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Guggulsterones
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To begin the discussion about guggulipid, we must first talk about thyroid hormone. Thyroid hormones are very important for normal growth and development. Thyroid hormones maintain metabolic stability by regulating oxygen requirements, body weight, and intermediary metabolism (1). Thyroid hormones have effects in almost all tissues of the body. Thyroid hormones exert effects on thermogenesis and temperature regulation. This can explain some of the effects they have on energy metabolism. Thyroid hormones can actually stimulate protein synthesis, which is a big plus for bodybuilders and other athletes. Thyroid hormones have also been implicated in lowering cholesterol. Now let’s get to the most important effect of thyroid hormone on athletes. Thyroid hormones can enhance lipolysis (fat burning) in adipose (fat) tissue. More lipolysis… more fat loss. Capish!
The two main thyroid hormones that have any relevance are T4 (thyroxine) and T3 (3,5,3’ triiodothyronine). T4 is also inactive thyroid while T3 is active thyroid. T4 can convert into T3 in the liver by the enzyme 5’ deiodinase, which in turn can help maintain a healthy metabolism and cause fat loss to occur. Okay, let’s move on and talk about the benefits of Guggulipid.
Guggulipid (also known as Guggulsterones) has been around for hundreds of years in ayruvedic medicine. Ayruvedic medicine is a naturalistic approach to medicine that has been practiced in India for centuries. There have been several research studies done on this herb showing very positive benefits. Keep reading, the interesting part is coming up! One study entitled Clinical Trials On Guggulipid: A Hypolipidaemic Agent published in The Journal of Association of Physicians in India in 1989 (2) showed that guggulipid had a very strong effect in decreasing triglycerides (fats) as well as LDL (bad cholesterol) levels while increasing HDL (good cholesterol) levels in human subjects. It has these functional effects because it may cause an increase in thyroid hormone levels (both T4 and T3). There are several other studies that have shown similar effects of guggulipid as a fat reducing compound (3,4). Another use for guggulipid seems to be in the treatment of joint inflammation and helping to decrease joint discomfort (5). This natural compound has also been shown to be very safe and completely non-toxic in humans. This is all very good news for athletes. When choosing a guggulipid product, make sure it is a standardized guggulsterone of type E and Z from the plant commiphora mukul. Based on the research behind this supplement and the "real world" results I have seen, this supplement is a must for any athlete trying to lose bodyfat.
Many people following a diet and training program over a fairly long period of time complain that they just cannot lose that last bit of fat no matter what they do. Well, thyroid hormones may play a key role in this. You see, you’re body adapts to any diet program for fat loss that has a caloric deficit in it by reducing thyroid hormone output. By taking guggul, thyroid hormones can be normalized and you can continue burning fat!
This natural compound has also been shown to be very safe and completely non-toxic in humans. Plus some research suggests that it may even help reduce acne—nice bonus effect!
DOSAGE: When choosing a guggulipid product, make sure it is a standardized guggulsterone of type E and Z from the plant commiphora mukul. A good dose is 25 mg active guggulsterones after standardization taken three times daily. One dose with plenty of water 30 minutes before cardiovascular exercise can be helpful.
References Cited
Griffin J, Ojeda S. Textbook of endocrine physiology, 3rd ed. New York : Oxford University Press, 1996.
S. Nityanand, et al., "Clinical Trials with gugulipid. A new hypolipidaemic agent," J Assoc Physicians India 37.5 (1989): 323-328.
K Gopal, et al., "Clinical trial of ethyl acetate extract of gum gugulu (gugulipid) in primary hyperlipidemia," J Assoc Physicians India 34.4 (1986): 249-251.
R. Agarwal, et al., " Clinical trials of gugulipid—a new hypolipidemic agent of plant origin in primary hyperlipidemia," Indian J Med Res 84 (1986): 626-634.
J Sharma, et al., "Comparison of the anti-inflammatory activity of Commiphora mukul with those of phenylbutazone and ibuprofen in experimental arthritis by mycobacterial adjuvant, " Arzneimittelforschung 27.7 (1977) : 1455-1457.
