Differential activation of protein kinase C isoforms by euxanthone, revealed by an in vivo yeast phenotypic assay.
The protein kinase C (PKC) modulatory effects of euxanthone, isolated from the wood of Cratoxylum maingayi, on isoforms alpha, betaI, delta, eta and zeta were characterised using an alternative in vivo yeast phenotypic assay. The present study shows that euxanthone can activate isoforms alpha, betaI, delta, eta and zeta, being more effective on PKC-betaI, -delta, -eta and -zeta than the established PKC activators used (the phorbol ester PMA and arachidonic acid for PKC-zeta). Furthermore, euxanthone presents differences on its potency towards individual PKC isoforms, showing a remarkable selectivity for PKC-zeta. These results can help to clarify the molecular basis of the euxanthone-mediated effects.
Saraiva
Lucília
L
Fresco
Paula
P
Pinto
Eugénia
E
Kijjoa
Anake
A
Gonzalez
Maria José
MJ
Gonçalves
Jorge
J
D028084:Clusiaceae; D004305:Dose-Response Relationship, Drug; D006801:Humans; D020128:Inhibitory Concentration 50; D007527:Isoenzymes / Q000187:drug effects / Q000378:metabolism; D010641:Phenotype; D008517:Phytotherapy; D011493:Protein Kinase C / Q000187:drug effects* / Q000378:metabolism; D014966:Xanthenes / Q000008:administration & dosage / Q000494:pharmacology*; D044004:Xanthones; D015003:Yeasts / Q000187:drug effects* / Q000235:genetics / Q000378:metabolism
D007527:Isoenzymes; D014966:Xanthenes; D044004:Xanthones; C404221:euxanthone; D011493:Protein Kinase C