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gugglulsterone?

You and var.

LOL


Guggles are known to do a lot of things......


Regulates cholesterol

As effective as Accutane

...they are most effective when on a low carb diet due their up-pacing of thyroid output.

They are OTC and relatively cheap.
 
guggulsterones are effective with acne, not because of thryroid effects but because they are anti-androgens.

guggulsterones actually have no proven affect on thyroid or cholesterol (recent studies indicate that they actually cause a rise in LDL-C)


1: Mol Pharmacol. 2005 Mar;67(3):948-54. Epub 2004 Dec 15. 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. [email protected]

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.
 
Has anyone used these without raising their LDL - C and does it cause weight loss and is it good with acne.
 
Carefully planned scientific studies show that guggulsterones are highly effective at accelerating fat loss, mainly due to their stimulating effect on the thyroid gland. The thyroid hormones are among the most important hormones. They control your metabolic rate, which dictates how many calories you burn each day. When your metabolic rate slows down, which it does when you go on a diet, you automatically burn fewer calories each day. This means that the rate at which you lose weight slows down [5].

However, guggulsterones naturally stimulate the activity of the thyroid gland, returning your metabolic rate to where it should be. This means that weight loss becomes faster and easier, as your body naturally burns more calories each day. In one study carried in the journal Current Therapeutic Research, test subjects using a supplement containing guggulsterones lost fat three times faster compared to those using diet and exercise alone [1].

Following the six-week program, the group using the guggulsterone-based supplement lost 9.5 pounds of fat, compared to 3.1 pounds in those who just followed the diet and exercise programme. When the research team measured thyroid activity in three of the subjects, they found an 8-10% increase in thyroid hormone levels.

Guggulsterones are considered to be one of the safest supplements available, and do not stimulate the nervous system in the same way as products like ephedrine. They're also approved in India for lowering elevated cholesterol and triglyceride levels [2, 4]. Studies show that guggulsterones lower triglycerides and cholesterol as well as LDL and VLDL cholesterol (the “bad” cholesterol) [3]. At the same time, it raises levels of HDL cholesterol (the “good” cholesterol).

Research
1. Antonio, J., Colker, C.M., Torina, G.C., & Shi, Q., Brink, W.D., & Kalman, D. (1999). Effects of a standardized guggulsterone phosphate supplement on body composition in overweight adults: A pilot study. Current Therapeutic Research Clinical and Experimental, 60, 220-227
2. Satyavati GV.(1988). Gum guggul (Commiphora mukul)-The success of an ancient insight leading to a modern discovery. Indian Journal of Medicine, 87, 327-335
3. Nityanand S, Kapoor NK. (1971). Hypocholesterolemic effect of Commiphora mukul resin (Guggal). Indian Journal of Experimental Biology, 9, 367-77
4. Singh K, Chander R, Kapoor NK. (1997). Guggulsterone, a potent hypolipidaemic, prevents oxidation of low density lipoprotein. Phytotherapy Research, 11, 291-294
5. Rosenbaum, M., Hirsch, J., & Leibel, R.L. (2000). Effects of changes in body weight on carbohydrate metabolism, catecholamine excretion, and thyroid function. American Journal of Clinical Nutrition, 71, 1421-1432




No recent studies listed there.



I have personally used them and charted my basal rising temp and there was a noticible increase once I added them to my stack.



: Indian J Physiol Pharmacol. 1996 Jul;40(3):237-40. Related Articles, Links


A study of effect of guggulsterone on hyperlipidemia of secondary glomerulopathy.

Beg M, Singhal KC, Afzaal S.

Department of Medicine, J.N. Medical College, A.M.U., Aligarh.

Hyperlipidemia in patients of secondary glomerulopathies, a well established entity with very little knowledge of its management modifies its prognosis by predisposing these patients to develop atherosclerosis, coronary artery disease, hypertension cerebro-vascular accidents and also thromboembolic phenomenon leading to renal vein thrombosis and renal failure. Guggulsterone was administered orally in these patients in a daily divided dose of 75 mg for a period of 8 weeks together with supportive measures like high protein diet, diuretics and hematinics. Total serum lipid, total serum cholesterol, triglycerides, phospholipids, HDL, LDL, and VLDL were analysed at 4 and 8 weeks of therapy. Significant reduction was observed in the values of total serum lipid and total serum cholesterol. Other parameters of lipid profile showed downward trend except rise of HDL with insignificant difference. There was no significant side effect throughout the study.



One study that showed adverse blood panels were based on 3000-6000mg of 2.5% gugglesterones.



That's well above the daily recommendation for fat loss.
 
does anybody have any personal expierience with this gugglulsterone???

