A little more Icariin info, plus PDE5 inhibitor info- ENJOY!!

[rms80]

The prerequisites of a SARM (selective androgen reuptake modulator) are the ability of a compound to: "stimulate increases in strength and fat-free mass through testosterone mimetic properties, supporting bone growth, and maintaining and restoring sexual function and general "maleness", while being orally bioavaliable and not effecting blood pressure or blood lipids." Icariin fits every one of these prerequesites, here are some studies:

Asian J Androl. 2006 Sep;8(5):601-5. Epub 2006 Jun 5.Click here to read Links
The testosterone mimetic properties of icariin.

* Zhang ZB,
* Yang QT.

Department of Urology, Second Affiliated Hospital, Shantou University Medical College, Shantou 515041, China. [email protected]

AIM: To evaluate the testosterone mimetic properties of icariin. METHODS: Forty-eight healthy male Sprague-Dawley rats at the age of 15 months were randomly divided into four groups with 12 rats each: the control group (C), the model group (M), the icariin group (ICA) and the testosterone group (T). The reproductive system was damaged by cyclophosphamide (intraperitoneal injection, 20 mg/kg x day) for 5 consecutive days for groups M, ICA and T, at the sixth day, ICA (gastric gavage, 200 mg/kg x day) for the ICA group and sterandryl (subcutaneous injection, 5 mg/rat . day) for the T group for 7 consecutive days, respectively. The levels of serum testosterone, luteinizing hormone (LH), follicle stimulating hormone (FSH), serum bone Gla-protein (BGP) and tartrate-resistant acid phosphatase activity in serum (StrACP) were determined. The histological changes of the testis and the penis were observed by microscope with hematoxylin-eosin (HE) staining and terminal deoxynucleotidyl transferase biotin-dUTP-X nick end labeling (TUNEL), respectively. RESULTS: (1) Icariin improved the condition of reproductive organs and increased the circulating levels of testosterone. (2) Icariin treatment also improved the steady-state serum BGP and might have promoted bone formation. At the same time, it decreased the serum levels of StrACP and might have reduced the bone resorption. (3) Icarrin suppressed the extent of apoptosis of penile cavernosal smooth muscle cells. CONCLUSION: Icariin has testosterone mimetic properties and has therapeutic potential in the management of hypoandrogenism.


Pharmazie. 2005 Dec;60(12):939-42. Links
Icariin, a flavonoid from the herb Epimedium enhances the osteogenic differentiation of rat primary bone marrow stromal cells.Chen KM, Ge BF, Ma HP, Liu XY, Bai MH, Wang Y.
Institute of Orthopaedics, Lanzhou General Hospital, Lanzhou, Gansu 730050, PR China. [email protected]

The herb Epimedium has long been used in Traditional Chinese Medicine to treat bone fracture and prevent osteoporosis. Researchers believe that the flavonoids contained in the herb are the effective component for this activity. However, no single flavonoid has been studied for its effect on bone-related cells. In the present study, icariin, one of the major flavonoids of the herb, supplemented the primary culture medium of rat bone marrow stromal cells (rMSCs) at 0.1 microM , 1 microM and 10 microM respectively. It was found that icariin stimulated the proliferation of rMSCs and increased the number of CFU-F stained positive for alkaline phosphatase in a dose-dependent manner. Icariin also dose-dependently increased the alkaline phosphatase activity, osteoalcin secretion and calcium deposition level of rMSCs during osteogenic induction. The addition of 10 microM icariin caused four times more mineralized bone nodules to be formed by rMSCs than in the control. The results demonstrated that icariin should be an effective component for bone-strengthening activity, and one of the mechanisms is to stimulate the proliferation and enhance the osteogenic differentiation of MSCs.

Pharmacol Biochem Behav. 2005 Dec;82(4):686-94. Epub 2005 Dec 27. Links
Antidepressant-like effect of icariin and its possible mechanism in mice.Pan Y, Kong L, Xia X, Zhang W, Xia Z, Jiang F.
State Key Laboratory of Pharmaceutical Biotechnology, Immunobiological Laboratory, Institute of Functional Biomolecule, Nanjing University, PR China.

The behavioral, neurochemical and neuroendocrine effects of icariin isolated from Epimedium brevicornum were investigated in behavioral despair models of KunMing strain of male mice. Icariin was found to significantly shorten immobility time in the forced swimming test (FST) after orally administration for 21 consecutive days. Icarrin also produced a marked reduction in immobility time in the tail suspension test (TST) when administered for at least 7 consecutive days. The preferable antidepressant action by icariin was obtained at 17.5 and 35 mg/kg in the present study. Moreover, it was observed that the stress of FST exposure induced increases in brain monoamine oxidase (MAO) A and B activities, serum corticotropin-releasing factor (CRF) levels, as well as decreases in brain monoamine neurotransmitter levels. Treatment of icariin for 21 consecutive days mainly reversed the above effects in the mouse FST. These results suggested that icarrin possessed potent antidepressant-like properties that were mediated via neurochemical and neuroendocrine systems.

Asian J Androl. 2005 Dec;7(4):381-8. Links
Effects of icariin on erectile function and expression of nitric oxide synthase isoforms in castrated rats.Liu WJ, Xin ZC, Xin H, Yuan YM, Tian L, Guo YL.
Andrology Center of Peking University First Hospital, Beijing 100009, China.

