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Apoptosis induction and modulation of P-glycoprotein mediated multidrug resistance by new macrocyclic lathyrane-type diterpenoids

dc.contributor.authorDuarte, Noelia
dc.contributor.authorVarga, Andras
dc.contributor.authorCherepnev, Georg
dc.contributor.authorRadics, Rita
dc.contributor.authorMolnar, Joseph
dc.contributor.authorFerreira, Maria-Jose U.
dc.date.accessioned2015-12-30T10:18:09Z
dc.date.available2015-12-30T10:18:09Z
dc.date.issued2007
dc.description.abstractThe macrocyclic lathyrane diterpenes, latilagascenes D-F (1-3) and jolkinol B (4), were isolated from the methanol extract of Euphorbia lagascae, and evaluated for multidrug resistance reversing activity on mouse lymphoma cells. All compounds displayed very strong activity compared with that of the positive control, verapamil. The structure-activity relationship is discussed. The evaluation of compounds 1 and 4, and of latigascenes A-C (5-7), isolated from the same species, as apoptosis-inducers was also carried out. Compound I was the most active. Furthermore, in the model of combination chemotherapy, the interaction between the doxorubicine and latilagascene B (6) was studied in vitro, on human MDR1 gene transfected mouse lymphoma cells, showing that the type of interaction was synergistic. Latilagascenes D-F (1-3) are new compounds whose structures were established on the basis of spectroscopic methods, including 2D NMR experiments (COSY, HMQC, HMBC and NOESY). (c) 2006 Elsevier Ltd. All rights reserved.
dc.formatapplication/pdf
dc.identifier.citationBIOORGANIC & MEDICINAL CHEMISTRY. - Vol. 15, n. 1 (2007), p. 546-554
dc.identifier.doihttp://dx.doi.org/10.1016/j.bmc.2006.09.028
dc.identifier.issn0968-0896
dc.identifier.urihttp://hdl.handle.net/10451/21437
dc.language.isoeng
dc.publisherPERGAMON-ELSEVIER SCIENCE LTD
dc.subjectBiochemistry & Molecular Biology
dc.subjectChemistry, Medicinal
dc.subjectChemistry, Organic
dc.titleApoptosis induction and modulation of P-glycoprotein mediated multidrug resistance by new macrocyclic lathyrane-type diterpenoids
dc.typejournal article
dspace.entity.typePublication
oaire.citation.endPage554por
oaire.citation.startPage546por
oaire.citation.titleBIOORGANIC & MEDICINAL CHEMISTRYpor
oaire.citation.volumeVol. 15por
rcaap.rightsrestrictedAccess
rcaap.typearticle

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