Icariin

Icariin

1. Identity: Chemical Classification, Botanical Source, and Common Forms

Chemical Identity

Icariin is a chemical compound classified as a prenylated flavonol glycoside, a type of flavonoid. It is the 8-prenyl derivative of kaempferol 3,7-O-diglucoside. More precisely, icariin is a member of the class of flavonols that is kaempferol substituted at position 8 by a 3-methylbut-2-en-1-yl group (a prenyl group), with the hydroxy groups at positions 3, 4′, and 7 converted to the corresponding 6-deoxy-alpha-L-mannopyranoside (rhamnose), methyl ether, and beta-D-glucopyranoside (glucose), respectively. Its molecular formula is C₃₃H₄₀O₁₅ with a molecular weight of 676.67 g/mol. The CAS registry number is 489-32-7.

Icariin consists of a glucose group at C-3, a methoxy group at C-4′, an isoprenoid group at position C-8, and a rhamnose group at C-7, making it the primary active constituent of Epimedium extracts. ICA is a disaccharide, and several studies have shown that flavonoids in the form of glycosides have low bioactivity because of their low intrinsic absorption permeability.

Botanical Source

Icariin has been isolated from several species of plant belonging to the genus Epimedium, which are commonly known as horny goat weed, Yin Yang Huo, and Herba epimedii. Epimedii herba is the dried leaf of epimedium — an herbaceous plant belonging to the Berberidaceae family — and is commonly referred to as horny goat weed, Xian-Ling-Pi, Gang-Qian, and San-Zhi-Jiu-Ye-Cao. Epimedii herba is widely distributed across eastern, southern, and central Asia and Europe, and has an over 2,000-year history of clinical application in countries such as China, South Korea, and Japan.

Prenylflavonoids stand out as pivotal constituents of the genus, with over 270 compounds identified across 52 species. Prenylated flavonoids, notably icariin and epimedins A, B, and C, have been identified as key markers for quality assessment and chemotaxonomy. Icariin is one of the most abundant flavonoids in Epimedium and is often used as a marker for quality control in Epimedium herbal preparation and chemical taxonomy.

These plants have a discontinuous distribution from Algeria in North Africa to East Asia, where the majority of the species (approximately 52) have undergone continuous evolution. Notable species used medicinally include Epimedium brevicornum Maxim., Epimedium sagittatum, Epimedium pubescens, and Epimedium pseudowushanense.

Key Related Compounds and Preparations

The essential components of epimedium include icariin, icaritin, desmethylicaritin, icariside I, and icariside II. Modern studies have shown that epimedium herb is rich in icariin, and 91.2% of icariin is converted to icariside II (ICA II) by hydrolytic enzymes in intestinal bacteria after oral administration. The metabolites produced by human gut bacteria include icariside II, icaritin, and desmethylicaritin; in human serum, the peak of icaritin was observed at 8 hours after Epimedium decoction intake, suggesting that the conversion of icariin to icaritin occurs primarily at the intestinal level.

Epimedium has found widespread use in functional foods, dietary supplements, and beverages like tea and wine; various forms including extracts, tablets, and capsules make it accessible to a diverse range of consumers. Recognized by the Chinese Pharmacopoeia, multiple Epimedium species have been identified, each containing a rich array of bioactive compounds.

2. Traditional and Historical Use

Origins and Documentation in Classical Texts

Epimedii herba was initially documented in Sheng Nong Ben Cao Jing, the oldest classical text on medicinal plants in China. Herba Epimedium, as one of the representative Chinese medicinal herbs, is described in "Shen Nong's Herbal Classic," first published in the Han dynasty (202 BC–220 AD). Epimedium was first recorded in Shennong Ben Cao Jing and is recognized as a "medium" herb in the most famous Chinese medical text, Ben Cao Gang Mu. Ben Cao Gang Mu, another important compendium of traditional Chinese medicine, describes Epimedii herba as pungent, cold, and nontoxic.

