Synonyms: Icariside II
CAS No.: 113558-15-9
Mol. Formula: C27H30O10
Mol. Weight: 514.52
Botanical Source: Epimedium spp.
Purity: 90%~99% by HPLC
Identification Method: Mass, NMR
Analysis Method of Purity: HPLC-DAD or/and HPLC-ELSD
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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-1alpha 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-1alpha. 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-1alpha.
1, Icariin and its derivative icariside II extend healthspan via insulin/IGF-1 pathway in C. elegans. PLoS One. 2011;6(12):e28835. Epub 2011 Dec 21.
2, Icariside II from Epimedium koreanum inhibits hypoxia-inducible factor-1alpha in human osteosarcoma cel. EurJ Pharmacol. 2008 Jan 28;579(1-3):58-65. Epub 2007 Oct 15.