AIM: To investigate the effect of icariin on erectile function and the expression of nitric oxide synthase (NOS) isoforms in castrated rats. METHODS: Thirty-two adult male Wistar rats were randomly divided into one sham-operated group (A) and three castrated groups (B, C and D). One week after surgery, rats were treated with normal saline (groups A and cool.gif or oral icariin (1 mg/[kg.day] for group C and 5 mg/[kg.day] for group D) for 4 weeks. One week after treatment, the erectile function of the rats was assessed by measuring intracavernosal pressure (ICP) during electrostimulation of the cavernosal nerve. The serum testosterone (ST) levels, the percent of smooth muscle (PSM) in trabecular tissue, and the expression of mRNA and proteins of neuronal nitric oxide synthase (nNOS), inducible nitric oxide synthase (iNOS), endothelial nitric oxide synthase (eNOS) and phosphodiesterase V (PDE5) in corpus cavernosum (CC) were also evaluated. RESULTS: ICP, PSM, ST and the expression of nNOS, iNOS, eNOS and PDE5 were significantly decreased in group B compared with those in group A (P 0.01). However, ICP, PSM and the expression of nNOS and iNOS were increased in groups C and D compared with those in group B (P 0.05). Changes in ST and the expression of eNOS and PDE5 were not significant (P 0.05) in groups C and D compared with those in group B. CONCLUSION: Oral treatment with icariin ( 98.6 % purity) for 4 weeks potentially improves erectile function. This effect is correlated with an increase in PSM and the expression of certain NOS in the CC of castrated rats. These results suggest that icariin may have a therapeutic effect on erectile dysfunction.

Wei Sheng Yan Jiu. 2005 Mar;34(2):191-3. Links
[Effects of Icariin on ovariectomized osteoporotic rats][Article in Chinese]
Bao JR, Yang JW, Li SF, Zhao W, Zhang Q, Yan Y.
Life Science College, Northeast Agricultural University, Harbin 150030, China.

OBJECTIVE: To observe the effects of Icariin on ovariectomized osteoporotic rats. METHODS: Female Wistar rats were ovariectomized and administered different dosage of Icariin and 17beta-estradiol for eight weeks. Bone mineral density (BMD), indexes of biomechanics and bone metabolism-associated biochemical markers were measured. RESULTS: Icariin increased the BMD, maximum load and flexural rigidity in the osteoporotic rats. The activities of serum tartrate-resistant acid phosphatase (TRACP) and bone alkaline phosphatase (BALP) were decreased in the Icraiin-fed ovariectomized rats. CONCLUSION: Icariin 225mg/kg per day could increase the BMD and improve indexes of bone biomechanics in ovariectomized osteoporotic rats. It was effective in preventing bone loss induced by ovariectomy.


Icariin fits all of the criteria for a SARM, except it is in a very well-researched phytochemical extract, not an undeveloped potential pharmaceutical drug- hence the title Phytochemical SARM (P-SARM)


I included these two because Icariin is a strong PDE5 inhibitor, just like Viagra and Cialis

Clin Endocrinol (Oxf). 2004 Sep;61(3):382-6. Links
Type V phosphodiesterase inhibitor treatments for erectile dysfunction increase testosterone levels.
Carosa E,
Martini P,
Brandetti F,
Di Stasi SM,
Lombardo F,
Lenzi A,
Jannini EA.
Department of Experimental Medicine, University of L'Aquila, L'Aquila, Italy.
OBJECTIVE: Lack of sexual activity due to erectile dysfunction (ED) decreases testosterone (T) levels through a central effect on the hypothalamic-pituitary axis. In this paper we studied the effect of different type V phosphodiesterase (PDE5) inhibitor treatments for ED on the reversibility of this endocrine pattern. DESIGN: Open-label, retrospective study. PATIENTS: Seventy-four consecutive patients were treated on demand with sildenafil (Sild) (50 mg) and tadalafil (Tad) 20 mg. MEASUREMENTS: The success in sexual intercourse was recorded and total (tT) and free testosterone (fT) levels were studied before and after 3 months of treatment. RESULTS: Basal level of tT and fT were at the bottom of the normal range and LH levels were at the top of the high normal range. After treatments, this endocrine pattern was reversed in both groups. However, the T increase in Sild-treated patients was significantly lower than in those treated with Tad (4.7 +/- 2.7 vs. 5.1 +/- 0.9, P < 0.001). fT levels followed a directly proportional pattern, while the inverse was found when LH production was studied. The intercourse rate reflected this effect: in fact, the Sild group showed a 4.9 +/- 2.9/month full sexual intercourse rate while in the Tad group a significantly higher rate of sexual intercourse was found (6.9 +/- 4.6/month, P = 0.04). However, drug consumption was comparable between the groups (Sild 4.9 +/- 2.9 vs. Tad 4.4 +/- 2.8 pills/month, P = 0.72). CONCLUSIONS: As it is unlikely that the two drugs have a different direct effect on the pituitary-testis axis, this effect is probably due to the higher frequency of full sexual intercourse in the Tad-treated group, because of the drug's longer half-life.



