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Icariin powder is a bioactive flavonoid compound extracted from the Epimedium plant (commonly known as "horny goat weed"). It is renowned for its potential health benefits, particularly in enhancing libido, improving erectile function, and supporting bone health. As a natural PDE-5 inhibitor, icariin may boost blood flow and testosterone levels, making it popular in male vitality supplements. Additionally, it exhibits anti-inflammatory, antioxidant, and neuroprotective properties, with research suggesting roles in combating osteoporosis, cardiovascular diseases, and cognitive decline. The powder is typically yellow-brown, water-soluble, and standardized to contain 10%-98% icariin for therapeutic use. While generally safe, high doses may cause mild side effects like dizziness. Its multifaceted applications span traditional medicine, sports nutrition, and modern pharmacology.
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Chemical Formula |
C33H40O15 |
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Exact Mass |
676 |
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Molecular Weight |
677 |
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m/z |
676 (100.0%), 677 (35.7%), 678 (6.2%), 678 (3.1%), 679 (1.1%) |
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Elemental Analysis |
C, 58.58; H, 5.96; O, 35.47 |
Icariin powder, also known as Xianlingpi, is the dried leaves of herbaceous plants in the Berberidaceae family, including Epimedium, Korean Epimedium, Soft haired Epimedium, and Arrow leaved Epimedium. The chemical components of Epimedium include flavonoids, lignans, phenolic glycosides, alkaloids, polysaccharides, volatile oils, trace elements, chromogens, phenanthrene, anthraquinone, tannins, sesquiterpenes, sterols, etc. Among them, flavonoids such as icariin, Asahuoding A, Asahuoding B, and Asahuoding C are its main active ingredients. Modern pharmacological research has shown that icariin has immunomodulatory, anti-inflammatory, anti-aging, anti-tumor and other activities, and has a certain improvement effect on neurological, immune, endocrine, cardiovascular, skeletal and other related diseases.
1. Promoting effect on the reproductive system
As one of the effective active ingredients of Epimedium, a kidney tonifying and yang boosting medicine, it can promote the function of the reproductive system. It can inhibit the oxidative stress damage of human sperm induced by ferrous sulfate/hydrogen peroxide, activate the ERK1/2 signaling pathway, promote the proliferation of Sertoli cells in the testes, and enhance male reproductive function; It can regulate the hypothalamic pituitary gonadal axis, upregulate the expression of dopamine and serotonin in the hypothalamus, activate the PI3K/AKT/eNOS/NO signaling pathway, increase the concentration of NO and serum testosterone, shorten the capture latency and ejaculation latency, increase the capture and ejaculation rate as well as testicular and prostate indices, and improve the sexual function of male mice; It can activate the NO cyclic guanosine monophosphate signaling pathway, inhibit the expression of type 5 phosphodiesterase, and improve erectile dysfunction.
It can also upregulate the levels of cytochrome P450 17 and 19, promote the expression of aromatase, induce the proliferation of ovarian granulosa cells, and increase the production of estrogen and progesterone; It can increase the weight of ovaries, uterus, and pituitary glands, promote puberty development in female rats, and prolong the duration of estrus in adolescent rats. In addition, it can reduce follicle stimulating hormone and luteinizing hormone levels, increase estradiol levels, upregulate ovarian anti Mullerian hormone expression, increase Bcl-2/Bax ratio in ovarian tissue, improve ovarian follicle development in aging mice, inhibit follicular atresia, and enhance their fertility.
It has a good improvement effect on various neurological diseases such as cerebral ischemia, Alzheimer's disease, Parkinson's disease, multiple sclerosis, and depression.
It can increase the level of superoxide dismutase (SOD), reduce the expression of amyloid precursor protein and β - secretase, decrease the production and accumulation of A β, weaken the axonal and dendritic atrophy mediated by A β, and improve the spatial learning and memory ability of Alzheimer's disease model rats. It can also inhibit the excessive phosphorylation of serine 396, 404, and threonine 205 sites in tau protein induced by A β, thereby exerting a protective effect on nerve cells.
It can activate the phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt) and MAPK/ERK signaling pathways, reverse the changes in the expression of B-cell lymphoma-2 gene (Bcl-2), Bcl-2 associated X protein (Bax), and cysteine asparate protease-3 (Caspase-3) in the striatum, inhibit the sustained decrease in dopamine content and loss of tyrosine hydroxylase immunoreactivity neurons. It can also inhibit the inflammatory damage and behavioral changes of dopamine neurons induced by 6-hydroxydopamine/lipopolysaccharide in rats.
