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Acetylated Resveratrol


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Poll: Would you be interested? (33 member(s) have cast votes)

Actylated Resveratrol

  1. Definitely (23 votes [69.70%])

    Percentage of vote: 69.70%

  2. No (10 votes [30.30%])

    Percentage of vote: 30.30%

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#31 niner

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Posted 20 May 2008 - 04:49 AM

So this would be messing around with blood clotting, in a presumably favorable way. You would want to know that you were not going to be giving someone a hemorrhagic stroke. That would be distinctly sub-optimal. I just don't see how you can sell this stuff without the FDA coming to call.

#32 Reverse

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Posted 20 May 2008 - 01:26 PM

So this would be messing around with blood clotting, in a presumably favorable way. You would want to know that you were not going to be giving someone a hemorrhagic stroke. That would be distinctly sub-optimal. I just don't see how you can sell this stuff without the FDA coming to call.


Not sure what you are implying from the first sentence. This compound would do the complete opposite. What you aren't realizing is that it is going to have the same effects as Resveratrol itself but to different degrees, whether it be more or less. As for the FDA, show me a dietary supplement that is actually approved by the FDA.

www.bulknutrition.com

Head over there and show me one. There is not one. Not to mention the vast amount of steroids and stimulants that saturate the market untouched. We are looking to improve health not make it worse. Heck even if we had millions of dollars to conduct research and go through 3 phases of clinical trials (for years) and the FDA approved it. What does this say? Nothing, look at all the pharmaceutical drugs causing problems; data can and IS skewed. The FDA can not keep up. Vioxx, Adderall, Oxycontin, all of these drugs are unsafe and they were all FDA approved.

Click HERE to rent this advertising spot to support LongeCity (this will replace the google ad above).

#33 maxwatt

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Posted 20 May 2008 - 05:57 PM

So this would be messing around with blood clotting, in a presumably favorable way. You would want to know that you were not going to be giving someone a hemorrhagic stroke. That would be distinctly sub-optimal. I just don't see how you can sell this stuff without the FDA coming to call.


Not sure what you are implying from the first sentence. This compound would do the complete opposite. What you aren't realizing is that it is going to have the same effects as Resveratrol itself but to different degrees, whether it be more or less. As for the FDA, show me a dietary supplement that is actually approved by the FDA.

www.bulknutrition.com

Head over there and show me one. There is not one. Not to mention the vast amount of steroids and stimulants that saturate the market untouched. We are looking to improve health not make it worse. Heck even if we had millions of dollars to conduct research and go through 3 phases of clinical trials (for years) and the FDA approved it. What does this say? Nothing, look at all the pharmaceutical drugs causing problems; data can and IS skewed. The FDA can not keep up. Vioxx, Adderall, Oxycontin, all of these drugs are unsafe and they were all FDA approved.


Not exactly a "Tu Quoque" argument, but close (actually it is a "tu quoque" vis-a-vis the FDA.)

The gist of Reverse's statement is "bulk nutrition is selling a lot of unapproved substances so I can too."

It's quite likely that tri-acetylated resveratrol is harmless, but having gone through as many papers as I could find that touched on the efficacy of resveratrol analogues as sirtuin activators, I think it is unlikely that tri-acetylated resveratrol will be metabolized so as to act on that pathway.

Cautionary tale: An organic chemist acquaintance of mine had the resources to synthesize some Mito-Q. Luckily for him, he thought to feed it to some pet mice before trying it himself. The mice all died.

How are your pet mice making out?

#34 Reverse

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Posted 20 May 2008 - 08:48 PM

So this would be messing around with blood clotting, in a presumably favorable way. You would want to know that you were not going to be giving someone a hemorrhagic stroke. That would be distinctly sub-optimal. I just don't see how you can sell this stuff without the FDA coming to call.


Not sure what you are implying from the first sentence. This compound would do the complete opposite. What you aren't realizing is that it is going to have the same effects as Resveratrol itself but to different degrees, whether it be more or less. As for the FDA, show me a dietary supplement that is actually approved by the FDA.

www.bulknutrition.com

Head over there and show me one. There is not one. Not to mention the vast amount of steroids and stimulants that saturate the market untouched. We are looking to improve health not make it worse. Heck even if we had millions of dollars to conduct research and go through 3 phases of clinical trials (for years) and the FDA approved it. What does this say? Nothing, look at all the pharmaceutical drugs causing problems; data can and IS skewed. The FDA can not keep up. Vioxx, Adderall, Oxycontin, all of these drugs are unsafe and they were all FDA approved.


