Antiangiogenic activity of herboxidiene via downregulation of vascular endothelial growth factor receptor-2 and hypoxia-inducible factor-1α

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• 作者：Hye Jin Jung ; Yonghyo Kim ; Ju Yong Shin ; Jae Kyung Sohng…
• 关键词：Antiangiogenesis ; Herboxidiene ; VEGFR2 ; HIF ; 1α
• 刊名：Archives of Pharmacal Research
• 出版年：2015
• 出版时间：September 2015
• 年：2015
• 卷：38
• 期：9
• 页码：1728-1735
• 全文大小：1,665 KB
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• 作者单位：Hye Jin Jung (1)
  Yonghyo Kim (2)
  Ju Yong Shin (1)
  Jae Kyung Sohng (1)
  Ho Jeong Kwon (2) (3)
  
  1. Department of BT-Convergent Pharmaceutical Engineering, Sun Moon University, 70, Sunmoon-ro 221, Tangjeong-myeon, Asan-si, Chungnam, 336-708, Republic of Korea
  2. Department of Biotechnology, Translational Research Center for Protein Function Control, College of Life Science and Biotechnology, Yonsei University, 50 Yonsei-ro, Seodaemun-gu, Seoul, 120-749, Republic of Korea
  3. Department of Internal Medicine, College of Medicine, Yonsei University, Seoul, 120-752, Republic of Korea
  
• 刊物主题：Pharmacy; Pharmacology/Toxicology;
• 出版者：Springer Netherlands
• ISSN：1976-3786

文摘

Antiangiogenesis is now thought of as one of the most important approaches for anticancer therapy. In this study, we determined the antiangiogenic property of herboxidiene, a polyketide natural product. Herboxidiene effectively inhibited the proliferation of human umbilical vein endothelial cells (HUVECs) at concentrations not exhibiting cytotoxicity. Furthermore, the natural product significantly suppressed vascular endothelial growth factor-induced invasion and tube formation in HUVECs as well as neovascularization of the chorioallantoic membrane in developing chick embryos. We also identified an association between the antiangiogenic activity of herboxidiene and the downregulation of both the phosphorylation of VEGF receptor 2 (KDR/Flk-1) and the expression of hypoxia-inducible factor-1α at the transcriptional level. These results suggest that herboxidiene functions as a potential antiangiogenic agent and may be applicable for anticancer therapy by targeting tumor angiogenesis. Keywords Antiangiogenesis Herboxidiene VEGFR2 HIF-1α