title: N-Caffeoyltyramine arrests growth of U937 and Jurkat cells by inhibiting protein tyrosine phosphorylation and inducing caspase-3.
abstract: N-Cinnamoyltyramine, N-caffeoyltyramine, N-feruloyltyramine, and N-sinapoyltyramine were synthesized and investigated to identify the most potent compound with anti-proliferation effect on HL-60, U937 and Jurkat cells. N-Caffeoyltyramine was the most potent with GI(50)=10 microM. The treatment of the cells with N-caffeoyltyramine activated caspase-3 activity, and inhibited the growth of cells via decreasing in protein tyrosine kinase activity including epidermal growth factor receptor. These data indicate that N-caffeoyltyramine is most potent compound, inducing cell death of the cancer cells by inhibiting protein tyrosine kinases and activating caspase-3 activity.
authors.affiliation: Phytonutrients Laboratory, US Department of Agriculture, Building 307, Room 313, PL, BHNRC, ARS, Beltsville, MD 20705, USA. park@307.bhnrc.usda.gov
authors.forename: Jae B
authors.initials: JB
authors.lastname: Park
authors.forename: Norberta
authors.initials: N
authors.lastname: Schoene
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology*; D002109:Caffeic Acids / Q000138:chemical synthesis / Q000494:pharmacology*; D053148:Caspase 3; D020169:Caspases / Q000187:drug effects*; D002455:Cell Division / Q000187:drug effects; D053938:DNA Fragmentation / Q000187:drug effects; D004789:Enzyme Activation / Q000187:drug effects; D066246:ErbB Receptors / Q000187:drug effects; D018922:HL-60 Cells; D006801:Humans; D019169:Jurkat Cells; D010766:Phosphorylation / Q000187:drug effects*; D014439:Tyramine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D014443:Tyrosine / Q000187:drug effects / Q000378:metabolism; D020298:U937 Cells
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D002109:Caffeic Acids; C481438:N-caffeoyltyramine; D014443:Tyrosine; C015566:3-tyrosine; D066246:ErbB Receptors; C505407:CASP3 protein, human; D053148:Caspase 3; D020169:Caspases; D014439:Tyramine