A Macrocyclic Ruthenium(III) Complex Inhibits Angiogenesis with Down-Regulation of Vascular Endothelial Growth Factor Receptor-2 and Suppresses Tumor Growth In Vivo

A macrocyclic ruthenium(III) complex [RuIII(N2O2)Cl2]Cl (Ru‐1) is reported as an inhibitor of angiogenesis and an anti‐tumor compound. The complex is relatively non‐cytotoxic towards endothelial and cancer cell lines in vitro, but specifically inhibited the processes of angiogenic endothelial cell t...

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Bibliographic Details
Published in:Angewandte Chemie 2016-10, Vol.128 (43), p.13722-13726
Main Authors: Kwong, Wai-Lun, Lam, Kar-Yee, Lok, Chun-Nam, Lai, Yau-Tsz, Lee, Pui-Yan, Che, Chi-Ming
Format: Article
Language:English
Subjects:
Angiogenese
Angiogenesis
Biotechnology
Cancer
Chemistry
Cytotoxicity
Down-regulation
Endothelial cells
Growth factors
Macrocyclic compounds
Rodents
Ruthenium
Tubes
Tumor cell lines
Tumors
Tumortherapeutika
Vascular endothelial growth factor
Vascular endothelial growth factor receptors
VEGFRs
Xenografts
Zebrafish
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Summary:A macrocyclic ruthenium(III) complex [RuIII(N2O2)Cl2]Cl (Ru‐1) is reported as an inhibitor of angiogenesis and an anti‐tumor compound. The complex is relatively non‐cytotoxic towards endothelial and cancer cell lines in vitro, but specifically inhibited the processes of angiogenic endothelial cell tube formation and cancer cell invasion. Moreover, compared with known anti‐cancer ruthenium complexes, Ru‐1 is distinct in that it suppressed the expression of vascular endothelial growth factor receptor‐2 (VEGFR2), and the associated downstream signaling that is crucial to tumor angiogenesis. In addition, in vivo studies showed that Ru‐1 inhibited angiogenesis in a zebrafish model and suppressed tumor growth in nude mice bearing cancer xenografts. Antiangiogenes RuIII: Ein makrocyclischer Ruthenium(III)‐Komplex wurde gefunden, der die Angiogenese von Endothelzellen und die Invasion von Krebszellen inhibiert. Der Komplex unterdrückt die Expression des Wachstumsfaktorrezeptors VEGFR2 und dessen Signalwege und zeigt Antitumoraktivität in vivo.
ISSN:0044-8249
1521-3757
DOI:10.1002/ange.201608094