Triacetyl Resveratrol- REVERSE!
- 05-18-2008, 01:32 PM
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)PharmD
- 05-18-2008, 01:56 PM
05-18-2008, 02:00 PM
05-18-2008, 02:05 PM
05-18-2008, 02:11 PM
05-18-2008, 02:16 PM
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!.
05-18-2008, 02:17 PM
05-18-2008, 02:17 PM
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.
05-18-2008, 02:33 PM
05-18-2008, 05:59 PM
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.
05-18-2008, 06:05 PM
05-18-2008, 06:17 PM
05-18-2008, 06:29 PM
The Lab rat has arrived so let me at it!
Trust in the LORD with all your heart, And lean not on your own understanding; In all your ways acknowledge Him, And He shall direct your paths . Proverbs 3:5-6
05-18-2008, 06:30 PM
05-18-2008, 06:32 PM
05-18-2008, 06:34 PM
05-18-2008, 06:39 PM
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05-18-2008, 06:48 PM
05-18-2008, 07:46 PM
No offence to the Québécois that frequent the forums, but does the French diet also promote douchebaggery?
05-18-2008, 11:57 PM
05-19-2008, 07:50 AM
05-19-2008, 12:52 PM
05-19-2008, 01:38 PM
05-20-2008, 05:32 PM
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?".
05-20-2008, 09:55 PM
05-20-2008, 10:48 PM
05-21-2008, 07:27 AM
05-21-2008, 08:33 AM
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.
05-21-2008, 10:06 AM
05-21-2008, 12:22 PM
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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