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Damiana
I keep reading about this stuff in muscle in fitness. I am not good at breaking down abstracts and studies but is this stuff worth a woot?
Anti-aromatase activity of the constituents from damiana (Turnera diffusa).
Zhao J, Dasmahapatra AK, Khan SI, Khan IA.
Department of Pharmacognosy, School of Pharmacy, University of Mississippi, University, MS 38677, United States.
Abstract
ETHNOPHARMACOLOGICAL RELEVANCE: Damiana (Turnera diffusa Willd. Ex Schult) has traditionally been used as an herbal aphrodisiac. AIM OF THE STUDY: The study was aimed to investigate the anti-aromatse activity and the estrogenic activity of the constituents isolated from Turnera diffusa. MATERIALS AND METHODS: The methanolic extract and 24 compounds isolated from the leaves of Turnera diffusa were evaluated for aromatase activity by using a tritiated-water release assay and for estrogenic activity by using yeast estrogen screen (YES) assay. RESULTS: The methanolic extract demonstrated a dose-dependent inhibitory activity of the aromatase enzyme with the IC(50) value of 63.1 microg/ml. Among the 24 tested compounds, pinocembrin and acacetin showed the most potent inhibition with IC(50) values of 10.8 and 18.7 microM, respectively. Estrogenic activity was also observed in the extract and three compounds including apigenin 7-glucoside, Z-echinacin and pinocembrin with EC(50) values of 10, 20 and 67 microuM, respectively. CONCLUSIONS: The extract of Turnera diffusa and two isolated compounds pinocembrin and acacetin could significantly suppress aromatase activity. Moreover, apigenin 7-glucoside, Z-echinacin and pinocembrin showed estrogenic activity.
PMID: 18948180 [PubMed - indexed for MEDLINE]
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[QUOTE]ETHNOPHARMACOLOGICAL RELEVANCE: Damiana (Turnera diffusa Willd. Ex Schult) has traditionally been used as an herbal aphrodisiac. AIM OF THE STUDY: The study was aimed to investigate the anti-aromatse activity and the estrogenic activity of the constituents isolated from Turnera diffusa. MATERIALS AND METHODS: The methanolic extract and 24 compounds isolated from the leaves of Turnera diffusa were evaluated for aromatase activity by using a tritiated-water release assay and for estrogenic activity by using yeast estrogen screen (YES) assay. RESULTS: The methanolic extract demonstrated a dose-dependent inhibitory activity of the aromatase enzyme with the IC(50) value of 63.1 microg/ml. Among the 24 tested compounds, [B]pinocembrin and acacetin showed the most potent inhibition[/B] with IC(50) values of 10.8 and 18.7 microM, respectively. [B]Estrogenic activity was also observed in the extract and three compounds including apigenin 7-glucoside, Z-echinacin and pinocembrin[/B] with EC(50) values of 10, 20 and 67 microuM, respectively. CONCLUSIONS: The extract of Turnera diffusa and [B]two isolated compounds pinocembrin and acacetin could significantly suppress aromatase activity. Moreover, apigenin 7-glucoside, Z-echinacin and pinocembrin showed estrogenic activity.[/B][/QUOTE]
[QUOTE=Ironman1578]I keep reading about this stuff in muscle in fitness. I am not good at breaking down abstracts and studies but is this stuff worth a woot?[/QUOTE]
While I would wait for in vivo evidence, the Damiana constituents pinocembrin and acacetin would have to be isolated, as the apigenin 7-glucoside, Z-echinacin and pinocembrin constituents displayed an opposing effect as evidenced by their estrogenic activity.
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[QUOTE=NO HYPE;516158673]While I would wait for in vivo evidence, the Damiana constituents pinocembrin and acacetin would have to be isolated, as the apigenin 7-glucoside, Z-echinacin and pinocembrin constituents displayed an opposing effect as evidenced by their estrogenic activity.[/QUOTE]
If the estrogenic activity is less than estradiol then it could be a good thing. A little competitive inhibition.
Let's not forget that damiana has a long history of use as a sexual aid. This facet of any herb is always worth something, imo. Regardless of MOA, we know simply from its centuries of use that it can benefit teh seks.
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[QUOTE=G.W. Hayduke;516160203]If the estrogenic activity is less than estradiol then it could be a good thing. A little competitive inhibition.[/quote]
I think the issue with any increased estrogenic activity is negative feedback.
