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Triacetyl Resveratrol- REVERSE!

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    Triacetyl Resveratrol- REVERSE!


    Many of you recently have asked me why it is we chose triacetyl resveratrol over other analogs and what makes triacetyl resveratrol so special in relation to normal resveratrol. I am going to give a quick summary of why it is triacetyl resveratrol is superior to the hydroxy form (normal Res).

    One of the biggest problems of trans-resveratrol is the known low bioavailability of it. In vitro resveratrol exhibits absolutely amazing effects such as anti-aging, anti-tumor, anti-inflammatory, antioxidant, anti-estrogenic, immunomodulatory, and positive effects on bone. In vivo, however, these effects are not as well seen in most doses given in the laboratory. Although these effects are dose dependent it is very common for mega doses of the compound be given to rats to force plasma levels to rise by overpowering the effects of glucorinidation and sulfation. Together glucorinidation and sufation are the biggest threat to achieving high plasma levels of resveratrol. To combat this problem many people have used compounds such as quercetin and piperine to compete for the process. However, there are downsides to this process as well and it is more of a bandaid to a problem rather than a fix.

    The second problem with resveratrol is that it is found in such small quantities in nature. Red wine has on average about 6mg per liter. To achieve 600mg resveratrol one would have to drink 100 liters of red wine, a feat only accomplished by maybe supersoldier and poppypants . One of the compounds that actually protects resveratrol is ethanol, but its use in dietary supplementation is impossible.

    There have been scores of resveratrol analogs studied, each of which had an up side and a down side. It seemed as though pure resveratrol was the absolute best overall compound, but it is sort of a catch 22 since getting high enough plasma levels of resveratrol without mega dosing and breaking the bank was near impossible. Obviously IV and intrathecal administration is out as well. Compounds such as trimethoxy resveratrol shined in anti-tumor studies, showing a 10 fold decrease in tumor growth over resveratrol and more potent inhbition than many anti-tumor pharmaceuticals already on the market. The down side is that trimethoxy resvertrol exhibits close to zero antioxidant properties. Resveratrol itself exhibits antioxidant properties greater than vitamin e.

    Our solution to these problems is simple. Create a compound that absorbs rapidly, resists breakdown, and returns to its natural form. Although triacetyl resveratrol itself exhibits many positive effects it is what happens to this compound in the body that will make it spectacular. First off is intestinal absorption. Resveratrol actually absorbs quite fast compared to many compounds, with absorption rates in vivo of ~ 70nm/s as opposed to the transport marker mannitol which absorbed at a rate of ~ 4nm/s. Since triacetyl resveratrol is much more lipid soluble than resveratrol it will absorb across these lipid membranes at a much faster rate, decreasing exposure to the enzymes responsible for glucorinidation and sulfation. The liver is the next point that triacetyl resveratrol will meet and although some will get broken down, it is well known that acetyl groups resist breakdown better than hydroxy groups. Ester hydrolysis will occur in the body and the product of ester hydrolysis is pure resveratrol. This will allow the highest levels of pure resveratrol to enter the blood stream.




    Triacetyl Resveratrol: R1,R2,R3 = COCH3
    Resveratrol: R1,R2,R3 = H

    Another good article is Enhancement of the oral bioavailability of phenyto...[Biol Pharm Bull. 1998] - PubMed Result.


    Enhancement of the oral bioavailability of phenyto...[Biol Pharm Bull. 1998] - PubMed Result
    Ch20: Hydrolysis of Esters (from picture above)

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    ETA?
    •   
       

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    Quote Originally Posted by slow-mun View Post
    ETA?
    LoL

    As soon as it is done being capsuled. As I have stated before, there will be a little surprise with the capsulation. Takes a little longer but it is worth it.
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    Quote Originally Posted by LakeMountD View Post
    LoL

    As soon as it is done being capsuled. As I have stated before, there will be a little surprise with the capsulation. Takes a little longer but it is worth it.
    Sounds great. I'm eager to snag a couple of bottles and see how they compare to the others that I've ran. I've found my best results with around 3000mg of 50% Trans Res-V. It would be nice to have a lower dosed alternative.
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    I had to take 8-12 caps of Post Cycle Support to notice anything at all. So I really don't know about trans-resveratrol. I haven't heard any amazing results from the transdermal product either from P.P....I think this product is just too expensive to dose high enough to get results. In other words the cost/results ration is too high!.
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    looking forward to it lake
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    I havent read the links yet, but as an example the following abstract would indicate an effective dose for a 200lb male would only be 1800mg's/day (after kg conversion and study it is applied IV). What dose for example would you say is needed to equal this 1800mg's orally to produce the same effect?

