http://www.anthonyroberts.info/2010/...or-antagonist/
Raspberry Ketone is an androgen receptor antagonist
Posted by Anthony Roberts in Other | 0 comments
A couple of years ago, I remember Biotest sending me some free samples of their new fat burner, and it smelled like raspberries. I thought that was kind of odd, but then I read the product description:
Raspberry Ketone: The Fat Slicer
Raspberry ketone (RK) is an aromatic
compound found in red raspberries. In other words, it's the
stuff that makes raspberries smell like, well, raspberries. Its
molecular structure is similar to capsaicin, which is also
thermogenic.
However, instead of getting its actions through
agonizing beta receptors (like capsaicin), RK causes HSL
(hormone-sensitive lipase) to translocate to within the fat
cell. HSL is the enzyme that, once inside the fat cell, slices
apart fat molecules into various fatty acids in preparation for
fat metabolism.
Furthermore, this particular activity is the
rate-limiting step in lipolysis within the cell. This means that
you cannot have maximum lipolysis without ample supplies of HSL
inside the fat cell. And, RK delivers just like Domino's —
fast!
Fair enough. And I know that they recommended the stuff on the forums pretty aggressively for every kind of fat loss goal, whether it was leaning down for the Summer or cutting up for a bodybuilding contest. Again, fair enough because it looked like a great compound. Unfortunately, it’s not. It actually acts as an androgen receptor antagonist – it lessens the effects of androgens (steroids) on the receptor, and prevents them from exerting their full effects. It makes your natural androgens (testosterone and dihydrotestosterone) less effective, and it also makes your not-so-natural androgens (*ANABOLIC STEROIDS) less effective. Because of this anti-androgenic activity, it can keep your physique from looking as hard as possible at the beach or on contest day, not to mention messing with your gains in general. I don’t even know if they’re still selling the stuff, but I remember thinking that Biotest had actually done something moderately worthwhile, i.e. they introduced an ingredient to the market that nobody else had yet. Well… I guess I spoke too soon, because it turned out to be a crap ingredient. It’s not the worst in the world (it does work for fat loss), it’s just far from ideal (because it is an androgen receptor antagonist), and worth avoiding.
Bioorg Med Chem Lett. 2010 Feb 21. [Epub ahead of print]
Effect of essential oils, such as raspberry ketone and its derivatives, on antiandrogenic activity based on in vitro reporter gene assay.
Ogawa Y, Akamatsu M, Hotta Y, Hosoda A, Tamura H.
Department of Environmental Bioscience, Meijo University, Nagoya 468-8502, Japan.
The effect of essential oils, such as raspberry ketone, on androgen (AR) receptor was investigated using a MDA-kb2 human breast cancer cell line for predicting potential AR activity. Among them, eugenol had the highest AR antagonistic activity with its IC(50) value of 19muM. Raspberry ketone, which has threefold higher anti-obese activity than that of capsaicin, also had AR antagonist activity with its IC(50) value of 252muM. Based on these findings, a more precise CoMFA model was proposed as follows: pIC(50) [log (1/IC(50))]=3.77+[CoMFA field terms] (n=39, s=0.249, r(2)=0.834, s(cv)=0.507, q(2)=0.311 (three components). Copyright 2010. Published by Elsevier Ltd.
PMID: 20226658 [PubMed - as supplied by publisher]
Interesting
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