...what were your ...doses? ...results? ...sides, if any?
 
the body temp increases that guggulsterones cause are NOT due to thyroid, they are most likely due to PROGESTENIC binding (much like a menapausal hot flash)

you will note all the positive studies are done in india and bangladesh (the two largest exporters of guggul and guggulsterones) and many are published in "pay to print" journals or ones with very loose peer review.

here is the study that was in JAMA

: JAMA. 2003 Aug 13;290(6):765-72. Links
Comment in:
JAMA. 2003 Dec 3;290(21):2800-1; author reply 2801.
JAMA. 2003 Dec 3;290(21):2800; author reply 2801.
Guggulipid for the treatment of hypercholesterolemia: a randomized controlled trial.Szapary PO, Wolfe ML, Bloedon LT, Cucchiara AJ, DerMarderosian AH, Cirigliano MD, Rader DJ.
Department of Medicine, University of Pennsylvania School of Medicine, Philadelphia 19104-6021, USA. [email protected]

CONTEXT: Herbal extracts from Commiphora mukul (guggul) have been widely used in Asia as cholesterol-lowering agents, and their popularity is increasing in the United States. Recently, guggulsterones, the purported bioactive compounds of guggul, have been shown to be potent antagonists of 2 nuclear hormone receptors involved in cholesterol metabolism, establishing a plausible mechanism of action for the hypolipidemic effects of these extracts. However, there are currently no published safety or efficacy data on the use of guggul extracts in Western populations. OBJECTIVE: To study the short-term safety and efficacy of 2 doses of a standardized guggul extract (guggulipid, containing 2.5% guggulsterones) in healthy adults with hyperlipidemia eating a typical Western diet. DESIGN: Double-blind, randomized, placebo-controlled trial using a parallel design, conducted March 2000-August 2001. PARTICIPANTS AND SETTING: A total of 103 ambulatory, community-dwelling, healthy adults with hypercholesterolemia in the Philadelphia, Pa, metropolitan area. INTERVENTION: Oral, 3 times daily doses of standard-dose guggulipid (1000 mg), high-dose guggulipid (2000 mg), or matching placebo. MAIN OUTCOME MEASURES: Percentage change in levels of directly measured low-density lipoprotein cholesterol (LDL-C) after 8 weeks of therapy. Secondary outcome measures included levels of total cholesterol, high-density lipoprotein cholesterol (HDL-C), triglycerides, and directly measured very low-density lipoprotein cholesterol (VLDL-C), as well as adverse events reports and laboratory safety measures including electrolyte levels and hepatic and renal function. RESULTS: Compared with participants randomized to placebo (n = 36), in whom levels of LDL-C decreased by 5%, both standard-dose guggulipid (n = 33) and high-dose guggulipid (n = 34) raised levels of LDL-C by 4% (P =.01 vs placebo) and 5% (P =.006 vs placebo), respectively, at 8 weeks, for a net positive change of 9% to 10%. There were no significant changes in levels of total cholesterol, HDL-C, triglycerides, or VLDL-C in response to treatment with guggulipid in the intention-to-treat analysis. While guggulipid was generally well tolerated, 6 participants treated with guggulipid developed a hypersensitivity rash compared with none in the placebo group. CONCLUSIONS: Despite plausible mechanisms of action, guggulipid did not appear to improve levels of serum cholesterol over the short term in this population of adults with hypercholesterolemia, and might in fact raise levels of LDL-C. Guggulipid also appeared to cause a dermatologic hypersensitivity reaction in some patients.
 
..would the hot flashes account for a basal temp increase of 0.25 degrees on average when taken 7-9 hours after last dosing?
 
yes (well to be fair, quite possibly). it has an extended metabolism (though exact #'s are not available)-- hot flashes in women are due to natural pulsatile increases in progesterone. an exogenous agent will provide a different effect.

btw- used to be a proponent of guggulsterones (they were in liporexin) but subsequent research and evaluation of the previous (and with scrutiny, highly questionable) research ....decided otherwise
 
macrophage69alpha said:
yes. it has an extended metabolism (though exact #'s are not available)-- hot flashes in women are due to natural pulsatile increases in progesterone. an exogenous agent will provide a different effect.

btw- used to be a proponent of guggulsterones (they were in liporexin) but subsequent research and evaluation of the previous (and with scrutiny, highly questionable) research ....decided otherwise



But wouldn't the extended metabolism lead to a situation of ultimately burning more cals, regardless of the mechanism??
 
The Shadow said:
But wouldn't the extended metabolism lead to a situation of ultimately burning more cals, regardless of the mechanism??


no. what was meant was that its just extended metabolism of the active (it has a longer half life)--

and if its progestenic effect did have some impact on fat loss (which it might) or at least fat distribution (as progestins tend to increase IM fat)-- IMO that would likely be offset by the anti-androgenic effects.

its just too promiscuous :p
 
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