It can inhibit the degradation and activation of NF - κ B inhibitory protein alpha, upregulate the protein levels of peroxisome proliferators activated receptors (PPARs) alpha and gamma, and alleviate neuroinflammation. Epimedium glycoside can also reduce lactate dehydrogenase and malondialdehyde levels, weaken SOD activity, enhance antioxidant capacity, inhibit the increase of intracellular calcium concentration, and weaken neuronal damage caused by ischemia/reperfusion. In addition, it can inhibit the activation of myelin associated growth inhibitory factors, myelin associated glycoproteins, and oligodendrocyte myelin glycoproteins in ischemic areas, promote axonal sprouting and regeneration, and improve neurological function.
It can promote the formation and activation of osteoblasts, while inhibiting the formation and function of osteoclasts to alleviate osteoporosis. It can activate the ER α - Wnt/β - catenin and Notch signaling pathways, upregulate the expression of key osteoblast gene runt related transcription factor 2, and exert osteogenic effects; It can activate the mitogen activated protein kinase (MAPK) signaling pathway, increase the gene expression of type I collagen, osteocalcin, and osteopontin, enhance the self-renewal ability of bone mesenchymal stem cells (BMSCs) in vitro and in vivo, induce BMSCs to differentiate into osteoblasts, and thereby enhance osteogenic differentiation. In addition, it can promote estrogen synthesis and has estrogen like effects, activating extracellular signal regulated kinase (ERK) and c-jun N-terminal kinase (JNK), promoting osteoblast proliferation, activating BMP-2/Smad4, and increasing osteoblast vitality.
By inhibiting the activity of MAPKs and nuclear factor kappa-B (NF - κ B), downregulating the synthesis of hypoxia inducible factor-1 α, prostaglandin E2, and receptor activator of NF - κ B ligand (RANKL), hematopoietic cell differentiation into osteoclasts can be inhibited. Its derivatives can inhibit the expression of RANKL that promotes osteoclastogenesis, promote the expression of alkaline phosphatase, osteocalcin, type I collagen, and osteoprotegerin that have osteogenic effects, and inhibit osteoclast differentiation. In addition, it can reduce the generation of superoxide anions and the size and quantity of actin rings, lower intracellular calcium concentration, inhibit osteoclast activity, and thus suppress bone resorption.
Cardiovascular disease is one of the main causes of human death in modern society. Epimedium glycoside can protect myocardial cells, promote myocardial cell generation, improve endothelial dysfunction, and exert a protective effect on the cardiovascular system.
It can block angiotensin II induced cardiomyocyte hypertrophy and apoptosis by inhibiting the activation of JNK and p38 pathways; Activate ERK, eliminate reactive oxygen species, and inhibit oxidative stress in myocardial cells. It can also activate the PI3K/Akt/endothelial nitric oxide synthase (eNOS) signaling pathway, reduce creatine kinase, ischemia modified albumin, and lactate dehydrogenase levels, decrease apoptotic cells and myocardial infarction area, and improve myocardial ischemia-reperfusion injury in rats; Downregulate the activity of matrix metalloproteinases 2 and 9, improve myocardial cell apoptosis, alleviate left ventricular dysfunction and cardiac remodeling.
It can activate the p38MAPK pathway, increase the expression of peroxisome proliferator activated receptor gamma co activator factor-1 α, PPAR α, and nuclear respiratory factor 1, promote the differentiation of embryonic stem cells into cardiomyocytes, upregulate the expression of specific myosin light chain-1v, atrial natriuretic peptide, cardiac troponin I, sarcoplasmic reticulum calcium protein, and sodium calcium exchanger in differentiated cardiomyocytes, and maintain the normal functional structure of myocardial cell pulsation. In addition, it can activate the ERK dependent signaling pathway to stimulate the differentiation of adipose derived stem cells from mice into cardiomyocytes.
It can inhibit the activation of caspase-3, upregulate eNOS levels, promote the production of nitric oxide (NO), and alleviate oxidative stress damage to endothelial cells. It can reduce the level of reactive oxygen species, activate the PI3K/Akt/eNOS signaling pathway, and delay homocysteine induced endothelial cell aging. It can reduce the expression of intercellular adhesion molecule-1, vascular cell adhesion molecule-1 and E-selectin, inhibit the adhesion of monocytes and endothelial cells, and improve atherosclerosis.
It can improve the condition of autoimmune diseases such as rheumatoid arthritis, bronchial asthma, multiple sclerosis, and systemic lupus erythematosus, and is related to its regulation of lymphocyte function. It can inhibit the differentiation of helper T cells (Th) 1 and 17 and improve autoimmune encephalomyelitis in mice. Icariin powder can inhibit the activation of STAT3 in T cells, downregulate the proportion of Th17 cells, inhibit the production of interleukin-17, and improve symptoms of rheumatoid arthritis; It can regulate the ratio of Th1/Th2 cells in lung tissue of asthmatic rats and the balance of Th17/regulatory T cells in asthmatic mice, improving asthma; Can enhance the activity of lymphokines activated killer cells and natural killer cells, and improve human immunity.