Not exactly a "Tu Quoque" argument, but close (actually it is a "tu quoque" vis-a-vis the FDA.)

The gist of Reverse's statement is "bulk nutrition is selling a lot of unapproved substances so I can too."

It's quite likely that tri-acetylated resveratrol is harmless, but having gone through as many papers as I could find that touched on the efficacy of resveratrol analogues as sirtuin activators, I think it is unlikely that tri-acetylated resveratrol will be metabolized so as to act on that pathway.

Cautionary tale: An organic chemist acquaintance of mine had the resources to synthesize some Mito-Q. Luckily for him, he thought to feed it to some pet mice before trying it himself. The mice all died.

How are your pet mice making out?


No I promise you that I am not trying to say because they do something then I can too. All I am saying is that just because something is FDA approved does NOT mean it is safe.

As for the acetylated resveratrol and sirtuin activity, ester hydrolysis occurs and the end products are as I showed in the previous page (regular resveratrol). Will there be other analogues? Sure will. Will there be other analogues by simply taking regular resveratrol? Sure will. There are more metabolic processes than we can count. We do currently have a study going on about resveratrol blood levels after acetylated res. supplementation.

I can assure you this would be safer than taking 3g of resveratrol daily like a lot of people on this board. It amazes me! In fact resveratrols effects are vastly different depending on plasma concentrations. Small, medium, and large concentrations have 3 different effects.

#35 Hedgehog

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Posted 20 May 2008 - 10:08 PM

So this would be messing around with blood clotting, in a presumably favorable way. You would want to know that you were not going to be giving someone a hemorrhagic stroke. That would be distinctly sub-optimal. I just don't see how you can sell this stuff without the FDA coming to call.


Not sure what you are implying from the first sentence. This compound would do the complete opposite. What you aren't realizing is that it is going to have the same effects as Resveratrol itself but to different degrees, whether it be more or less. As for the FDA, show me a dietary supplement that is actually approved by the FDA.

www.bulknutrition.com

Head over there and show me one. There is not one. Not to mention the vast amount of steroids and stimulants that saturate the market untouched. We are looking to improve health not make it worse. Heck even if we had millions of dollars to conduct research and go through 3 phases of clinical trials (for years) and the FDA approved it. What does this say? Nothing, look at all the pharmaceutical drugs causing problems; data can and IS skewed. The FDA can not keep up. Vioxx, Adderall, Oxycontin, all of these drugs are unsafe and they were all FDA approved.


Not exactly a "Tu Quoque" argument, but close (actually it is a "tu quoque" vis-a-vis the FDA.)

The gist of Reverse's statement is "bulk nutrition is selling a lot of unapproved substances so I can too."

It's quite likely that tri-acetylated resveratrol is harmless, but having gone through as many papers as I could find that touched on the efficacy of resveratrol analogues as sirtuin activators, I think it is unlikely that tri-acetylated resveratrol will be metabolized so as to act on that pathway.

Cautionary tale: An organic chemist acquaintance of mine had the resources to synthesize some Mito-Q. Luckily for him, he thought to feed it to some pet mice before trying it himself. The mice all died.

How are your pet mice making out?


Even enantiomers can have very different properties.

Posted Image
Enantiomers are mirror-image molecules that are structurally
equivalent but cannot be superimposed because of their
"handedness," or chirality. Also called optical isomers,
in pure solutions one of a pair rotates the plane of polarized
light to the right, the other to the left.

  • the enantiomers of the quinolones and the b-lactam antibiotics are all antibacterial instances in which one member of a pair was pharmacologically active and the other inactive (l-propranolol is a b-blocker; d-propranolol is not),
  • the enantiomers had completely different activities (d-sotalol is a type 3 antiarrhythmic while l-sotalol is a b-blocker) or
  • had different concentration-response relationships for a given propert
http://www.fda.gov/c...ance/stereo.htm

#36 Reverse

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Posted 21 May 2008 - 01:53 AM

So this would be messing around with blood clotting, in a presumably favorable way. You would want to know that you were not going to be giving someone a hemorrhagic stroke. That would be distinctly sub-optimal. I just don't see how you can sell this stuff without the FDA coming to call.