    Btw the study uses pterostilbene and quercetin. Pterostilbene (3,5-dimethoxy-4'-hydroxystilbene; PTER) is just methyloxylated res...

    Also how does this equate to triacetyl Resveratrol? What is going to be the recommended daily dosing and any idea on price?

    Association between pterostilbene and quercetin inhibits metastatic activity of B16 melanoma.Ferrer P, Asensi M, Segarra R, Ortega A, Benlloch M, Obrador E, Varea MT, Asensio G, Jordá L, Estrela JM.
    Department of Physiology, University of Valencia, Spain.

    Inhibition of cancer growth by resveratrol (trans-3,5,4'-trihydroxystilbene; RESV), a phytoalexin present in many plant species, is limited by its low bioavailability. Pterostilbene (3,5-dimethoxy-4'-hydroxystilbene; PTER) and quercetin (3,3',4',5,6-pentahydroxyflavone; QUER), two structurally related and naturally occurring small polyphenols, show longer half-life in vivo. In vitro growth of highly malignant B16 melanoma F10 cells (B16M-F10) is inhibited (56%) by short-time exposure (60 min/day) to PTER (40 microm) and QUER (20 microm) (approximate mean values of plasma concentrations measured within the first hour after intravenous administration of 20 mg/kg each polyphenol). Intravenous administration of PTER and QUER (20 mg/kg per day) to mice inhibits (73%) metastatic growth of B16M-F10 cell in the liver, a common site for metastasis development. The anti-metastatic mechanism involves: 1) a PTER-induced inhibition of vascular adhesion molecule 1 expression in the hepatic sinusoidal endothelium, which consequently decreases B16M-F10 cell adhesion to the endothelium through very late activation antigen 4; and 2) a QUER- and PTER-induced inhibition of Bcl-2 expression in metastatic cells, which sensitizes them to vascular endothelium-induced cytotoxicity. Our findings demonstrate that the association of PTER and QUER inhibits metastatic melanoma growth and extends host survival.
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    Quote Originally Posted by Royd The Noyd View Post
    I havent read the links yet, but as an example the following abstract would indicate an effective dose for a 200lb male would only be 1800mg's/day (after kg conversion and study it is applied IV). What dose for example would you say is needed to equal this 1800mg's orally to produce the same effect?

    Btw the study uses pterostilbene and quercetin. Pterostilbene (3,5-dimethoxy-4'-hydroxystilbene; PTER) is just methyloxylated res...

    Also how does this equate to triacetyl Resveratrol? What is going to be the recommended daily dosing and any idea on price?
    Well one thing that I do want to point out is that I can't tell you an exact dosage to take. Most of the human studies conducted on resveratrol are different from one another, some giving lower dosages, some giving much higher dosages and each showing different uM amounts in the blood. I feel it would be impossible to guess at what the equivalent dosage would be for Reverse compared to regular resveratrol without some sort of study. With that being said we are going to start this sort of testing very soon. We have a few companies that we are looking at to conduct our research. We want to answer these sorts of questions but it isn't completely cheap and it does take a little time.

    I have noticed a LOT of people are megadosing res. I don't feel this to be necessary though. Remember you don't always have to "feel" something working for it to work. No one is positive if resveratrol is responsible for the French paradox or not but if it is then it would suggest that resveratrol in low doses taken regularly would be sufficient to exhibit sirt1 activity.
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    Quote Originally Posted by LakeMountD View Post
    Well one thing that I do want to point out is that I can't tell you an exact dosage to take. Most of the human studies conducted on resveratrol are different from one another, some giving lower dosages, some giving much higher dosages and each showing different uM amounts in the blood. I feel it would be impossible to guess at what the equivalent dosage would be for Reverse compared to regular resveratrol without some sort of study. With that being said we are going to start this sort of testing very soon. We have a few companies that we are looking at to conduct our research. We want to answer these sorts of questions but it isn't completely cheap and it does take a little time.