The classic Chinese medicine literature, "Shen Nong's Materia Medica," recorded more than 400 years ago that Herba Epimedii has the effects of "tonifying kidney yang," "strengthening muscles and bones," and "dispelling rheumatism."

The Shepherds' Legend and Naming

The history of Epimedium in erectile dysfunction therapy can be traced back to the ancient Chinese North and South Dynasties (420–589 AD). The famous medical scientist Tao Hongjing learned from shepherds that male sheep consumed a plant that significantly increased the times of penile erections and mating; Tao believed this plant could enhance the "YANG" energy, known in Chinese as "Yin Yang Huo" — literally the herb of sexual vigour. This folkloric observation gave rise to one of the plant's most enduring common names in English: "horny goat weed."

Traditional Indications and Preparations

Epimedium brevicornum Maxim has been used in traditional Chinese medicine for the treatment of impotence, sinew and bone disorders, "painful impediment caused by wind-dampness," numbness, spasms, hypertension, coronary heart disease, menopausal syndrome, bronchitis, and neurasthenia for many years in China. Epimedium dispels wind and disperses cold, tonifies the kidneys, and strengthens tendons; traditional medicine posits that tonifying kidney yang can nourish kidney essence, thereby promoting bone marrow production and nourishing bones to strengthen tendons and bones, as well as alleviate joint stiffness and pain.

Plants of the genus Epimedium have been utilized in Traditional Chinese Medicine (TCM) for centuries and were typically consumed as a tea in combination with other herbal products, purported to be useful in the treatment of arthritis, osteoporosis, and heart disorders. In Asian countries, it has been used as a traditional tonic agent for ageing, male sexual dysfunction, and major human body systems. Its history of clinical application spans over 2,000 years in countries such as China, South Korea, and Japan.

According to the Chromatographic Fingerprint Analysis of Herbal Medicines, Epimedii herba has been used to treat neurasthenia, climacteric hypertension, chronic bronchitis, viral myocarditis, and leucopenia.

3. Key Constituents, Metabolites, and Mechanisms of Action

Chemical Activity and Primary Targets

Icariin is obtained from several species of plants in the genus Epimedium and is thought to be the main active ingredient of the Chinese herbal medicine Herba Epimedii (yinyanghuo). It has a role as a bone density conservation agent, a phytoestrogen, a phosphodiesterase-5 (PDE5) inhibitor, and an antioxidant. Icariin inhibited the activity of PDE5 and PDE4 in a dose- and concentration-dependent manner; the IC₅₀ of icariin on PDE5 was 0.43 μM, and the IC₅₀ on PDE4 was 73.50 μM.

Phytoestrogenic and Estrogen Receptor Activity

Icariin, a flavonoid glycoside derived from Epimedium brevicornum Maxim., exerts bone protective effects via estrogen receptors (ERs); research has investigated the role of ER-α66, ER-α36, and GPER in bone metabolism in osteoblasts following treatment with icariin. Icariin and estradiol (E2) elicit rapid estrogenic responses in bone through recruiting ER-α66, ER-α36, and GPER; notably, in osteoblasts lacking ER-α66, ER-α36 and GPER mediate the estrogenic effects of icariin and E2, while in intact osteoblasts, ER-α36 and GPER act as negative regulators of ER-α66.

Bone Metabolism: Osteoblast and Osteoclast Pathways

A series of studies have demonstrated multiple mechanisms through which icariin treats bone and joint diseases, including the induction of bone formation, inhibition of bone resorption, and effects on angiogenesis. Icariin can inhibit bone resorption of osteoclasts through regulating the OPG/RANKL signal pathway. Icariin activates both ERα and Akt via enhancing rapid induction of IGF-1 signaling in osteoblastic cells for osteogenesis and might be regarded as a novel pathway-selective phytoestrogen for management of postmenopausal osteoporosis.

