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




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Institute of Oceanology, Chinese Academy of Sciences, Qingdao 266071, China



These authors contributed equally to this work.





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Academic Editor: Vassilios Roussis

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

Keywords: bromophenol; anti-angiogenesis; RTKs; multi-target inhibitor; NO; PKB-Akt; eNOS bromophenol; anti-angiogenesis; RTKs; multi-target inhibitor; NO; PKB-Akt; eNOS





Autor: Shuaiyu Wang †, Li-Jun Wang †, Bo Jiang, Ning Wu, Xiangqian Li, Shaofang Liu, Jiao Luo and Dayong Shi *

Fuente: http://mdpi.com/



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