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    Senior Member Jakeshorts's Avatar
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    Novel phytoandrogens and lipidic augmenters from Eucommia ulmoides.



    Ong VY, Tan BK.

    Department of Pharmacology, Yong Loo Lin School of Medicine, National University of Singapore, 10 Kent Ridge Crescent, 119260, Singapore. yekcheng@yahoo.com <yekcheng@yahoo.com>

    BACKGROUND: Plants containing compounds such as the isoflavonoids, with female hormone-like effects that bind to human estrogen receptors, are known. But none has been previously shown to have corresponding male hormone-like effects that interact with the human androgen receptor. Here, we report that the tree bark (cortex) of the Gutta-Percha tree Eucommia ulmoides possesses bimodal phytoandrogenic and hormone potentiating effects by lipidic components. METHODS: The extracts of E. ulmoides were tested using in-vitro reporter gene bioassays and in-vivo animal studies. Key compounds responsible for the steroidogenic effects were isolated and identified using solid phase extraction (SPE), high performance liquid chromatography (HPLC), thin layer chromatography (TLC), gas chromatography-mass spectroscopy (GC-MS), electron spray ionisation-mass spectroscopy (ESI-MS) and nuclear magnetic resonance (NMR). RESULTS: The following bioactivities of E. ulmoides were found: (1) a phenomenal tripartite synergism exists between the sex steroid receptors (androgen and estrogen receptors), their cognate steroidal ligands and lipidic augmenters isolated from E. ulmoides, (2) phytoandrogenic activity of E. ulmoides was mediated by plant triterpenoids binding cognately to the androgen receptor (AR) ligand binding domain. CONCLUSION: In addition to well-known phytoestrogens, the existence of phytoandrogens is reported in this study. Furthermore, a form of tripartite synergism between sex steroid receptors, sex hormones and plant-derived lipids is described for the first time. This could have contrasting clinical applications for hypogonadal- and hyperlipidaemic-related disorders.

    PMID: 17261169 [PubMed - indexed for MEDLINE]





    Benson first mentioned this with a study of his which I'll be getting here in a second. Pubmed seems to have a good host of research for this shit. Seems interesting to say the least.





    Novel phytoandrogens and lipidic augmenters from Eucommia ulmoides

    Victor YC Ong1,2 and Benny KH Tan1



    Background

    Plants containing compounds such as the isoflavonoids, with female hormone-like effects that bind to human estrogen receptors, are known. But none has been previously shown to have corresponding male hormone-like effects that interact with the human androgen receptor. Here, we report that the tree bark (cortex) of the Gutta-Percha tree Eucommia ulmoides possesses bimodal phytoandrogenic and hormone potentiating effects by lipidic components.

    Methods

    The extracts of E. ulmoides were tested using in-vitro reporter gene bioassays and in-vivo animal studies. Key compounds responsible for the steroidogenic effects were isolated and identified using solid phase extraction (SPE), high performance liquid chromatography (HPLC), thin layer chromatography (TLC), gas chromatography-mass spectroscopy (GC-MS), electron spray ionisation-mass spectroscopy (ESI-MS) and nuclear magnetic resonance (NMR).

    Results

    The following bioactivities of E. ulmoides were found: (1) a phenomenal tripartite synergism exists between the sex steroid receptors (androgen and estrogen receptors), their cognate steroidal ligands and lipidic augmenters isolated from E. ulmoides, (2) phytoandrogenic activity of E. ulmoides was mediated by plant triterpenoids binding cognately to the androgen receptor (AR) ligand binding domain.

    Conclusion

    In addition to well-known phytoestrogens, the existence of phytoandrogens is reported in this study. Furthermore, a form of tripartite synergism between sex steroid receptors, sex hormones and plant-derived lipids is described for the first time. This could have contrasting clinical applications for hypogonadal- and hyperlipidaemic-related disorders.









    May also be some evidence suggesting it help deter lipogenesis:





    Hypoglycemic and hypolipidemic action of Du-zhong (Eucommia ulmoides Oliver) leaves water extract in C57BL/KsJ-db/db mice.



