Icariin

Icariin is a prenylated flavonoid that has been found in E. pubescens and has diverse biological activities.^1,2,3,4 It induces the differentiation of ES-D3 embryonic stem cells into cardiomyocytes when used at concentrations of 10 and 100 µM.¹ Icariin (10 µM) increases the mRNA expression of RUNX family transcription factor 2 (Runx2), osteocalcin (Bgp), and bone sialoprotein (Bsp), gene markers of osteogenesis, in MC3T3-E1 preosteoblast cells.² It reduces IL-6 and TNF-α protein levels induced by LPS in HeLa and RAW 264.7 cells when used at a concentration of 30 µM.³ Icariin (0.1 µM) prevents decreases in the levels of the neural integrity markers neurofilament heavy polypeptide (NF-H) and microtubule-associated protein 2 (MAP-2) induced by amyloid-β (1-42) (Aβ42) in primary E18 rat cortical neurons, and it improves spatial memory impairments in the Morris water maze in a 5XFAD transgenic mouse model of Alzheimer's disease when administered at a dose of 34 mg/kg for eight days.⁴

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1. Zhu, D., Qu, L., Zhang, X., et al. Icariin-mediated modulation of cell cycle and p53 during cardiomyocyte differentiation in embryonic stem cells. Eur. J. Pharmacol. 514(2-3), 99-110 (2005).

2. Zhao, J., Ohba, S., Shinkai, M., et al. Icariin induces osteogenic differentiation in vitro in a BMP- and Runx2-dependent manner. Biochem. Biophys. Res. Commun. 369(2), 444-448 (2008).

3. Sun, X., Deng, X., Cai, W., et al. Icariin inhibits LPS-induced cell inflammatory response by promoting GRα nuclear translocation and upregulating GRα expression. Life Sci. 195, 33-43 (2018).

4. Urano, T., and Tohda, C. Icariin improves memory impairment in Alzheimer’s disease model mice (5xFAD) and attenuates amyloid β-induced neurite atrophy. Phytother. Res. 24(11), 1658-1663 (2010).