"the total daily consumption would then be 6.7 g, a pharmacological amount that is not advisable, especially for men, based on studies showing that resveratrol can act as a <span style='color:red'>powerful systemic aromatase inhibitor </span>when very large amounts are taken."
Can someone explain the above statement and ramifications please?
I searched Pub Med with the terms "resveratrol aromatase"
Toxicol Sci. 2006 Jul;92(1):71-7. Epub 2006 Apr 11. Links
The red wine polyphenol resveratrol displays bilevel inhibition on aromatase in breast cancer cells.Wang Y, Lee KW, Chan FL, Chen S, Leung LK.
PMID: 16611627
The administration of 10 nmol/l testosterone-a substrate of aromatase-produced a 50% increase in the MCF-7aro cell number. This cell proliferation specifically induced by testosterone was significantly reduced by 10 microM resveratrol. In addition, 50 microM resveratrol significantly reduced the CYP19-encoding mRNA abundance in SK-BR-3 cells.
Not long ago it was debated here whether serum levels anywhere near this high could be obtained.
ChemMedChem. 2007 Oct 1; [Epub ahead of print] Links
Combining Computational and Biochemical Studies for a Rationale on the Anti-Aromatase Activity of Natural Polyphenols.Neves MA, Dinis TC, Colombo G, Sá E Melo ML.
PMID: 17910019
Aromatase, an enzyme of the cytochrome P450 family, is a very important pharmacological target, particularly for the treatment of breast cancer. The anti-aromatase activity of a set of natural polyphenolic compounds was evaluated in vitro. Strong aromatase inhibitors including flavones, flavanones, resveratrol, and oleuropein, with activities comparable to that of the reference anti-aromatase drug aminoglutethimide, were identified. Through the application of molecular modeling techniques based on grid-independent descriptors and molecular interaction fields, the major physicochemical features associated with inhibitory activity were disclosed, and a putative virtual active site of aromatase was proposed. Docking of the inhibitors into a 3D homology model structure of the enzyme defined a common binding mode for the small molecules under investigation. The good correlation between computational and biological results provides the first rationalization of the anti-aromatase activity of polyphenolic compounds. Moreover, the information generated in this approach should be further exploited for the design of new aromatase inhibitors.
PMID: 17910019
One would expect mild aromatase inhibition over time to cause increased testosterone production.
Resveratrol was once thought to be estrogenic because of its structure, and does show some such effects
in vitro. The situation is complicated, and warrants further study. I don't think anyone can draw definite conclusions yet based on the data available.
I've taken as much as 5g daily, single dose, and the endurance increase was definite. Currently at 2.5 g, still have improved endurance. Even at around 1 g/day there I noted a 5% increase in maximum sustainable power on a cycling ergonometer last spring. I've not used the device since then, but believe subjectively I have more power than I normally would given my level of training. Velopismo has reported similar effects with cycling on similar doses, and other riders in his club have noted his improved performance.
Edited by maxwatt, 25 October 2007 - 07:44 PM.