Guggul and Guggulsterones

Gum Guggul Extract Benefits (Guggulipid)

The Guggul plant, also known as Commiphora mukul, is a flowering plant that can be found from northern Africa to central Asia including India, Bangladesh, and Pakistan. The plant can reach up to a height of 4 meters. Guggul is widely used in Indian Ayurvedic medicine, and because of overuse, it has become scarce, and has been listed as endangered species by the World Conservation Union.

Guggul is widely used in Asia and in Indian Ayurvedic medicine to treat a variety of diseases and ailments such as obesity, diabetes, atherosclerosis, rheumatism, and hyper-cholesterolemia. One of its most important uses is for lowering cholesterol. Guggul produces a sap known as gum guggul, and the extract of this is called guggulipid, which has been used in Ayurvedic medicine for almost 3,000 years. The active ingredient of the guggul extract has been identified as Guggulsterone, which is responsible for Guggul's therapeutic effects. Because of its cholesterol lowering ability, Guggul extract has seen increasing popularity in North America and Western Europe.

Health Benefits of Gum Guggul & Guggulsterones

The health benefits of Guggulsterones are many, and there are numerous clinical studies that have reported these benefits. Below we list some guggulsterone health benefits:

• There are various cardiovascular benefits associated with the multiple pharmacological activities associated with guggul or guggulsterone, notably its hypolipidemic, antioxidant, and anti-inflammatory activities. [1]
• Guggulipid is found to help significantly decrease LD cholesterol (bad cholesterol), and in some cases increased HDL (good) cholesterol by 60% [2, 3, 5]
• There is some limited contradicting evidence against Guggul's ability to help lower cholesterol levels - where some studies found that guggulipid did not appear to improve serum cholesterol levels [4]
• Guggulsterone is found to effectively inhibit LDL oxidation, and the combination of antioxidant and lipid-lowering properties of guggul and guggulsterone makes them especially beneficial against atherogenesis [6]
• Studies have found Guggulsterone to induce apoptosis in human prostate cancer cells [7]
• Some studies have also found Guggulsterone to inhibit the proliferation of wide variety of human tumor cell types including leukemia, head and neck carcinoma, multiple myeloma, lung carcinoma, melanoma, breast carcinoma, and ovarian carcinoma. Guggulsterone also inhibited the proliferation of some drug-resistant cancer cells [8]
• Guggulsterone is found to decrease lipid accumulation and has anti-obesity effects [9]; it also inhibits preadipocytes and promotes lipolysis of mature adipocytes (fat cells) [11]
• Guggulsterone has hypoglycemic and hypolipidemic effects, which can help to cure type II diabetes [10]

Guggulipid Cholesterol & Cardiovascular Benefits

There are numerous studies performed on Guggulipid's benefits for lowering cholesterol - most of these studies have found guggul to help lower LDL cholesterol; some have found guggul to help increase HDL cholesterol while decreasing LDL; and some have found some contradicting evidence suggesting Guggulipid did not lower cholesterol levels. However, the majority of the evidence speaks positively of Guggul's beneficial effects on cholesterol.

Guggulsterone extracted from guggul has been identified as the bioactive constituent responsible for its therapeutic effects. One of the first studies demonstrating this was done in 1966. Guggulsterone benefits include hypolipidemic, antioxidant, and anti-inflammatory activities. [1] In an Indian study, 205 patients participated in a 12 week trial with guggulipid. The results found a significant lowering of serum cholesterol (23.6%) and serum triglycerides (22.6%). The study reported HDL (good) cholesterol levels increased by 60% in some cases along with a significant decrease in LDL cholesterol. [2] Another study with 43 men and women with moderately increased cholesterol were supplemented with Guggul or a placebo for 12 weeks found a reduced level of total cholesterol levels; however, some side effects were reported, and the study mentioned that additional research is needed. [3]

While most studies have found guggul to have cholesterol lowering benefits, a limited few studies were not able to to confirm this finding. For example, a study done at the University of Pennsylvania School of Medicine found that guggulipid did not improve levels of serum cholesterol over the short term. Their study involved 103 subjects who were given 3 daily doses of guggulipid or a placebo. Contrary to other studies, this trial found that Guggul did not lower cholesterol levels, and appears to in fact raises the levels of cholesterol slightly. [4]

However, the majority of studies done on Guggulipid find it to have cholesterol lowering benefits. When 50mg of guggulipid or placebo were administered twice daily for 24 weeks, total cholesterol level decreased by 11.7% in a study involving 61 patients. The study reported LDL cholesterol decreased by 12.5% and HDL cholesterol had no changes. The study went on to state that the combined effect of diet and guggulipid at 36 weeks was as great as the reported lipid-lowering effect of modern drugs. [5]

Guggulsterone, Anti-Obesity, and Other Benefits

There are studies that have found Guggul to have anti cancer benefits. Guggulsterones have been found to cause apoptosis (programmed cell death) in cancer cells; however, how it causes cell death is poorly understood. It has been found to induce cell death in human prostate cancer cells. [7] Another study found that "guggulsterone inhibits the proliferation of wide variety of human tumor cell types including leukemia, head and neck carcinoma, multiple myeloma, lung carcinoma, melanoma, breast carcinoma, and ovarian carcinoma. Guggulsterone also inhibited the proliferation of drug-resistant cancer cells." [8]

