Horny Goat Weed or Epimedium Herb:Botanical Origin,Archeology,Traditional and Pharmacological findings of Epimedium species,fractions and isolated components.
- Botanical info of Horny Goat Weed or Epimedium.
- Botanical Origin:What is Herba Epimedii?
- Archeology:How did Horny Goat Weed get its name?
- Mechanism of Action:How Does Horny Goat Weed Work?
- Horny Goat Weed:Salvation Weed For Male Sex Lives.
- Epimedium Herb and its Traditional Applications.
- Applicational pharmacological findings of Epimedium species,fractions and isolated components.
- Cautions,Side Effects and Toxicity of Epimedium Herb.
- A Tradition from Erxian Tang:Two Immortals Decoction?
- Phytochemicals and Constituents of Herba Epimedii.
- How Search engine think about Horny Goat Weed.
- Research update literature of Epimedium species,fractions and components.
- Photo Gallery of Epimedium Herb.
Applications and Properties:
Applications and Properties identified:
Epimedium herb is an old chinese herb used since ancient days thousand years ago,its family member majorly included Epimedium brevicornum Maxim.;Epimedium sagittatum (Siebold. et Zucc.) Maxim., Epimedium koreanum Nakai.,Epimedium pubescens Maxim.,Epimedium sinense, Epimedium wushanense T.S.Ying.and some others.This herb got used wildly and effectively in below field:
Libido Stimulating,ED treatment and related similar symptoms treatment,such like Chronic Renal Insufficiency and end-state renal failure(ESRF),sexual disorder in chronic renal failure cases:
Mechanism of Epimedium herb and its useful fractions and isolated components on the effects related with phallus got attentioned from a lot of modern scientific studies,the compositive mechanism could be briefly identified and understood as:
(1).Works on multitargets in nitric oxide (NO)/cyclic guanosine monophosphate(cGMP)/phosphodiesterase 5(PDE 5) pathway;(2).PDE5 mRNA expression inhibition especially PDE5A1 inhibition,works to inhibitory to all three PDE5 isoforms(PDE5A1, A2, and A3) ,also inhibite PDE-6(phosphodiesterase-6);(3).cAMP-PDE(cyclic adenosine monophosphate-phosphodiesterase) inhibition;(4).Regulates the activity of NO-cGMP signal pathway on CC to enhance erectile function;(5).increases the erectile function (ICP) and restores the eNOS(expression of the nitrogen oxide synthase) expression,PSM(percent of smooth muscle) increase in the CC(corpus cavernosum);(6).Estradiol Production of Granulosa cells promption,Corticosterone Production stimulation,Release Erectogenic and Neurotrophic effects,Testosterone mimetic properties;
Components specific of ED treatment got attentioned included: Epimedium brevicornum Maxim Water Extract(EbM) and Hydrophobic compounds,isolated components icariin,icaritin(3,7-bis(2-hydroxyethyl)),inhibitors with molecular weights over 500 still effective.
Some combinative investigation of TCM recipe EXD(Er Xian Decoction) and another recipe named Etana got compared yet.The component icariin combined with resveratrol and LBP got found release strong property of Spermatogenic disturbance anti-radiation.
Chronic Renal Insufficiency:Epimedium sagittatum(EP) may works effective for Chronic Renal Insufficiency and end-state renal failure(ESRF),useful for sexual disorder in chronic renal failure cases,by the way (1).decreased level of BUN and serum creatinine,inhibited the hypertrophy of glomeruli in ,inhibited deposition of IgG, C3, Fib and FN along the glomerular capillary;(2).resture sIL-2R and IL-6 levels etc.
Estrogenic Activity:Estrogenic property of Epimedium herb got attentioned since ancient,the latest scientific studies provide a brief mechanism explain on it:
(1).ER-stimulatory activity:increased ERalpha(estrogenic receptor) and ERbeta activity,(2).Strongly Oestrogenic Property due to phytoestrogens of the prenyl-flavone family;
Components specific of related got attentioned:Epimedium brevicornum leaf polyphenolic extract,prenylflavone named breviflavone B,70% EtOH Extract of Epimedium brevicornum displays EC(50) level 2.30 x 10(-4),icaritin(ICT) and desmethylicaritin.(DICT),Epimedium prenylflavonoids,trace flavonoid aglycones (kaempferol, apigenin, quercetin, luteolin and breviflavone B);icariin metabolites(desmethylicaritin, and icaritin)
Species specific difference got attention:six rare Epimedium.May not included Epimedium pubescens.Screening specific attentioned got an EC(50) value order of 11 TCM herb candidate,which maybe useful for related application reference.