J Sex Med. 2006 Jul;3(4):716-22. Links
Testosterone:estradiol ratio changes associated with long-term tadalafil administration: a pilot study.
Greco EA,
Pili M,
Bruzziches R,
Corona G,
Spera G,
Aversa A.
Internal Medicine, Department of Medical Pathophysiology, University of Roma La Sapienza, Rome, Italy.
INTRODUCTION: It has been reported that lack of sexual activity due to erectile dysfunction (ED) may be associated with testosterone (T) decline. AIM: To investigate whether the known changes in sex hormones associated with resumption of sexual activity are sustained in the long term. MAIN OUTCOME MEASURES: Primary endpoints were variations from baseline of steroid hormones: total T, free T (f T), and estradiol (E). Secondary endpoints were variations of erectile function domain scores at International Index of Erectile Function-5 (IIEF-5). METHODS: In an open-label fashion, 20 patients (mean age 54.8 +/- 8.4 years) received tadalafil 10-20 mg on demand for 12 months. Exclusion criteria were those reported for phosphodiesterase inhibitors, including hypogonadism and hyperprolactinemia. RESULTS: Tadalafil assumption was safe and well tolerated (overall adverse effects in 15% of patients) and none discontinued medication. A significant decrease in E levels occurred at the end of the study (from 19.9 +/- 9.6 to 16.6 +/- 8.1 ng/dL, P = 0.042 vs. baseline), with parallel increase in the T:E ratio (26.3 +/- 15.3 to 32.6 +/- 17.7, P = 0.05), whereas no changes in T and f T serum levels were observed, respectively (411.4 +/- 131.4 to 434.2 +/- 177.1 ng/dL and 47.7 +/- 15.3 to 49.9 +/- 19.1 pmol/L, not significant). Interestingly, nonparametric subgroup analysis for related samples revealed that E decrease was detectable only in lean (N = 14) but not in obese (N = 6, body mass index > 27.5 kg/m2) subjects (17.8 +/- 10.1 vs. 13.5 +/- 6.8, P < 0.05). A net increase in IIEF-5 scores was observed at the endpoint (13.7 +/- 5.9 vs. 25.7 +/- 2.9, P < 0.0001). CONCLUSIONS: Sustained improvement in sexual function after 12 months of tadalafil administration is associated with increased T:E ratio mainly related to reduction of E levels. We hypothesize that androgen-estrogen cross-talk and possible inhibition of aromatase activity during chronic exposure to tadalafil might have a role in the regulation of erectile function.

 

[rms80]

Urology. 2006 Dec;68(6):1350-4.
Effects of icariin on phosphodiesterase-5 activity in vitro and cyclic guanosine monophosphate level in cavernous smooth muscle cells.

* Ning H,
* Xin ZC,
* Lin G,
* Banie L,
* Lue TF,
* Lin CS.

Knuppe Molecular Urology Laboratory, Department of Urology, University of California, San Francisco, School of Medicine, San Francisco, California 94115, USA.

OBJECTIVES: To investigate the effect of icariin on the cyclic guanosine monophosphate (cGMP)-hydrolytic activity of phosphodiesterase-5 (PDE5) isoforms and the cGMP levels in cavernous smooth muscle cells treated with sodium nitroprusside (SNP). METHODS: PDE5 isoforms (PDE5A1, A2, and A3) were isolated from sf9 insect cells infected with baculoviruses carrying PDE5 isoform cDNA. Icariin was isolated from Epimedii herba. Varying amounts (10(-6) to 10(-11) M) of icariin or zaprinast were added to reaction mixtures containing PDE5 isoforms and cGMP. The inhibitory effects of icariin and zaprinast were analyzed by GraphPad Software and are expressed as concentration that inhibits 50% (IC50) values. Cavernous smooth muscle cells were isolated from 3-month-old rats, treated with icariin (100 and 200 microM) or zaprinast (200 microM) for 15 minutes, and then with 10 microM SNP for 30, 60, 120, 240, and 360 minutes. The cells were then analyzed for the cGMP concentration using an enzyme immunoassay system. RESULTS: Icariin inhibited PDE5A1, A2, and A3 with an IC50 value of 1.0, 0.75, and 1.1 microM, respectively. The corresponding IC50 values for zaprinast were 0.33, 0.23, and 0.32 microM. Icariin consistently outperformed the control (SNP-only treatment) in maintaining greater cGMP levels, particularly at the greater concentration of 200 microM. In contrast, zaprinast at 200 microM did better than the control only at 60 and 360 minutes. CONCLUSIONS: Icariin was inhibitory to all three PDE5 isoforms with similar IC50 values, which were approximately three times greater than those for zaprinast. Icariin was able to enhance cGMP levels in SNP-treated cavernous smooth muscle cells.


J Huazhong Univ Sci Technolog Med Sci. 2006;26(4):460-2.
Effect of icariin on cyclic GMP levels and on the mRNA expression of cGMP-binding cGMP-specific phosphodiesterase (PDE5) in penile cavernosum.

* Jiang Z,
* Hu B,
* Wang J,
* Tang Q,
* Tan Y,
* Xiang J,
* Liu J.

Department of Pharmacology, School of Basic Medical Sciences, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China.

