Guggulsterone Gum Extract
Also known as: pregna-4,17-diene-3,16-dione, Guggul, Indian bdellium gum extract, Guggulsterone
Overview
Guggulsterone is a bioactive phytosterol extracted from the gum resin of Commiphora wightii, a plant traditionally used in Ayurvedic and Unani medicine. It is primarily investigated for its anti-inflammatory, lipid-lowering, and anticancer properties. As a supplement, it is commonly explored for cholesterol management and as an anti-inflammatory agent, with emerging research into its potential anticancer effects. While extensive in vitro and preclinical studies exist, particularly regarding its anticancer mechanisms, human clinical trials are limited. The available evidence is largely preclinical, with some human data on lipid metabolism, but insufficient high-quality randomized controlled trials (RCTs) for definitive clinical recommendations.
Benefits
Guggulsterone has demonstrated several potential benefits, primarily in preclinical settings: * **Anticancer effects:** A systematic review and meta-analysis of 40 studies (23 included in meta-analysis) showed that guggulsterone induces apoptosis (programmed cell death) in a wide range of cancer cell lines, including pancreatic, hepatocellular, breast, colon, prostate, and lung cancers. The meta-analysis indicated a significant, time-dependent increase in apoptotic cell death, with odds ratios of 3.98 after 24 hours and 11.17 for longer exposures (p < 0.001). This suggests a strong potential for guggulsterone to inhibit cancer cell proliferation and promote their demise in laboratory settings. * **Lipid metabolism improvement:** In animal models, guggulsterone acts as a farnesoid X receptor (FXR) antagonist, which plays a crucial role in cholesterol and bile acid metabolism. Studies have shown it can reduce plasma levels of trimethylamine N-oxide (TMAO), a pro-atherogenic metabolite, and improve overall lipid profiles by lowering total cholesterol, triglycerides, LDL (low-density lipoprotein), and VLDL (very-low-density lipoprotein), while increasing HDL (high-density lipoprotein). These effects suggest potential cardiovascular benefits, though human clinical data are currently limited.
How it works
Guggulsterone exerts its effects by modulating several key biological pathways. It functions as an antagonist of the farnesoid X receptor (FXR), a nuclear receptor critical for regulating bile acid and cholesterol homeostasis, thereby influencing lipid metabolism. In cancer cells, guggulsterone induces apoptosis by activating caspases and engaging mitochondrial pathways, leading to programmed cell death. Additionally, it is believed to possess anti-inflammatory properties by inhibiting NF-κB and other pro-inflammatory signaling pathways. Absorption and bioavailability data are limited but are likely variable due to its lipophilic nature.
Side effects
Comprehensive human safety data for guggulsterone are currently lacking, although traditional use suggests an acceptable safety profile. Common side effects and adverse events are not well documented in the provided research, and preclinical studies have not reported significant safety signals. However, due to its action as an FXR antagonist and potential influence on liver metabolism, there is a possibility of drug interactions. Specific interactions require further investigation. Contraindications and data for special populations (e.g., pregnant or breastfeeding individuals, children) are not available from the current sources. Users should exercise caution and consult a healthcare professional before use, especially if taking other medications or having pre-existing health conditions.
Dosage
There are no standardized dosing guidelines for guggulsterone established from human clinical trials. In vitro studies investigating its anticancer effects have used effective concentrations ranging from 5–75 μM. Animal studies have employed variable doses, but these do not directly translate to human recommendations. Due to the lack of robust human clinical data, specific human dosing recommendations are not well defined. For anticancer effects observed in cell studies, longer exposure times (greater than 24 hours) were associated with increased efficacy. Factors such as formulation and absorption, which can significantly impact bioavailability and effective dosage, remain to be fully clarified.
FAQs
Is guggulsterone effective for cancer treatment?
Current evidence is limited to in vitro and preclinical studies showing promising apoptotic effects in various cancer cell lines. Clinical trials are needed to confirm its efficacy and safety in humans for cancer treatment.
Can it lower cholesterol?
Animal studies suggest lipid-lowering effects by antagonizing the FXR receptor, which influences cholesterol and bile acid metabolism. However, human evidence is currently insufficient to make definitive claims.
Is guggulsterone safe?
Traditional use suggests an acceptable safety profile, but rigorous human safety data are lacking. Comprehensive clinical trials are needed to fully assess its safety profile, potential side effects, and drug interactions.
How long does it take to see effects?
In vitro studies on cancer cells indicate that anticancer effects are time-dependent, increasing with longer exposure. However, clinical timelines for any potential effects in humans are currently unknown due to limited research.
Research Sources
- https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2023.1155163/full – This systematic review and meta-analysis of 40 studies (23 meta-analyzed) demonstrated that guggulsterone significantly induces apoptosis in a broad range of cancer cell lines, showing a time-dependent effect. It highlights guggulsterone's preclinical anticancer potential but notes the lack of clinical data.
- https://pmc.ncbi.nlm.nih.gov/articles/PMC10185795/ – This PMC article, likely a duplicate or closely related to the Frontiers in Pharmacology study, confirms the apoptotic effects of guggulsterone in various cancer cell lines based on a systematic review and meta-analysis. It emphasizes the need for further in vivo and clinical studies to translate these preclinical findings.
- https://pubmed.ncbi.nlm.nih.gov/37201024/ – This PubMed entry likely corresponds to one of the systematic reviews or meta-analyses on guggulsterone's anticancer effects. It would summarize the findings regarding its ability to induce apoptosis in cancer cells and underscore the need for clinical validation.
- https://journals.sagepub.com/doi/full/10.1177/0960327118817862 – This animal study investigated guggulsterone's effects in rats on a choline diet. It found that guggulsterone reduced plasma levels of TMAO and improved lipid profiles, including lowering total cholesterol, triglycerides, LDL, and VLDL, while increasing HDL, suggesting potential cardiovascular benefits.
