Anti-Angiogenic Properties of BDDPM, a Bromophenol from Marine Red Alga Rhodomela confervoides, with Multi Receptor Tyrosine Kinase Inhibition Effects.

摘要: Bis-(2,3-dibromo-4,5-dihydroxy-phenyl)-methane (BDDPM) is a bromophenol first isolated from Rhodomelaceae confervoides. Our previous studies showed that BDDPM exerts PTP1B-inhibiting activity and anti-cancer against wide range of tumor cells while it also lower cytotoxicity normal cells. In the present study, we found exhibits significant activities toward angiogenesis in vitro. inhibits multiple processes, including endothelial cell sprouting, migration, proliferation, tube formation. Further kinase assays investigations potent selective, but multi-target, receptor tyrosine (RTKs) inhibitor. (10 μM) fibroblast growth factor 2 3 (FGFR2, 3), vascular (VEGFR2) platelet-derived α (PDGFRα) (inhibition rate: 57.7%, 78.6%, 78.5% 71.1%, respectively). Moreover, decreases phosphorylation protein B (PKB/Akt) nitric oxide synthase (eNOS), as well (NO) production dose dependent manner. These results indicate can be exploited an anti-angiogenic drug, or lead compound for development novel multi-target RTKs inhibitors.