[QUOTE=G.W. Hayduke;516160203]it can benefit teh seks.[/QUOTE]
haha
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[QUOTE=PinchTheBear;516163943]I think the issue with any increased estrogenic activity is negative feedback.
[/QUOTE]
But if the overall activation is lower and binding affinity higher than estradiol, wouldn't the feedback be lessened? I'm thinking, with no real evidence, that possibly it could function as a sort of SERM.
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[QUOTE=G.W. Hayduke;516164533]But [b]if the overall activation is lower and binding affinity higher than estradiol,[/b] wouldn't the feedback be lessened? I'm thinking, with no real evidence, that possibly it could function as a sort of SERM.[/QUOTE]
Even so, more estrogen (doesn't need to be e2) = less feedback-induced GnRH
My masters in the art of BS makes that irrefutable
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[QUOTE=G.W. Hayduke;516160203]If the estrogenic activity is less than estradiol then it could be a good thing. A little competitive inhibition. Let's not forget that damiana has a long history of use as a sexual aid. This facet of any herb is always worth something, imo. Regardless of MOA, we know simply from its centuries of use that it can benefit teh seks.[/QUOTE]
Noted [which coincides with my in vivo comment]. In contrast however, I was merely evaluating the lower micromolar concentration that was required to activate estrogenic activity vs. the higher concentration needed to inhibit aromatase activity i.e. apigenin 7-glucoside activated estrogenic activity at an EC50 micromolar concentration of 10, whereas pinocembrin required a higher IC50 micromolar concentration of 10.8 to cause inhibition of aromatase activity.
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[QUOTE=NO HYPE;516186003]Noted [which coincides with my in vivo comment]. In contrast however, I was merely evaluating the lower micromolar concentration that was required to activate estrogenic activity vs. the higher concentration needed to inhibit aromatase activity i.e. apigenin 7-glucoside activated estrogenic activity at an EC50 micromolar concentration of 10, whereas pinocembrin required a higher IC50 micromolar concentration of 10.8 to cause inhibition of aromatase activity.[/QUOTE]
So to anyone using whole herb or full-spectrum extract, the point at which anti-aromatase activity begins would probably be offset by the increased estrogenic effects.
[QUOTE=PinchTheBear;516168513]
My masters in the art of BS makes that irrefutable[/QUOTE]
You took the MBS track too? High five! :D
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[QUOTE=G.W. Hayduke;516164533]But if the overall activation is lower and binding affinity higher than estradiol, wouldn't the feedback be lessened? I'm thinking, with no real evidence, that possibly it could function as a sort of SERM.[/QUOTE]
If they are mild estrogen agonists you have a point... kinda want an answer on whether or not this means a synergistic effect (GnRH agonism w/ anti-aromatase) at 10.8+ mircoM concentrations.
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what about mixing it with ganja and smoking it
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[QUOTE=d0ntlookback;516462283]what about mixing it with ganja and smoking it[/QUOTE]
[img]http://teacherweb.com/NJ/ChurchillJuniorHighSchool/MrEitner/DOIT.gif[/img]
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[QUOTE=PinchTheBear;516342543]If they are mild estrogen agonists you have a point... kinda want an answer on whether or not this means a synergistic effect (GnRH agonism w/ anti-aromatase) at [b]10.8+ mircoM concentrations[/b].[/QUOTE]
WTF does that mean?
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[QUOTE=NO HYPE;516186003]Noted [which coincides with my in vivo comment]. In contrast however, I was merely evaluating the lower micromolar concentration that was required to activate estrogenic activity vs. the higher concentration needed to inhibit aromatase activity i.e. apigenin 7-glucoside activated estrogenic activity at an EC50 micromolar concentration of 10, whereas pinocembrin required a higher IC50 micromolar concentration of 10.8 to cause inhibition of aromatase activity.[/QUOTE]
Also WTF does that mean? I should have multi-quoted.
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[QUOTE=Ironman1578;516726883]WTF does that mean?[/QUOTE]
microM is the prefix "micro" meaning one-millionth and M which stands for molar which is a chemical measurement used to measure physical amounts in comparison to a carbon standard. So, microM would be 10^-6 molar. In the case you bolded, it is measuring the amount of solute. 10.8+ refers to the amounts being at least 10.8 microM to achieve the effect.
[QUOTE=Ironman1578;516727363]Also WTF does that mean? I should have multi-quoted.[/QUOTE]
He was contrasting the amount of "stuff" needed to be estrogenic versus the amount needed to act as an anti-aromatase.