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Guggulipid | | |
A purified form of the yellow resin derived from the mukul myrrh
(Commiphora mukul) tree in India has long been used by Ayurvedic healers
for centuries. Active compounds called guggulsterones are believed to be
responsible for its success in treating conditions such as arthritis and
obesity. Medoroga, a condition identified in ancient times, was associated
with rich foods and a sedentary lifestyle. Guggul resins were used to
treat this condition which bears similarities to atherosclerosis
and high cholesterol - conditions for which guggul extract are used today.
Guggulipids have also been used for stroke prevention, thyroid function,
ulcers, sore throats and inflammation, and respiratory disorders. While
controversial, there is evidence that supports the use of guggulipids for
high cholesterol and high triglycerides, in addition to some of the
aforementioned health concerns.
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| Common Name | | | Guggulipid
| | | Botanical Latin Name / Classification | | | Commiphora mukul
| | | Parts Used | | | Gum resin "guggul"
| | | Other Names | | | Guggulu
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| | | Description | | | Guggul and gum guggulu are the names given to a yellowish resinous sap
produced by the stem of the mukul myrrh (Commiphora mukul) tree, found
throughout India.
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| | | Traditional Internal Uses | | | For over 2000 years, traditional Ayurvedic healers in India have used
purified forms of this resin, specifically for the active compounds called
guggulsterones, to treat arthritis and obesity.
As early as 600
B.C., this medicinal resin was given to people with a condition known then
as "medoroga": those who overindulged in rich foods and lived a
sedentary lifestyle - habits we now associate with atherosclerosis and
high cholesterol. Not coincidentally, guggulipids are recommended for high
cholesterol and high triglycerides today in alternative medicine. In
India, standardized guggul extracts are approved for lowering elevated
serum cholesterol and triglyceride levels.
Guggulipids have also
been used to help inhibit platelet aggregation, an important factor in the
prevention of strokes. It also appears to stimulate thyroid function,
reduce arterial plaques, and has been used for ulcers, sore throat, nasal
inflammation, tonsilitis, and bronchitis.
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| | | Indications | | | Primary Indications: Hypercholesterolemia, High Triglycerides, Arteriosclerosis / Atherosclerosis
Secondary Indications: Stroke / Stroke Prevention, Thyroid Disorders (Hypothyroidism / Hyperthyroidism)
Other Indications: Bronchitis, Nasal Infections, Tonsillitis, Ulcers
Other Indications: Sore Throat
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| | | Actions | | | Alterative (Restorative), Anti-Atherogenic, Anti-Inflammatory, Anticholesterolemic, Antioxidant, Expectorant, Immunoactive / Immunomodulatory / Immunostimulative
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| | | Constituents / Nutrients | | | Guggul contains resin, volatile oils, and gum. The extract isolates
ketonic steroid compounds known as guggulsterones. These compounds have
been shown to provide the cholesterol- and triglyceride-lowering actions
noted for guggul.1
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| | | Pharmacological Summary | | | While statins and statin drugs (including red yeast rice extracts) work by
inhibiting cholesterol production in the liver, guggulsterones work by
clocking a substance that stops the body from getting rid of
cholesterol.
There have been a few large scale clinical trials
involving guggul confirming its pharmacological cholesterol and
triglyceride-lowering actions. One study involving 205 patients showed how
guggul matched up well with a popular prescription drug, clofibrate
(Lopid) in terms of decreased serum cholesterol levels and
triglycerides.
A 2003 study in the Journal of the American Medical
Association (JAMA) revealed contrary effects of guggulipids where
cholesterol is concerned. Patients who took guggul in pill form for eight
weeks actually showed increased LDL cholesterol levels, the study alleged.
However, the data from this study has since been re-examined, and it was
discovered that guggul was able to lower fasting blood sugar, blood
pressure, insulin levels, and guggul had anti-inflammatory activity,
reducing the levels of C-reactive protein.
Guggulipids still
remain a contoversial cholesterol-lowering alternative to the standard
crop of prescription drugs, with some people citing the potentially flawed
JAMA study as support of this position. Results of studies in India
versus America have been incompatible, perhaps attributed to different
dietary habits. However, scientific data seems to be reliable and
relatively consistent supporting guggulipids ability to lower
triglycerides.
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| | | Scientific Research and Pharmacologicial Actions | | | Guggulipids significantly lower serum triglycerides and cholesterol as
well as LDL and VLDL cholesterols (the "bad" cholesterols).2 At
the same time, they raise levels of HDL cholesterol (the "good"
cholesterol). As antioxidants, guggulsterones keep LDL cholesterol from
oxidizing, an action which protects against
atherosclerosis.3
Guggul has also been shown to reduce the
stickiness of platelets - another effect that lowers the risk of coronary
artery disease.4 One double-blind trial found guggul extract similar to
the drug clofibrate for lowering cholesterol levels.5 The study compared
the use of guggul to clofibrate (Lopid) in 125 patients. The average fall
in serum cholesterol and triglycerides in patients treated with guggul was
11 and 16.8 percent, respectively and with clofibrate, 10 and 21.6 percent
respectively. HDL cholesterol was increased in 60 percent of cases
responding to guggulipid therapy. Other clinical trials in India (using
1,500 mg of extract per day) have confirmed guggul extracts improve lipid
levels in humans.6
A combination of guggul, phosphate salts,
hydroxycitrate, and tyrosine coupled with exercise has been shown in a
double-blind trial to improve mood with a slight tendency to improve
weight loss in overweight adults.7
One small clinical trial found
that guggul (Commiphora mukul) compared favorably to tetracycline in the
treatment of cystic acne.8 The amount of guggul extract taken in the trial
was 500 mg twice per day.