Icariin is an anabolic agent that can exert rapid estrogenic actions via ligand-independent activation of estrogen receptor alpha (ERα) in osteoblastic cells to promote osteogenesis. Computerized molecular docking techniques and competitive solid-phase binding ELISA assays have confirmed that icariin can act as a direct ligand of integrin alpha 5 beta 1 (α5β1), and can also increase the protein expression of integrin α5β1 for mechanosensing.

PDE5 inhibition by icariin analogues promotes osteoblast differentiation by activating the cAMP/protein kinase G (PKG)/SHP2 pathway, thereby stimulating aromatase expression. Icariin from Epimedium brevicornum has been found to promote the production of estrogen in human ovarian granulosa cells and osteoblastic cells.

Neuroprotective Mechanisms

Icariin has been reported to exhibit numerous pharmacological activities, including anti-oxidant, anti-inflammatory, and anti-apoptotic effects, which may contribute to therapeutic benefits in disorders of the nervous system such as cerebral ischemia, Alzheimer's disease, Parkinson's disease, multiple sclerosis, and depression. It has been shown to protect neurons in the central nervous system from degeneration by inhibiting neuronal apoptosis and tau protein hyperphosphorylation.

As the main active component of the icariin metabolite pathway, icariside II can suppress Aβ production via promoting the non-amyloidogenic APP cleavage process and markedly decrease PDE5A expression to potentially treat Alzheimer's disease. Substantial studies indicate that icariin may be beneficial in Alzheimer's disease by reducing the production of extracellular amyloid plaques and intracellular neurofibrillary tangles and by inhibiting phosphodiesterase-5 activity. Increasing evidence has also indicated that icariin exerts a protective role in Alzheimer's disease by limiting inflammation, oxidative stress, and reducing potential risk factors such as atherosclerosis.

Anti-Inflammatory Mechanisms

Multiple targets and mechanisms of icariin are reported, which relate to regulating lymphocyte balance, anti-inflammatory/inflammatory cytokines, and signal pathways such as NF-κB and Erk-p38-JNK, as well as lymphocyte transcription factors and other targets including TLRs, STAT, and PTEN. Icariin and its derivatives exert powerful suppression of proinflammatory signaling such as NF-κB and MAPKs, and can also upregulate anti-inflammatory signaling, such as GR and Nrf2.

Antioxidant Activity

Icariin belongs to the flavonoid glycosides with molecular formula C₃₃H₄₀O₁₅; it contains an isopentyl group, phenolic hydroxyl groups, and a methoxy group, which may be related to its antioxidant, anti-inflammatory, or immunomodulatory activities. A 2024 meta-analysis found that icariin and its derivatives exhibited notable efficacy as antioxidative stress indicators, including significant upregulation of SOD levels and inhibition of MDA activity, thereby achieving an anti-oxidative stress effect.

Anticancer Mechanisms

Icariin and its derivatives treat various types of cancers through induction of apoptosis, regulation of autophagy, and inhibition of angiogenesis. Preclinical studies demonstrate that icariin modulates key oncogenic pathways, including PI3K/Akt, MAPK, NF-κB/SIRT6, and AMPK/mTOR, to inhibit tumor cell proliferation, induce apoptosis, and regulate autophagy.

Cardiovascular Mechanisms

Icariin can minimize myocardial cell damage and the immune response in mice after acute myocardial infarction by alleviating inflammatory factors, and can also activate the Nrf2/HO1 pathway. Icariin has also been evaluated for prevention and treatment of thrombosis in atherosclerosis, as it reduces platelet adhesiveness and aggregation besides decreasing serum cholesterol.

4. Pharmacokinetics and Bioavailability

Despite the numerous studies on icariin, the main challenge remains its very low oral bioavailability due to its physicochemical characteristics, and P-glycoprotein-mediated efflux in intestinal mucosa. Different studies have indicated the importance of icariin hydrolysis by lactase phlorizin hydrolase in the small intestine and by microbiota β-glucosidase to release metabolites before absorption; furthermore, the prenyl-moiety decreases the bioavailability and plasma absorption of prenylated flavonoids.

