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Caffeic Acid phenethyl ester

April 22, 2010

What’s In BPI Arimedex?

A new product called Arimedex HD by B.P.I. (Brain Pharma Inc – formerly known as C.M.I) lists some of the most obscure nomenclature I’ve ever seen on a supplement label.    I called up to B.P.I. and asked to speak to someone in the R&D (research & development) department to try to get a clear answer on what these ingredients are so my customers don’t end up putting something in their body that they have no clue what it is.    I was transfered to a man who didn’t identify himself but had a low wraspy voice like someone who’d been drinking scotch or smoking cigars all day, and had what I’d consider a NY or NJ accent.  I politely asked him what those ingredients really are in their “common and usual” names.   He informed me that they “aren’t releasing that information yet”.  Now this is a clear violation of whats called the DSHEA (Dietary Supplement Health Enforcement Act) which states the label of a dietary supplement must include “a list of the ingredients by their common or usual names” and furthermore the DSHEA was put in place to allow consumers to know what is in a supplement before they put it into their bodies so they can make an informed choice.   So I informed this guy that this is a dietary supplement, not a top secret research drug and that his label was not DSHEA compliant and he didn’t have the right to withhold information like that.   He basically told me “so what, you want me to change the rules for you?”……I’m sorry guy, apparently you’re under the assumption that you make the rules when you don’t.   So a little research and thanks to this handy little tool called Google, if BPI won’t release the common names to their Arimedex HD….I WILL.    Here are the ingredients and a their common names along with a little background research and some opinions…..all of this in less than 5 minutes.    I should have told him “we can do this the easy way, or the hard way”:

(3s,4s)-4-[(3,4-dimethoxyphenyl)methyl]-3-hydroxy-3-[[3-methoxy-4-[(2s,3r,4s,5r,6r)-3, 4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-phenyl]methyl]oxolan-2-one is tracheloside

Quote:
An anti-estrogenic lignan glycoside, tracheloside, from seeds of Carthamus tinctorius.

Yoo HH, Park JH, Kwon SW.

College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul, Korea.
Abstract

The lignan glycoside, tracheloside, was isolated from seeds of Carthamus tinctorius (Compositae) as an anti-estrogenic principle against cultured Ishikawa cells by employing a bioassay-linked HPLC-ELSD method. Tracheloside significantly decreased the activity of alkaline phosphatase (AP), an estrogen-inducible marker enzyme, with an IC(50) value of 0.31 microg/ml, a level of inhibition comparable to that of tamoxifen (IC(50) = 0.43 microg/ml).

(2r,3r)-2,3-bis[(4-hydroxy-3-methoxyphenyl)methyl] butane-1,4-diol;(2r,3r,4s,5s,6r)- 6-(hydroxymethyl)oxane-2,3,4,5-tetrol is Secoisolariciresinol diglycoside which is a flaxseed lignan and phytoestrogen there a few studies on it but nothing impressive.

4-[(e)-2-(3,5-dimethoxyphenyl)ethenyl]phenol is a Pterostilbene which is a Stilbenoid, a close cousin of Resveratrol found in grapes.

s)-5-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-3-decanone is Gingerol comes from Ginger, there one study showing how it upregulated depleted testosterone levels in mice with prostate cancer but I didn’t find anything else.

phenethyl(e)-3-(3,4-dihydroxyphenyl)prop-2-enoate is Caffeic Acid phenethyl ester

Quote:
Phytother Res. 2010 Feb;24(2):295-300.
Caffeic acid phenethyl ester, a component of beehive propolis, is a novel selective estrogen receptor modulator.

Jung BI, Kim MS, Kim HA, Kim D, Yang J, Her S, Song YS.

College of Pharmacy, Sookmyung Women’s University, Seoul, Republic of Korea.
Abstract

Caffeic acid phenethyl ester (CAPE) is an active ingredient of beehive propolis with a structure similar to phenolic acid. The estrogenic effects of propolis were previously demonstrated through the activation of an estrogen receptor. To identify the estrogenic properties of propolis, CAPE was evaluated using in vitro and in vivo methods. CAPE showed selective binding affinity to human estrogen receptor beta (hERbeta) rather than hERalpha. CAPE also reduced ERalpha expression in MCF-7 and MDA 231 cells. In the yeast estrogen receptor transcription assay, CAPE produced the transcriptional activity of estrogen-responsive element with EC(50) values of 3.72 x 10(-6) M. CAPE did not increase the growth of MCF-7 estrogen receptor-positive breast cancer cells in doses ranging from 10(-7) to 10(-5) M. In order to understand how CAPE acts in animals, CAPE was tested by a uterotrophic bioassay. Treatment with CAPE (100, 500 mg/kg) did not increase the uterine weight relative to 3 microg/kg 17beta-estradiol treatment. The results indicate that CAPE, which is a selective agonist to hERbeta, but does not show any estrogenic effect on estrogen receptor-positive breast cancer cells and in immature rat uterine tissue, is a potential selective estrogen receptor modulator. (c) 2009 John Wiley & Sons, Ltd.

PMID: 19655397 [PubMed - indexed for MEDLINE]

So there you have it folks…..BPI Arimedex HD – demystified.    Next time you supplement companies think you’re so smart remember, you’re never smarter than Google.

On a personal note:  The guy actually told me he “didn’t appreciate me lecturing him on the DSHEA” and then told me he didn’t care if I carried their products.   Basically saying F-U to your retailers doesn’t go far in this industry so I wish him luck….because he’s going to need it.

Tags: Arimedex HD ingredients, BPI Arimedex, Caffeic Acid phenethyl ester, DSHEA compliance, Gingerol, Pterostilbene, Secoisolariciresinol diglycoside, tracheloside.

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