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Possible New use for TageX (anti-estrogen?)!
TargeX
TargeX is a transdermal fat-burner, which uses Glycyrrhetinic acid, a compound actually found in licorice. When applied to the skin and absorbed transdermally, can reduce the thickness of subcutaneous fat. In this case, the mechanism of action would appear to be mediated by the catabolic hormone known as cortisol. Specifically, this acid inhibits the ability of 11b-HSD (an enzyme), and this reduces the availability of cortisol at the level of adipocytes (fat cells)(1). Cortisol is involved in aiding lipogenesis (formation of new fat tissue) as well as regulating both the distribution as well as the deposition of fat tissue. (2) In short, the more cortisol you have in a given area, the more likely that area is to be stimulated to create and store new fat.(3)
In a clinical study, the effect of topical Glycyrrhetinic cream was evaluated. In this study, measurements of thigh fat, before and after 1 month of treatment with the cream were taken. In both areas (circumference and the fat layer thickness) the thighs receiving the cream had significantly lower levels of fat.(1) In this particular case, it was also shown that by applying Glycyrrhetinic Acid transdermally, there was only a local inhibition of cortisol and not a systemic (blood plasma) lowering of cortisol. (1) This is important, because although bodyfat levels are lowered by systemic (*oral) ingestion of Glycyrrhetinic Acid, serum testosterone levels are sometimes lowered (4) [and sometimes not (5)]. However, this is why I feel that it’s important to only use a topical Glycyrrhentinic Acid containing product like Targex, and not to actually ingest it orally.
So while its use as a fat-loss compound is fairly well established, I am speculating that TargeX has another possible use. You see, Cortisol seems to be one of the contributing factors in the production of Estrogen via the Aromatase enzyme from androgens present in many types of adipose tissue. (6,7) This is particularly true when looking at mature adipocytes (fat cells), where the presence of cortisol (and other growth factors) strongly influences the conversion of androgens to estrogen. Here’s the full story:
The aromatase enzyme is responsible for transforming androgens such as androstenedione into estrogens such as estrone, as well as for transforming testosterone into estrogen. This enzyme is present in various nonendocrine tissues, particularly in mature fat cells, or “adipocytes”. Aromatase Activity in these cells is modest, though, as this is not a primary site of aromatization. (8) Mature adipocytes express aromatase, which is stimulated to increase by cortisol (when in the presence of adequate insulin) in both sexes. Insulin and cortisol also independently have the potential to induce preadipocyte differentiation with both having a synergistic effect. (9) There are, however, gender differences in pre-adipocyte formation, and this could contribute to a gender-specific pattern of fat distribution. (10) In both cases, however, it is likely that reducing cortisol in the mature adipocyte will also serve to reduce peripheral conversion of Testosterone to Estrogen (E2) and androstenedione (delta) to Estrogen (E1). In obese men, conversion in various peripheral tissues were all increased in proportion to the percentage above their ideal weight, and obese men exhibit increased blood levels and production rates of estrogens. (10)
Now, as you recall from the opening paragraph, Glycyrrhetinic acid reduces the availability of cortisol in adipocytes. Since aromatization seems to be enhanced or promoted to some extent by the presence of cortisol in adipocytes, and this acid reduces the availability of cortisol in adipocytes, it’s possible that Targex may also serve to locally inhibit estrogen production.
So far this theory hasn’t been tested, and there remains a lot of research to do. But I’m reasonably confident that the reason that TargeX is so effective for reducing fat on women’s thighs, is that it not only inhibits cortisol (and therefore lipogenesis), but also serves to moderately inhibit estrogen production locally. I’m not sure how potent this effect will really be, but I think that application of TargeX to existing gyno could be highly beneficial, as could the use of Targex on low to moderate dose cycles to prevent gyno. Again, I’m not saying this is going to be useful as a primary anti-estrogenic compound for steroid users (I don’t feel any topical Anti-Estrogen can be used for that), but I suspect that it’s going to be very useful as an adjunct to other Anti-Estrogens.
References:
1. Steroids. 2005 Jul;70(8):538-42. Epub 2005 Apr 12.
2. J Clin Endocrinol Metab 64:832–835
3. Journal of Clinical Endocrinology & Metabolism, Vol 64, 832-835, Copyright © 1987 by Endocrine Society
4. Exp Clin Endocrinol Diabetes. 2003 Sep;111(6):341-3.
5. Horm Res. 2006;65(2):106-10. Epub 2006 Feb 3.
6. FEBS Lett. 1994 Mar 21;341(2-3):177-81.
7. Int J Obes Relat Metab Disord. 2000 Jul;24(7):875-81.
8. Adipose tissue as as source of hormones. Am J Clin Nutr 47:277–282
9. Eighth International Congress on Obesity (Paris, France, August 29–September 3, 1998). Int J Obes 22[Suppl 3]:P18, p S100
10. Increased estrogen production in obese men. J Clin Endocrinol Metab 48:633–638
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