guggulsteroni

greatescape · **guggulsteroni -** 29-06-2007, 12:12 AM

in questi giorni stavo cercando un prodotto tipo lipo 6 che mi desse una mano a tirarmi ancora un po di piu per l'estate ...

girando un po per la rete ho trovato un articolo che parlava di questo integratore e di una ricerca medica a riguardo .. posto l'articolo in inglese ...

the guggulsterone issue
First the study that it raises cholesterol and now this study.

Why are people still putting this in supplements?

Mol Pharmacol. 2005 Mar;67(3):948-54. Epub 2004 Dec 15. Related Articles, Links

The hypolipidemic natural product guggulsterone is a promiscuous steroid receptor ligand.

Burris TP, Montrose C, Houck KA, Osborne HE, Bocchinfuso WP, Yaden BC, Cheng CC, Zink RW, Barr RJ, Hepler CD, Krishnan V, Bullock HA, Burris LL, Galvin RJ, Bramlett K, Stayrook KR.

Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285, USA. burris@lilly.com

Guggulsterone (GS) is the active substance in guggulipid, an extract of the guggul tree, Commiphora mukul, used to treat a variety of disorders in humans, including dyslipidemia, obesity, and inflammation. The activity of GS has been suggested to be mediated by antagonism of the receptor for bile acids, the farnesoid X receptor (FXR). Here, we demonstrate that both stereoisomers of the plant sterol, (E)- and (Z)-GS, bind to the steroid receptors at a much higher affinity than to FXR. Both stereoisomers bind to the mineralocorticoid receptor (MR) with a Ki value of approximately 35 nM, which is greater than 100 times more potent than their affinity for FXR. Both (E)- and (Z)-GS also displayed high affinity for other steroid receptors, including the androgen (AR), glucocorticoid (GR), and progesterone receptors (PR) with Ki values ranging from 224 to 315 nM. In cell-based functional cotransfection assays, GSs behaved as antagonists of AR, GR, and MR, but as agonists of PR. Agonist activity was also demonstrated with estrogen receptor (ER) alpha; however, the potency was very low (EC50 > 5000 nM). In addition, GS displayed activity in functional assays in cell lines expressing endogenous AR, GR, ER, and PR. These data suggest that the variety of pharmacological effects exhibited by GS may be mediated by targeting several steroid receptors.

praticamente ...
basically that it blocks the androgen receptor (the receptor that makes testosterone and other steroids "work")

and that it activates the progesterone receptor, which I beleive is why people fell "hot", basically a menapausal "hotflash"

volevo sapere cosa ne pensavate dell'articolo .. se quacluno ne era a conoscenza ... io sapevo che se ne parlava bene dei guggulsteroni e avevano anche proprieta positive sull'organismo e sul sangue ...

ditemi cosa ne pensate e se sono da evitare ...

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greatescape All the Truth Member Messaggi: 20,462 Data registrazione: Jun 2007	guggulsteroni - 29-06-2007, 12:12 AM guggulsteroni in questi giorni stavo cercando un prodotto tipo lipo 6 che mi desse una mano a tirarmi ancora un po di piu per l'estate ... girando un po per la rete ho trovato un articolo che parlava di questo integratore e di una ricerca medica a riguardo .. posto l'articolo in inglese ... the guggulsterone issue First the study that it raises cholesterol and now this study. Why are people still putting this in supplements? Mol Pharmacol. 2005 Mar;67(3):948-54. Epub 2004 Dec 15. Related Articles, Links The hypolipidemic natural product guggulsterone is a promiscuous steroid receptor ligand. Burris TP, Montrose C, Houck KA, Osborne HE, Bocchinfuso WP, Yaden BC, Cheng CC, Zink RW, Barr RJ, Hepler CD, Krishnan V, Bullock HA, Burris LL, Galvin RJ, Bramlett K, Stayrook KR. Lilly Research Laboratories, Lilly Corporate Center, Indianapolis, IN 46285, USA. burris@lilly.com Guggulsterone (GS) is the active substance in guggulipid, an extract of the guggul tree, Commiphora mukul, used to treat a variety of disorders in humans, including dyslipidemia, obesity, and inflammation. The activity of GS has been suggested to be mediated by antagonism of the receptor for bile acids, the farnesoid X receptor (FXR). Here, we demonstrate that both stereoisomers of the plant sterol, (E)- and (Z)-GS, bind to the steroid receptors at a much higher affinity than to FXR. Both stereoisomers bind to the mineralocorticoid receptor (MR) with a Ki value of approximately 35 nM, which is greater than 100 times more potent than their affinity for FXR. Both (E)- and (Z)-GS also displayed high affinity for other steroid receptors, including the androgen (AR), glucocorticoid (GR), and progesterone receptors (PR) with Ki values ranging from 224 to 315 nM. In cell-based functional cotransfection assays, GSs behaved as antagonists of AR, GR, and MR, but as agonists of PR. Agonist activity was also demonstrated with estrogen receptor (ER) alpha; however, the potency was very low (EC50 > 5000 nM). In addition, GS displayed activity in functional assays in cell lines expressing endogenous AR, GR, ER, and PR. These data suggest that the variety of pharmacological effects exhibited by GS may be mediated by targeting several steroid receptors. praticamente ... basically that it blocks the androgen receptor (the receptor that makes testosterone and other steroids "work") and that it activates the progesterone receptor, which I beleive is why people fell "hot", basically a menapausal "hotflash" volevo sapere cosa ne pensavate dell'articolo .. se quacluno ne era a conoscenza ... io sapevo che se ne parlava bene dei guggulsteroni e avevano anche proprieta positive sull'organismo e sul sangue ... ditemi cosa ne pensate e se sono da evitare ...