Guggul

Guggul is derived from the resin of a medicinal plant that has been used for thousands of years in Ayurveda. Extracts of the plant are traditionally used alone or in combination with other botanicals to treat various disorders including rheumatism, arthritis, neurological diseases, hemorrhoids, urinary disorders, and skin diseases.

Preclinical studies suggest that the compound guggulsterone has antiangiogenic and antitumor properties ^{(4) (5) (6) (7)}. In an animal study, guggul had cardioprotective effects ⁽¹⁶⁾.

Studies in humans are limited, but suggest guggul may be effective for hypercholesterolemia ^{(1) (2) (11)}. However, other trials indicate uncertain benefit ⁽²⁰⁾ or that guggul may actually raise cholesterol levels ⁽³⁾. It also showed no benefit when taken with Triphala, an Ayurvedic formulation ⁽²¹⁾. Additional research is needed to determine safety and efficacy.

• Acne
• Arthritis
• Hemorrhoids
• High cholesterol
• Urinary tract disorders
• Weight loss

In vitro, guggulsterone affected biosynthesis of cholesterol in the liver ⁽²⁾. Cholesterol-lowering activity in mice was attributed to inhibition of FXR, a nuclear hormone receptor that is activated by bile acids. FXR mediates a negative feedback loop to decrease bile acid production by the liver. This loop is an important component of cholesterol metabolism regulation ⁽¹⁰⁾. In humans, hypolipidemic outcomes may be better for those with a higher capacity to metabolize Z-guggulsterone with moderate carboxylesterase induction ⁽¹⁹⁾.

In tumor cells, guggulsterone induced apoptosis by activating JNK ⁽⁵⁾ and repressing Akt signaling ⁽⁶⁾.

Guggulsterone activates nuclear receptors such as estrogen receptor alpha, pregnane X receptor, and progesterone receptor and may induce CYP3A genes ⁽⁸⁾.

Headache, mild nausea, eructation, hiccups, and loose stools; hypersensitivity rash ^{(2) (3) (20) (21)}

Case reports

• Allergic reactions: Contact dermatitis attributed to guggul in slimming and anticellulite creams ^{(13) (14)}.
• Severe hypertransaminasemia: In a 63-year old woman after using an over-the-counter lipid-lowering product for 6 months that contained guggulsterol and red yeast rice extract. Symptoms resolved after product discontinuation ⁽¹²⁾.
• Acute hepatic failure requiring transplant: In a healthy woman who took a dietary supplement containing usnic acid, green tea, and guggul tree extract ⁽¹⁵⁾. Although usnic acid was considered the predominating factor, its effects could have been amplified by the other ingredients.

CYP3A4 substrates: Lab studies suggest that guggul induces CYP3A4 and may affect the intracellular concentration of drugs metabolized by this enzyme ⁽⁸⁾.

Reduced serum triglycerides ⁽²⁾
Elevated TSH, T3, and T4 ⁽⁹⁾