Negative Non-Estrogenic property got attentioned to:Epimedium pubescens,icariin,interestly icariin may diaplays its estrogenic activity via its metabolites such like desmethylicaritin and icaritin instead icariin itself,which may give some explain of the seemingly contradictive result from several studies.
Prostate Protection:A combination recipe named Equiguard with Epimedium and other 8 herbs got attentioned show its prostate protection effects via prevent AD and AI prostate carcinoma,anti-prostatic activities.
Osteoblastic Property:Epimedium herb and its recipes has long been used for the treatment of osteoporosis in China since ancient days,the property effects it brings for related may briefly explained as:(1).activity against osteoporosis:including inhibited bone resorption,stimulated bone formation;inhibit the formation and bone resorption activity of osteoclasts;(2).stimulating osteoblasts,including prompting proliferation in osteoblast;promote the differentiation of BMSCs into osteoblast;(3).significant new bone formation and new bone thickness:induction of osteoblasts proliferation and differentiation;(4).increase the BMD(Bone mineral density) and improve indexes of bone biomechanics;(5).preventing bone loss in late postmenopausal women;(6).prevention of abnormal bone lysis such as osteoporosis, rheumatoid arthritis, and periodontal bone erosion;(7).antiosteoporotic effect;(8).enhanced the differentiation and proliferation of osteoblasts, and facilitated matrix calcification;(9).prevent OVX(ovariectomy)-induced bone loss;(10).prevent inflammatory bone loss;inhibited LPS-induced osteoclastogenesis;(11).shortening the course of distraction osteogenesis;(12).improve the growth of cartilage and proliferation of cartilage cell;
For the mechanisms works on molecular level,its mechanism may be understood via a series of combinative ways: inhibition of osteoclast-specific genes[mRNA of MMP9,BMP2, BMP4,TRAP,RANK,cathepsin K,Cbfa1(Core binding factor alpha1 )/Runx2, OPG,and RANKL,TGF-beta1],enhances significantly the proliferation and differentiation of human osteoblasts,induction of Runx2 expression, production of BMP-4 and activation of BMP signaling,stimulate the proliferation and enhance the osteogenic differentiation of MSCs(bone marrow stromal cells); significantly promote the expression of OPN mRNA and type I collagen; accelerate the proliferation and ALP(alkaline phosphatase) excretion of BMSCs(bone mesenchymal stem cells); activating ER(oestrogen receptor) in a ligand-independent manner;suppressing activation of the p38 and JNK pathway; Icariin/beta-TCP ceramic.Enhancing the osteogenic differentiation of MSCs( bone marrow stroma cells),promoting the ALP activity.