To further investigate the mechanisms of action of icariin (ICA), we assessed the effects of ICA on the in vitro formation of cGMP and cAMP in isolated rabbit corpus cavernosum. Isolated segments of rabbit corpus cavernosum were exposed to increasing concentrations of ICA and the dose-dependent accumulation of cGMP and cAMP was determined in the tissues samples by means of 125I radioimmunoassay. Responses of the isolated tissues preparations to ICA were compared with those obtained with the reference compounds sildenafil (Sild). Furthermore, the effects of ICA on the mRNA expression of specific cGMP-binding phosphodiesterase type V (PDE5) in rat penis were also observed. After incubation with ICA for 6 h or 14 h respectively, the levels of PDE5 mRNA were examined by reverse transcriptase polymerase chain reaction (RT-PCR). The results showed that ICA increased cGMP concentrations directly (P < 0.05), but there was no significant effect on cAMP concentrations (P > 0.05). In the presence of sodium nitroprusside (SNP), a stimulatory agent of cGMP, both ICA and Sild increased cGMP concentrations with increasing dose (P < 0.01). Their EC50 was 4.62 (ICA) and 0.42 (Sild) micromol/L respectively. Under the same condition, ICA and Sild unaltered cAMP level significantly (P > 0.05). There were PDE5A1 and PDE5A2 mRNA expressions in rat corpus cavernosum with PDE5A2 being the dominant isoform. ICA could obviously inhibit these two isoforms mRNA expression in rat penis, and decrease PDE5A1 more pronouncedly (P < 0.01). The present study indicated that the aphrodisiac mechanisms of icariin involved the NO-cGMP signal transduction pathway, with increasing cGMP levels in the corpus cavernosum smooth muscle. The inhibitory effect of icariin on PDE5 mRNA expression, especially on PDE5A1, might account for its molecular mechanisms for its long-term activity.


Asian J Androl. 2003 Mar;5(1):15-8. Links
Effects of icariin on cGMP-specific PDE5 and cAMP-specific PDE4 activities.

* Xin ZC,
* Kim EK,
* Lin CS,
* Liu WJ,
* Tian L,
* Yuan YM,
* Fu J.

Department of Urology, the 1st Hospital, Peking University, 8 Xishiku Street, Xicheng District, Beijing 100034, China. [email protected]

AIM: To clarify the mechanism of the therapeutic action of icariin on erectile dysfunction (ED). METHODS: PDE5 was isolated from the human platelet and PDE4 from the rat liver tissue using the FPLC system (Pharmacia, Milton Keynes, UK) and the Mono Q column. The inhibitory effects of icariin on PDE5 and PDE4 activities were investigated by the two-step radioisotope procedure with [(3)H]-cGMP/[(3)H]-cAMP. Papaverine served as the control drug. RESULTS: Icariin and papaverine showed dose-dependent inhibitory effects on PDE5 and PDE4 activities. The IC(50) of Icariin and papaverine on PDE5 were 0.432 micromol/L and 0.680 micromol/L, respectively and those on PDE4, 73.50 micromol/L and 3.07 micromol/L, respectively. The potencies of selectivity of icariin and papaverine on PDE5 (PDE4/PDE5 of IC(50)) were 167.67 times and 4.54 times, respectively. CONCLUSION: Icariin is a cGMP-specific PDE5 inhibitor that may be developed into an oral effective agent for the treatment of ED.

 

[DAdams91982]

Am I missing something? Is it in a current product, or are you teasing us with prospects? If its the latter, thats not very nice. :rant:

Adams

 

[rms80]

Am I missing something? Is it in a current product, or are you teasing us with prospects? If its the latter, thats not very nice. :rant:

Adams

Teasing you to death Adams!!! J/K- AN is bringing a product to market (RPM) in a couple weeks that contains large amounts of icariin- it will bring your training to the next level!!!!

PS- would you like to try some? PM me- we are giving out samples- don't think they will last long tho....:ntome:

 

[DAdams91982]

Teasing you to death Adams!!! J/K- AN is bringing a product to market (RPM) in a couple weeks that contains large amounts of icariin- it will bring your training to the next level!!!!

PS- would you like to try some? PM me- we are giving out samples- don't think they will last long tho....:ntome:

I just found the other thread, and emailed you from work.

DEFINATELY looking forward to this now. SARM, but c0ck of steel... count me In... Many times!!!!!!

Adams

 

[rms80]

I just found the other thread, and emailed you from work.

DEFINATELY looking forward to this now. SARM, but c0ck of steel... count me In... Many times!!!!!!

Adams

Cool!!! Love the enthusiasm!!!!

 

[ugab37]

Ill PM you my bank account # and you just send me as many bottles as possible. If its whats in the yellow caps(or the white/purple), It will be worth it. Anybody that doesnt try this is missing out on an BIGTIME. I would think this would be huge PCT item as well.

 

[rms80]

Ill PM you my bank account # and you just send me as many bottles as possible. If its whats in the yellow caps(or the white/purple), It will be worth it. Anybody that doesnt try this is missing out on an BIGTIME. I would think this would be huge post cycle therapy item as well.

M-
Thanks bud!! That means a lot coming from you- I think you actually have tried everything on the market!!! Not many people can say that:box:

 

[poison]

Dammit, I'll take a bottle now, blind, and I haven't even tried it yet. No joke.