Guggulsterone has also been shown to have anti obesity benefits. Studies have found guggulsterones to decrease lipid accumulation, and enhance lipolysis (breakdown of fats). [9] Guggulsterone has both hypoglycemic and hypolipidemic effects, which can help cure type II diabetes. [10] Guggul exerts its antiobesity effects by inhibiting differentiation of preadipocytes. (Preadipocytes are present throughout adult life in adipose tissues and can proliferate and differentiate into mature adipocytes, or fat cells. [14]) It also promotes the lipolysis of mature adipocytes. [11] In one study where 75mg guggulsterone was given orally to patients daily for 8 weeks, it was found that there was a significant reduction in the values of total serum lipid and total serum cholesterol. The lipid profile of patients showed downward trend, and a rise in HDL levels. [12]

Guggul Extract Side Effects

There are various possible side effects associated with guggul extract, and many of these studies have also reported some of these side effects. Below is a list of some of the potential side effects of guggul.

• Gastrointestinal symptoms and discomfort [2, 13]
• Possible thyroid problems [3]
• Some generalized skin rash symptoms [3] and allergic rash [13]
• Guggulipid also appeared to cause a dermatologic hypersensitivity reaction in some patients. [4]
• Other side effects of guggulipid were headache, mild nausea, eructation, and hiccup in a few patients. [5]
• Guggul should be avoided by pregnant women and women who are breast feeding [13]

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1. Cardiovasc Drug Rev. 2007 Winter;25(4):375-90.
Therapeutic effects of guggul and its constituent guggulsterone: cardiovascular benefits.
Deng R.

2. J Assoc Physicians India. 1989 May;37(5):323-8.
Clinical trials with gugulipid. A new hypolipidaemic agent.
Nityanand S, Srivastava JS, Asthana OP.

3. Complement Ther Med. 2009 Jan;17(1):16-22.
Resin from the mukul myrrh tree, guggul, can it be used for treating hypercholesterolemia? A randomized, controlled study.
Nohr LA, Rasmussen LB, Straand J.

4. JAMA. 2003 Aug 13;290(6):765-72.
Guggulipid for the treatment of hypercholesterolemia: a randomized controlled trial.
Szapary PO, Wolfe ML, Bloedon LT, Cucchiara AJ, DerMarderosian AH, Cirigliano MD, Rader DJ.

5. Cardiovasc Drugs Ther. 1994 Aug;8(4):659-64.
Hypolipidemic and antioxidant effects of Commiphora mukul as an adjunct to dietary therapy in patients with hypercholesterolemia.
Singh RB, Niaz MA, Ghosh S.

6. Atherosclerosis. 2004 Feb;172(2):239-46.
The hypolipidemic natural product Commiphora mukul and its component guggulsterone inhibit oxidative modification of LDL.
Wang X, Greilberger J, Ledinski G, Kager G, Paigen B, Jürgens G.

7. Cancer Res. 2007 Aug 1;67(15):7439-49.
Guggulsterone-induced apoptosis in human prostate cancer cells is caused by reactive oxygen intermediate dependent activation of c-Jun NH2-terminal kinase.
Singh SV, Choi S, Zeng Y, Hahm ER, Xiao D.

8. Biochem Pharmacol. 2007 Jun 30;74(1):118-30. Epub 2007 Mar 30.
Guggulsterone inhibits tumor cell proliferation, induces S-phase arrest, and promotes apoptosis through activation of c-Jun N-terminal kinase, suppression of Akt pathway, and downregulation of antiapoptotic gene products.
Shishodia S, Sethi G, Ahn KS, Aggarwal BB.

9. J Med Food. 2009 Aug;12(4):846-53.
Anti-obesity effects of xanthohumol plus guggulsterone in 3T3-L1 adipocytes.
Rayalam S, Yang JY, Della-Fera MA, Park HJ, Ambati S, Baile CA.

10. Food Chem Toxicol. 2009 Oct;47(10):2631-9. Epub 2009 Jul 25.
Effects of guggulsterone isolated from Commiphora mukul in high fat diet induced diabetic rats.
Sharma B, Salunke R, Srivastava S, Majumder C, Roy P.

11. Obesity (Silver Spring). 2008 Jan;16(1):16-22.
Guggulsterone inhibits adipocyte differentiation and induces apoptosis in 3T3-L1 cells.
Yang JY, Della-Fera MA, Baile CA.

12. Indian J Physiol Pharmacol. 1996 Jul;40(3):237-40.
A study of effect of guggulsterone on hyperlipidemia of secondary glomerulopathy.
Beg M, Singhal KC, Afzaal S.

13. Complement Ther Med. 2005 Dec;13(4):279-90. Epub 2005 Sep 23.
Guggul for hyperlipidemia: a review by the Natural Standard Research Collaboration.
Ulbricht C, Basch E, Szapary P, Hammerness P, Axentsev S, Boon H, Kroll D, Garraway L, Vora M, Woods J; Natural Standard Research Collaboration.

14. Preadipocyte Conversion to Macrophage
Guillaume Charrière, Béatrice Cousin, Emmanuelle Arnaud, Mireille André Francis Bacou, Luc Pénicaud and Louis Casteilla

May 2010