the project PTDC/MAR-BIO/4694/2014 (POCI-01-0145-FEDER-016790 and Project 3599-PPCDT) in the framework of the programme PT2020pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.doi10.3390/molecules24030409pt_PT
dc.identifier.urihttp://hdl.handle.net/10400.22/16394
dc.language.isoengpt_PT
dc.publisherMDPIpt_PT
dc.relation.publisherversionhttps://www.mdpi.com/1420-3049/24/3/409/htmpt_PT
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/pt_PT
dc.subjectCarbonatespt_PT
dc.subjectTumor Cell Linespt_PT
dc.subjectCell Proliferationpt_PT
dc.subjectDrug Carrierspt_PT
dc.subjectGliomapt_PT
dc.subjectGlucosept_PT
dc.subjectGlycosylationpt_PT
dc.subjectHumanspt_PT
dc.subjectLiposomespt_PT
dc.subjectSilver Compoundspt_PT
dc.subjectXanthonespt_PT
dc.subjectNanotechnologypt_PT
dc.subjectProliposomespt_PT
dc.titleDiscovery of a New Xanthone against Glioma: Synthesis and Development of (Pro)liposome Formulationspt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.citation.issue3pt_PT
oaire.citation.startPage409pt_PT
oaire.citation.titleMoleculespt_PT
oaire.citation.volume24pt_PT
person.familyNamePinto Lisboa Martins Rodrigues Sarmento
person.givenNameFrancisca
person.identifier.ciencia-id4F19-3D98-2CBA
person.identifier.orcid0000-0001-8803-0041
rcaap.rightsopenAccesspt_PT
rcaap.typearticlept_PT
relation.isAuthorOfPublication176ed0e9-7da4-4265-bc19-50b694ea58ab
relation.isAuthorOfPublication.latestForDiscovery176ed0e9-7da4-4265-bc19-50b694ea58ab

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