Guggul (Commiphora mukul) potentially
ameliorates hypothyroidism in female mice.
Phytother Res. 2005
Jan;19(1):78-80.
The efficacy of guggul, the gum resin of
Commiphora mukul in regulating hypothyroidism was evaluated in female
mice. In addition to estimating serum levels of thyroxine and
triiodothyronine, hepatic 5' monodeiodinase, hepatic glucose-6-phospatase
and lipid-peroxidation (LPO), the activities of the anti-oxidative
enzymes, superoxide dismutase (SOD) and catalase (CAT), were investigated.
While 6-n-propyl-2-thiouracil (PTU, 10.00 mg/kg/d for 30 days) induced
hypothyroidism in mice, as evidenced by a decrease in thyroid hormone
concentration and in hepatic 5'D-I activity, simultaneous administration
of guggul (200 mg/kg/d for 30 days) reversed this effect, indicating its
potential to stimulate thyroid function. Although in PTU treated animals a
marginal increase in hepatic LPO was observed, when simultaneously treated
with guggul, it was decreased. A parallel increase in the activity of
endogenous antioxidants, SOD and CAT, in the latter group indicated the
safe and antiperoxidative nature of guggul. These findings suggest the
possible use of guggul in the amelioration of
hypothyroidism.
Guggul and Prescription Drugs
The
Journal of Pharmacology and Experimental Therapeutics, August
2004.
Guggul may interfere with many prescription drugs,
including the popular anti-cholesterol drugs called statins. In a
preliminary study, guggulsterone, the active ingredient in the herbal
remedy guggul, causes changes in human and rodent cells that induce the
body to break down many drugs, including cancer drugs and AIDS
medications. Resin from the guggul tree has been used for more than 3,000
years in India to treat a range of disorders. Previous research showed
that guggul lowers cholesterol by blocking a substance that keeps the body
from getting rid of cholesterol. Guggulsterone likely affects other drugs
because it binds to a protein known as pregnane X receptor (PXR). This, in
turn, induces the body to "turn on" a gene that encodes another protein
that breaks down many different types of drugs, thereby reducing their
levels in the body. Some anticancer drugs, such as cyclophosphamide, need
to be broken down by PXR to become active. Guggulsterone may interfere by
augmenting that process, thereby raising levels of the drugs in the body.
Moreover, guggulsterone appears to also turn some other drugs, such as
acetaminophen, into toxic compounds. St. John's wort, also activates PXR,
and can therefore interfere with other drugs. Guggulsterone has been used
for years, and is likely safe if people are not taking any prescription
medications. However, guggulsterone should be used cautiously by people
who take prescription drugs.
Guggulipid for the treatment of
hypercholesterolemia: a randomized controlled trial.
JAMA. 2003
Aug 13;290(6):765-72.
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 guggul (1000 mg), high-dose guggul (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 guggul (n = 33) and high-dose
guggul (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
guggul in the intention-to-treat analysis. While guggul was generally well
tolerated, 6 participants treated with guggul developed a hypersensitivity
rash compared with none in the placebo group.
Conclusions:
Despite plausible mechanisms of action, guggul 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.
The effectiveness of Commiphora mukul (guggul)
for osteoarthritis of the knee: an outcomes study.
Singh BB,.
Southern California University of Health Sciences, USA.
Altern Ther
Health Med. 2003 May-Jun;9(3):74-9.
Context: Ayurveda,
the traditional system of healthcare in India, has many remedies for
Osteoarthritis (OA). One of the ingredients most commonly found in
Ayurvedic arthritis formulas is guggul, an oleoresin of the herb
Commiphora mukul. The authors have conducted both preclinical and clinical
investigations of guggul for reduction of pain, stiffness, and improved
function, and to determine tolerability in older patients with a diagnosis
of OA of the knee.
Conclusions: Overall data indicate
significant improvement with guggul for participants during the trial in
both scales and objective measures used for assessment purposes. There
were no side effects reported during the trial. Guggul appears to be a
relatively safe and effective supplement to reduce symptoms of
OA.
Guggul Laboratory Studies The hypolipidemic natural product
Commiphora mukul and its component guggulsterone inhibit oxidative
modification of LDL.
Atherosclerosis. 2004
Feb;172(2):239-46.