The two main thyroid hormones that have any relevance are T4 (thyroxine) and T3 (3,5,3’ triiodothyronine). T4 is also inactive thyroid while T3 is active thyroid. T4 can convert into T3 in the liver by the enzyme 5’ deiodinase, which in turn can help maintain a healthy metabolism and cause fat loss to occur. Okay, let’s move on and talk about the benefits of Guggulipid.
Guggulipid (also known as Guggulsterones) has been around for hundreds of years in ayruvedic medicine. Ayruvedic medicine is a naturalistic approach to medicine that has been practiced in India for centuries. There have been several research studies done on this herb showing very positive benefits. Keep reading, the interesting part is coming up! One study entitled Clinical Trials On Guggulipid: A Hypolipidaemic Agent published in The Journal of Association of Physicians in India in 1989 (2) showed that guggulipid had a very strong effect in decreasing triglycerides (fats) as well as LDL (bad cholesterol) levels while increasing HDL (good cholesterol) levels in human subjects. It has these functional effects because it may cause an increase in thyroid hormone levels (both T4 and T3). There are several other studies that have shown similar effects of guggulipid as a fat reducing compound (3,4). Another use for guggulipid seems to be in the treatment of joint inflammation and helping to decrease joint discomfort (5). This natural compound has also been shown to be very safe and completely non-toxic in humans. This is all very good news for athletes. When choosing a guggulipid product, make sure it is a standardized guggulsterone of type E and Z from the plant commiphora mukul. Based on the research behind this supplement and the "real world" results I have seen, this supplement is a must for any athlete trying to lose bodyfat.
Many people following a diet and training program over a fairly long period of time complain that they just cannot lose that last bit of fat no matter what they do. Well, thyroid hormones may play a key role in this. You see, you’re body adapts to any diet program for fat loss that has a caloric deficit in it by reducing thyroid hormone output. By taking guggul, thyroid hormones can be normalized and you can continue burning fat!
This natural compound has also been shown to be very safe and completely non-toxic in humans. Plus some research suggests that it may even help reduce acne—nice bonus effect!
DOSAGE: When choosing a guggulipid product, make sure it is a standardized guggulsterone of type E and Z from the plant commiphora mukul. A good dose is 25 mg active guggulsterones after standardization taken three times daily. One dose with plenty of water 30 minutes before cardiovascular exercise can be helpful.
References Cited
Griffin J, Ojeda S. Textbook of endocrine physiology, 3rd ed. New York : Oxford University Press, 1996.
S. Nityanand, et al., "Clinical Trials with gugulipid. A new hypolipidaemic agent," J Assoc Physicians India 37.5 (1989): 323-328.
K Gopal, et al., "Clinical trial of ethyl acetate extract of gum gugulu (gugulipid) in primary hyperlipidemia," J Assoc Physicians India 34.4 (1986): 249-251.
R. Agarwal, et al., " Clinical trials of gugulipid—a new hypolipidemic agent of plant origin in primary hyperlipidemia," Indian J Med Res 84 (1986): 626-634.
J Sharma, et al., "Comparison of the anti-inflammatory activity of Commiphora mukul with those of phenylbutazone and ibuprofen in experimental arthritis by mycobacterial adjuvant, " Arzneimittelforschung 27.7 (1977) : 1455-1457.
macrophage69alpha
New member
guggulsterones have been shown to raise LDL (bad)
the evidence for their effect on thyroid is controversial at best. its likely that any metabolic activity, anecdotally reported, is actually due to steroidal and farsenoid receptor activity.
Mol Pharmacol. 2004 Dec 16; [Epub ahead of print] 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 KS, Stayrook KR.
Lilly Research Laboratories.
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, obestity, 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 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 Kis ranging from 224 nM 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 ERalpha, 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.
the evidence for their effect on thyroid is controversial at best. its likely that any metabolic activity, anecdotally reported, is actually due to steroidal and farsenoid receptor activity.
Mol Pharmacol. 2004 Dec 16; [Epub ahead of print] 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 KS, Stayrook KR.
Lilly Research Laboratories.
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, obestity, 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 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 Kis ranging from 224 nM 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 ERalpha, 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.
