Icariin pde5 inhibitor benefit and use for erectile dysfunction or impotence treatment by Ray Sahelian, M.D. Uses of icariin extract from horny goat weed herb and review of the latest published studies

Icariin, a flavonol glycoside, is an interesting substance found in certain herbs, particularly horny goat weed. known as the botanical name epimedium. Icariin has been studied as a substance that dilates blood vessels and can potentially be helpful in the treatment of erectile dysfunction. Icariin has been found to have phosphodiesterase type 5 inhibitor activity.
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Purchase Horny Goat Weed extract with 20 percent icariin, 300 mg, 90 Capsules - formulated by Ray Sahelian, M.D.
Horny goat weed is one of the most valued tonics of Chinese herbalism.  In China it is especially used for supporting healthy sexual activity - thus its name, Horny Goat Weed. Horny Goat Weed 300 mg has epimedium extract (standardized to 20% flavonoids as icariin).

Each pill contains:
Epimedium Sagittatum  - 300 mg Standardized Leaf Extract (20% flavonoids as icariin)


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Icariin and erections, PDE5 inhibitor
Icariin appears to have some properties similar to Viagra. Icariin is a cGMP-specific PDE5 inhibitor that may have potential in treating erectile dysfunction.

J Sex Med. 2011. Effects of icariin on improving erectile function in streptozotocin-induced diabetic rats.
Icariin treatment preserved penile hemodynamics, smooth muscle and endothelial integrity, and neuronal nitric oxide synthase expression in the penis of diabetic rats. Down-regulation of TGFβ1/Smad2 signaling pathway might mediate this effect.

Potent inhibition of human phosphodiesterase-5 by icariin derivatives.
J Nat Prod. 2008. Department of Pharmacological Sciences, University of Milan, Milan, Italy.
Plant extracts traditionally used for male impotence such as Tribulus terrestris, Ferula hermonis, Epimedium brevicornum, Cinnamomum cassia, and the individual compounds cinnamaldehyde, ferutinin, and icariin, were screened against phosphodiesterase-5A1 (PDE5A1) activity. Only E. brevicornum extract and its active principle icariin were active.

Effects of icariin on intracavernosal pressure and systematic arterial blood pressure of rat
Zhonghua Yi Xue Za Zhi. 2004.
We tested the effect of icariin on erectile function of the penis. Icariin, sidenafil and papaverine increased the intracavernous pressure in a dose-depended manner. Icariin increases intracavernous pressure.

Effects of icariin on cGMP-specific PDE5 and cAMP-specific PDE4 activities.
Asian J Androl. 2003.
We evaluated the therapeutic action of icariin on erectile dysfunction. PDE5 was isolated from human platelet and PDE4 from the rat liver tissue. The inhibitory effects of icariin on PDE5 and PDE4 activities were investigated. Papaverine served as the control drug. Icariin and papaverine showed dose-dependent inhibitory effects on PDE5 and PDE4 activities. Icariin is a cGMP-specific PDE5 inhibitor that may be developed into an oral effective agent for the treatment of erectile dysfunction. For more information on phosphodiesterase inhibitor enzymes.

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Icariin side effects, safety, risk, danger
Icariin side effects have not yet been mentioned in the medical literature. Since icariin is not sold by itself as a supplement, we have not tested it ourselves to see if it has side effects. At present you can only find icariin as part of a horny goat weed herbal supplement. As such, the horny goat weed supplement will have many other substances within it, therefore it would be difficult to determine what role icariin, alone, would have in the horny goat weed side effect profile. Side effects of high dose horny goat weed herb include rapid heart beat and insomnia.

Icariin extracts
Epimedium is sold in various extract potencies, including various percentages of icariin and epimediosides. for instance you can find epimedium sagitattum sold by herb and ingredient suppliers as 5 percent icariin, 10 percent, 20 percent, 30 percent, 60 percent and even 90 percent. Hardly any human research has been done on these various extract concentrations to determine which are the best options for use as sexual enhancers.

Is there any difference between icariin and the group of chemicals known as icariins that are found in horny goat weed extract? I tried to purchases some of teh raw material and the one that was icariin alone was more expensive.
   Icariins contains 2-3 chemical substances, and one of these is icariin. The manufacturing process of purifying icariin takes several more stepd, thus the cost is higher than Icariins as a group of several substances.

