Icariin, a prenylated flavonol glycoside, has been extracted from several species of Epimedium plant (horny goat weed, Yin Yang Huo). Epimedium is one of the most representative herbs in Chinese medicine, which was first recorded in Shennong’s Herbal Classics (200-300 CE). It has been used in traditional Chinese medicine for centuries to treat a variety of conditions, including erectile dysfunction, fatigue, and kidney problems.

The chemical components of Epimedium include flavonoids, lignans, phenol glycosides, alkaloids, polysaccharides, volatile oils, trace elements, chromatic proketones, phenanthrene, anthraquinone, tannin, sesquiterpene, sterols, etc. Among them, flavonoids such as Icariin, Epimedin A, Epimedin B, Epimedin C  and so on. Icariin is one of the important active substances in the total flavonoids of icariin(Shown below). Metabolic and pharmacokinetic studies have demonstrated that icariin is converted into icariin, icariin I, icariin II and demethylicariin.

In recent years, epimedium icariin has also been studied for its potential benefits in other areas, such as improving athletic performance, boosting the immune system, and protecting against cancer. While several previous studies have demonstrated the safety of herba medium, the complex reaction between herba medium components makes dose-toxicity still unclear. Hepatotoxicity of icariin I and icariin A, the main components of Epimedium, has been reported. Therefore, it is necessary to explore the chemical components of epimedium and their pharmacological activities.

Epimedium icariin for the reproductive system

Icariin, one of the active components of icariin, which is a traditional Chinese medicine herb for invigorating kidneys and strengthening Yang, can promote the function of reproductive system. The results showed that icariin could inhibit the oxidative stress damage of sperm induced by ferrous sulfate/hydrogen peroxide, promote the proliferation of Sertoli’s vegetative cells of testis and enhance male reproductive function. It can also regulate the hypothalamic-pituitary-gonadal axis, up-regulate the expression of dopamine and 5-hydroxytryptamine in hypothalamus, activate PI3K/AKT /eNOS /NO signaling pathway, increase the concentration of NO and serum testosterone, and improve the sexual function of male mice. It can also activate the No-cyclic guanosine phosphate signaling pathway, inhibit the expression of type 5 phosphodiesterase, and improve erectile dysfunction.

Epimedium icariin can also up-regulate the levels of cytochrome P450 17 and 19, promote the expression of aromatase, and increase the production of estrogen and progesterone. Promote pubertal development of female rats and prolong the duration of estrus in pubertal rats. In addition, icariin can reduce the levels of FSH and luteinizing hormone, improve ovarian follicle development, inhibit follicle atresia and enhance fertility in aging mice.

Icariin has excellent antioxidant and anti-inflammatory properties, is a popular natural remedy for erectile dysfunction. It can be taken as a supplement or applied directly to the penis. Icariin is a potent PDE5 inhibitor, which means it can help to relax the smooth muscles in the penis and improve blood flow. This can be helpful for men with erectile dysfunction. It also has been shown to protect the kidneys from damage and improve kidney function.

Epimedium icariin for Antinervous system

Epimedium icariin has a good effect on a variety of neurological diseases such as cerebral ischemia, Alzheimer’s disease, Parkinson’s disease, multiple sclerosis and depression. Icariin can increase the level of superoxide dismutase (SOD), reduce the expression of amyloid precursor protein and β-secretase, reduce the production and accumulation of Aβ, weaken the axonal and dendrite atrophy mediated by Aβ, and improve the spatial learning and memory ability of Alzheimer’s disease model rats. Icariin can also inhibit the hyperphosphorylation of tau protein serine 396, 404 and threonine 205 induced by Aβ, which is thought to have A protective effect on nerve cells.

Epimedium icariin for Antiskeletal system

Epimedium icariin can promote the formation and activation of osteoblasts, and inhibit the formation and function of osteoclasts to alleviate osteoporosis. It was found that it can activate the ERα-Wnt /β-catenin and Notch signaling pathways, up-regulate the expression of RUNt-related transcription factor 2, a key gene of osteoblasts, and play an osteogenic role. It can activate mitogen-activated protein kinase (MAPK) signaling pathway and increase gene expression of type I collagen, osteocalcin and ostein. The self-renewal ability of bone mesenchymal stem cells (BMSCs) was enhanced in vivo and in vitro, and BMSCs were induced to differentiate into osteoblasts, thus enhancing osteogenic differentiation. In addition, icariin has estrogen-like effects, promoting osteoblast proliferation and increasing osteoblast viability.

Epimedium icariin for Immune system

Icariin can improve the condition of rheumatoid arthritis, bronchial asthma, multiple sclerosis and systemic lupus erythematosus and other autoimmune diseases, and its regulation of lymphocyte function is related. Icariin has been shown to boost the immune system by increasing the production of white blood cells. White blood cells are essential for fighting off infection.

Icariin can inhibit the differentiation of T helper cells 1 and 17 and improve the autoimmune encephalomyelitis in mice. Icariin can also inhibit the activation of STAT3 in T cells, down-regulate the proportion of Th17 cells, inhibit the production of interleukin-17, and improve the symptoms of rheumatoid arthritis. It enhances lymphokine activated killer cells as well as natural killer cell activity, improving the body’s immunity.

Epimedium icariin extract powder is a natural compound with a number of potential benefits for the body. It is most commonly used to treat erectile dysfunction, but it may also be helpful for improving athletic performance, reducing fatigue, protecting the kidneys, boosting the immune system. It has been shown to have anti-cancer properties. If you are considering taking icariin extract powder, talk to your doctor first to make sure it is right for you.

Source: https://pubmed.ncbi.nlm.nih.gov/32089233/

Ye Tao