There is accumulating evidence that LDL
oxidation is essential for atherogenesis, and that antioxidants that
prevent this oxidation may either slow down or prevent atherogenesis. In
the present study, we found that Commiphora mukul (guggul) and its
cholesterol-lowering component, guggulsterone, effectively inhibited LDL
oxidation. This inhibition by guggul was assessed by the decrease in the
following parameters describing LDL oxidation: conjugated dienes, relative
electrophoretic mobility (REM), thiobarbituric acid reactive substances,
lipid hydroperoxides, oxidation-specific immune epitopes as detected with
a monoclonal antibody against oxidized LDL, and the accumulation of LDL
derived cholesterol esters in mouse peritoneal macrophages. We concluded
that guggul and its lipid-lowering component, guggulsterone, significantly
inhibit LDL oxidation. The combination of antioxidant and lipid-lowering
properties of guggul and guggulsterone makes them especially beneficial
against atherogenesis.
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| | | Research | | | "Supplement Update: Guggulipid"
"Hypothyroidism: Symptoms and Successful Treatment"
"Using Guggulipid to Lower High Cholesterol Levels"
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| | | Precautions / Contraindications | | | Be sure to consult your doctor before trying guggulipids if you suffer
from liver disease, inflammatory bowel disease, or diarrhea. Pregnant
women should not take it.
When selecting a product, look for one
clearly marked as a guggulipid supplement and not guggul or guggulu -
crude and unrefined forms of the resin that could easily contain toxic
compounds. A dangerous loss of appetite, stomach pain, diarrhea, and
rashes could develop from guggul or guggulu. Gugulipid, on the other hand,
has been refined to contain only the active ingredients without the
toxins. In rare cases, however, even gugulipid may cause side effects such
as mild nausea, gas, diarrhea, hiccups, restlessness, anxiety, or
headaches.
Don't stop seeing your doctor for a cholesterol
problem, or substitute guggulipid for a cholesterol-lowering medication
without your doctor's approval.
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| | | Interaction with Medications | | | None documented.
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| | | Possible Side Effects | | | Early studies with the crude oleoresin reported numerous side effects,
including diarrhea, anorexia, abdominal pain, and skin rash. Modern
extracts are more purified, and fewer side effects (e.g., mild abdominal
discomfort) have been reported with long-term use. Rash was reported,
however, as a fairly common side effect in one recent study.10 Guggul
should be used with caution by people with liver disease and in cases of
inflammatory bowel disease and diarrhea. A physician should be consulted
before treating elevated cholesterol and triglycerides.
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| | | Dosage | | | Daily recommendations for the purified guggul extract are typically based
on the amount of guggulsterones in the extract.9 A common intake of
guggulsterones is 25 mg three times per day. Most extracts contain 2.5-5%
guggulsterones and can be taken daily for 12 to 24 weeks for lowering high
cholesterol and/or triglycerides.
Dried Extracts: Guggulipid
capsules are generally available in strengths that range from 250 to 750
mg. Within herbal blends, quantities of guggulipid are significantly
smaller. Typically, a capsule strength of 400 to 500 mg is recommended to
be taken 3 times daily.
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| | | References | | | 1. Satyavati GV. Gum guggul (Commiphora mukul)-The success of an ancient
insight leading to a modern discovery. Indian J Med 1988;87:327-35.
2.
Nityanand S, Kapoor NK. Hypocholesterolemic effect of Commiphora mukul
resin (Guggal). Indian J Exp Biol 1971;9:367-77.
3. Singh K, Chander
R, Kapoor NK. Guggulsterone, a potent hypolipidaemic, prevents oxidation
of low density lipoprotein. Phytother Res 1997;11:291-4.
4. Mester L,
Mester M, Nityanand S. Inhibition of platelet aggregation by guggulu
steroids. Planta Med 1979;37:367-9.
5. Malhotra SC, Ahuja MMS,
Sundarum KR. Long-term clinical studies on the hypolipidemic effect of
Commiphora mukul (guggul) and clofibrate. Ind J Med Res
1977;65:390-5.
6. Nityanand S, Srivastava JS, Asthana OP. Clinical
trials with gugulipid-a new hypolipidemic agent. J Assoc Phys India
1989;37:323-8.
7. Antonio J, Colker CM, Torina GC, et al. Effects of a
standardized guggulsterone phosphate supplement on body composition in
overweight adults: A pilot study. Curr Ther Res 1999;60:220-7.
8.
Thappa DM, Dogra J. Nodulocystic acne: oral gugulipid versus tetracycline.
J Dermatol 1994;21:729-31.
9. Brown D, Austin S. Hyperlipidemia and
Prevention of Coronary Artery Disease. Seattle, WA: NPRC, 1997, 4-6.
10. Szapary PO, Wolfe ML, Bloedon LT, et al. Guggulipid for the treatment
of hypercholesterolemia: an randomized controlled trial. JAMA
2003;290:765-72.
Our thanks to the following information
resources: WholehealthMD.com, Vitacost.com, Herbal-Provider.com, and
Raysahelian.com.
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