Inhibitory effects of artesunate on angiogenesis / 药学学报

ABSTRACT

<p><b>AIM</b>To investigate the inhibitory effects of artesunate on angiogenesis.</p><p><b>METHODS</b>The in vitro anti-angiogenic effect of artesunate was tested on models of angiogenesis proliferation, migration and tube formation of human umbilical vein endothelial (HUVE) cells; The anti-angiogenic effect in vivo was evaluated in nude mice by means of human ovarian cancer HO-8910 implantation and immunohistochemical stainings for microvessel (CD31), vascular endothelial growth factor (VEGF) and VEGF receptor KDR/flk-1.</p><p><b>RESULTS</b>Artesunate significantly inhibited angiogenesis in a concentration-dependent form in range of 0.5-50 mumol.L-1. The IC50 of artesunate for HUVE cells was (21 +/- 3) mumol.L-1. Growth of xenograft tumor was decreased and microvessel density was reduced following drug-treatment with no apparent toxicity to the animals. Artesunate also remarkably lowered VEGF expression on tumor cells and KDR/flk-1 expression on endothelial cells as well as tumor cells.</p><p><b>CONCLUSION</b>Artesunate was shown to inhibit angiogenesis in vitro and in vivo. These findings together with the known low toxicity of artesunate are clues that artesunate may be a promising angiogenesis inhibitor.</p>