Fractions and components specific attentioned:flavonoids(icariin, epimedin B and epimedin C),Epimedium-derived phytoestrogen flavonoids(EPFs),Ikarisoside A,astragalosid I,icaritin,icariside II,Epimedium sagittatum polysaccharides,metabolites of TFE(total flavonoid extract of Epimedium sagittatum),flavonoids from E. koreanum Nakai.Species specific related attentioned:E. brevicornum Maxim. extracts,E. brevicornum and E. sagittatum group MTT significantly higher than others
Effects on the immune system:Mechanism of Epimedium herb works on immume system combinatively composed of multi-ways:(1).regulating Immune related cell activity,including Macrophage,T-lymphocytes,B-lymphocytes,NK(natural killer cell) and LAK cells(lymphokine-activated killer cell),spleen antibody-forming cells (SAFC),interleukin-2 (IL-2) production;(2).promotes the phagocytic activity and stimulate lymphocyte proliferation;(3).stimulated the production of tumor necrosis factor-alpha in monocytes;(4).decrease CD25, IL-2, IL-4 and IL-10;(5).enhance the cell-mediated immunity reaction;Specific fraction of related got attentioned:polysaccharide,70% methanolic extract (E-S),flavone glycosides,icariin
Anti-Tumor and Anti-Canceractivity:Anti-Tumor and Anti-Cancer activity mechanism of Epimedium can be understood breifly from:(1).cell cycle blockage via either the inhibition of CDK2 and CDK4 activities;(2).increase inhibitors, p21(Cip1) and p27(Kip1) or negatively modulates the ERK/c-Fos/AP-1 signaling pathway;(3).HL-60 cells differentiation induction via elevating the cAMP/cGMP ratio;(4).antioxidantive activity of flavonoids;(5).overexpression of tumor-selective therapeutic target such like HIF-1alpha,and Hypoxia-inducible factor-1 (HIF-1) for solid tumors;(6).induce apoptosis by ways such like anti-inflammatory effects in PC-3 prostate cancer cells,through a ROS/JNK-dependent mitochondrial pathway;(7).inhance membrane fluidity of PG and increase the expression of membrane HLA-ABC antigen;(8).anti-angiogenesis and anti-proliferative effects in tumors;(9).suppressed tumor cells migration and invasion via the Rac1-dependent VASP( vasodilator-stimulated phosphoprotein) pathway;Specific fraction and components related got attentioned:Epimedin C,icariin,flavonoids;Icariside II;
Anti-inflammatory Activity:Anti-inflammatory property and mechanism of Epimedium can be understood briefly compositively from:(1).inhibit LPS-induced production of inflammatory cytokines by blocking NF-kappaB and MAPK signaling in RAW264.7 cells;(2).inhibition of NO, cytokine, chemokine and growth factor production in macrophages;(3).inhibits the production of NO by inhibiting the activity of p38 MAPK and NF-kappaB;(4).induces apoptosis in PC-3 prostate cancer cells;(5).inhibition of nitric oxide and MMP synthesis,then reduce the extracellular matrix destruction;(6).intervention on pro-inflammatory cytokines (TNF-alpha, IL-6), inflammatory mediators (NO) and adhesion molecules (CD11b);(7).activation of the PI3K/Akt pathway;
Specific fractions and components of related attentioned:2''-hydroxy-3''-en-anhydroicaritin(isolated from Epimedium brevicornum);Epimedium brevicornum water extract,Ikarisoside A;Icariside II;icariin and some novel derivate of icariin such like ICT[3,5,7-Trihydroxy-4'-methoxy-8-(3-hydroxy-3-methylbutyl)-flavone] and another derivate named (3,5-dihydroxy-4'-methoxy-6'',6''-dimethy1-4'',5''-dihydropyrano[2'',3'':7,8]-flavone).
Neuroprotective Property:Neurons are damaged following prolonged exposure to high concentrations of corticosterone, particularly during chronic inflammatory and immune diseases.One of the main mechanisms underlying neuronal injury is apoptosis.Epimedium herb and its fraction derivatives show neuroprotective property via wide-spectrum combinative ways,which got understood briefly as composed of:
(1).Release Neuroendocrino-immunological effect via relieve neuroendocrino-immunological effect inhibited by exogenous glucocorticoid;
(2).Show neuroprotective by increasing monoamines levels,inhibiting oxidative damage and decreasing acetylcholinesterase activity(AChE);
(3).Anti-Neuroinflammatory effects by inhibited the release of nitric oxide (NO), prostaglandin E (PGE)-2, reactive oxygen species (ROS) and mRNA expression of proinflammatory cytokines(such as tumor necrosis factor (TNF)-alpha, interleukin (IL)-1beta and IL-6);blockade of p38 MAPK phosphorylation;
(4).Antidepressant-like effect mediated via neurochemical and neuroendocrine systems;improving the abnormalities in the HPA axis functions,attenuates the neuroendocrinological alterations;