 

[ugab37]

Dammit, I'll take a bottle now, blind, and I haven't even tried it yet. No joke.

Poison, you got a sample bottle coming your way, dont you?

Well, please post some feedback when you try it.

Actually, it sucks, go ahead and sent it to me, so I can properly dispose of it. Ill send you the KIC stack by MuscleTech and you'll be Mr.Olympia in a week. Watch out for the new ones called manunitKIC and nutbashingKIC(WARNING: These are only for people that spend money on MT supps and are not intended for individuals that have any brain activity)

 

[poison]

:lol:

Yes, samples are on their way. My point is that I'd buy a bottle now despite that, without testing. I haven't seen feedback this good on anything in quite a while, and the ingredient is interesting.

Keep your KIC; I'll take some Assplodan, however, if you could?

 

[buffhunk29]

AHHH HAHA P0ISON YOU crack me up!!

I better see a review from you when you get that sample bottle!!!!!

 

[poison]

You better believe it!

 

[buffhunk29]

Ahhh Yeah Boy!!

Prepare Yourself!!! The Day Of Reckoning Is Coming For You!!!!

 

[bioman]

I'd be down for a sample..I'm in PCT right now.

I've tried lots of different HGW products in the past and liked them a lot. The only problem was that they stopped working after about 3-4 weeks.

 

[buffhunk29]

HEY BIO

I honestly dont think you will have this Problem with RPM!! It just keeps delivering punch after punch!!!

 

[mmowry]

After all the reading I was thinking that this looks like the pct silver bullet!!!!

 

[thewilman]

After all the reading I was thinking that this looks like the post cycle therapy silver bullet!!!!

Hey MM --->>> I was about to ask that! Would you still have to run a SERM also? I'm guessing no?

 

[rms80]

Hey MM --->>> I was about to ask that! Would you still have to run a SERM also? I'm guessing no?

RPM (is based on what I have seen from taking it for 5 weeks) has a very strong AI/anti-estrogenic quality- so probably not- BUT always have one around just in case- just to cover your bases...

 

[thewilman]

Thanks Dirk... can't wait to try it.

And thanks for the awesome customer service! :thumbsup:

I'm the guy that had his IGF-2 Sample taken out of the envelope in transit!

 

[buffhunk29]

YES I was thinking PCT will NEVER BE THE SAME!!!

YOu would have the potential to retain the muscle mass and get even harder and knock out that dirty estrogen!!

 

[supersoldier]

In the first study mentioned, were there any results given as to what happened to the FSH, LH, and Test levels at the end?

Are you guys planning on any bloodwork done, preferably in a healthy subject, like someone who hasn't ran a cycle in a while and has normal values for the above hormones? I'd be really interested in seeing that. :box:

 

[rms80]

Thanks Dirk... can't wait to try it.

And thanks for the awesome customer service! :thumbsup:

I'm the guy that had his IGF-2 Sample taken out of the envelope in transit!

that was weird- postal workers are a funny bunch....

 

[macedaddy]

M-
Thanks bud!! That means a lot coming from you- I think you actually have tried everything on the market!!! Not many people can say that:box:

hey now! i am as big a supplement whore as anyone else!

i want some! :rofl:

 

[rms80]

SS-
Here is the whole shebang- scroll down to the bottom for the results- in a nutshell- FSH and LH were not changed, but free testosterone was increased- SHBG activity was NOT measured, but I am willing to bet that at least some inhibition occurred, and that this was at least part of the M.O.A behind the alterations in free test levels.

My reasoning behind this is plausible- one of the main pharmacological characteristics of aromatase inhibitors is decreased SHBG, and other PDE5 inhibitors such as tadalafil (Cialis) have been shown to have the ability to inhibit aromatase (reference the conclusions of the second tadalafil study)- and positively skew the testosterone:estrogen ratio. Icariin is a PDE5 inhibitor, so I don't think it would be much of a stretch to surmise that this could be the mechanism of action behind this.

That being said, RPM is going to have this effect regardless, because grape seed extract and naringenin are also included in the formula, both of which have AI characteristics- could Icariin be synergistic with these two compounds to further this effect? Not sure- I guess that is where blood work could come in handy- guess we should talk- I'd like to see what this does to blood levels after 5 weeks as well (the duration I have been taking RPM)......

In the first study mentioned, were there any results given as to what happened to the FSH, LH, and Test levels at the end?

Are you guys planning on any bloodwork done, preferably in a healthy subject, like someone who hasn't ran a cycle in a while and has normal values for the above hormones? I'd be really interested in seeing that. :box:

Asian J Androl 2006; 8 (5): 601-605

　

This web only provides the extract of this article. If you want to read the figures and tables, please reference the PDF full text on Blackwell Synergy. Thank you.