Studies of icariin metabolism and distribution in humans are limited; what has emerged is that icariin is scarcely present in plasma because of its rapid elimination, and the tissue distribution of icariin in the brain is scarce — a finding that appears inconsistent with the large body of literature supporting neuroprotective effects.

In a 2019 randomized controlled human trial, at all doses tested, either very low or undetectable blood levels of icariin were observed, demonstrating the low bioavailability of the oral formulation and preventing a determination of pharmacokinetic properties. Different drug formulations and delivery methods may be needed to adequately assess the pharmacokinetic profile of icariin.

5. Scientific Evidence by Health Area

5.1 Bone Health and Osteoporosis

Preclinical evidence: Recent studies have demonstrated significant positive effects of icariin on bone metabolism and remodeling, including promoting osteoblast proliferation and mineralization, reducing osteoclast activity, and inhibiting inflammation and oxidative stress. Administration of icariin to ovariectomized (OVX) rats significantly protected them against bone loss at the long bone and lumbar spine without inducing uterotrophic effects. Ex vivo studies using bone marrow stromal cells (BMSCs) and osteoclast precursors confirmed the stimulatory effects of icariin on osteoblastogenesis and its inhibitory effects on osteoclastogenesis.

Clinical evidence: Human data on icariin are limited; to date, only one placebo-controlled trial has been broadly reported. A randomized, double-blind, placebo-controlled trial of Epimedium-derived flavonoids that included icariin (60 mg/day) in 100 postmenopausal women found significantly greater bone mineral density in the icariin group compared with the placebo group after 24 months; the authors did not report safety and tolerability data.

In another randomized, double-blind, controlled clinical trial of osteoporosis patients (360 cases in the Epimedium total flavonoid capsule group and 120 cases in the Gusongbao capsule group), the overall efficacy rates of the main symptoms were 90.83% and 75.00%, respectively, and the rates of BMD improvement were 47.38% and 34.23%, suggesting that Epimedium Total Flavonoid Capsule may increase BMD and improve major symptoms in osteoporosis patients. The reported adverse events in this trial included rash, constipation, diarrhea, palpitations, tinnitus, and gastrointestinal dysfunction, with an incidence of 6.67%.

Evidence strength: The preclinical evidence base for bone protection is extensive and mechanistically detailed. Human evidence is limited to a small number of trials using mixed Epimedium flavonoid extracts rather than purified icariin, and further high-quality, large-scale randomized controlled trials are needed.

5.2 Erectile Function and Male Sexual Health

Preclinical evidence: Daily treatment with low-dose, purified icariin improves penile hemodynamic parameters four weeks after cavernous nerve injury in a rat model of erectile dysfunction; improved functional outcomes in icariin-treated animals are associated with increased penile nNOS and smooth muscle content.

Mechanism: Icariin has a similar structural profile to PDE5 inhibitors (PDE5Is). It inhibited the activity of PDE5 in a dose- and concentration-dependent manner with an IC₅₀ on PDE5 of 0.43 μM.

Clinical evidence: Icariin and some of its derivatives could be a potential treatment for restoring spontaneous erections; more clinical and basic research with high quality and large samples are recommended. In people, rigorous trials targeting erectile dysfunction are limited; most human data come from safety, pharmacokinetic, or extract-level studies rather than purified icariin with clinical endpoints.

Evidence strength: Predominantly preclinical (animal models and in vitro). The direct clinical evidence for purified icariin in human erectile dysfunction is weak and currently insufficient to draw firm conclusions.

5.3 Neurological and Neurodegenerative Conditions

Alzheimer's Disease: Recent animal experimental studies indicate that icariin, a major bioactive component of epimedium, may effectively treat Alzheimer's disease, cerebral ischemia, depression, Parkinson's disease, and multiple sclerosis, as well as delay ageing. Icariin has been found to possess multiple neuroprotective effects: it improves survival and function of neurons and triggers their self-renewal through neural stem cells.

