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Design and synthesis of novel quinic acid derivatives: in vitro cytotoxicity and anticancer effect on glioblastoma

dc.contributor.authorMurugesan, Akshaya
dc.contributor.authorHolmstedt, Suvi
dc.contributor.authorBrown, Kenna C.
dc.contributor.authorKoivuporras, Alisa
dc.contributor.authorMacedo, Ana S.
dc.contributor.authorNguyen, Nga
dc.contributor.authorFonte, Pedro
dc.contributor.authorRijo, Patricia
dc.contributor.authorYli-Harja, Olli
dc.contributor.authorCandeias, Nuno R.
dc.contributor.authorKandhavelu, Meenakshisundaram
dc.date.accessioned2021-06-24T11:35:09Z
dc.date.available2021-06-24T11:35:09Z
dc.date.issued2020-11
dc.description.abstractAim: Quinic acid (QA) is a cyclic polyol exhibiting anticancer properties on several cancers. However, potential role of QA-derivatives against glioblastoma is not well established. Methodology & results: Sixteen novel QA-derivatives and QA-16 encapsulated poly (lactic-co-glycolic acid) nanoparticles (QA-16-NPs) were screened for their anti-glioblastoma effect using standard cell and molecular biology methods. Presence of a tertiary hydroxy and silylether groups in the lead compound were identified for the antitumor activity. QA-16 have 90% inhibition with the IC50 of 10.66 mu M and 28.22 mu M for LN229 and SNB19, respectively. The induction of apoptosis is faster with the increased fold change of caspase 3/7 and reactive oxygen species. Conclusion: QA-16 and QA-16-NPs shows similar cytotoxicity effect, providing opportunity to use QA-16 as a potential chemotherapeutic agent.
dc.description.sponsorshipAcademy of Finland European Commission [297200, 326487, 326486]
dc.description.sponsorshipFinnish Cultural FoundationFinnish Cultural Foundation [00190336]
dc.description.sponsorshipFCT - Foundation for Science and TechnologyPortuguese Foundation for Science and Technology [UIDB/04326/2020, UIDB/04565/2020, UIDB/50006/2020]
dc.description.versioninfo:eu-repo/semantics/publishedVersion
dc.identifier.doi10.4155/fmc-2020-0194
dc.identifier.issn1756-8919
dc.identifier.urihttp://hdl.handle.net/10400.1/16356
dc.language.isoeng
dc.peerreviewedyes
dc.publisherFuture Sci Ltd
dc.subjectChemotherapeutic drugs
dc.subjectCytotoxicity
dc.subjectGlioblastoma
dc.subjectNanoparticle
dc.subjectPLGA
dc.subjectQuinic acid
dc.subject.otherPharmacology & Pharmacy
dc.titleDesign and synthesis of novel quinic acid derivatives: in vitro cytotoxicity and anticancer effect on glioblastoma
dc.typejournal article
dspace.entity.typePublication
oaire.citation.endPage1910
oaire.citation.issue21
oaire.citation.startPage1891
oaire.citation.titleFuture Medicinal Chemistry
oaire.citation.volume12
person.familyNameFonte
person.givenNamePedro
person.identifier.ciencia-id2410-123D-3385
person.identifier.orcid0000-0002-1115-9282
person.identifier.ridK-3215-2013
person.identifier.scopus-author-id55146900200
rcaap.rightsrestrictedAccess
rcaap.typearticle
relation.isAuthorOfPublicationa5a5c2b2-9112-4bf4-8618-8c2051bbc116
relation.isAuthorOfPublication.latestForDiscoverya5a5c2b2-9112-4bf4-8618-8c2051bbc116

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