- Complementary Medicine -

The testosterone mimetic properties of icariin

Zhen-Bao Zhang, Qing-Tao Yang

Department of Urology, Second Affiliated Hospital, Shantou University Medical College, Shantou 515041, China

Abstract

Aim: To evaluate the testosterone mimetic properties of icariin. Methods: Forty-eight healthy male Sprague-Dawley rats at the age of 15 months were randomly divided into four groups with 12 rats each: the control group (C), the model group (M), the icariin group (ICA) and the testosterone group (T). The reproductive system was damaged by cyclophosphamide (intraperitoneal injection, 20 mg/kg·day) for 5 consecutive days for groups M, ICA and T, at the sixth day, ICA (gastric gavage, 200 mg/kg·day) for the ICA group and sterandryl (subcutaneous injection, 5 mg/rat·day) for the T group for 7 consecutive days, respectively. The levels of serum testosterone, luteinizing hormone (LH), follicle stimulating hormone (FSH), serum bone Gla-protein (BGP) and tartrate-resistant acid phosphatase activity in serum (StrACP) were determined. The histological changes of the testis and the penis were observed by microscope with hematoxylin-eosin (HE) staining and terminal deoxynucleotidyl transferase biotin-dUTP-X nick end labeling (TUNEL), respectively. Results: (1) Icariin improved the condition of reproductive organs and increased the circulating levels of testosterone. (2) Icariin treatment also improved the steady-state serum BGP and might have promoted bone formation. At the same time, it decreased the serum levels of StrACP and might have reduced the bone resorption. (3) Icarrin suppressed the extent of apoptosis of penile cavernosal smooth muscle cells. Conclusion: Icariin has testosterone mimetic properties and has therapeutic potential in the management of hypoandrogenism. (Asian J Androl 2006 Sep; 8: 601_605 )

Keywords: andropause; partial androgen deficiency of the aging male; icariin; hypoandrogenism; testosterone; rats

Correspondence to: Dr Zhen-Bao Zhang, Department of Urology, Second Affiliated Hospital, Shantou University Medical College, Shantou 515041, China.
Tel: +86-754-891-5622, Fax: +86-754-834-6543
E-mail: [email protected]; [email protected]
Received 2005-12-17 Accepted: 2006-03-18
DOI: 10.1111/j.1745-7262.2006.00197.x

1 Introduction

The terms, andropause, partial androgen deficiency of the aging male (PADAM) or late-onset hypogonadism (LOH), describe a clinical entity which has been defined as a syndrome associated with advanced age. This syndrome is characterized by a deficiency in serum testosterone levels that might result in significant alterations in the quality of life and adversely affect the function of multiple organ systems [1]. Profound and diffuse alterations in the reproductive endocrine function and bone metabolism are associated with hypoandrogenism, and will result in a significant decline of physical function and quality of life. Although reports indicate that testosterone supplement therapy (TST) might be an effective way to manage this condition[1], TST has the risk of therapy, and there might be adverse effects on the prostate and cardiovascular risk factors [2].

Icariin (C33H40O15, molecular weight: 676.67) is a flavonoid isolated from the plant Herba epimedii [3, 4], which has been used as

 

[supersoldier]

If I am understanding this correctly here's what I gather:

The rats were given a drug to suppress their reproductive systems. This would equate to a similar scenario with a person using anabolic steroids, in that the testis would be impaired along with suppression of LH and FSH.

Results: (1) Icariin improved the condition of reproductive organs and increased the circulating levels of testosterone.

the concentration of serum testosterone in the ICA group was higher than that in the C group and lower than that in the T group

However, in the present study, there was no significant difference in serum levels of LH and FSH between ICA group and the others. It seems that icariin mainly affects the testis, but further study is required.

So the Icariin is actling very similar to HCG, in that it is directly stimulating the testis. This is why I'd like to see labwork on a person with a functional HPTA (not on, or just coming off cycle), to see if it causes suppression of gonadatropins like HCG would.

It would seem to me (if my above logic is correct), that a good use for the product would be to use it while on cycle to keep the boys going, also boost testosterone while on. I'm a HUGE fan of HCG, and if it were more readily available I would recommend that it be ran during any cycle.

 

[rms80]

If I am understanding this correctly here's what I gather:

The rats were given a drug to suppress their reproductive systems. This would equate to a similar scenario with a person using anabolic steroids, in that the testis would be impaired along with suppression of LH and FSH.
So the Icariin is actling very similar to HCG, in that it is directly stimulating the testis. This is why I'd like to see labwork on a person with a functional HPTA (not on, or just coming off cycle), to see if it causes suppression of gonadatropins like HCG would.

It would seem to me (if my above logic is correct), that a good use for the product would be to use it while on cycle to keep the boys going, also boost testosterone while on. I'm a HUGE fan of HCG, and if it were more readily available I would recommend that it be ran during any cycle.

Interesting- I agree with most of the above- yes, the use (but not overuse) of HCG in-cycle is a good thing, just to keep the boys functioning (a Dr. John-type protocol). I think that some mechs. of action of Icariin are similar to HCG in the testes, BUT (and this is just anecdotal from people who have used RPM) RPM has a profound physique-hardening effect- which is very noticeable, even at higher body fat %'s. HCG has the tendency to cause increased testicular aromatase expression, which will result in increased estrogen levels- now here is the million dollar question:

If Icariin does act like HCG (mimicking LH), wouldn't it increase testicular aromatase, and cause you to hold more water? OR are the AIs included in RPM simply overpowering this effect?