    Park SA, Choi MS, Kim MJ, Jung UJ, Kim HJ, Park KK, Noh HJ, Park HM, Park YB, Lee JS, Lee MK.

    Department of Food and Nutrition, Yeungnam University, Gyeongsan 712-749, Republic of Korea.

    The anti-diabetic efficacy of Du-zhong (Eucommia ulmoides Oliver) leaves water extract (WDZ) was investigated in type 2 diabetic animals. The WDZ was given to C57BL/KsJ-db/db mice as a dietary supplement based on 1% dried whole Du-zhong leaves (0.187 g WDZ/100 g standard diet) for 6 weeks. The WDZ supplementation significantly lowered the blood glucose level and enhanced the glucose disposal in an intraperitoneal glucose tolerance test. The plasma insulin and C-peptide levels were significantly higher in the WDZ group than in the control group, while the glucagon level was lower. The hepatic glucokinase activity was significantly higher in the WDZ group, whereas, the glucose-6-phosphatase and phosphoenolpyruvate carboxykinase activities were significantly lower. The WDZ supplementation also significantly lowered the hepatic fatty acid synthase, HMG-CoA reductase and ACAT activities compared to the control group, while it elevated the lipoprotein lipase activity in the skeletal muscle. The WDZ also altered the plasma and hepatic lipid levels by lowering the cholesterol and triglyceride concentrations, while elevating the plasma HDL-cholesterol level. Therefore, these results suggest that WDZ may partly ameliorate hyperglycemia and hyperlipidemia with type 2 diabetes through increasing glycolysis, suppressing gluconeogenesis and the biosynthesis of fatty acid and cholesterol in the liver.





    I know I did some mild searching once before found the extract for Du-zhong at a chinease medicinal herb shop on line. I think I might try to refind that shop and do a trial.
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    Senior Member Benson's Avatar
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    love to see the fulltext Jake.
    Remember, believe none of what you hear and half of what you see...





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    Senior Member Jakeshorts's Avatar
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    I'm going to assume it's the first one your interested in:



    http://www.biomedcentral.com/1472-6882/7/3



    I'll be reading it myself shortly. Are you skeptic Benson or do phytoandrogens work in a different way that normal androgenic compounds?
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    Senior Member Jakeshorts's Avatar
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    Something else to mention... not sure how beneficial it is considering it's in the prostate AND it apparently has estrogenic activity....



    1: Prostate. 2007 Apr 1;67(5):457-62. Links

    By modulating androgen receptor coactivators, daidzein may act as a phytoandrogen.Chen JJ, Chang HC.

    Department of Urology, En Chu Kong Hospital, Taipei, Taiwan.



    BACKGROUND: To identify the phytoandrogen from phytohormone, we established an assay to assess the androgenicity of phytoestrogens by using androgen receptor (AR) cofactors to modulate the AR transcriptional activity. METHODS: A Dual-luciferase reporter assay was used to evaluate the transcriptional activity of AR stimulated by the phytoestrogen daidzein. RESULTS: The Dual luciferase data showed that daidzein can enhance androgenic effects in AR negative PC-3 cells cotransfected with AR and AR cofactors. In AR and ARA70 positive LNCaP cells, daidzein can enhance ARA55-mediated induction of AR transcriptional activity. With increasing amounts of transfected ARA55, AR transcriptional activity was enhanced by daidzein in a dose-dependent manner. CONCLUSIONS: Although daidzein is a phytoestrogen, it can create androgenic effects when cells are cotransfected with AR cofactors. When screening for phytoandrogens, the modulating effects of AR cofactors with AR should be considered in the assay system.



    PMID: 17252558 [PubMed - indexed for MEDLINE]
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    Senior Member ozzman's Avatar
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    How do you modulate AR cofactors?
    It is in the admission of ignorance and the admission of uncertainty that there is a hope for the continuous motion of human beings in some direction that doesn't get confined, permanently blocked, as it has so many times before in various periods in the history of man. --Richard Feynman

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    Ozz - no expert here, but the the name of the study you asked about seems to imply that daidzeins ARE the method of modulation.... at least the title does. Someone more wise than I (many qualifiers here boys) will have to chime in.



