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Guggul extract and guggulsterones

The resin of Guggul, whose name translates as "that which protects against disease", is used as incense to ward off mosquitoes. In Ayurveda, Guggul is used internally, especially for joint problems such as rheumatism, osteoarthritis or arthritis, which is attributed to its antiseptic, anti-inflammatory and analgesic effects. But Guggul is also used in Ayurveda for obesity, high cholesterol, arteriosclerosis, cysts and abscesses.

The first scientific work on Guggul, published in 1966, focused on its effect on fat metabolism, particularly the relationship between obesity and arteriosclerosis. It was observed that patients who were given Guggul resin not only improved the condition of their blood vessels, but also their obesity.

Today we know from clinical trials that Guggul extract

  • stimulates the proliferation of fibroblasts (fibroblasts play an important role in the formation of connective tissue and in wound healing)
  • increases collagen type I synthesis
  • Matrix metalloproteinases (during the formation of tumor cells, the formation of tumor-specific blood vessels and the degradation of basement membranes are supported by matrix metalloproteinases; matrix metalloproteinases are therefore enzymes that help malignant cancer cells to metastasize) inhibits
  • Elastase expression (pancreatic elastase is a digestive enzyme; an increased value indicates pancreatitis) inhibits

Guggul extract was also tested in vitro and showed

  • an inhibitory effect on HMG-CoA reductase activity (inhibits cholesterol biosynthesis by inhibiting an early step of biosynthesis and thus lowers LDL cholesterol in particular)
  • Inhibition of alpha-glucosidase activity and thus reduced absorption of glucose (à diabetes)
  • an anti-adipogenic effect by inhibiting pre-adipocyte differentiation and lipolysis of adipocytes (during lipolysis, stored fats are gradually broken down into glycerol (or cholesterol) and free fatty acids)
  • Regulation of both glucose metabolism and fat burning by stimulating AMPK activity (AMP-activated protein kinase increases fat burning)

active ingredients

The main active ingredients of Guggul extract are its steroids, the so-called guggulsterones, which, in terms of therapeutic use, make the big difference between Guggul (Commiphora mukul), the gum resin of the balsam tree, and all other Commiphora (= myrrh) plants.

Two of the guggulsterones are primarily responsible for the cholesterol and weight-reducing effects of the resin: E- and Z-guggulsterones. The fact that they interfere with fat metabolism is now well documented scientifically. How exactly this interference occurs is still the subject of current scientific discussion: guggulsterones could reduce fat absorption through their influence on the bile or directly stimulate thyroid function and thus "hormonal fat breakdown". It has also been found that guggul extract activates certain receptors in the liver, which cause more LDL cholesterol to be bound from the body.

cholesterol and lipid metabolism

According to a recent study by the UT Southwestern Medical Center in Dallas, guggulu blocks the so-called famesoid-X receptor, which plays a central role in human cholesterol levels.According to this, a daily dose of 10 to 15 g (note: this is powder / 10g powder corresponds to 2 g (4 capsules) of the 5:1 extract) leads to a reduction in cholesterol of up to 25% and a reduction in triglycerides of up to 30% in the blood after three months. The first improvements in blood lipid levels occur after about 2 weeks.

The most notable study on guggul in terms of its effect on body weight dates back to 1995 and was carried out at the Ayurveda Research Centre in Mumbai. 58 overweight patients were divided into two groups: both groups were encouraged to eat a low-calorie diet and go for a half-hour walk every day; the other group also received a guggul extract. After just one month, both groups showed a significant reduction in weight. However, the guggul patients had lost an average of 0.6 kg more in body weight, and subjects with a body weight of >90 kg had even lost 2.25 kg more than those in the control group.

acne

Several studies have shown that Guggul is suitable both as an adjuvant and as a complete alternative therapy for nodulocystic acne (a particularly severe form of acne) (see: https://pubmed.ncbi.nlm.nih.gov/16473756/ ). A study with 21 subjects was able to prove that taking just 25 mg of guggulsterone is as effective as tetracycline (an antibiotic often used for acne) (see. https://pubmed.ncbi.nlm.nih.gov/7798429/ ). In addition, people with oily skin responded significantly better to guggulsterone than to tetracycline treatment. Another study was able to show that taking guggul for six weeks helped treat acne without causing any significant side effects (see. https://ijdvl.com/oral-gugulipid-in-acne-vulgaris-management/ ).

hypothyroidism

Studies suggest that guggul extracts may alleviate hypothyroidism by increasing iodine absorption and increasing the activity of enzymes produced by the thyroid gland (see below). https://pubmed.ncbi.nlm.nih.gov/17340256/ and https://pubmed.ncbi.nlm.nih.gov/15798994/ ). A human study investigated the treatment of hypothyroidism using guggul tablets and a punarnavadi kashayam infusion. The results showed that this treatment reduced signs and symptoms of hypothyroidism such as weakness, fatigue and muscle pain (see. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6287405/ ).

osteoarthritis

The authors of a 2003 study conducted both preclinical and clinical studies using guggul for pain relief and tolerability in elderly patients with osteoarthritis. The study enrolled 30 male and female participants who met the inclusion/exclusion criteria and had a score of 2 or more on the Kellegran-Lawrence scale for at least one knee. Guggul was administered in capsule form (500 mg extract) with food. At the end of treatment, there was a significant difference in outcomes compared to the control group. The primary outcome measure, the WOMAC total score (the Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC)  is a patient-based self-assessment questionnaire and offers the possibility to evaluate the most important and everyday relevant consequences of osteoarthritis), the participants improved significantly after one month of taking the dietary supplement (P < 0.0001) and continued to improve after two months and at the follow-up examination.No side effects were reported during the trial, so the authors conclude that guggul extract is recommended as an adjuvant therapy for osteoarthritis (cf. https://pubmed.ncbi.nlm.nih.gov/12776478/ ).

sport

For athletes and especially for bodybuilders, guggul extract is interesting as a diet support, since the conversion of the thyroid hormone T4 into T3 is not reduced as much when guggulsterones are taken, despite calorie reduction. Taking the ephedrine/caffeine combination and guggulsterones at the same time could significantly accelerate fat loss. Many athletes compare the effect to that of clembuterol combined with low-dose synthetic thyroid hormones.

dosage

For preventive use, ~50 mg daily (1 capsule) is recommended. For the treatment of obesity and lipid metabolism disorders, relevant studies recommend 70-90 mg (~2 capsules) of guggulsterone, divided into 2 portions per day.

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