You can reach the brain, but in a limited amount

3. interactions nerves

Bio X4. Kinetics

Icariin is able to cross the blood-brain [16] and the barrier after intravenous injection icariin and three vehicles Epimedium] diglycoside (AC) located in the brain, although the most Epimedium] icariin C. seems to be more local in the sciatic nerve. [17] study using intravenous liposome icariin and found 1.83% of the injected dose in the brain after injection of 20 mg / kg liposome icariin and neural levels exceeded 0.2mcg / g of brain mass. [12]

You can reach the brain, but in a limited amount

3.2. Neurological

Has Icariin also have the ability to act as a neuroprotective by inhibiting the pro-oxidant and pro-inflammatory markers in response to stress [18] [19] and can alleviate cognitive impairment resulting from Alhakn- D galactose at a dose of 60 mg / kg of body weight (injection). [20] In vitro studies suggest that it can also protect nerve cells from damage caused by lipopolysaccharide in (Under pro-inflammatory) [21] [22] and theoretically against old age, according to the assessment of the rat model of accelerated aging. [23] High oral Icariin (75-150 mg / kg of body weight) dose was associated with better cognitive biomarkers such as superior and glutathione in these mice. [2. 3]

The study shows that the practice of protective effects through the expression of SIRT1 expression and later PCG-1A. [24]



4. interact with the bone

4.1. Osteoporosis

In vitro studies suggest that icariin is more effective than soy isoflavones in the prevention of osteoporosis because it is more osteogenic (bone formation). [25] similar effects in mice was observed, but not compared to genistein. [26] study was conducted in women after menopause with a combination of soy isoflavones (soy isoflavones 3 mg and 15 mg daidzein) with icariin 60 mg daily for 2 years, and osteoporosis and debilitating bone mineral dramatically. [27]


4.2. Oestrogenicity

Derivatives Icariin, and DesmethylIcaritin Icaritin, has been shown in the laboratory that have estrogenic activity in breast cancer cells. [4] and then I noticed this discovery in vivo (mice) to increase uterine weight of immature mouse and prolong the rut mouse mature. [4] This led to the later study found horny goat weed in postmenopausal women to increase estrogen levels. [28] as Icariin practiced pro-estrogenic effects in itself, but its metabolite (Icaritin) causes other effects Icariin by mouth are uncertain. It also found Icaritin Desmethylicaritin and horny goat weed in the same papers. [29] [2] Another study in men who use 50 grams of hot water extract of Epimedium] Pubescens not find estrogenicity throughout the study period. [30]

Possible explanations for this finding (estrogenicity in women, but not men) may be in Icariin and related structures which both estrogenic and anti-estrogenic activity, and the final result depends on the context. [31]

A structural interpretation of the possible effects of the above is hydroxyl in carbon 4 'in flavonoids main series, which seems to give the carcinogenic effects of flavonoids. 4 'carbon in the main chain is Icariin R3 in the chart above, and desmethyliscaritin the presence of hydroxyl group here. [32] [33] However, carbon 7 'of the ring can also be involved in the estrogenicity. [4]

Estrogenicity also applies to the icariin and related compounds is a complex, many of the relevant bioflavonoids vehicles. There appears to be enough interest to prevent the possible use of testosterone as a large, however.

Bio X4. interact with hormones

5.1. Testosterone

Supplements showed oral Icariin in 1-5mg / kg of body weight in the castrated mice are considerable differences in the strength of erection, but minor changes in testosterone. Specifically 0.1 mg / kg of body weight restore testosterone baseline after injury to the penis, while the weight 5,10mg / kg body ineffective. Not Found [34] results in mice testes removed empty, without any change in testosterone in 1 and 10 mg / kg of body weight icariin. [35]

Study using 200 mg / kg (less than the purity of 0.40%, biologically equivalent to 80 mg / kg) and pointed out more than 7 days icariin that chemically castrated group (average of testosterone was 0.78 +/- 0.44ng / ml) capable to increase testosterone to nearly three times (10.93 +/- 2.03ng / ml) in the control group (3.01 +/- 0.41ng / ml). [3] LH FSH and did not differ between the groups, and assumed mechanism of action to be in the testes of previous studies on rats without testicles ever showed any change in testosterone serum raised, [35] despite the fact that the difference in dose is also the possibility, since A study of cavernous crush any difference observed in the 1 mg / kg of body weight, was higher doses reckoned with in the fight against repression. [35]

Oral doses above 80 mg / kg of pure icariin, after conversion to humans based on the body surface, [36] seems to 12.8mg / kg of body weight per day icariin and icariin 1163mg of man £ 200.

It seems to have to increase testosterone mechanisms, but there are no human studies on this subject.


6. sexual interactions

6.1. Erection

Icariin is a PDE5 (enzyme) selective inhibitors [37] with IC50 between 0.75-1.1mM depending on PDE5 isoform [37] and EC50 about 4.62mmol / L in the compound increase in the corpus cavernosum of the penis. [38] icariin is nearly 100 times higher around for another similarities PDE enzyme PDE5. [39] This effect can be enhanced by adjusting the two halves of hydroxyethyl ether compound, the inhibition of more than 80 times, [40] but this amendment does not occur naturally. A 10 mg / kg of body weight in mice (110 mg for a person 150 £) Icariin practiced pro-erectile dysfunction [35] seems to be more properties and effectiveness after repeated doses. [34] [35] The effectiveness of more than 30 days is proven in the 5-10 mg / kg in an animal model of erectile dysfunction related to blood flow, [41] which is associated with dose 55-110mg for a man 150 £.

And other compounds derived from the family of Epimedium PDE5 inhibitor likely presence of Epimedium second Icarisid] wanshanense (and not different possibilities to a large extent of icariin, about half of Viagra) [42]

Secondary to the inhibition of PDE5, icariin seems to be a strong pro agent for erectile dysfunction. Outperform clearly by Viagra
Lower doses (kg 1-5mg /) able to enhance neural nitric oxide synthase (NOS) expression [35] and inducible (iNOS) expression [34] [35] In addition to the content inhibtion PDE5. Does not seem to effects on iNOS and nNOS are very different from each other at a dose of 1 mg 0.5 mg and 10 mg / kg of body weight [35] indicate that low doses can also exercise benefit, but by different means.

Icariin can also enhance nitric oxide indicates through increased expression of NOS enzymes that can work in synergy with the inhibition of PDE5
Icariin has also been associated with increased neurite outgrowth decade main basin in vitro [35] that may be downstream of P13K and activation of MEK / ERK. [43]