Not sure what you are implying from the first sentence. This compound would do the complete opposite. What you aren't realizing is that it is going to have the same effects as Resveratrol itself but to different degrees, whether it be more or less. As for the FDA, show me a dietary supplement that is actually approved by the FDA.

www.bulknutrition.com

Head over there and show me one. There is not one. Not to mention the vast amount of steroids and stimulants that saturate the market untouched. We are looking to improve health not make it worse. Heck even if we had millions of dollars to conduct research and go through 3 phases of clinical trials (for years) and the FDA approved it. What does this say? Nothing, look at all the pharmaceutical drugs causing problems; data can and IS skewed. The FDA can not keep up. Vioxx, Adderall, Oxycontin, all of these drugs are unsafe and they were all FDA approved.


Not exactly a "Tu Quoque" argument, but close (actually it is a "tu quoque" vis-a-vis the FDA.)

The gist of Reverse's statement is "bulk nutrition is selling a lot of unapproved substances so I can too."

It's quite likely that tri-acetylated resveratrol is harmless, but having gone through as many papers as I could find that touched on the efficacy of resveratrol analogues as sirtuin activators, I think it is unlikely that tri-acetylated resveratrol will be metabolized so as to act on that pathway.

Cautionary tale: An organic chemist acquaintance of mine had the resources to synthesize some Mito-Q. Luckily for him, he thought to feed it to some pet mice before trying it himself. The mice all died.

How are your pet mice making out?


Even enantiomers can have very different properties.

Posted Image
Enantiomers are mirror-image molecules that are structurally
equivalent but cannot be superimposed because of their
"handedness," or chirality. Also called optical isomers,
in pure solutions one of a pair rotates the plane of polarized
light to the right, the other to the left.

  • the enantiomers of the quinolones and the b-lactam antibiotics are all antibacterial instances in which one member of a pair was pharmacologically active and the other inactive (l-propranolol is a b-blocker; d-propranolol is not),
  • the enantiomers had completely different activities (d-sotalol is a type 3 antiarrhythmic while l-sotalol is a b-blocker) or
  • had different concentration-response relationships for a given propert
http://www.fda.gov/c...ance/stereo.htm


Yeah, I am a chemist, I understand enantiamers, but we are not talking about enantiamers here, we aren't referring to the rotation of plane polarized light. This is merely taking the H off of a hydroxyl and replacing it. This is a VERY common thing to do with compounds that have poor bioavailability. Acetyl-L-Carnitine is a good example to use.

#37 Hedgehog

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Posted 21 May 2008 - 03:09 AM

So this would be messing around with blood clotting, in a presumably favorable way. You would want to know that you were not going to be giving someone a hemorrhagic stroke. That would be distinctly sub-optimal. I just don't see how you can sell this stuff without the FDA coming to call.


Not sure what you are implying from the first sentence. This compound would do the complete opposite. What you aren't realizing is that it is going to have the same effects as Resveratrol itself but to different degrees, whether it be more or less. As for the FDA, show me a dietary supplement that is actually approved by the FDA.

www.bulknutrition.com

Head over there and show me one. There is not one. Not to mention the vast amount of steroids and stimulants that saturate the market untouched. We are looking to improve health not make it worse. Heck even if we had millions of dollars to conduct research and go through 3 phases of clinical trials (for years) and the FDA approved it. What does this say? Nothing, look at all the pharmaceutical drugs causing problems; data can and IS skewed. The FDA can not keep up. Vioxx, Adderall, Oxycontin, all of these drugs are unsafe and they were all FDA approved.


Not exactly a "Tu Quoque" argument, but close (actually it is a "tu quoque" vis-a-vis the FDA.)

The gist of Reverse's statement is "bulk nutrition is selling a lot of unapproved substances so I can too."

It's quite likely that tri-acetylated resveratrol is harmless, but having gone through as many papers as I could find that touched on the efficacy of resveratrol analogues as sirtuin activators, I think it is unlikely that tri-acetylated resveratrol will be metabolized so as to act on that pathway.

Cautionary tale: An organic chemist acquaintance of mine had the resources to synthesize some Mito-Q. Luckily for him, he thought to feed it to some pet mice before trying it himself. The mice all died.

How are your pet mice making out?