    I have noticed a LOT of people are megadosing res. I don't feel this to be necessary though. Remember you don't always have to "feel" something working for it to work. No one is positive if resveratrol is responsible for the French paradox or not but if it is then it would suggest that resveratrol in low doses taken regularly would be sufficient to exhibit sirt1 activity.

    French Paradox?. You mean why the French are not as fat as Americans?
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    Quote Originally Posted by T-Bone View Post
    French Paradox?. You mean why the French are not as fat as Americans?
    Basically.

    Being that the chemical structure is changed there is obviously potential for unknown toxicity here...definitely interesting product though. I'll just let these guys above try it first.
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    The Lab rat has arrived so let me at it!


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    Quote Originally Posted by Royd The Noyd View Post
    Basically.

    Being that the chemical structure is changed there is obviously potential for unknown toxicity here...definitely interesting product though. I'll just let these guys above try it first.

    That is just because they practice portion control. They just don't over-eat and they eat fresh foods, nothing instant, nothing manufactured. Food you have to cook that takes time to prepare.
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    Quote Originally Posted by T-Bone View Post
    French Paradox?. You mean why the French are not as fat as Americans?
    has nothing to do with fat, just to do with heart attack rates. for all the amount of rich high saturated fats, cheeses, cream sauces, etc they take in, they have some of the lowest incidence of heart disease.
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    Quote Originally Posted by EasyEJL View Post
    has nothing to do with fat, just to do with heart attack rates. for all the amount of rich high saturated fats, cheeses, cream sauces, etc they take in, they have some of the lowest incidence of heart disease.
    Exactly, as well as a longer lifespan.
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    No offence to the Québécois that frequent the forums, but does the French diet also promote douchebaggery?
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    Quote Originally Posted by slow-mun View Post
    No offence to the Québécois that frequent the forums, but does the French diet also promote douchebaggery?
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    Quote Originally Posted by slow-mun View Post
    No offence to the Québécois that frequent the forums, but does the French diet also promote douchebaggery?
    or it might be the hiding from any military conflict that gives the longer average lifespan....
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    do we have an expected dosage/price range yet?
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    Quote Originally Posted by EasyEJL View Post
    do we have an expected dosage/price range yet?
    Not sure of pricing just yet but I believe we are going to do 400mg/serving.
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    French and French-Canadian are completely different. So don't mix up the two. Seriously when I was a young-un we had a french exchange student staying with our family. She over-heard some french canadians, and asked - "What language are they speaking?".
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    good stuff man! looking forward to using the hell out of it!

    Quote Originally Posted by LakeMountD View Post
    Not sure of pricing just yet but I believe we are going to do 400mg/serving.
    will it be 400mg once or twice a day? 30 servings per bottle?
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    Is this anything like what iForce is putting out?
    Just curious...
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    Quote Originally Posted by Iron Lungz View Post
    Is this anything like what iForce is putting out?
    Just curious...
    IForce's ingredient hasnt been released as far as I know. So I'm guessin thats an impossible question to answer at this point. I'm betting its different though (with res being the only similarity).
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    Quote Originally Posted by Iron Lungz View Post
    Is this anything like what iForce is putting out?
    Just curious...
    I think they are making theirs a PCT product, or so I have heard. I think Res in PCT is a dumb idea, so I am not sure why there is the crazy lately.

    By the way dosing is 300mg per serving and there will be a 30 day supply. The cost of this compound is very expensive but the fact that you will be getting higher plasma levels means you don't have to take as much.
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    Quote Originally Posted by LakeMountD View Post
    I think they are making theirs a PCT product, or so I have heard. I think Res in PCT is a dumb idea, so I am not sure why there is the crazy lately.