    Found this for justification I'm not completely insane.. or rather - I'm not the only one with possible insanity when it comes to this compound..



    http://www.aphrodisiology.com/phytoandrogens



    it's cheesy, but it was neat to see other's have their eye on it.
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    Senior Member Jakeshorts's Avatar
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    sourced it at a 5:1 extract - 25bucks for 100gs... Looks like th equality is nuts.. but that's salty for 100grams
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    Interesting...



    One angle to consider: Flax was often used as a gynecomastia preventative/reverser. One explanation for its mechanism of action is that the phytoestrogens in flax attach to estrogen receptors, effectively reducing the effect of estrogen. I wonder if it's possible that a phytoandrogen might work in a similar manner - in which case it wouldn't be desirable.


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    Conclusion

    The novel discoveries reported in this study add phytoandrogens and lipidic augmenters to the emerging list of hormomimetics (such as phytoestrogens) known to exist in plants. Pharmaceutical utility of lipidic augmenters in the treatment of hypogonadal conditions such as menopause or andropause could be exploited based on this mechanism of tripartite synergism. The link between excess dietary lipids, hyperandrogenism and hormone-related disorders should also be further explored in the light of these findings.



    from the full text



    I'm not claiming to fully understand what's going, on but they mention specifically treatment for hypogonadal conditions...
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    Senior Member nightop's Avatar
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    Quote Originally Posted by Kimbo' post='446720' date='Jan 7 2008, 02:28 PM
    Interesting...



    One angle to consider: Flax was often used as a gynecomastia preventative/reverser. One explanation for its mechanism of action is that the phytoestrogens in flax attach to estrogen receptors, effectively reducing the effect of estrogen. I wonder if it's possible that a phytoandrogen might work in a similar manner - in which case it wouldn't be desirable.


    Exactly. The molecular pharmacology will have to be explored before one could hypothesize that such compounds would be useful for desirable effects on body comp and health/performance.
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    Senior Member Jakeshorts's Avatar
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    I have no idea what this oil is... but I'm going to research it riiiiggghhttt.... now.





    Effect of Satureja khuzestanica essential oil on male rat fertility.Haeri S, Minaie B, Amin G, Nikfar S, Khorasani R, Esmaily H, Salehnia A, Abdollahi M.

    Laboratory of Toxicology, Department of Toxicology and Pharmacology, Faculty of Pharmacy, and Pharmaceutical Sciences Research Centre, Tehran University of Medical Sciences, Iran.



    This study was undertaken to study the effect of Satureja khuzestanica essential oil (SKEO) in male rat fertility. SKEO was administered orally at doses of 75, 150, and 225 mg/kg/day for 45 days through drinking water. Treated and control rats were mated with female on day 45 of treatment. SKEO significantly improved all the parameters evaluated such as potency, fecundity, fertility index, and litter size. Moreover, concentrations of FSH and testosterone were significantly increased in SKEO-treated groups. Also the weights of testes, seminal vesicles, and ventral prostate weights were increased by SKEO (225 mg/kg). Histopathological analysis showed that in male rats treated with SKEO (150, 225 mg/kg) the number of spermatogonium, spermatid cords, Leydig cells, and spermatozoids was increased. Also in these groups, the Sertoli cells were hypertrophic.



    PMID: 16889906 [PubMed - indexed for MEDLINE]





    looks like it maybe something of merit for the time being... lipid modulation -



    Antioxidant, antidiabetic, antihyperlipidemic,reproduction stimulatory properties and safety of essential oil of Satureja Khuzestanica in rat in vivo: a oxicopharmacological study.Abdollahi M, Salehnia A, Mortazavi SH, Ebrahimi M, Shafiee A, Fouladian F, Keshavarz K, Sorouri S, Khorasani R, Kazemi A.

