Antiestrogenic Activity - The estrogenic and antiestrogenic activities of Epimedii Herba, which is a traditional medicinal herb used in Korea and China were investigated in this study. The in vitro estrogen receptor (ER) mediated estrogenic/antiestrogenic activities of an Epimedii Herba extract (Epi ext) and its major components were determined using an estrogen responsive element driven reporter gene assay in MCF-7/ERE and HEK293T cells.

These results collectively suggest that phytoestrogens possess both estrogenic and antiestrogenic activity, and that the differential expression of these two compounds with opposing activities is dependent on the physiological environment in terms of estrogen level, which may be the case in humans.

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Anti-Tumor - 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.

Overall, these results suggest the potential use of Icariside II as a therapeutic candidate against various diseases that involve overexpression of HIF-1α.

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Epimedium koreanum is one of the most popular medicinal plants in China, its major constituents being 8‐prenyl flavonoids. We studied the effects of one of these flavonoids, icariside II (3, 5, 7‐trihydroxy‐4′‐methoxyflavone‐3‐O‐α‐L‐rhamnopyranoside) on the invitro growth of five human tumour cell lines.

The results suggest that icariside II may be a potentially useful antitumour agent.

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Our studies demonstrated the polysaccharide (180 × 10⁴ Da) purified from Epimedium koreanum Nakai could promote maturation and Ag presentation function of DCs, increase the level of immunomodulatory cytokines and activate CD4 T-cell differentiation. Furthermore, it may inhibit the tumor growth in LLC-bearing mice through regulating host immune system function

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Antiproliferative - We investigated whether the addition of Epimedium koreanum Nakai extract (EEF) to gefitinib could overcome the resistance of NSCLC cells to gefitinib. In our study, the growth inhibitory effects of cotreatment differed between mutant EGFR and wild type EGFR. A synergistic antiproliferative effect was observed in the combined treatments in H1975 and PC-9GR cells carrying T790M EGFR.

The results indicate that the addition of EEF to gefitinib is a promising strategy to overcome T790M-mediated drug resistance.

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Antioxidative - To study the antioxidative and antitumor activities of flavonoids isolated from Epimedium koreanum.The compounds were separated by column chromatography with silica gel and Sephadex LH-20, and identified by spectral a- nalysis (ESI-MS, 1H-NMR and 13C-NMR) respectively.

The antitumor activity of E. koreanum may be partially related to the antioxidantive activity of flavonoids.

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Anti-Viral - In this study, the broad antiviral spectrum and mode of action of an aqueous extract from Epimedium koreanum Nakai was evaluated in vitro, and moreover, the protective effect against divergent influenza A subtypes was determined in BALB/c mice.

The oral administration of Epimedium koreanum Nakai exhibited preventive effects on BALB/c mice against lethal doses of highly pathogenic influenza A subtypes (H1N1, H5N2, H7N3 and H9N2).

Therefore, an extract of Epimedium koreanum Nakai and its components play roles as immunomodulators in the innate immune response, and may be potential candidates for prophylactic or therapeutic treatments against diverse viruses in animal and humans.

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Cytotoxic Effects for Osteoporosis - Seven flavonol glycosides and four nonflavonoid compounds were isolated from Epimedium koreanum. Nakai (Berberidaceae), and their effects on the proliferation of rat osteoblast-like (ROB) cells were evaluated with a mitochondrial activity assay.

Considering the antiosteoporotic effect of flavonoids in vivo., these results suggest that the flavonoids may enhance the development of osteoblasts through their active metabolites, and the mechanism between proliferation and differentiation of osteoblasts needs to be further studied to fully evaluate the mechanism of E.. koreanum. in the treatment of osteoporosis.

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Anti-Androgens - Anti-androgens are regarded as potential therapeutic agents for the treatment of prostate cancer. We determined that an epimedium herb (EH) extract exhibited anti-androgenic activity in a luciferase assay using androgen receptor-positive prostate cancer LNCaP cells.

A quantitative RT-PCR analysis confirmed that the flavonol suppressed the expression of the androgen-responsive KLK3 gene.

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