Icariside II from Epimedium koreanum inhibits hypoxia-inducible factor-1α in human osteosarcoma cells

Hwa Jung Choi, Jae Soon Eun, Dae Keun Kim, Ri Hua Li, Tae Yong Shin, Hyunsung Park, Nam Pyo Cho, Yunjo Soh

Research output: Contribution to journalArticlepeer-review

54 Scopus citations

Abstract

Hypoxia-inducible factor-1 (HIF-1) is an important tumor-selective therapeutic target for solid tumors. Icariside II was isolated from Epimedium koreanum through successive fractionation with ethyl acetate, n-butanol, chloroform and hexane, followed by gel column chromatography. Icariside II attenuated the protein level of HIF-1α induced by hypoxia in human osteosarcoma (HOS) cells in a concentration-dependent manner, probably by enhancing the interaction rate between von Hippel-Lindau (VHL) and HIF-1α. Furthermore, Icariside II down-regulated the levels of HIF-inducible genes involved in angiogenesis, metastasis, and glucose metabolism, such as vascular endothelial growth factor (VEGF), urokinase plasminogen activator receptor (uPAR), adrenomedullin (ADM), matrix metalloproteinase 2 (MMP2), aldolase A, and enolase 1 in HOS cells. Icariside II also inhibited the migration rate in HOS cells and tube formation rate in human umbilical vein endothelium cells (HUVECs). Overall, these results suggest the potential use of Icariside II as a therapeutic candidate against various diseases that involve overexpression of HIF-1α.

Original languageEnglish
Pages (from-to)58-65
Number of pages8
JournalEuropean Journal of Pharmacology
Volume579
Issue number1-3
DOIs
StatePublished - 28 Jan 2008

Keywords

  • Angiogenesis
  • Epimedium koreanum
  • HIF-1α
  • HOS
  • Hypoxia
  • Icariside
  • Invasion
  • Metastasis
  • VEGF
  • VHL

Fingerprint

Dive into the research topics of 'Icariside II from Epimedium koreanum inhibits hypoxia-inducible factor-1α in human osteosarcoma cells'. Together they form a unique fingerprint.

Cite this