A little more Icariin info, plus PDE5 inhibitor info- ENJOY!!
04-18-2007 07:40 AM
A little more Icariin info, plus PDE5 inhibitor info- ENJOY!!
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. firstname.lastname@example.org
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. Chkeming@yahoo.com.cn
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.
Di Stasi SM,
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.
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.
04-18-2007 07:48 AM
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@example.com
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.
04-18-2007 07:56 AM
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.
04-18-2007 08:02 AM
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!!!!
Originally Posted by DAdams91982
PS- would you like to try some? PM me- we are giving out samples- don't think they will last long tho....
04-18-2007 08:03 AM
I just found the other thread, and emailed you from work.
Originally Posted by rms80
DEFINATELY looking forward to this now. SARM, but c0ck of steel... count me In... Many times!!!!!!
04-18-2007 08:06 AM
Cool!!! Love the enthusiasm!!!!
Originally Posted by DAdams91982
04-18-2007 08:20 AM
Applied Nutriceuticals Rep.
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.
04-18-2007 08:26 AM
Originally Posted by ugab37
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
04-18-2007 09:32 AM
Dammit, I'll take a bottle now, blind, and I haven't even tried it yet. No joke.
04-18-2007 09:39 AM
Applied Nutriceuticals Rep.
Poison, you got a sample bottle coming your way, dont you?
Originally Posted by poison
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)
04-18-2007 11:23 AM
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?
04-18-2007 11:42 AM
AI Sports Fitness Expert
AHHH HAHA P0ISON YOU crack me up!!
I better see a review from you when you get that sample bottle!!!!!
04-18-2007 12:26 PM
04-18-2007 12:42 PM
AI Sports Fitness Expert
Ahhh Yeah Boy!!
Prepare Yourself!!! The Day Of Reckoning Is Coming For You!!!!
04-18-2007 12:50 PM
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.
04-18-2007 12:59 PM
AI Sports Fitness Expert
I honestly dont think you will have this Problem with RPM!! It just keeps delivering punch after punch!!!
04-18-2007 07:13 PM
After all the reading I was thinking that this looks like the pct silver bullet!!!!
Trust in the LORD with all your heart, And lean not on your own understanding; In all your ways acknowledge Him, And He shall direct your paths . Proverbs 3:5-6
04-19-2007 10:00 AM
Hey MM --->>> I was about to ask that! Would you still have to run a SERM also? I'm guessing no?
Originally Posted by mmowry
04-19-2007 10:56 AM
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...
Originally Posted by thewilman
04-19-2007 11:38 AM
Thanks Dirk... can't wait to try it.
And thanks for the awesome customer service!
I'm the guy that had his IGF-2 Sample taken out of the envelope in transit!
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