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Isorhamnetin derivatives and piscidic acid for hypercholesterolemia: cholesterol permeability, HMG-CoA reductase inhibition, and docking studies

2017-11Journal article Restricted access
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dc.contributor.authorRESSAISSI, Asma
dc.contributor.authorATTIA, Nebil
dc.contributor.authorFalé, Pedro Luís
dc.contributor.authorPacheco, Rita
dc.contributor.authorVictor, Bruno L.
dc.contributor.authorMachuqueiro, Miguel
dc.contributor.authorSerralheiro, Maria Luísa M.
dc.date.accessioned2018-02-27T14:31:36Z
dc.date.available2018-02-27T14:31:36Z
dc.date.issued2017-11
dc.description.abstractBioactive compounds, such as isorhamnetin and piscidic acid, were obtained from decoctions of cladodes (stem pads from Opuntia ficus-indica). The effect of these phenolic compounds, in a fiber-free extract, were evaluated as inhibitors of cholesterol permeation through a Caco-2 cell monolayer and as 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor. A reduction of 38% in cholesterol permeation through the Caco-2 cell monolayer was obtained, and the phenolic compounds all permeated between 6 and 9%. A mixture of these compounds showed an IC50 of 20.3 mu g/mL as an enzyme inhibitor, whereas piscidic acid alone showed an IC50 of 149.6 mu g/mL; this was slightly outperformed by the isorhamnetin derivatives. Docking studies confirmed that both piscidic acid and isorhamnetin derivatives, present in the decoction, could adequately bind to the enzyme active site. These results reveal that O. ficus-indica, and cladodes derived there from, is a promising plant for use in the development of new functional foods and pharmaceutical products.pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.citationRESSAISSI, Asma; [et al] – Isorhamnetin derivatives and piscidic acid for hypercholesterolemia: cholesterol permeability, HMG-CoA reductase inhibition, and docking studies. Archives of Pharmacal Research. ISSN 0253-6269. Vol. 40, N.º 11, (2017), pp. 1278-1286.pt_PT
dc.identifier.doi10.1007/s12272-017-0959-1pt_PT
dc.identifier.issn0253-6269
dc.identifier.issn1976-3786
dc.identifier.urihttp://hdl.handle.net/10400.21/8143
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherSpringer Publishing Companypt_PT
dc.relation.publisherversionhttps://link.springer.com/content/pdf/10.1007%2Fs12272-017-0959-1.pdfpt_PT
dc.subjectIsorhamnetin derivativespt_PT
dc.subjectCholesterol permeabilitypt_PT
dc.subjectCell linespt_PT
dc.subjectHMG-CoA reductasept_PT
dc.subjectDocking studiespt_PT
dc.subjectPiscidic acidpt_PT
dc.titleIsorhamnetin derivatives and piscidic acid for hypercholesterolemia: cholesterol permeability, HMG-CoA reductase inhibition, and docking studiespt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/5876/UID%2FMulti%2F00612%2F2013/PT
oaire.citation.endPage1286pt_PT
oaire.citation.issue11pt_PT
oaire.citation.startPage1278pt_PT
oaire.citation.titleArchives of Pharmacal Researchpt_PT
oaire.citation.volume40pt_PT
oaire.fundingStream5876
person.familyNameRESSAISSI
person.familyNameATTIA
person.familyNamePacheco
person.familyNameMachuqueiro
person.givenNameAsma
person.givenNameNebil
person.givenNameRita
person.givenNameMiguel
person.identifier1022927
person.identifier1433605
person.identifier.ciencia-id9F13-D310-B5A3
person.identifier.ciencia-idD416-CB5B-AC3D
person.identifier.orcid0000-0002-0073-6785
person.identifier.orcid0000-0002-9945-3143
person.identifier.orcid0000-0001-5192-3006
person.identifier.orcid0000-0001-6923-8744
person.identifier.ridC-3062-2012
person.identifier.ridC-8012-2011
person.identifier.scopus-author-id8853708300
person.identifier.scopus-author-id57221975472
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.nameFundação para a Ciência e a Tecnologia
rcaap.rightsclosedAccesspt_PT
rcaap.typearticlept_PT
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