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

Hye Jin Jung, Yonghyo Kim, Ju Yong Shin, Jae Kyung Sohng, Ho Jeong Kwon

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)1728-1735
Number of pages8
JournalArchives of pharmacal research
Volume38
Issue number9
DOIs
Publication statusPublished - 2015 Sep 22

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Hypoxia-Inducible Factor 1
Vascular Endothelial Growth Factor Receptor-2
Down-Regulation
Endothelial cells
Human Umbilical Vein Endothelial Cells
Biological Products
Polyketides
Chorioallantoic Membrane
Phosphorylation
Vascular Endothelial Growth Factor Receptor
Angiogenesis Inhibitors
Chick Embryo
Cytotoxicity
Vascular Endothelial Growth Factor A
Tumors
Association reactions
Membranes
herboxidiene
Therapeutics
Neoplasms

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery
  • Organic Chemistry

Cite this

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abstract = "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.",
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Antiangiogenic activity of herboxidiene via downregulation of vascular endothelial growth factor receptor-2 and hypoxia-inducible factor-1α. / Jung, Hye Jin; Kim, Yonghyo; Shin, Ju Yong; Sohng, Jae Kyung; Kwon, Ho Jeong.

In: Archives of pharmacal research, Vol. 38, No. 9, 22.09.2015, p. 1728-1735.

Research output: Contribution to journalArticle

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T1 - Antiangiogenic activity of herboxidiene via downregulation of vascular endothelial growth factor receptor-2 and hypoxia-inducible factor-1α

AU - Jung, Hye Jin

AU - Kim, Yonghyo

AU - Shin, Ju Yong

AU - Sohng, Jae Kyung

AU - Kwon, Ho Jeong

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AB - 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.

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