    By the way dosing is 300mg per serving and there will be a 30 day supply. The cost of this compound is very expensive but the fact that you will be getting higher plasma levels means you don't have to take as much.
    people are using it in PCT because it has SERM like properties. this is true, isn't it? lol.
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    Quote Originally Posted by bassgod272 View Post
    people are using it in PCT because it has SERM like properties. this is true, isn't it? lol.
    This is the most debated subject right now. Resveratrol alone is a phytoestrogen. Depending on the uM concentrations in plasma and depending on which cell types we are referring to it can be estrogenic or anti-estrogenic. In fact in some cell types it is considered a superagonist, where it binds much much stronger than estradiol, in other tissues its affinity for the estrogen receptor is equal to that of estradiol, and again in others it has antagonistic effects. With that being said there isn't really any studies that show whether or not this has any effect on the HPTA. I can't really figure out why people are using it for this purpose anyways considering there are such better options out there. It is like trying to use tylenol for controlling pain while having a tooth removed instead of novocaine (extreme example).

    Not to mention the fact there are studies that show that it increases progesterone levels significantly in vitro. I am the first to say that in vitro isn't a good determining factor, but it is a start and it still shows that it has these properties.
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    I like the AGE reducing properties of Resveratrol. The life extension crowd should love this as will I
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    Quote Originally Posted by LakeMountD View Post
    This is the most debated subject right now. Resveratrol alone is a phytoestrogen. Depending on the uM concentrations in plasma and depending on which cell types we are referring to it can be estrogenic or anti-estrogenic. In fact in some cell types it is considered a superagonist, where it binds much much stronger than estradiol, in other tissues its affinity for the estrogen receptor is equal to that of estradiol, and again in others it has antagonistic effects. With that being said there isn't really any studies that show whether or not this has any effect on the HPTA. I can't really figure out why people are using it for this purpose anyways considering there are such better options out there. It is like trying to use tylenol for controlling pain while having a tooth removed instead of novocaine (extreme example).

    Not to mention the fact there are studies that show that it increases progesterone levels significantly in vitro. I am the first to say that in vitro isn't a good determining factor, but it is a start and it still shows that it has these properties.
    I believe there is also a study showing a 600% increase in prolactin. However it was done on rats with doses that are realistically not attainable in humans if I remember correctly. Definitely different positives/sides at different doses.
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    Quote Originally Posted by LakeMountD View Post
    This is the most debated subject right now. Resveratrol alone is a phytoestrogen. Depending on the uM concentrations in plasma and depending on which cell types we are referring to it can be estrogenic or anti-estrogenic. In fact in some cell types it is considered a superagonist, where it binds much much stronger than estradiol, in other tissues its affinity for the estrogen receptor is equal to that of estradiol, and again in others it has antagonistic effects. With that being said there isn't really any studies that show whether or not this has any effect on the HPTA. I can't really figure out why people are using it for this purpose anyways considering there are such better options out there. It is like trying to use tylenol for controlling pain while having a tooth removed instead of novocaine (extreme example).

    Not to mention the fact there are studies that show that it increases progesterone levels significantly in vitro. I am the first to say that in vitro isn't a good determining factor, but it is a start and it still shows that it has these properties.
    i have only used it once and that was in POST cycle support. i used it as my "PCT" for an epistane 8 week pulse. i took that with Drive and had no issues. i did not get bloodwork, so just going by how i felt doesn't prove anything at all. i didn't get gyno though! i felt good the entire time also. i agree 100% that there are much better options available for the PCT time frame. thanks a lot for the solid info, reps.
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    Quote Originally Posted by LakeMountD View Post
    This is the most debated subject right now. Resveratrol alone is a phytoestrogen. Depending on the uM concentrations in plasma and depending on which cell types we are referring to it can be estrogenic or anti-estrogenic. In fact in some cell types it is considered a superagonist, where it binds much much stronger than estradiol, in other tissues its affinity for the estrogen receptor is equal to that of estradiol, and again in others it has antagonistic effects. With that being said there isn't really any studies that show whether or not this has any effect on the HPTA. I can't really figure out why people are using it for this purpose anyways considering there are such better options out there. It is like trying to use tylenol for controlling pain while having a tooth removed instead of novocaine (extreme example).