It is a good theory- really gets me thinking- I am still leaning toward the icariin acting as an AI theory (and a subsequent reduction of SHBG), simply because as a PDE5 inhibitor it shares so many pharmokinetics w/ tadalafil- but, like you said, I guess a blood test is the best way to find out- I would like to take SHBG levels Pre- and Post- as well, along with Free Testosterone, LH, and FSH......

 

[supersoldier]

If Icariin does act like HCG (mimicking LH), wouldn't it increase testicular aromatase, and cause you to hold more water? OR are the AIs included in RPM simply overpowering this effect?

It is a good theory- really gets me thinking- I am still leaning toward the icariin acting as an AI theory (and a subsequent reduction of SHBG), simply because as a PDE5 inhibitor it shares so many pharmokinetics w/ tadalafil- but, like you said, I guess a blood test is the best way to find out- I would like to take SHBG levels Pre- and Post- as well, along with Free Testosterone, LH, and FSH......

Bloodwork would be good in two scenarios:

1. Someone not on or coming off a cycle, with normal LH, FSH, test, etc. to see if it suppresses gonadatropins and increases testosterone. It seems like it'll definitely do the latter, just the former is in question...

2. Someone on a steroid known to cause hard shutdown, ie M1T, with pre bloodwork done maybe 1-2 weeks into the M1T showing low/nil test, LH, FSH levels and then another 2 weeks or so after adding the Icariin to see if testosterone levels rise. With HCG in that scenario test will rise, I've seen it in my bloodwork. In this scenario, user testimony would also be very helpful just by observing testicle size, ejaculation volume <--- they'd go up, and also how they feel. M1T would make them feel like ****, and adding HCG would improve overall sense of well being a lot.

I'm not working in a lab anymore, though I think I only have one more unemployment check. :lol: So who knows what the near future will bring...

 

[rms80]

Bloodwork would be good in two scenarios:

1. Someone not on or coming off a cycle, with normal LH, FSH, test, etc. to see if it suppresses gonadatropins and increases testosterone. It seems like it'll definitely do the latter, just the former is in question...

2. Someone on a steroid known to cause hard shutdown, ie M1T, with pre bloodwork done maybe 1-2 weeks into the M1T showing low/nil test, LH, FSH levels and then another 2 weeks or so after adding the Icariin to see if testosterone levels rise. With HCG in that scenario test will rise, I've seen it in my bloodwork. In this scenario, user testimony would also be very helpful just by observing testicle size, ejaculation volume <--- they'd go up, and also how they feel. M1T would make them feel like ****, and adding HCG would improve overall sense of well being a lot.

I'm not working in a lab anymore, though I think I only have one more unemployment check. :lol: So who knows what the near future will bring...

Yeah- M1T will shut you down quick- definitely one of the more abusive compounds on the HPTA- I would love to have access to my own blood panel screening- you really could figure out a TON of stuff real quick- my wife is an RN, and DOES have access- but it kind of has to be for a legitimate medical concern- not just testing some of our crazy-ass theories (j/k we are on the same page) :cheers:

 

[tuberman]

Yeah- M1T will shut you down quick- definitely one of the more abusive compounds on the HPTA- I would love to have access to my own blood panel screening- you really could figure out a TON of stuff real quick- my wife is an RN, and DOES have access- but it kind of has to be for a legitimate medical concern- not just testing some of our crazy-ass theories (j/k we are on the same page) :cheers:

rms,

Some trime in the next few years should we should see at-home blood testing kits that will become very capable as the future arrives. We should be able to test liver and kidney function, and all the basic blood work without going to the doctor. Also, we should be able to screen many genetic propensities for progressive heart disease, syndrome X, and various cancers. Of course, you will be able to check more mundane things such as mineral levels (optimal or not) and vitamin levels.

This is according to "The End of Medicine: How Silcon Valley Will Reboot Your Doctor."

Yet, I've seen other evidence of these trends too. There is a quiet revolution going on and not just by the techies of silcon valley. It includes many, many more options for preventive medicine.

Sports medicine and physiology has always pushed the envelope for many years, but what was once only available to the elite athlete is becoming more available to the average Joe and Janet.

There will be a struggle by doctors to prevent some of this from happening, but the cost of health care will cause a flood tide to push the new technologies and information access through.

:djparty:

 

[rms80]

rms,

Some trime in the next few years should we should see at-home blood testing kits that will become very capable as the future arrives. We should be able to test liver and kidney function, and all the basic blood work without going to the doctor. Also, we should be able to screen many genetic propensities for progressive heart disease, syndrome X, and various cancers. Of course, you will be able to check more mundane things such as mineral levels (optimal or not) and vitamin levels.

This is according to "The End of Medicine: How Silcon Valley Will Reboot Your Doctor."

Yet, I've seen other evidence of these trends too. There is a quiet revolution going on and not just by the techies of silcon valley. It includes many, many more options for preventive medicine.

Sports medicine and physiology has always pushed the envelope for many years, but what was once only available to the elite athlete is becoming more available to the average Joe and Janet.

There will be a struggle by doctors to prevent some of this from happening, but the cost of health care will cause a flood tide to push the new technologies and information access through.

:djparty:

Good post!!!!! Man, I hope you are right- I have heard rumors of impending legislation, but I think public outcry would FAR outweigh and type of effectiveness regarding an FDA-mandated shift to prescription supplements, vitamins, and minerals.

