Relationship between phosphatase activity and cytotoxic effect of two protein phosphatase inhibitors, okadaic acid and pervanadate, on human myeloid leukemia cell line

dc.creatorFreire, ACG
dc.creatorAoyama, H
dc.creatorHaun, M
dc.creatorFerreira, CV
dc.date2003
dc.dateAUG
dc.date2014-11-15T09:05:50Z
dc.date2015-11-26T17:19:12Z
dc.date2014-11-15T09:05:50Z
dc.date2015-11-26T17:19:12Z
dc.date.accessioned2018-03-29T00:06:52Z
dc.date.available2018-03-29T00:06:52Z
dc.identifierJournal Of Enzyme Inhibition And Medicinal Chemistry. Taylor & Francis Ltd, v. 18, n. 5, n. 425, n. 429, 2003.
dc.identifier1475-6366
dc.identifierWOS:000184981900007
dc.identifier10.1080/147563031000155634
dc.identifierhttp://www.repositorio.unicamp.br/jspui/handle/REPOSIP/80139
dc.identifierhttp://www.repositorio.unicamp.br/handle/REPOSIP/80139
dc.identifierhttp://repositorio.unicamp.br/jspui/handle/REPOSIP/80139
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/1282845
dc.descriptionProtein phosphatases are signalling molecules that regulate a variety of fundamental cellular processes including cell growth, metabolism and apoptosis. The aim of this work was to correlate the cytotoxicity of pervanadate and okadaic acid on HL60 cells and their effect on the phosphatase obtained from these cells. The cytotoxicity of these protein phosphatase inhibitors was evaluated on HL60 cells using phosphatase activity, protein quantification and MTT reduction as indices. The major phosphatase presents in the cellular extract showed high activity (80%) and affinity (Km=0.08 mM) to tyrosine phosphate in relation to p -nitrophenyl phosphate (pNPP)--(Km=0.51 mM). Total phosphatase (pNPP) was inhibited in the presence of 10 mM vanadate (98%), 200 muM pervanadate (95%) and 100 muM p-chloromercuribenzoate (80%) but okadaic acid caused a slight increase in enzyme activity (25%). When the HL60 cells were treated with the phosphatase inhibitors (pervanadate and okadaic acid) for 24 hours, only 20% residual activity was observed in presence of 200 muM pervanadate, whereas in the presence of okadaic acid this inhibitory effect was not observed. However, in respect to mitochondrial function, cell viability decreased about 80% in the presence of 100 nM okadaic acid. The total protein content was decreased 25% when the cells were treated with 100 nM okadaic acid in combination with 200 muM pervanadate. Our results suggest that both phosphatase inhibitors presented different mechanisms of action on HL60 cells. However, their effect on the cell redox status have to be considered.
dc.description18
dc.description5
dc.description425
dc.description429
dc.languageen
dc.publisherTaylor & Francis Ltd
dc.publisherAbingdon
dc.publisherInglaterra
dc.relationJournal Of Enzyme Inhibition And Medicinal Chemistry
dc.relationJ. Enzym. Inhib. Med. Chem.
dc.rightsfechado
dc.rightshttp://journalauthors.tandf.co.uk/permissions/reusingOwnWork.asp
dc.sourceWeb of Science
dc.subjectpervanadate
dc.subjectokadaic acid
dc.subjectcytotoxicity
dc.subjectHL60
dc.subjectprotein phosphatase
dc.subjectTyrosine Phosphatases
dc.subjectVanadate
dc.titleRelationship between phosphatase activity and cytotoxic effect of two protein phosphatase inhibitors, okadaic acid and pervanadate, on human myeloid leukemia cell line
dc.typeArtículos de revistas


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