The advantages of this method are: high yield of the extraction process, simple separation process, no energy consumption, and convenient, concise, and fast extraction. A preparation process of Icariin powder, characterized by the following steps:
a:
Take Epimedium herb, soak it in water at room temperature for 2-5 hours, then soak it in a water bath at a temperature of 50-60 ℃ for 4-5 hours, filter, separate the filter residue and extract initial solution;
01
b:
Place the filter residue obtained in step a in a water bath at a temperature of 60-80 ℃ for 2-3 hours, filter and separate the filter residue from the solution;
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c:
Combine the initial solution of the extract obtained in step a with the solution obtained in step b, let it stand for 1-2 hours, separate the upper clear night, concentrate under reduced pressure, and obtain the crude extract;
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d:
Pass the concentrated crude extract obtained in step c through a chromatography column containing macroporous resin, then introduce deionized water into the column until the effluent is identified, and then introduce 70-80% ethanol into the column to collect the eluent;
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e:
Let the eluent obtained in step d stand, crystallize, filter, and then dry at a temperature of 50-60 ℃ for 5-6 hours to obtain icariin extract from Epimedium.
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Epimedium brevicornum Maxim, a plant in the Berberidaceae family Epimedium sagitatum Maxim Epimedium pubescens Maxim Dried stem and leaf extracts of Epimedium wushanense T.S. Ying from Wushan or Epimedium koreanum Nakai from Korea.
Specifications: 10%, 20%, 50%, 98%
Ecological environment:
Born on damp slopes or under forests in valleys.
Born in mountainous areas, dense forests, rock crevices, streams, or shady wetlands.
Born by streams and valleys.
Born in the forests or shrubs of the Dominican Republic, it prefers soil rich in humus and relatively moist.
Born on mountain slopes, in grassy areas under forests, and prefers damp and shady areas.
resource distribution
Distributed in Inner Mongolia, Beijing, Hebei, Shanxi, Shaanxi, Ningxia, Gansu, Qinghai, Xinjiang, Anhui, Henan, Hubei, Hunan, Guangxi, Sichuan and other places.
Distributed in Shaanxi, Gansu, Jiangsu, Anhui, Zhejiang, Jiangxi, Fujian, Taiwan, Hubei, Hunan, Guangdong, Guangxi, Sichuan, Guizhou and other places.
Distributed in Shaanxi, Guangxi, Sichuan, Guizhou and other places.
Distributed in Heilongjiang, Jilin, Liaoning and other places.
Distributed in Inner Mongolia, Hebei, Shaanxi, Gansu, Anhui, Zhejiang, Jiangxi, Henan, Hubei, Sichuan, Guizhou and other places.
adverse reaction
Icariin is a flavonol glycoside extracted from the traditional Chinese medicine Epimedium. Its chemical structure includes C33H40O15 and its molecular weight is 676.66. As a PDE5 (phosphodiesterase 5) and PDE4 inhibitor, Icariin exerts vasodilatory effects by regulating the cGMP signaling pathway, while also participating in lipid metabolism regulation as a PPAR α activator. Its pharmacological effects involve multi system regulation, including cardiovascular protection, bone metabolism promotion, neuroprotection, and immune regulation.
Cardiovascular system function
Icariin can inhibit PDE5 activity (IC50=432 nM), promote vascular smooth muscle relaxation by increasing cGMP levels, and increase cardiovascular and cerebrovascular blood flow. Animal experiments show that it can improve endothelial dysfunction, inhibit platelet activation, and show anti atherosclerosis characteristics. For example, in the mouse model of atherosclerosis induced by high-fat diet, Icariin significantly reduces inflammatory response and foam cell formation by regulating PI3K/Akt and NF - κ B pathways.
Bone metabolism regulation
Icariin can stimulate osteoblast proliferation and differentiation, promoting bone formation by upregulating BMP-2 (bone morphogenetic protein 2) expression. Preclinical studies have confirmed that it can increase bone density and improve the bone microstructure of osteoporosis model animals. A randomized controlled trial targeting postmenopausal women showed that after continuous use of 60 mg Icariin daily for 12 months, lumbar spine bone density increased by 2.3% compared to baseline, significantly higher than the placebo group.
Neuroprotection and Cognitive Function
Icariin reduces neuronal apoptosis by inhibiting the JNK/p38 MAPK pathway and caspase-3 activation. In a traumatic brain injury mouse model, continuous administration of 30 mg/kg for 7 days significantly improved motor coordination and spatial memory, while upregulating BDNF (brain-derived neurotrophic factor) and synaptophysin expression.
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