An in vitro comparative study with furyl-1,4-quinones endowed with anticancer activities

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dc.contributor.authorBenites, Julio
dc.contributor.authorValderrama, Jaime A.
dc.contributor.authorTaper, Henryk
dc.contributor.authorCalderon, Pedro Buc
dc.date.accessioned2025-01-21T00:00:51Z
dc.date.available2025-01-21T00:00:51Z
dc.date.issued2011
dc.description.abstractWe describe the biological activity of some furylbenzo- and naphthoquinones (furylquinones) on hepatocarcinoma cells and healthy rat liver slices. The effects of furylquinones on cancer cells (Transplantable Liver Tumor, TLT) were assessed by measuring cell death (membrane cell lysis); intracellular contents of ATP and GSH and the activity of caspase-3 were used to determine the type of cell death. Most of the furylquinones tested (at a concentration of 25 mu g/ml) induced caspase-independent cell death but compound 4 had no cytotoxic effects. The levels of both ATP and GSH were severely affected by quinones 1, 2 and 5, while no effect was observed with compound 4. These cytotoxic properties of quinones are associated with physico-chemical properties as shown by the LUMO energies and lipophilicity. Interestingly, no cytotoxic effects of furylquinones were detected when the in vitro model of precision-cut liver slices (PCLS) was used. Indeed, although CYP2E1 activity was slightly affected, ATP and GSH levels as well as protein synthesis were not modified by furylquinones. Paracetamol, a well-known hepatotoxicant, reduced these parameters by more than 80% compared to control conditions. Taking into account the considerable incidence of adverse-effects induced by most current anticancer drugs, the selective cytotoxicity shown by compounds 1, 2 and 5, in particular that of 1, represents a safety factor that encourages the further development of these quinones as new drugs in cancer therapy.
dc.description.funderUNAP
dc.fuente.origenWOS
dc.identifier.doi10.1007/s10637-010-9419-1
dc.identifier.issn0167-6997
dc.identifier.urihttps://doi.org/10.1007/s10637-010-9419-1
dc.identifier.urihttps://repositorio.uc.cl/handle/11534/95360
dc.identifier.wosidWOS:000294223500005
dc.issue.numero5
dc.language.isoen
dc.pagina.final767
dc.pagina.inicio760
dc.revistaInvestigational new drugs
dc.rightsacceso restringido
dc.subjectApoptosis
dc.subjectCancer therapy
dc.subjectCell death
dc.subjectOxidative stress
dc.subjectQuinones
dc.subject.ods03 Good Health and Well-being
dc.subject.odspa03 Salud y bienestar
dc.titleAn in vitro comparative study with furyl-1,4-quinones endowed with anticancer activities
dc.typeartículo
dc.volumen29
sipa.indexWOS
sipa.trazabilidadWOS;2025-01-12
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