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

Overview

Journal Angew Chem Int Ed Engl

Specialty Chemistry

Date 2016 Oct 8

PMID 27717148

Citations 11

Authors

Wai-Lun Kwong

Kar-Yee Lam

Chun-Nam Lok

Yau-Tsz Lai

Pui-Yan Lee

Chi-Ming Che

Affiliations

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Abstract

A macrocyclic ruthenium(III) complex [Ru (N O )Cl ]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.

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