Alzheimer's disease
Icariin attenuates beta-amyloid-induced neurotoxicity by inhibition of tau protein hyperphosphorylation in PC12 cells.
Natural Neuropharmacology. 2010. Products Research Center, Korea Institute of Science and Technology Gangneung Institute, Republic of Korea;.
Our observations indicate that icariin is capable of attenuating Abeta(25-35)-induced tau protein hyperphosphorylation and promoting survival of neuronal cells, meanwhile also provide some insights into the potential signaling pathway that is involved. Thus, this study promises a great potential agent for Alzheimer's disease and other tau pathology-related neuronal degenerative diseases.

Icariin research as anti cancer agent
In laboratory studies, icariin appears to have anti-cancer abilities. Icariin also helps protect the liver from toxicity.

Anti-proliferative efficacy of Icariin on HepG2 hepatoma and its possible mechanism of action.
Am J Chin Med. 2009; Integrated Laboratory of TCM and Western Medicine of Peking University First Hospital and Integrated Institute of TCM and Western Medicine of Peking University, Beijing, China.
The aim of the present work was to explore the anti-hepatoma effects of icariin both in vitro and in vivo and to elucidate its potential mechanism of action. Icariin showed anticancer efficacy both in vitro and in vivo. The possible mechanism of action could be related to its anti-angiogenesis and anti-proliferative effects in tumors.

Experimental studies of icariin on anticancer mechanism
Zhong Yao Cai. 2000.
In order to further elucidate the reversion of malignant phenotypes of tumor cells and the mechanism of its action, highly metastatic human lung cancer cells (PG) were treated with Icariin in vitro. The results showed that icariin could influence the distribution of PG cells cycle and reduce S phase. Moreover, Icariin increased the level of cAMP in PG cells, reduced the level of cGMP and increased the cAMP/cGMP ratio. These data demonstrate that Icariin maybe a type of effective anticancer drug.

For joint health
Icariin protects murine chondrocytes from lipopolysaccharide-induced inflammatory responses and extracellular matrix degradation.
Nutr Res. 2010; School of Pharmacy, Taipei Medical University, Sinyi District, Taipei City, Taiwan, ROC.
Septic arthritis is an inflammatory arthropathy characterized by degeneration of articular cartilage. Icariin, the main active flavonoid glucoside isolated from Epimedium pubescens, is used as antirheumatics (or antiinflammatory), tonics, and aphrodisiacs in traditional Chinese medicine. In this study, we used lipopolysaccharide (LPS) to simulate the in vitro inflammatory response of chondrocytes during septic arthritis. Our hypothesis is that the icariin can protect chondrocytes from LPS-induced inflammation and extracellular matrix degradation. Our results demonstrate that icariin is a safe anabolic agent of chondrocytes. Icariin may exert its protective effects through inhibition of nitric oxide and MMP synthesis, and may then reduce the extracellular matrix destruction.

Questions
Is icarin the only ingredient in horny goat weed that is helpful for erectile function?
   Most herbs used for sexual enhancement have several substances that have an influence on sexual function. Icariin is the predominant substance in horny goat weed, but there are others. The right icariin dosage has yet to be determined. Some people misspell it as icarrin or icarin.

Icariin is a product contained in Horny Goat Weed in various %’s such as 10, 20 and up to 90%. It has reported pro-sexual side effects relative to firmer erections and delayed ejaculations. Therefore, what would be the generally recommended % of Icarrin for an on demand use prior to sexual activity? What would be the generally recommended amount of time to consume icarrin prior to sexual activity?
    I have not studied this substance enough to know the exact answers regarding the higher percentages and little human research is available to give us much clues. As a general rule, the lower percentages need to be taken several days to be effective.

I am medical student in London, and I am doing research on sex as a whole. I was wondering if you shed some light in why some other manufacturers of Horny Weed Goat have about 60% Icariin in theirs, while yours has 10%. I am a follower of your work and please keep it up.
    Actually our new batch of hgw has 20 instead of 10 percent. I have not tested higher percentages yet but will in the future. Thanks for asking and we both wish you great success with your studies and keep us up to date on your findings and thoughts,