Even enantiomers can have very different properties.

Posted Image
Enantiomers are mirror-image molecules that are structurally
equivalent but cannot be superimposed because of their
"handedness," or chirality. Also called optical isomers,
in pure solutions one of a pair rotates the plane of polarized
light to the right, the other to the left.

  • the enantiomers of the quinolones and the b-lactam antibiotics are all antibacterial instances in which one member of a pair was pharmacologically active and the other inactive (l-propranolol is a b-blocker; d-propranolol is not),
  • the enantiomers had completely different activities (d-sotalol is a type 3 antiarrhythmic while l-sotalol is a b-blocker) or
  • had different concentration-response relationships for a given propert
http://www.fda.gov/c...ance/stereo.htm


Yeah, I am a chemist, I understand enantiamers, but we are not talking about enantiamers here, we aren't referring to the rotation of plane polarized light. This is merely taking the H off of a hydroxyl and replacing it. This is a VERY common thing to do with compounds that have poor bioavailability. Acetyl-L-Carnitine is a good example to use.


I guess the point I was trying to make was that you can have almost the same structure but have vastly different biological activities. I'm also a chemist and work directly with the FDA and reviewed a company’s data a few months ago. They had two compounds their lead compound had a Methoxy group however, in the animal study they had a few tox issues (not major but enough to raise some eyes). They changed this group back to a hydroxyl group and had a lot less tox issues and actually became the FDA approved version of this drug. I have no idea if Methoxy resveratrol will have any tox issues.

If you don't have any plasma data on this compound or tox issues this is what I could see happening.

Lets use numbers 1,2,3 for each hydroxy group. You could have any one of these methoxy groups getting converted to a hydroxyl group. This gives a few new compounds that we don't know what proteins they will target or if they will target SIRT1. I agree a methoxy version will not be metabolized as fast but do any of its metabolites have deleterious effects? Maybe we could all pitch in a get some mice? That would be pretty cool. We could have a control group on just pure resveratrol and then a group on methoxy resveratrol. Do you have the ability to do this?

#38 maxwatt

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Posted 21 May 2008 - 03:57 AM

(snip)

If you don't have any plasma data on this compound or tox issues this is what I could see happening.

Lets use numbers 1,2,3 for each hydroxy group. You could have any one of these methoxy groups getting converted to a hydroxyl group. This gives a few new compounds that we don't know what proteins they will target or if they will target SIRT1. I agree a methoxy version will not be metabolized as fast but do any of its metabolites have deleterious effects? Maybe we could all pitch in a get some mice? That would be pretty cool. We could have a control group on just pure resveratrol and then a group on methoxy resveratrol. Do you have the ability to do this?


For one thing, he is talking about tri-acetylated resveratrol, not methoxy. Published data on 4'methoxy-resveratrol indicates it is inactive vis-a-vis Sirt1. 4'-acetyl-resveratrol is very active, almost time release on the cellular level, according to published papers by Sinclair and other Sirtris scientists. Tri-acetyl resveratrol I have seen no published data for. I do know a chemist who synthesized it, it's much easier to make than 4', but I have no idea what he did with it, if it worked, or if he even took it or fed it to mice. That he disappeared shortly after he announced he had synthesized it doesn't give me a warm fuzzy feeling, even though that's probably a coincidence. He also got his masters and took a real job.

It is a very good idea to keep some pet mice around. If you tell me the results on the mice, I would have more confidence in possible human applications. There is a good possibility this is superior to resveratrol by avoiding conjugation by the liver before it is absorbed by one's cells. This could be a very good thing. But until we see some test results, this is all wishful thinking.

For that matter, speaking of resveratrol analogues, polydatin is promising and available if you know where to look. Some Japanese researchers have reported on its metabolites, and it results in high blood levels of resveratrol, higher than one gets by taking resveratrol. It seems to bypass intestinal glucoronidation and first pass liver metabolism, giving quite a spike.

#39 Reverse

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Posted 21 May 2008 - 12:31 PM

For one thing, he is talking about tri-acetylated resveratrol, not methoxy. Published data on 4'methoxy-resveratrol indicates it is inactive vis-a-vis Sirt1. 4'-acetyl-resveratrol is very active, almost time release on the cellular level, according to published papers by Sinclair and other Sirtris scientists. Tri-acetyl resveratrol I have seen no published data for. I do know a chemist who synthesized it, it's much easier to make than 4', but I have no idea what he did with it, if it worked, or if he even took it or fed it to mice.



