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Antiproliferative effect and apoptotic activity of linear geranylphenol derivatives from phloroglucinol and orcinol

dc.contributor.authorTaborga L.
dc.contributor.authorEspinoza L.
dc.contributor.authorMoller A.
dc.contributor.authorCarrasco H.
dc.contributor.authorCuellar M.
dc.contributor.authorVillena J.
dc.date.accessioned2020-09-02T22:29:18Z
dc.date.available2020-09-02T22:29:18Z
dc.date.issued2016
dc.identifier10.1016/j.cbi.2016.01.016
dc.identifier.citation247, , 22-29
dc.identifier.issn00092797
dc.identifier.urihttps://hdl.handle.net/20.500.12728/6404
dc.descriptionSixteen synthetic linear derivatives geranylphenols, were obtained from phloroglucinol and orcinol, and cytotoxic activity was evaluated in vitro against cancer cell lines (HT-29, PC-3, MDA-MB231, DU-145) and one non-tumor cell line, human dermal fibroblast (HDF). IC50 values were determined at concentrations of 0-100 μM of each compound for 72 h. Compounds 12, 13, 17, 21, 22 and 25, showed cytotoxic activity. To elucidate whether these compounds reduce cell viability by inducing apoptosis, cell lines MCF-7, PC-3 and DHF were treated with each active compound 12, 13, 17, 21, 22 and 25 and were examined after Hoechst 33342 staining. The compounds 12, 13 and 17 induced apoptosis in various cancer cell lines, as shown by nuclear condensation and/or fragmentation. In addition, it was found that compounds 12 and 13, induced changes in mitochondrial membrane permeability in those cancer cell lines. Such induction was associated with the depletion of mitochondrial membrane potential. These activities led to the cleavage of caspases inducing the cell death process. © 2016 Elsevier Ireland Ltd. All rights reserved.
dc.language.isoen
dc.publisherElsevier Ireland Ltd
dc.subjectApoptosis
dc.subjectCancer cell lines
dc.subjectCaspase-3 activity
dc.subjectCytotoxic activity
dc.subjectLinear geranylphenols
dc.subjectMitochondrial membrane permeability
dc.subject2 (3,7 dimethylocta 2,6 dienyl) 1,3 dimethoxy 5 methylbenzene
dc.subject2 (3,7 dimethylocta 2,6 dienyl) 1,3,5 trimethoxybenzene
dc.subject2 (3,7 dimethylocta 2,6 dienyl) 1,5 dimethoxy 3 methylbenzene
dc.subject2 geranylphloroglucinol derivative
dc.subject2,4 bis (3,7 dimethyloctan 2,6 dienyl) 1,3 dimethoxy 5 methylbenzene
dc.subjectantineoplastic agent
dc.subjectcaspase 3
dc.subjectgeranylmethoxy derivative
dc.subjectunclassified drug
dc.subjectantineoplastic agent
dc.subjectorcinol
dc.subjectphloroglucinol
dc.subjectresorcinol derivative
dc.subjectantiproliferative activity
dc.subjectapoptosis
dc.subjectArticle
dc.subjectcell membrane permeability
dc.subjectcell viability
dc.subjectchromatin condensation
dc.subjectcontrolled study
dc.subjectcytotoxicity
dc.subjectdrug structure
dc.subjectdrug synthesis
dc.subjectenzyme activation
dc.subjectenzyme activity
dc.subjectfragmentation reaction
dc.subjecthuman
dc.subjecthuman cell
dc.subjectIC50
dc.subjectin vitro study
dc.subjectmitochondrial membrane potential
dc.subjectprotein cleavage
dc.subjectstructure activity relation
dc.subjectanalogs and derivatives
dc.subjectapoptosis
dc.subjectcell proliferation
dc.subjectdrug effects
dc.subjecttumor cell line
dc.subjectAntineoplastic Agents
dc.subjectApoptosis
dc.subjectCell Line, Tumor
dc.subjectCell Proliferation
dc.subjectHumans
dc.subjectPhloroglucinol
dc.subjectResorcinols
dc.titleAntiproliferative effect and apoptotic activity of linear geranylphenol derivatives from phloroglucinol and orcinol
dc.typeArticle


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