    Not to mention the fact there are studies that show that it increases progesterone levels significantly in vitro. I am the first to say that in vitro isn't a good determining factor, but it is a start and it still shows that it has these properties.
    As I understand it, Res is used in PCT not for stimulating the HTPA, but to prevent Gyno as studies suggest it inhibits Breast Tissue stimulation by estrogen (a factor in breast cancer) by binding to receptor sites in the area without activating them. Although, some rat or mouse studies showed increases in sperm count with the use of RES suggesting that it does perhaps do something to the HPTA.

    I too keep reading that it is a phyto estrogen ect, so I'm just not sure about it's real world applications or side effects thereof when it comes to PCT, or anything else beyond Anti-Ox properties for that matter.
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    Quote Originally Posted by saludable24 View Post
    I too keep reading that it is a phyto estrogen ect, so I'm just not sure about it's real world applications or side effects thereof when it comes to PCT, or anything else beyond Anti-Ox properties for that matter.
    well the fact that it is a phyto estrogen is the reason it has serm like capabilities. serm is "selective estrogen receptor modulator" and like you said it tends to bind with the receptors in breast tissue, which means estradiol can't, so it reduces chance of gyno (as a phytoestrogen its far weaker than estradiol is).
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    Quote Originally Posted by EasyEJL View Post
    as a phytoestrogen its far weaker than estradiol is).
    This is actually incorrect as stated. As I have mentioned before, it depends on the cell type. In some cell types, such as MCF-7, resveratrol functioned as a superagonist, meaning it was far stronger than estradiol in promoting an estrogen response. MCF-7 is the human breast adenocarcinoma cell line. Resveratrol also increased the expression of native estrogen-regulated genes, and it stimulated the proliferation of estrogen-dependent
    T47D breast cancer cells, so saying that it rids the body of breast cancer is also false given some studies that are out there. Bottom line is there isn't much research on resveratrol and its effects on androgens in males and females. This is why I think it is stupid to use it in PCT. Everyone wants the newest thing, but frankly there are a lot better choices out there for controlling estrogen levels and blocking estrogen receptors than resveratrol trust me. I will note, however, that some studies stated the opposite in the above cell lines, but then it comes down to who you want to believe?

    The biggest thing here is SIRT1 activation. We all want to live longer and that is the most promising area of research right now. Quercetin and these other ingredients can actually inhibit activation, so using it to prevent glucorinidation isn't going to do you a lot of good.
  37. Never enough
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    yah, there really needs to be more studies, and in actual humans in vivo.
    This space for rent

    Phenadrol Log http://anabolicminds.com/forum/suppl...-hell-did.html - AMAZING fat loss results so far
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    Quote Originally Posted by EasyEJL View Post
    yah, there really needs to be more studies, and in actual humans in vivo.
    Problem is, it is not profitable yet. Big pharma who has the money to conduct these studies won't do so until they see a reason to do so and rightfully so. The rest of the studies are not by any means standardized and I am sure there is a large error base out there by research groups using poor scientific method.
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    Quote Originally Posted by LakeMountD View Post
    This is actually incorrect as stated. As I have mentioned before, it depends on the cell type. In some cell types, such as MCF-7, resveratrol functioned as a superagonist, meaning it was far stronger than estradiol in promoting an estrogen response. MCF-7 is the human breast adenocarcinoma cell line. Resveratrol also increased the expression of native estrogen-regulated genes, and it stimulated the proliferation of estrogen-dependent
    T47D breast cancer cells, so saying that it rids the body of breast cancer is also false given some studies that are out there. Bottom line is there isn't much research on resveratrol and its effects on androgens in males and females. This is why I think it is stupid to use it in PCT. Everyone wants the newest thing, but frankly there are a lot better choices out there for controlling estrogen levels and blocking estrogen receptors than resveratrol trust me. I will note, however, that some studies stated the opposite in the above cell lines, but then it comes down to who you want to believe?

    The biggest thing here is SIRT1 activation. We all want to live longer and that is the most promising area of research right now. Quercetin and these other ingredients can actually inhibit activation, so using it to prevent glucorinidation isn't going to do you a lot of good.

    Any better options that are legal without a script and easily obtainable?
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    sounds good lake really looking forward to this
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