(5).Alzheimer's disease(AD) and other tau pathology-related neuronal degenerative diseases prevention,via decreased production of insoluble fragments of Abeta through suppression of beta-secretase expression;blocking Abeta(25-35)-induced toxicity by estrogen receptor antagonist ICI 182,780 and well matched binding affinity with estrogen receptor,via the balance intracelluar calcium homeostasis; inhibited Abeta42-induced neurotoxicity in a dose-dependent manner;improve memory dysfunction in AD and potential to extend neurites;
(6).Ischemic brain injury/Cerebral ischemia/reperfusion neuron injury/Stroke protection protection,mainly through decreasing cell apoptosis, preventing intracellular calcium concentration elevation and enhancing anti-oxidant capacity,against brain ischemic injury by increasing the SIRT1 and PGC-1alpha expression;inhibit H(2) O(2) -induced neurotoxicity partially involved with the up-regulation or increasing of SIRT1;obvious inhibition on H/R-induced PTK activation,PTK inhibition and protection from I/R- or H/R-induced damages;
(7).Learning and memory deficits improve:the mechanism composed of improving the spatial learning and memory via increased anti-oxidant capacity and decreased lipid peroxidation and Abeta(1-40) levels;improve spatial learning and memory abilities with case brain dysfunction induced by LPS(lipopolysaccharide) via decreased expressions of TNF-alpha, IL-1beta and COX-2 in the hippocampus,some recipe of icariin and Panax notoginseng saponins may ameliorate learning and memory deficit and blood viscosity by protecting neurons from oxidative stress in ischemic brain.
(8).improving peripheral nerve regeneration effect.
Specific fraction and components of related attentioned:Epimedium brevicornum (EB),icariin,icaritin,icariside etc.Specific combinative recipe with epimedium attentioned to its strong potential neuro-pharmacological activities such as anti-fatigue, improving cognitive-deficiency.
Cardiovascular System:Cardiovascular effects of Epimedium herb may be understood in a combinative way:lowers the blood pressure,lowers whole blood viscosity,lowers the rate of ADP-induced blood platelet aggregation,protective effect on hypoxia injured VECs,Vasorelaxant effects,protective effects on endothelial cells which contribute to its cardiovascular protective effects via NF-kappaB activation in EA,eNOS(endothelial nitric oxide synthase) gene expression stimulation,bioactive NO production enhancement,Anti-atherosclerosis.Specific fractions and components attentioned to Epimedium alcohol fraction,total flavone glycoside,icariin.
Coronary Heart Disease Prevention:Coronary Heart Disease protection mechanism of Epimedium herb may composed of:ameliorates LV dysfunction and cardiac remodeling through down-regulating matrix metalloproteinase-2 and -9 activity and myocardial apoptosis;promoting on cardiac differentiation etc.Specific fraction or components related got attentioned:ethanol extract of epimedium (EPI-ext);prenylflavonoids;icariin.
Antioxidative Effect and Atherosclerosis Prevention:Antioxidative property of Epimedium and related derivatives(majorly icariin and its structural analogues) could be understood composed as:(1).against oxidative injuries of ECV-304 cells via caspase expression decreasing;(2).protected human erythrocytes against free-radical-induced haemolysis;(3).protects LH(linoleic acid) against AAPH(2,2'-azobis(2-amidinopropane) dihydrochloride)-induced peroxidation of LH;(4).protects DNA against AAPH-induced(2,2'-azobis(2-amidinopropane) dihydrochloride) oxidative damage in a concentration-dependent manner;Specific fractions and components got attentioned:icariin and its two structural analogues(acacetin and norwogonin).
Other identified application and property included:Diabetic Property,Angiogenetic Activity,Antihepatotoxic Activity,Obesity Treatment,Melanogenesis Inhibitor,Hypopigmentation,Splenocyte Proliferation Inhibition,Antibacteria Property,etc.
Safety and Toxicity:
Acute toxicity(LD50):LD50-Lethal dose,50 percent kill. Intraperitoneal. Rodent-mouse, 80gm/kg.IC50:Lethal dose,50 percent kill.Chinese hamster lung cells: 55.4 mg/ml.IC50:Lethal dose,50 percent kill.Chinese hamster ovary cells: 19.53 mg/ml.
- 1.Horny Goat Weed or Epimedium Herb:Botanical Origin,Archeology,Traditional and Pharmacological findings of Epimedium species,fractions and isolated components.
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