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Gugglesterone

Review of Gugglesterone (Guggulipid)

What is Gugglesterone (Guggulipid)?

Gugglesterone is the active substance in guggulipid, an extract of the guggul tree (Comiphora mukul), which has been used in the ancient Ayuruvedic medicine for nearly 3000 years, to treat a variety of conditions including obesity. It is widely used in Asia as a cholesterol lowering agent, and is gaining popularity in the United States and Europe.  Research suggests that gugglesterone may lower cholesterol and help to decrease body-fat levels.

Who Should Consider Taking Gugglesterone (Gugul)?

Gugglesterone may be of benefit to people looking to control/ reduce cholesterol levels and body-fat levels.

Summary of Gugglesterone's (Gugulipid) Phyiological Effects:

  • Early research suggested it lowered cholesterol levels
  • Recent research has shown that it has no effect on cholesterol levels and may actually increase the levels of the "bad" LDL cholesterol
  • No strong evidence to support a thyroid raising effect - recent research suggests there is no thyroid raising effect
  • No real evidence to support it as a weight loss supplement
  • It may cause serious drug interactions
  • Can cause stomach upsets, headaches, and allergic skin reactions

Gugglesterone (Gugulipid) Research

The active ingredients in gugglesterone are known as E-gugglesterone and Z-gugglesterone. They are believed to lower blood lipid levels by inhibiting a key receptor called the farnesoid X-receptor which plays a role in regulating fatty acids, cholesterol, and bile acid synthesis (Urizar et al., 2002; Brobst et al., 2004).

Early research looking at the effects of gugglesterone appeared to have positive effects.  Studies, in both animals and humans, appeared to demonstrate that gugglesterone may significantly lower blood lipid levels (Singh et al., 1990 & 1997; Urizar and Moore, 2003; Wang et al., 2004).  Several studies have shown that gugglesterone may lower cholesterol levels (Dev, 1997; Wu et al., 2002; Urizar et al., 2002).  These studies suggest that whilst it lowers the level of the “bad” low-density lipoproteins (LDL cholesterol) it may actually increases the levels of the “good” high-density lipoproteins (HDL cholesterol) (Wu et al., 2002).  It may also decreases the rate of oxidation of LDL cholesterol which would help to prevent the build up of fatty deposits on artery walls (Wang et al., 2004).

LDL cholesterol is considered bad cholesterol because it increases the rate of artherosclerosis and blockage of arteries by increasing the amount of fatty deposits on artery walls.  In contrast, HDL cholesterol increases the removal of the fatty deposits from artery walls.  These cholesterol altering properties have led to claims that gugglesterone may be of benefit in the treatment/prevention of high cholesterol and hardening/blockage of arteries (Wang et al., 2004).

Gugglesterone was also found to have a thyroid stimulating effect (Tripathi et al., 1984).  Since thyroid hormones control your metabolic rate, any increase in thyroid hormones can increase metabolic rate, increase daily calorie expenditure and increase the amount of fat your body burns.

Researchers have found that gugglesterone may help to decrease body mass and body fat (Antonio et al., 1999).  In this study the combined consumption of 750mg of gugglesterone along with 1650mg of phosphates, daily, led to a significant decrease in bodymass (3.2%) and decreased body-fat by 20.6% compared with 8.6% in the control group (no supplement).  The researchers concluded that the ingestion of gugglesterone phosphate salt compound, when combined with exercise, will result in a significant reduction in bodyweight.  Many nutritional companies quickly started to include gugglesterone in their products and made many claims about the benefits of gugglesterone for weight loss.

Although in this study gugglesterone appeared to have been effective for weight loss, we must rememeber that the phosphate (1650mg daily) that was also used in the study, may well of been responsible for some of the weight lost in the study and may have made a significant contribution to the weight loss.  In fact researchers have found that phosphate supplementation can lead to a 19% increase the resting metabolic rate (Nazar et al., 1996) and therefore may contribute to weight loss. Therefore, we cannot conclude – as some nutritional manufacturers have reported – that gugglesterone was solely responsible for this weight loss.  However, when combined with phosphates it did appear to be effective at enhancing fat loss.

Despite all of these positive findings question marks have been raised about the use of gugglesterone.  A recent study by Szapay et al., (2003) found that gugglesterone when taken at 1000-2000mg, 3 times daily, had no significant effect on cholesterol levels.  In fact the researchers found that gugglesterone may actually raise the levels of the “bad” LDL cholesterol.  Also, some of the subjects in the study experienced a skin hypersensitivity reaction that was attributed to the gugglesterone.

Further research has also raised doubts over the use of gugglesterone (Brobst et al., 2004).  They found that gugglesterone may actually activate the estrogen receptor alpha isoform and the pregnane X receptor.  Of most significance is the activation of the pregnane X receptor which is known to cause herb-drug interactions.  The researchers suggested that gugglesterone should be used cautiously by patients taking prescriptive medication.

In fact a review by Ulbricht et al., (2005) raised serious doubts about the use of gugglesterone.  They raised serious questions about the early studies stating that most of the early studies that found positive results with gugglesterone were "small and not well designed or reported".  They questioned the effectivenes of gugglesterone for raising thyroid function by pointing out that a recent study (Szapary et al., 2003) found that gugglesterone had no significant effect on thyroid function.  Therefore the effectiveness of gugglesterone as a weight loss supplement must be seriously questioned.