Yeah, 4'-acetyl-res is a pain because you have to use CAL in 1:1 mass ratios with Res. This gets REALLY pricey really fast and most companies aren't willing to do it.

I would love to do a study with you though Hedgehog. You are a very bright guy obviously and I am currently restricted to equipment but maybe we can work together on something for the good of everyone. I am currently working on my Dr. of Pharmacy degree so I am limited to analytical chemistry devices.

#40 raptor2003

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Posted 22 May 2008 - 12:44 PM

For one thing, he is talking about tri-acetylated resveratrol, not methoxy. Published data on 4'methoxy-resveratrol indicates it is inactive vis-a-vis Sirt1. 4'-acetyl-resveratrol is very active, almost time release on the cellular level, according to published papers by Sinclair and other Sirtris scientists. Tri-acetyl resveratrol I have seen no published data for. I do know a chemist who synthesized it, it's much easier to make than 4', but I have no idea what he did with it, if it worked, or if he even took it or fed it to mice.



Yeah, 4'-acetyl-res is a pain because you have to use CAL in 1:1 mass ratios with Res. This gets REALLY pricey really fast and most companies aren't willing to do it.

I would love to do a study with you though Hedgehog. You are a very bright guy obviously and I am currently restricted to equipment but maybe we can work together on something for the good of everyone. I am currently working on my Dr. of Pharmacy degree so I am limited to analytical chemistry devices.


ibelabs is releasing Triacetyl Resveratrol- product name 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

#41 docmaas

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Posted 24 May 2008 - 02:54 PM

What kinds of toxicity tests have you run or are planning to run. This formulation is quite appealing but since it apparently doesn't appear in nature and hasn't been tested for safety I am reluctant to try it. Moreover, I think you need some kind of toxicity tests and some kind of plasma presence testing before it goes to market.

Mike

For one thing, he is talking about tri-acetylated resveratrol, not methoxy. Published data on 4'methoxy-resveratrol indicates it is inactive vis-a-vis Sirt1. 4'-acetyl-resveratrol is very active, almost time release on the cellular level, according to published papers by Sinclair and other Sirtris scientists. Tri-acetyl resveratrol I have seen no published data for. I do know a chemist who synthesized it, it's much easier to make than 4', but I have no idea what he did with it, if it worked, or if he even took it or fed it to mice.



Yeah, 4'-acetyl-res is a pain because you have to use CAL in 1:1 mass ratios with Res. This gets REALLY pricey really fast and most companies aren't willing to do it.

I would love to do a study with you though Hedgehog. You are a very bright guy obviously and I am currently restricted to equipment but maybe we can work together on something for the good of everyone. I am currently working on my Dr. of Pharmacy degree so I am limited to analytical chemistry devices.


ibelabs is releasing Triacetyl Resveratrol- product name 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




#42 Reverse

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Posted 27 May 2008 - 02:45 PM

What kinds of toxicity tests have you run or are planning to run. This formulation is quite appealing but since it apparently doesn't appear in nature and hasn't been tested for safety I am reluctant to try it. Moreover, I think you need some kind of toxicity tests and some kind of plasma presence testing before it goes to market.

Mike

For one thing, he is talking about tri-acetylated resveratrol, not methoxy. Published data on 4'methoxy-resveratrol indicates it is inactive vis-a-vis Sirt1. 4'-acetyl-resveratrol is very active, almost time release on the cellular level, according to published papers by Sinclair and other Sirtris scientists. Tri-acetyl resveratrol I have seen no published data for. I do know a chemist who synthesized it, it's much easier to make than 4', but I have no idea what he did with it, if it worked, or if he even took it or fed it to mice.



Yeah, 4'-acetyl-res is a pain because you have to use CAL in 1:1 mass ratios with Res. This gets REALLY pricey really fast and most companies aren't willing to do it.

I would love to do a study with you though Hedgehog. You are a very bright guy obviously and I am currently restricted to equipment but maybe we can work together on something for the good of everyone. I am currently working on my Dr. of Pharmacy degree so I am limited to analytical chemistry devices.


ibelabs is releasing Triacetyl Resveratrol- product name 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



It actually is found in nature. It is found in various forms of sea life mostly. I will try to find the study that names the genus and species of each. We had our computers stolen a while back so I apologize for the fact that I don't have it on hand.