Depression: Herba Epimedii has demonstrated pharmacological actions including anti-inflammatory, antioxidative stress, and antidepressive properties. Evidence for icariin's antidepressant effects comes from preclinical animal models; no controlled human clinical trials specifically targeting depression with icariin have been published to date.

Evidence strength: Almost entirely preclinical (rodent and cell models). Human clinical evidence for neurological indications is absent. The finding that icariin shows low brain tissue distribution further complicates the translation of animal findings to human disease.

5.4 Anti-Inflammatory and Immune Modulation

A 2024 meta-analysis aimed to define the anti-inflammatory activities of icariin and its derivatives and to create a reference framework for evaluating preclinical evidence, combining machine learning and meta-analysis to identify underlying biological pathways, using data from PubMed, Embase, Web of Science, and the Cochrane Library. Icariin and its derivatives showed substantial effects on the modulation of apoptotic regulators; they significantly increased BCL-2 levels and reduced caspase-1 activity.

Icariin can decrease IL-17 and IFN-γ expression in the CNS and peripheral lymphoid organs of mice, and it alleviates inflammatory infiltration and decreases blood-brain barrier leakage.

Evidence strength: The anti-inflammatory evidence is mechanistically robust in preclinical models and supported by meta-analyses of animal data. Human intervention studies are lacking.

5.5 Anticancer Activity

In recent years, icariin has attracted the attention of the scientific and medical community owing to its anticancer properties, low cost, and few adverse effects. Research has investigated the mechanisms by which icariin and its derivatives treat various types of cancers, such as induction of apoptosis, regulation of autophagy, and inhibition of angiogenesis. Treating A549 lung cancer cells with 0–400 μmol/L icariin found that the survival rate of cells treated with icariin (≥100 μmol/L) significantly reduced in a dose-dependent manner; further mechanistic studies demonstrated that this inhibitory effect was associated with the suppression of the PI3K/AKT signaling pathway.

Icariin has been shown to exert an anti-tumor effect on liver cancer cells in a concentration-dependent manner; mechanisms of action include inhibition of tumor cell proliferation and induction of apoptosis. Icaritin, one of the metabolites of icariin, is currently utilized as an active component of an anti-cancer drug.

Evidence strength: All anticancer evidence for icariin itself is preclinical — in vitro cell-line experiments and animal models. No human clinical trials have evaluated icariin as a standalone anticancer agent. Icaritin (a metabolite) has moved further toward clinical development. These findings should not be extrapolated to clinical outcomes in cancer patients.

5.6 Cardiovascular Health

Icariin has been widely examined over the last few years and has been shown to have antioxidant, anti-inflammatory, and anti-apoptotic properties; it is presently being investigated as a possible treatment for a multitude of diseases, ranging from cancer to cardiovascular disease. Icariin has been proven in previous investigations to preserve myocardium function in rats following myocardial ischemia/reperfusion (I/R) damage.

Evidence strength: Exclusively preclinical; no controlled human trials targeting cardiovascular endpoints with icariin have been published.

5.7 Liver Protection

The flavonoid icariin is a main functional component of Epimedium brevicornum Maxim.; although the protective mechanisms of icariin and its metabolites against liver injury are not yet comprehensively understood, an increasing number of studies have confirmed their liver-protective and anticancer effects. Preclinical evidence at doses of 25–50 mg/kg in mice suggests hepatoprotective activity against acute acetaminophen-induced liver injury. All such data are from animal studies.

6. Dosage Forms and Reported Dosages

Epimedium is incorporated into functional foods, dietary supplements, and beverages like tea and wine; various forms including extracts, tablets, and capsules make it accessible to a diverse range of consumers.