Therefore, although gugglesterone appeared to have potential as a weight loss supplement further research is needed to establish whether it truly is effective.

Most early research appeared to show that gugglesterone was free of serious side effects.  However, studies have demonstrated that it can cause: headaches in up to 70% of patients (Arora et al., 1972); may cause stomach upsets including diarrhea, and vomiting (Szapary et al., 2003); and may cause allergic skin reactions (Szapary et al., 2003).

Is Gugglesterone (Guggulipid) effective?

The answer to this is not clear, as some studies have found positive effects, but more recent large scale trials have shown no positive effects.  At present there is not enough scientific evidence to support its use for any medical condition (Ulbricht et al., 2005).  Therefore, we must conclude that you would be better off saving your money and using more effective and safe weight loss and cholesterol lowering supplements.  Alternative cholesterol lowering supplements include: green tea extract, alpha-lipoic acid and tumeric.  Alternative weight loss supplements include: Caffeine, CLA and green tea extract.

How to take Gugglesterone (Guggulipid)?

Most researchers have used 100-200mg of pycnogenol, daily, for specific health Although a number of studies have shown positive cholesterol lowering effects recent studies have failed to observe this and have also raised doubts about the safety of gugglesterone.  At present it is unclear as to whether gugglesterone is of benefit for people looking to reduce cholesterol levels.  Research also suggetsts that it is unlikely to be of benefit in weight loss.  If you take any medication be aware that gugglesterone may cause interfere with the effectiveness of the medication so always consult your doctor or health practitioner before consuming gugglesterone.

Gugglesterone References

Antonio, J., Colker, C. M., Torina, G. C., Shi, Q., Brink, W. and Kaiman, D. (1999) Effects of a standardized gugglesterone phosphate supplement on body composition in overweight adults: A pilot study. Curr Ther Res. 60 (4), 220-227. 

Arora, R. B., Kapoor, V., Gupta, S. K. and Sharma, R. C. (1971) Isolation of crystalline steroidal compound from commiphora mukul and its anti-inflammatory activity. Indian J Exp Biol. 9 (3), 403-404.

Brobst, D. E., Ding, X., Creech, K. L., Goodwin, B., Kelley, B. and Staudinger, J. L. (2004) Gugglesterone Activates Multiple Nuclear Receptors and Induces CYP3A Gene Expressionthrough the Preganane X Receptor. J Phar Exp Ther. 310 (2), 528-535. 

Dev, S. (1997) Ethnotherapeutics and modern drug development: The potential of Ayurveda. Curr Sci. 73, 909-928. 

Nazar, K., Kaciuba-Uscilko, H., Sczepanik, J., Zemba, A. W., Kruk, B., Chwalbinska-Moneta, J., Titow-Stupnicka, E., Bicz, B. and Krtkeiwski, M. (1996) Phosphate supplementation prevents a decrease of triiodothyronine and increases resting metabolic rate during low energy diet. J Physiol Pharmacol. 47 (2), 373-383. 

Singh, V., Kaul, S., Chander, R. and Kapoor, N. K. (1990) Stimulation of low density lipoprotein receptor activity in liver membrane of gugglesterone treated rats. Pharmacol Res. 22, 37-44. 

Singh, K., Chander, R. and Kapoor, N. K. (1997) Gugglesterone, a potent hypolipidaemic, prevents oxidation of low density lipoprotein. Phytotherapy Res. 11, 291-294. 

Szapary, P. O., Wolfe, M. L., Bloedon, L. T., Cucchiara, A. J., DerMarderosian, A. H., Cirigliano, M. D. and Rader, D. J. (2003) Guggulipid for the treatment of hyperocholesterolemia: a randomized controlled trial. JAMA. 290 (6), 765-772. 

Tripathi, Y. B., Malthotra, O. P. and Tripathi, S. N. (1984) Thyroid stimulating action of Z-gugglesterone obtained from Commiphora mukul. Planta Med. 50, 78-80. 

Ulbricht, C., Basch, E., Szapary, P., Hammerness, P., Axentsev, S., Boon, H., Kroll, D., Garraway, L., Vora, M. and Woods, J. (2005) Guggul for hyperlipidermia: A review by the Natural Standard Research Collaboration. Complementary Therapies in Medicine. ARTICLE IN PRESS.

Urizar, N. L., Liverman, A. B., Dodds, D. T., Silva, F. V., Ordentlich, P., Yan, Y., Gonzalez, F. J., Heyman, R. A., Mangelsdorf, D. J. and Moore, D. D. (2002) A natural product that lowers cholesterol as an antagonist ligand for FXR. Science. 296 (5573), 1703-1706. 

Urizar, N. L. and Moore, D. D. (2003) GUGULIPID: a natural cholesterol-lowering agent. Annu Rev Nutr. 23, 303-313. 

Wang, X., Greilberger, J., Ledinski, G., Kager, G., Paigen, B. and Jurgens, G. (2004) The hypolipidermic natural product Commiphora mukul and its component gugglesterone inhibit oxidative modification of LDL. Atherosclerosis. 172 (2), 239-246. 

Wu, J., Xia, C., Meier, J., Li, S., Hu, X. and Lala, D. (2002) The Hypolipidemic Natural Product Gugglesterone Acts as an Antagonist of the Bile Acid Receptor. Molecular Endocrinology. 16 (7), 1590-1597.