    Department of Toxicology, Pharmaceutical Sciences Research Center and Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran. mohammad.abdollahi@utoronto.ca



    BACKGROUND: Satureja Khuzestanica is an endemic plant of Iran that is widely distributed in the southern part of the country. It is famous for its medical uses as an analgesic and antiseptic in folk medicine. The present study was designed to explore the toxicological and pharmacological effects of essential oil of Satureja Khuzestanica (SKEO) in vivo. MATERIAL/METHODS: The intraperitoneal LD50 of SKEO was determined. Teratogenicity was determined by administration of SKEO at doses of 500, 1000 and 1500 ppm to pregnant rats during days 6 to 015 of gestation. FRAP and TBARS assays were used to determine total antioxidant power and lipid peroxidation respectively. Diabetes and hyperlipidemia were induced by administration of streptozocin and lipid regimen in rats. SKEO (1000 ppm) was administered in drinking water for 10 days. RESULTS: SKEO is not lethal up to a dose of 2 g kg-1 in rats. In the teratogenicity test, dams of the treated group were active and did not show any signs of toxicity. A significant increase in the number of implantation and live fetuses were observed with SKEO (500 and 1000 ppm) in comparison to the control group. SKEO treatment decreased the normal blood lipid peroxidation level and increased total antioxidant power. Significant decreases in fasting blood glucose and triglyceride levels were observed with SKEO in diabetic and antihyperlipidemic rats respectively. CONCLUSIONS: This preliminary study indicates the safety and interesting stimulatory effect of SKEO on reproduction. The antioxidant properties of SKEO may explain its antidiabetic and triglyceride-lowering effects.



    PMID: 12960922 [PubMed - indexed for MEDLINE]
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    Senior Member Jakeshorts's Avatar
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    any one able to find a source on this shit? I've looked but found literally - nothing.



    Info: it's an aromatic medicinal plant from Iran. It can be injested as well as used for scent. It's part of the Lamiaceae Satureja family and genus. I wasn't able to find the extract OR raw materials. Any help?
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    Pfaffia paniculata-induced changes in plasma estradiol-17beta, progesterone and testosterone levels in mice.Oshima M, Gu Y.

    Graduate School of Medical Imaging, Suzuka University of Medical Science, 1001-1 Kishioka-cho, Suzuka-shi, Mie 510-0293, Japan.



    The present study undertook chemical analysis of components of Pfaffia paniculata roots. In addition, an animal experiment was conducted in which mice had ad libitum access to water enriched with powdered P. paniculata root for 30 days. Changes in plasma concentrations of estradiol-17beta and progesterone in female mice and of testosterone in male mice were ascertained. The results revealed that P. paniculata roots contain two types of phytosteroids, beta-sitosterol and stigmasterol, in addition to other compounds such as pfaffic acid, allantoin, saponins, beta-sitosteryl-beta-D-glucoside, and stigmasteryl-beta-D-glucoside. Regarding changes in plasma concentrations of hormones, levels of the sex hormones estradiol-17beta, progesterone and testosterone were clearly higher for mice that drank P. paniculata root-enriched water than for mice that drank plain water. Powdered P. paniculata root is easily dissolved in feed or water, and as no adverse reactions were seen in mice within 30 days of oral intake, consumption of P. paniculata for long periods of time appears safe.



    PMID: 14967943 [PubMed - indexed for MEDLINE]
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    Senior Member Jakeshorts's Avatar
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    Anabolic effect of Hibiscus rosasinensis Linn. leaf extracts in immature albino male rats.Olagbende-Dada SO, Ezeobika EN, Duru FI.

    Department of Pharmacognosy, Faculty of Pharmacy, College of Medicine, University of Lagos, Idi-Araba, Lagos, Nigeria.



