title: Ta1722, an anti-angiogenesis inhibitor targeted on VEGFR-2 against human hepatoma.
abstract: In order to investigate the anti-angiogenesis potential and related mechanisms of Ta1722 (a novel taspine derivative compound), a series of experiments in vivo and in vitro were carried out. The proliferation on human cell lines of SMMC-7721, A549, MCF-7, Lovo, and ECV304 was examined by MTT. Angiogenesis inhibition was examined by chick embryo chorioallantoic membrane (CAM) angiogenesis and tube formation assays. Related angiogenesis proteins and their mRNA expression were determined by western blotting and RT-PCR. In addition, the SMMC-7721 nude mouse xenotransplant model was used to evaluate the inhibition of tumor growth. The results showed that Ta1722 inhibited cell proliferation, angiogenesis of CAM and tube formation, and downregulated related positive angiogenesis proteins. The above indicated Ta1722 could serve as a promising candidate of angiogenesis inhibitors by interrupting the VEGF/VEGFR-2 pathway.
authors.affiliation: School of Medicine, Xi'an Jiaotong University, Xi'an, Shaanxi Province, PR China.
authors.forename: Lei
authors.initials: L
authors.lastname: Zheng
authors.forename: Xu
authors.initials: X
authors.lastname: He
authors.forename: Weina
authors.initials: W
authors.lastname: Ma
authors.forename: Bingling
authors.initials: B
authors.lastname: Dai
authors.forename: Yingzhuan
authors.initials: Y
authors.lastname: Zhan
authors.forename: Yanmin
authors.initials: Y
authors.lastname: Zhang
mesh_terms: D000083:Acetanilides / Q000494:pharmacology*; D020533:Angiogenesis Inhibitors / Q000494:pharmacology*; D000818:Animals; D001549:Benzamides / Q000494:pharmacology*; D015153:Blotting, Western; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy* / Q000473:pathology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002642:Chick Embryo; D049033:Chorioallantoic Membrane / Q000098:blood supply / Q000187:drug effects; D015536:Down-Regulation / Q000187:drug effects; D006801:Humans; D008114:Liver Neoplasms, Experimental / Q000098:blood supply / Q000188:drug therapy* / Q000473:pathology; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D009389:Neovascularization, Pathologic / Q000188:drug therapy / Q000473:pathology; D012333:RNA, Messenger / Q000378:metabolism; D020133:Reverse Transcriptase Polymerase Chain Reaction; D042461:Vascular Endothelial Growth Factor A / Q000378:metabolism; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000378:metabolism; D023041:Xenograft Model Antitumor Assays
chemical_list: D000083:Acetanilides; D020533:Angiogenesis Inhibitors; D001549:Benzamides; C579036:N,N'-diisopropyl-5,5'-dimethoxy-6,6'-bis(2-oxo-2-((3-(trifluoromethyl)phenyl)amino)ethoxy)biphenyl-2,2'-dicarboxamide; D012333:RNA, Messenger; D042461:Vascular Endothelial Growth Factor A; D040301:Vascular Endothelial Growth Factor Receptor-2