Epimedokoreanin B is a natural isopentenylflavonoid compound isolated from Korean horny goat weed (Epimedium koreanum Nakai) that exhibits anticancer, anti-inflammatory, and antibacterial activities. Epimedokoreanin B is an anti-periodontitis agent that inhibits the growth and biofilm formation of gingival proteases and Porphyromonas gingivalis. Epimedokoreanin B can inhibit the growth of lung cancer cells through endoplasmic reticulum stress-mediated apoptosis accompanied by autophagy.
Icaritin (Anhydroicaritin) has hormone regulation activity and cardiovascular function improvement activity. Icaritin has anticancer activity, can induce S phase arrest and apoptosis, inhibit ENKL cell proliferation. Icaritin has anti-multiple myeloma activity, mainly mediated by inhibiting IL-6/JAK2/STAT3 signaling. Icaritin at low concentration (4 or 8 μMol/L) can promote rat chondrocyte proliferation and inhibit cell apoptosis, while the effect of Icaritin on rat chondrocyte at high concentration was reversed.
Icariin (Ieariline) belongs to the flavonol glycoside group of natural products, can inhibit PDE5 and PDE4 activity (IC50=432/73.50 μM), is also a PPARα activator. Icariin can increase cardiovascular and cerebrovascular blood flow, promote hematopoiesis, immunity and bone metabolism.
Icariside I (Lcariside I) is isolated from Epimedium herb. It can stimulate osteogenic differentiation of BMSCs and inhibit bone resorption activity of osteoclasts.
Noricaritin, a flavonoid derived from Epimedium root, induces cell proliferation in lung tissue and inhibits the production of pro-inflammatory cytokines and chemokines in human lung epithelial cells.
1. β-Anhydroicaritin exhibits immunosuppressive effect on the mouse macrophages stimulated by LPS. 2. β-Anhydroicaritin phytosomes can inhibit enhanced bone turnover induced by ovariectomy, improve BMD the biomechanical properties of vertebrae, without any stimulation on uterus. 3. β-Anhydroicaritin possesses significant protective effects on the zymosan-induced peritonitis mice, which might be associated with the regulation of Ca(2+); influx in macrophages and iNOS expression.
Epmedin C (Baohuoside-VI) was metabolized via desugarization, dehydrogenation, hydrogenation, dehydroxylation, hydroxylation, demethylation and glucuronidation pathways in vivo. It has potential activity against osteoporosis by stimulating osteoblasts.
Sagittatoside A (Icariin-A) is a flavonoid glycoside that can be extracted from Herba Epimedii. It induces the phosphorylation of serine 118 in the ERα, selectively activating estrogen response elements (ERE) and luciferase activity.
2''-O-Rhamnosylicariside II is beneficial for improving postmenopausal osteoporosis and demonstrates potent antioxidant activity, with IC50 values of 90.5 µM [90.5 uM].
Ikarisoside F and epimedin A can bind to AdoHcy hydrolase, inhibit the activity of AdoHcy hydrolase, thus regulating the cellular biomethylation as well as reducing cellular Hcy level.