    Many plants remedies have been employed in solving man's health needs especially the nutritive value which enhances health living. Aphrodisiac plants are plants with anabolic properties i.e. they help in protein synthesis and enhances sexual abilities in males. They are also known as androgenic plants because their properties are similar to that of androgen a male hormone. Cold aqueous extract of Hibiscus rosasinensis leaves is reported by local traditional practioners in Western Nigeria to be aphrodisiac. OBJECTIVE: To investigate the anabolic properties of Hibiscus rosasinensis. MATERIALS AND METHOD: Three groups (8/group) of immature male rats of known weights were administered equal doses of aqueous (cold and hot) and alcoholic extracts of Hibiscus rosasinensis leaves for 8 weeks. The gain in body and isolated sexual organs (testis, epididymis, seminal vesicle and prostate) weights were determined after treatment and compared to the value obtained from a fourth untreated group which served as the control. Section through the testes of both the treated and untreated rats were also examined microscopically and displayed as a photomicrograph for comparism. All data were statistically analysed and displaced in graphic form. RESULTS: Over the 8 weeks of treatment, the control, the cold aqueous extract dosed, hot aqueous extract dosed and alcoholic extract dosed rats gained 8%, 15%, 18% and 22% in body weights respectively. The increase in the weight of testis, epididymis, seminal vesicle and prostate of the alcoholic extract dosed rats was 19%, 30%, 31% and 40% respectively. CONCLUSION: The anabolic effect of the leaf extracts of H. rosasinensis is hereby established. More work needs to be done on these leaf extracts to know their effect on the gonadotrophin hormones which regulate the activity of the androgens in relation to spermatogenesis.



    PMID: 17688164 [PubMed - indexed for MEDLINE]
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    Senior Member Jakeshorts's Avatar
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    Effects of Basella alba and Hibiscus macranthus extracts on testosterone production of adult rat and bull Leydig cells.Moundipa PF, Beboy NS, Zelefack F, Ngouela S, Tsamo E, Schill WB, Monsees TK.

    Department of Biochemistry, University of Yaounde I, P. O. Box 812 Yaounde, Cameroon. pmoundipa@uycdc.uninet.cm



    AIM: To determine the androgenic effects of Basella alba and Hibiscus macranthus extracts in the rat and the bull, and to develop a novel in vitro test system using Leydig cells from bull testes. METHODS: The effect of methanol extracts from both plants on testosterone production in isolated Leydig cells from the rat and the bull was analyzed using 125I-radioimmunoassay (125I-RIA). Rat Leydig cells were obtained by common methods, whereas a novel technique was used to purify Leydig cells from bull testes. RESULTS: Bull testes from the slaughter house were a cheap source of pure Leydig cells. In culture, these cells produced testosterone for 5-6 days, which can be stimulated by human chorionic gonadotrophin (hCG). Basella alba extracts significantly enhanced testosterone production in bull and rat Leydig cells in a concentration-dependent manner. Hibiscus macranthus showed no androgenic effect but was shown to inhibit testosterone production at higher concentrations. CONCLUSION: Leydig cells purified from bull testes can be used as an alternative tool in experimental animal research. Certain fractions of Basella alba extract demonstrated androgenic potential whereas Hibiscus macranthus extracts did not.



    PMID: 16281090 [PubMed - indexed for MEDLINE]
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    Senior Member Jakeshorts's Avatar
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    Evaluation of androgenic activity of Zingiber officinale and Pentadiplandra brazzeana in male rats.Kamtchouing P, Mbongue Fandio GY, Dimo T, Jatsa HB.

    Laboratoire de Physiologie Animale, Faculté des Sciences, Université de Yaoundé I, Cameroun.



    AIM: Aqueous extracts of Zingiber officinale and Pentadiplandra brazzeana were tested for their possible androgenic activity in male Wistar rats. METHODS: The aqueous extracts of the two plants were gavaged separately to 2 groups of rats at a similar dose of 600 mg middot kg(-1) middot day(-1) for 8 days. At the end of the treatment, the animals were killed and the blood, testis, epididymis, seminal vesicles and prostate were collected for biochemical analysis. RESULTS: The aqueous extract of Z. officinale significantly increased in the relative weight of the testis, the serum testosterone level, testicular cholesterol level and epididymal a-glucosidase activity. The aqueous extract of P. brazzeana significantly increased the weights of the testis, seminal vesicles and prostate. It also significantly increased the serum and testicular testosterone level. The fructose, alpha-glucosidase and cholesterol levels in P. brazzeana-treated rats were increased by 28 %, 35 % and 114 %, respectively. CONCLUSION: The aqueous extracts of both P. brazzeana and Z. officinale have an androgenic activity, which seems to be more potent with P. brazzeana than with Z. officinale.



