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dc.contributor.authorVillagomez, Rodrigo
dc.contributor.authorRodrigo, Gloria C.
dc.contributor.authorCollado, Isidro G.
dc.contributor.authorCalzado, Marco A.
dc.contributor.authorMuñoz, Eduardo
dc.contributor.authorÅkesson, Björn
dc.contributor.authorSterner, Olov
dc.contributor.authorAlmanza, Giovanna R.
dc.contributor.authorDuan, Rui-Dong
dc.date.accessioned2014-10-20T12:43:23Z
dc.date.available2014-10-20T12:43:23Z
dc.date.issued2013-09
dc.identifier.citationAnticancer Res. 2013, 33 (9):3799-3805.en
dc.identifier.issn1791-7530
dc.identifier.pmid24023312
dc.identifier.urihttp://hdl.handle.net/10146/332936
dc.description.abstractTerpenoids in plants are important sources for drug discovery. In this study, we extracted damsin and coronopilin, two sesquiterpene lactones, from Ambrosia arborescens and examined their anticancer effects on cell cultures. Damsin and coronopilin inhibited cell proliferation, DNA biosynthesis and formation of cytoplasmic DNA histone complexes in Caco-2 cells, with damsin being more potent than coronopilin. Further studies using the luciferase reporter system showed that damsin and coronopilin also inhibited expressions of nuclear factor-κB (NF-κB) and signal transducer and activator of transcription-3 (STAT3), indicating that these sesquiterpenes can interfere with NF-κB and STAT3 pathways. Finally, we examined the effects of two synthetic dibrominated derivatives of damsin, 11α,13-dibromodamsin and 11β,13-dibromodamsin. While bromination appeared to weaken the antiproliferative effects of damsin, the β epimer had strong inhibitory effects on STAT3 activation. In conclusion, the sesquiterpene lactones damsin and coronopilin have inhibitory effects on cell proliferation, DNA biosynthesis and NF-κB and STAT3 pathways, thus being potentially important for discovery of drugs against cancer.
dc.description.sponsorshipThe study was supported by the Swedish International Development Agency to a joint project on Plant Biodiversity between the Major University of San Andres, La Paz, Bolivia and Lund University, Sweden. Support was also obtained from the EU NoE ECNIS (513943) and its successor ECNIS2.en
dc.language.isoenen
dc.relation.urlhttp://ar.iiarjournals.org/content/33/9/3799.longen
dc.rightsArchived with thanks to Anticancer researchen
dc.subjectAmbrosia arborescensen
dc.subjectDamsinen
dc.subjectCoronopilinen
dc.subjectSesquiterpenesen
dc.subjectApoptosisen
dc.subjectCell proliferationen
dc.subjectChemoselective brominationen
dc.subjectAnticancer effectsen
dc.subject.meshAmbrosia
dc.subject.meshAntineoplastic Agents, Phytogenic
dc.subject.meshAzulenes
dc.subject.meshCell Line, Tumor
dc.subject.meshCell Proliferation
dc.subject.meshDNA Replication
dc.subject.meshEnzyme-Linked Immunosorbent Assay
dc.subject.meshHumans
dc.subject.meshLactones
dc.subject.meshNF-kappa B
dc.subject.meshNeoplasms
dc.subject.meshSTAT3 Transcription Factor
dc.subject.meshSesquiterpenes
dc.titleMultiple anticancer effects of damsin and coronopilin isolated from Ambrosia arborescens on cell cultures.en
dc.typeArticleen
dc.identifier.journalAnticancer Researchen
html.description.abstractTerpenoids in plants are important sources for drug discovery. In this study, we extracted damsin and coronopilin, two sesquiterpene lactones, from Ambrosia arborescens and examined their anticancer effects on cell cultures. Damsin and coronopilin inhibited cell proliferation, DNA biosynthesis and formation of cytoplasmic DNA histone complexes in Caco-2 cells, with damsin being more potent than coronopilin. Further studies using the luciferase reporter system showed that damsin and coronopilin also inhibited expressions of nuclear factor-κB (NF-κB) and signal transducer and activator of transcription-3 (STAT3), indicating that these sesquiterpenes can interfere with NF-κB and STAT3 pathways. Finally, we examined the effects of two synthetic dibrominated derivatives of damsin, 11α,13-dibromodamsin and 11β,13-dibromodamsin. While bromination appeared to weaken the antiproliferative effects of damsin, the β epimer had strong inhibitory effects on STAT3 activation. In conclusion, the sesquiterpene lactones damsin and coronopilin have inhibitory effects on cell proliferation, DNA biosynthesis and NF-κB and STAT3 pathways, thus being potentially important for discovery of drugs against cancer.


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