The following dosages have been specifically reported in peer-reviewed studies:

• 60 mg/day of Epimedium-derived flavonoids containing icariin: used in a 24-month randomized double-blind placebo-controlled trial in 100 postmenopausal women examining bone mineral density.
• 100 to 1,680 mg/day (orally): the range of doses tested in a randomized, double-blind, placebo-controlled human safety and pharmacokinetics study in 24 healthy adult participants.
• 100 mg/day, 200 mg/day, 400 mg/day, or 800 mg/day: dose levels assigned in a registered clinical trial (NCT02112123) evaluating icariin to prevent corticosteroid-related memory changes in healthy volunteers over 5 days.
• In animal studies, icariin administered at 300 mg/kg/day restored bone conditions in osteoblast-specific estrogen receptor knockout (ER-α66 KO) mice.
• In mouse hepatoprotection experiments, icariin was orally administered at 25 mg/kg or 50 mg/kg for 7 consecutive days.

No established consensus human dosage for icariin exists, as clinical trials are few and have used widely variable doses. The dosages cited above are from specific study protocols and should not be interpreted as recommended therapeutic doses.

7. Safety Considerations and Drug Interactions

Human Tolerability Data

Tolerability of icariin was good except at the highest dose tested; two participants receiving 1,680 mg of icariin discontinued the study drug due to gastrointestinal symptoms. A statistically significant, but not clinically significant, increase in self-reported depressive symptom severity was observed with icariin relative to placebo. Bioavailability of oral icariin appears to be low at all doses tested, and although icariin appears generally to have a favorable tolerability profile, the highest doses may be associated with gastrointestinal distress.

Hepatotoxicity

Horny goat weed contains icariin, which may cause liver injury through oxidative stress or immune-related mechanisms; at least one published case report emphasizes the importance of detailed histories regarding herbal supplement use in patients with liver dysfunction. Although the protective mechanisms of icariin and its metabolites against liver injury are not yet comprehensively understood, an increasing number of studies have confirmed their liver-protective effects in preclinical models. This apparent paradox — hepatoprotective in animal models but potentially hepatotoxic in a clinical case — underscores the importance of monitoring liver function when using Epimedium-derived products.

Drug–Drug Interactions via UDP-Glucuronosyltransferases (UGTs)

Investigation of the effects of icariin and its intestinal metabolites on human UDP-glucuronosyltransferase (UGT) activities found that icariin exhibited potent inhibition against UGT1A3; the intestinal metabolites of icariin exhibited a different inhibition profile — icariside II was a potent inhibitor of UGT1A4, UGT1A7, UGT1A9, and UGT2B7, and icaritin was a potent inhibitor of UGT1A7 and UGT1A9. In vivo inhibition against intestinal UGT1A3, UGT1A4, and UGT1A7 would likely occur after a single oral administration of Epimedium pubescens decoction. These findings provide a basis for further investigation into the drug interaction potential between icariin and UGT substrates.

Because UGT enzymes are involved in the metabolism of many drugs — including analgesics, cardiovascular agents, and some antivirals — the UGT-inhibitory profile of icariin and its metabolites represents a pharmacokinetically relevant interaction risk that warrants caution when co-administering Epimedium products with medications relying on UGT-mediated clearance.

Estrogenic Activity Considerations

Icariin has a role as a phytoestrogen. Its estrogenic activity, while weaker than endogenous estrogens, is mechanistically documented across multiple receptor subtypes. This phytoestrogenic property carries implications for hormone-sensitive conditions. In ovariectomized rat studies, icariin administration significantly protected against bone loss without inducing uterotrophic effects, suggesting tissue-selective estrogenic activity, though this selectivity has not been confirmed in humans.

PDE5 Inhibition Context

Like sildenafil, icariin is a phosphodiesterase type-5 inhibitor. Its IC₅₀ for PDE5 inhibition (0.43 μM) is considerably weaker than pharmaceutical PDE5 inhibitors such as sildenafil. Nonetheless, co-administration with nitrates, other PDE5 inhibitors, or antihypertensives should be approached cautiously given the shared mechanism of vasodilation.

Populations Not Studied

No systematic safety data are available in pregnant or lactating women, children, or patients with severe hepatic or renal impairment. Animal studies and one human case report of hepatotoxicity constitute the available liver-safety signals.

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