#43 Reverse

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Posted 18 July 2008 - 04:10 PM

Just an update. I wanted to let everyone know that Shilajit and Glutathionylcobalamin (glutationyl B12) was added to the formulation.

#44 Reverse

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Posted 11 August 2008 - 05:47 PM

Presales will be up any day now. I will let you know the site as soon as our webmaster finishes. It will cost a little cheaper than comparable high purity formulas and contain triacetylated resveratrol, shilajit, and glutathionylcobalmin (glutathionyl b12). If you guys have any questions let me know!

#45 tintinet

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Posted 13 August 2008 - 05:03 PM

Presales will be up any day now. I will let you know the site as soon as our webmaster finishes. It will cost a little cheaper than comparable high purity formulas and contain triacetylated resveratrol, shilajit, and glutathionylcobalmin (glutathionyl b12). If you guys have any questions let me know!



Have you done any additional testing of your triacetylated resveratrol? Any new info, other than product readiness?

Thanks

#46 edward

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Posted 13 August 2008 - 09:02 PM

Presales will be up any day now. I will let you know the site as soon as our webmaster finishes. It will cost a little cheaper than comparable high purity formulas and contain triacetylated resveratrol, shilajit, and glutathionylcobalmin (glutathionyl b12). If you guys have any questions let me know!



Why shilajit (aka Mumiyo)? I was of the understanding that this was simply mineral rich dirt? Just google Shilajit and Mumiyo.

#47 maxwatt

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Posted 04 January 2009 - 01:14 PM

I would still like to see toxicity studies, and plasma level studies, at least in mice.

Edited by maxwatt, 10 January 2009 - 05:17 AM.


#48 renwosing

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Posted 04 January 2009 - 09:08 PM

Reverse,

You are representing IBE?

Product name is Reverse. 60 capsules.

How is the sales so far?

Renwosing

#49 zorba990

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Posted 20 January 2009 - 03:47 AM

Anybody using this?

#50 tintinet

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Posted 21 January 2009 - 04:23 PM

Anybody using this?


May not be available yet. IBE site takes pre-orders.

#51 renwosing

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Posted 22 January 2009 - 11:16 PM

Been available for awhile.

Renwosing

#52 Anthony_Loera

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Posted 25 January 2009 - 04:32 PM

Are there any toxicity studies yet... even on animals?

A

#53 tintinet

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Posted 29 January 2009 - 05:59 PM

Anybody using this?


May not be available yet. IBE site takes pre-orders.


Where?

#54 zorba990

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Posted 30 January 2009 - 03:44 AM

Anybody using this?


May not be available yet. IBE site takes pre-orders.


Where?


http://anabolicminds...re/1002014.html

Haven't tried it. I'll wait a bit...I can't even tell from the label how much is in there and that is a big red flag for me.

Edited by zorba990, 30 January 2009 - 03:49 AM.


#55 renwosing

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Posted 05 April 2009 - 07:29 PM

Any updates on this?

Anybody been taking it for some time? Feedbacks?

I be interested to try this along with injectable res.

Renwosing

#56 2tender

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Posted 05 April 2009 - 10:57 PM

I think you can find feedback at anabolicminds.com type reverse in the search box there.

#57 michael084

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Posted 06 April 2009 - 12:07 AM

I think you can find feedback at anabolicminds.com type reverse in the search box there.


The problem there is that most of the people giving feedback are being paid to do so.

#58 renwosing

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Posted 06 April 2009 - 01:24 PM

Yep. With free Reverse supplement for a period of time, on them.

That's why i ask here.

Renwosing

#59 maxwatt

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Posted 06 April 2009 - 06:38 PM

If it's so good why do they have to do that?

Click HERE to rent this advertising spot to support LongeCity (this will replace the google ad above).

#60 2tender

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Posted 06 April 2009 - 10:54 PM

I dont think they are all shills. Anyway, it doesnt seem to be as popular as some other Res. supplements, personally Im happy with the ones I currently use, which are probably considered "state of the Art" in terms of Resveratrol supplementation. If Acetylated was any better, it would be well known by now, considering the current popularity of Resveratrol, just my thoughts and opinion




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