    PMID: 12508133 [PubMed - indexed for MEDLINE]
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    Quote Originally Posted by ozzman' post='446700' date='Jan 7 2008, 10:56 AM
    How do you modulate AR cofactors?


    Retroviral transfection.



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    Daidzein & the case of the faulty prostate



    Quote Originally Posted by Jakeshorts' post='446698' date='Jan 7 2008, 10:51 AM
    Something else to mention... not sure how beneficial it is considering it's in the prostate AND it apparently has estrogenic activity....



    1: Prostate. 2007 Apr 1;67(5):457-62. Links

    By modulating androgen receptor coactivators, daidzein may act as a phytoandrogen.Chen JJ, Chang HC.

    Department of Urology, En Chu Kong Hospital, Taipei, Taiwan.



    BACKGROUND: To identify the phytoandrogen from phytohormone, we established an assay to assess the androgenicity of phytoestrogens by using androgen receptor (AR) cofactors to modulate the AR transcriptional activity. METHODS: A Dual-luciferase reporter assay was used to evaluate the transcriptional activity of AR stimulated by the phytoestrogen daidzein. RESULTS: The Dual luciferase data showed that daidzein can enhance androgenic effects in AR negative PC-3 cells cotransfected with AR and AR cofactors. In AR and ARA70 positive LNCaP cells, daidzein can enhance ARA55-mediated induction of AR transcriptional activity. With increasing amounts of transfected ARA55, AR transcriptional activity was enhanced by daidzein in a dose-dependent manner. CONCLUSIONS: Although daidzein is a phytoestrogen, it can create androgenic effects when cells are cotransfected with AR cofactors. When screening for phytoandrogens, the modulating effects of AR cofactors with AR should be considered in the assay system.



    PMID: 17252558 [PubMed - indexed for MEDLINE]


    The malfunction in prostate cancer cells often can be attributed/associated with messed up cofactors. Some act as promotors, some as inhibitors and some both depending on other factors. They can affect many things such as dimer stability, and can cause massive change in AR signalling (and I presume signalling in other nuclear receptors). IIRC one AR cofactor (I forget which one) can increase AR signalling thirty fold in prostate cancer cell lines.



    This study would not be relevent to muscles, recomp etc, but may have an impact on particular types of prostate cancer.



    SKEO and the case of the heavy testicle

    Has anyone got the full texts to 16889906 & 12960922 in english? These seem interesting and promising. One caveat is from what Jake was saying there does not seem to be any peer confirmation of that research groups findings (who produced both of the papers cited). That aside, it is still interesting.



    Zingiber and the case of Wistar's heavy tackle

    These are interesting invivo, although it does not say if they are mature or immature wistar. I am not sure if the first plant is acting as an androgen analog, because if it is effecting testicular weight, it maybe affecting the sertoli cells instead of leydig. The effect may be mediated upsstream eg via the pit or hypothal. It could also be playing with something else outside the HPTA in the testes eg StAR.



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    Senior Member Benson's Avatar
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    Quote Originally Posted by Josh' post='498160' date='Aug 8 2008, 09:06 PM
    These are interesting invivo, although it does not say if they are mature or immature wistar. I am not sure if the first plant is acting as an androgen analog, because if it is effecting testicular weight, it maybe affecting the sertoli cells instead of leydig. The effect may be mediated upsstream eg via the pit or hypothal. It could also be playing with something else outside the HPTA in the testes eg StAR.



    J


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    Board Sponsor zicario's Avatar
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    I found the 20 % phytoandrogen extract from eucommia ulmoides ( Du Zhong ) and about to try it myself soon ( on its way )

    Should be interesting [img]style_emoticons/<#EMO_DIR#>/smile.gif[/img]

    Z

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