That is the reason for these rumors- the pharmaceutical companies HAVE been trying to slowly push towards doing this, but will not have public support- so yes, I think what you are talking about above will happen, sooner rather than later!! Lack of affordable health care in the United States will eventually impair capitalism (through overpriced government-mandated health plans for small business and even corporations), and this will lead to a TON of people shifting toward the supplement industry for answers.

The only fix for this, at least in my eyes, is to mandate supplements and get certain crooks out of the industry, while at the same, educating individuals that preventative medicine (very ****ty in the US) is attainable (through SCHOOL). How can we teach kids to learn enormous amounts of things, but we can't teach them to eat healthy? Doesn't even make sense!!!!!

Long story short, making vitamins and supplements prescription would piss so many people off so quickly, that the FDA would be forced to overturn any decision of this nature.....

 

[tuberman]

Good post!!!!! Man, I hope you are right- I have heard rumors of impending legislation, but I think public outcry would FAR outweigh and type of effectiveness regarding an FDA-mandated shift to prescription supplements, vitamins, and minerals.

That is the reason for these rumors- the pharmaceutical companies HAVE been trying to slowly push towards doing this, but will not have public support- so yes, I think what you are talking about above will happen, sooner rather than later!! Lack of affordable health care in the United States will eventually impair capitalism (through overpriced government-mandated health plans for small business and even corporations), and this will lead to a TON of people shifting toward the supplement industry for answers.

The only fix for this, at least in my eyes, is to mandate supplements and get certain crooks out of the industry, while at the same, educating individuals that preventative medicine (very ****ty in the US) is attainable (through SCHOOL). How can we teach kids to learn enormous amounts of things, but we can't teach them to eat healthy? Doesn't even make sense!!!!!

Long story short, making vitamins and supplements prescription would piss so many people off so quickly, that the FDA would be forced to overturn any decision of this nature.....

rms,

I'll get back on topic of the thread for a short while. I find your RPM product to look impressive and will definitely give it a go for a couple of months very soon. I emailed for samples yesterday, hopefully there are some left.

You are right, much of the heat on supplements come from the FDA and big pharmacetutical companies, but these people have been rumored to have strong regulatory legislation in the works for years. That doesn't mean they might not get what they want some time soon.

But, can you imagine the fallout. If people think that respect for laws and government reached an all-time low during the Prohibition years. This would make that look small. The results would start a hugh black market without even a smattering of regulation, and the effects would flow over into all pharmaceticals. It would be humorous if not for the numerous deaths and illnesses that would to some extent be put on the heads of those who created the mess. So it's not so much that the government isn't capable of totally ignoring population wants or needs, it's just that here the consequences wouldn't take long to show, and heads would roll before the instigators could move on or move out.

Nope, I don't think the FDA and pharmacies can stop the revolution for long anyway. And, obviously, supplement companies and stores that actually interact with their customers in a serious manner are very much part of that revolution. It creates evangelist customers to help in their marketing, and those intelligent customers are given an input into the possible product decision making process. Very, very cool indeed.

I love your Hell Yeah thread idea too -- so I'll say my...

Hell Yeah

....right here.

 

[rms80]

rms,

I'll get back on topic of the thread for a short while. I find your RPM product to look impressive and will definitely give it a go for a couple of months very soon. I emailed for samples yesterday, hopefully there are some left.

You are right, much of the heat on supplements come from the FDA and big pharmacetutical companies, but these people have been rumored to have strong regulatory legislation in the works for years. That doesn't mean they might not get what they want some time soon.

But, can you imagine the fallout. If people think that respect for laws and government reached an all-time low during the Prohibition years. This would make that look small. The results would start a hugh black market without even a smattering of regulation, and the effects would flow over into all pharmaceticals. It would be humorous if not for the numerous deaths and illnesses that would to some extent be put on the heads of those who created the mess. So it's not so much that the government isn't capable of totally ignoring population wants or needs, it's just that here the consequences wouldn't take long to show, and heads would roll before the instigators could move on or move out.

Nope, I don't think the FDA and pharmacies can stop the revolution for long anyway. And, obviously, supplement companies and stores that actually interact with their customers in a serious manner are very much part of that revolution. It creates evangelist customers to help in their marketing, and those intelligent customers are given an input into the possible product decision making process. Very, very cool indeed.

I love your Hell Yeah thread idea too -- so I'll say my...

Hell Yeah

....right here.

Yeah- got plenty of samples going out this week

Agreed 100% on everything else- the quickest way to lose support/control is to take something away that people love (Prohibition was an EXCELLENT example), and to make them feel like their freedom as an American is being violated (which in this case, it is).

One positive out of potential legislation: it is going to change the way that people view the FDA/FTC and the pharmaceutical companies. I think if the right people ask the right questions, a lot of these organizations/companies are going to lose credibility fast- especially if the media gets involved. The media already IS involved, just on the wrong side of the issue. Drug companies spend millions of dollars advertising with major media outlets, and the conflict of interest/bias is STAGGERING. But if enough people stay informed and find out what is really going on, things can change fast!!!

 

[GotTest]

Bumpin'

 

[celc5]

Bumpin'

Hmm, are you jumpin on the HGW train too? I bet that's why you subbed to this thread... for the icariin studies :think: