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Journal articles on the topic 'Guggulsterone Z'

Author: Grafiati

Published: 5 June 2025

Last updated: 15 July 2025

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1

Duraipandi, Selvakumar, and Vijaya Selvakumar. "Comparative study of isolated Guggulsterones as marker compounds from Guggulu, Commiphora mukul with Ayurvedic Gugglu containing formulations by HPTLC, an in-house quality control method." JOURNAL OF PHARMACEUTICAL CHEMISTRY 1, no. 1 (2014): 1. http://dx.doi.org/10.14805/jphchem.2014.art3.

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The guggulu containing polyherbal formulations in Ayurveda have been used for treating various inflammatory conditions. A simple HPTLC method has been developed to qualitatively analyze the formulations that claimed to have contained guggulu using the Guggulsterones isolated from the guggulu raw material as a marker. The isolation of Guggulsterones from the resinous gum obtained from the plant was used as a marker to determine the Guggulsterone content in the formulations. The study showed that all the preparations taken for analysis that claimed to contain Guggulsterones was originally having the contents but in variable amounts depending on the amount of resin taken for the preparation. Due to the fact that Guggulsterones are very expensive marker compounds if procured separately as Guggulsterone E and Z forms, this method can be used for routine qualitative analysis of presence of Guggulsterones as an in-house quality control method.

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2

Nagarajan, Mythili, Ted W. Waszkuc, and Jidong Sun. "Simultaneous Determination of E- and Z-Guggulsterones in Dietary Supplements Containing Commiphora mukul Extract (Guggulipid) by Liquid Chromatography." Journal of AOAC INTERNATIONAL 84, no. 1 (2001): 24–28. http://dx.doi.org/10.1093/jaoac/84.1.24.

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Abstract Guggulipid, the standardized product from the extraction of the ole-gum-resin from the Commiphora mukul plant, has been marketed as a hypolipidemic agent. The ketosteroids, cis- and trans-4,17(20)-pregnadiene-3,16-dione, known as E- and Z-guggulsterones, respectively, are the main ingredients in guggulipid. A liquid chromatographic method was developed for simultaneous determination of E- and Z-guggulsterones in guggulipid preparations using synthetic E- and Z-guggulsterone standards. Realtively low amounts of guggulsterones (E and Z) were found in commercial guggulipid preparations in comparison with the manufacturer's claim of 2.5%. The mixture of E- and Z-guggulsterones was extracted and separated on a Symmetry C18 reversed-phase column, with a mobile phase of acetonitrile–water (46 + 54, v/v) and detected at 242 nm. The retention times of E- and Z-guggulsterones are approximately 8 and 11 min, respectively. Assay quantitation was based on the calibration curve obtained from a mixture of synthetic standard E- and Z-guggulsterones. Experimental data on selectivity, linearity, accuracy, and recoveries are presented.

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Lv, Ruxi, Min Zhu, Kun Chen, Haitao Xie, Hongxia Bai, and Qingfa Chen. "Z-Guggulsterone Induces Apoptosis in Gastric Cancer Cells through the Intrinsic Mitochondria-Dependent Pathway." Scientific World Journal 2021 (January 4, 2021): 1–6. http://dx.doi.org/10.1155/2021/3152304.

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Background. To study the effects of z-guggulsterone on gastric cancer cell apoptosis and the mechanism related. Materials and Methods. Human gastric tumor SGC-7901 cells and GES-1 normal epithelial cells were treated with z-guggulsterone (0–75 μM) for 24 h. MTT assay was applied to evaluate cell proliferation. Flow cytometry and Hoechst staining were used to assess cell apoptosis. Western blotting was applied to evaluate FXR, small heterodimer partner (SHP), Bcl-2, and Bax protein expression. ELISA was applied to gain the levels of active caspase-3 and the contents of TNF-α, TGF-β1, and VEGF. Results. The expression levels of FXR and SHP were higher in tumor cells than in normal epithelial cells. Inhibition of FXR signaling with z-guggulsterone dose-dependently inhibited SGC-7901 cell proliferation and promoted SGC-7901 cell apoptosis. Bcl-2 protein expression was significantly decreased, and active caspase-3 and Bax protein expression was increased in SGC-7901 cells incubated with z-guggulsterone. The content of TNF-α was significantly increased, and the contents of VEGF and TGF-β1 were decreased in SGC-7901 cells incubated with z-guggulsterone. Conclusions. Inhibition of FXR signaling with z-guggulsterone induced anticancer effects in SGC-7901 cells by decreasing cell proliferation and promoting apoptosis. Z-guggulsterone induced cell apoptosis through the mitochondria-dependent pathway.

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4

Gupta, Meenakshi, Shaikh Maryam Ghufran, Tasneem Kausar, et al. "Z-Guggulsterone Is a Potential Lead Molecule of Dawa-ul-Kurkum against Hepatocellular Carcinoma." Molecules 27, no. 16 (2022): 5104. http://dx.doi.org/10.3390/molecules27165104.

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An ancient saffron-based polyherbal formulation, Dawa-ul-Kurkum (DuK), has been used to treat liver ailments and other diseases and was recently evaluated for its anticancer potential against hepatocellular carcinoma (HCC) by our research team. To gain further insight into the lead molecule of DuK, we selected ten active constituents belonging to its seven herbal constituents (crocin, crocetin, safranal, jatamansone, isovaleric acid, cinnamaldehyde, coumaric acid, citral, guggulsterone and dehydrocostus lactone). We docked them with 32 prominent proteins that play important roles in the development, progression and suppression of HCC and those involved in endoplasmic reticulum (ER) stress to identify the binding interactions between them. Three reference drugs for HCC (sorafenib, regorafenib, and nivolumab) were also examined for comparison. The in silico studies revealed that, out of the ten compounds, three of them—viz., Z-guggulsterone, dehydrocostus lactone and crocin—showed good binding efficiency with the HCC and ER stress proteins. Comparison of binding affinity with standard drugs was followed by preliminary in vitro screening of these selected compounds in human liver cancer cell lines. The results provided the basis for selecting Z-guggulsterone as the best-acting phytoconstituent amongst the 10 studied. Further validation of the binding efficiency of Z-guggulsterone was undertaking using molecular dynamics (MD) simulation studies. The effects of Z-guggulsterone on clone formation and cell cycle progression were also assessed. The anti-oxidant potential of Z-guggulsterone was analyzed through DPPH and FRAP assays. qRTPCR was utilized to check the results at the in vitro level. These results indicate that Z-guggulsterone should be considered as the main constituent of DuK instead of the crocin in saffron, as previously hypothesized.

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5

Vijaykumar K. Parmar, Deepika Mohanta, and Harsh Shah. "A Validated High Performance Thin Layer Chromatographic Method for Simultaneous Estimation of Berberine Chloride and Guggulsterone Z in Herbal Formulation." Journal of Pharmaceutical Technology, Research and Management 7, no. 1 (2019): 7–13. http://dx.doi.org/10.15415/jptrm.2019.71002.

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A simple, precise, and robust high-performance thin layer chromatography (HPTLC) method was developed and validated for the determination of berberine chloride and guggulsterone Z in herbal formulation. Chromatographic separation was achieved on aluminium plates precoated with silica gel G60F254 as the stationary phase and toluene-acetonitrile-formic acid (5:3:0.5 v/v/v) as the mobile phase. Densitometric evaluation was carried out at 264 nm. The present method was validated according to ICH guidelines. The Rf value of berberine chloride and guggulsterone Z was found to be 0.40 ± 0.02 and 0.68 ± 0.02, respectively. The response in terms of peak area was found to be linear over the concentration range of 100-500 ng/spot for berberine chloride and 200-1000 ng/spot for guggulsterone Z with regression coefficient value greater than 0.995 for both the phytoconstituents. The method was validated by determining its accuracy, precision, robustness, specificity and system suitability. The method was found to be accurate, precise and robust to carry out the simultaneous estimation of berberine chloride and guggulsterone Z. The developed method was successfully applied for the simultaneous estimation of berberine chloride and guggulsterone Z in herbal formulation.

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6

Gupta, V. K., P. Bandhoria, B. D. Gupta, and K. K. Gupta. "Crystal structure of guggulsterone Z." Crystallography Reports 51, no. 2 (2006): 265–70. http://dx.doi.org/10.1134/s106377450602012x.

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7

Ahmad, Sufiyan, Aakanksha Dashpute, Mukesh Patil, et al. "Development and Validation of HPLC And HPTLC for Simultaneous Analysis of E and Z Guggulsterone, A-11–KBA And 11–KBA from Herbal Formulation." INTERNATIONAL JOURNAL OF PHARMACEUTICAL QUALITY ASSURANCE 14, no. 02 (2023): 393–96. http://dx.doi.org/10.25258/ijpqa.14.2.25.

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RP-HPLC and HPTLC are two easy, sensitive, efficient, and accurate procedures that allow for simultaneous estimates of Z and E guggulsterone, A-11-KBA, and 11-KBA. For the HPLC method, we recommend the use of a symmetry C18 column. Using a solvent gradient based on solvent A (orthophosphoric acid) and solvent B (methanol), the effluent was monitored at 250 nm with a 1.0 mL/min flow rate. The peaks of 11-KBA and A-11-KBA were eluted at 5.8 and 6.3 minutes, while those of Z and E-guggulsterone were at 4.8 and 5.3 minutes. For the HPTLC method of separation, a silica gel layer was applied on an aluminum plate prewashed in methanol using a Camag Linomat V applicator fitted with a 100 μL syringe. The linear expansion was carried out using a solvent mixture of n-hexane, chloroform, ethyl acetate, and methanol (v/v/v: 10:3:3:1, respectively). Camag T.L.C. scanner III (V 1.4.3.6336), operating in reflectance-absorbance mode at 254 nm and controlled by win CATS software, was used to carry out the densitometric scanning. The R.F. resolutions for 11-KBA, A-11-KBA, E-guggulsterone, and Z-guggulsterone in the selected mobile phase were 0.68, 0.61, 0.39, and 0.28, respectively. The linearity, accuracy, and precision of the techniques were all confirmed. The proposed methods were successful in estimating E- and Z-guggulsterone as well as 11-KBA and A-11-KBA.

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8

Ulrich, Judith, Svenja Stiltz, Alexis St-Gelais, et al. "Phytochemical Composition of Commiphora Oleogum Resins and Their Cytotoxicity against Skin Cancer Cells." Molecules 27, no. 12 (2022): 3903. http://dx.doi.org/10.3390/molecules27123903.

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Oleogum resins of the genus Commiphora have been used in traditional medicines for centuries. More than 200 Commiphora species exhibit highly variable phytochemical compositions. A novel highly selective, sensitive, accurate HPLC-MS/MS method was developed and validated to quantify five characteristic phytosteroids and furanosesquiterpenoids, namely (E)-guggulsterone, (Z)-guggulsterone, curzerenone, furanoeudesma-1,3-diene, and myrrhone. The resulting contents and additionally GC analysis were used to classify and differentiate Commiphora oleogum resins of the species C. myrrha, C. erythraea, C. mukul, C. holtziana, C. confusa, and C. kua, as well as unspecified resins. Interestingly, a Commiphora sample from Ogaden, Ethiopia, comprised 446 ng/mg guggulsterones presumed to be unique to C. mukul from the Indian subcontinent. However, Commiphora from Ogaden differed considerably from C. mukul in respect to guggulsterones isomer’s ratio. Moreover, the cytotoxicity of Commiphora extracts, essential oils, botanical drugs containing Commiphora, and pure compounds against the epidermoid carcinoma A431, malignant melanoma RPMI-7951 and SK-MEL-28 cells was investigated in vitro. Thereby, especially C. mukul extract and C. myrrha essential oil exhibited high cytotoxicity against skin cancer cells with IC50 of 2.9–10.9 µg/mL, but were less toxic to normal keratinocytes. In summary, Commiphora oleogum resins and its phytochemicals warrant further investigation aiming at chemotaxonomical classification as well as application in skin cancer treatment.

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Qaiyyum, Ifra Abdul, Mohammad Nawab, Ayesha Aijaz, and Anam Farah. "A REVIEW ON PHYTOCONSTITUENTS AND THERAPEUTIC USES OF MUQIL (COMMIPHORA MUKUL)." Indian Journal of Unani Medicine 15, no. 01 (2022): 33–41. http://dx.doi.org/10.53390/ijum.2022.15106.

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Muqilis one of the best drugs in traditional system of medicine since ancient. It belongs to Burseraceae family, has 540 species and is found in dry area of India known as Indian bdellium. It is bushy plant 1.2-1.8 m can provide yellowish gum resin also called as gugulipid. Most commonly gum of this plant used for therapeutic and medicinal purpose. According to Unani system of medicine (USM) it has two types: 1. Muqil-e-Saqalibi, 2. Muqil-e-Arabi. The plant Commiphora mukul is also known as Balsamodendron mukul Stock. Muqil has active constituents producing number of biological activities such as Antiinflammatory effect (guggulsterones Z and E), Osteoprotective effect (guggulsterone), Anti- inflammatory, analgesic antiarthritic activities (Guggulsterone), Anti-diabetic effect (gum resin 900 mg daily), Antimicrobial, antibacterial, antiviral and antifungal activities (Eugenol, ellagic acid alpha-pinene, masumbinoic acid and masumbinone), Anti-hemorrhoid activity (Muqil resin), Anti-neoplastic activity (GS, gugulipid and Z-guggusterone), Cardioprotective effect (gugulipid and guggusterone), Nephroprotective effect, Nodulocystic Acne (Guggulipid), Neuroprotective effects (guggulipid), Immunomodulatory effect, Stimulate Thyroid gland activity (Commiphora mukul gum) Anti-asthmatic (300 mg of gum resin thrice daily), Inflammatory Bowel Disease (gum resin at a dose of 900 mg daily). It is also useful for systemic disease such as Osteoarthritis, Rheumatoid arthritis, Gout, Cadio-protective effect and thyro-protective effect, nervous diseases and urinarydiseases. Skin disorders are leprosy, pyorrhea, muscle spasm, demulcent, and depurative.

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10

Sairkar, Pramod Kumar, Anjana Sharma, and N. P. Shukla. "Antimicrobial Activity of Guggulsterone E and Z." International Journal of Current Microbiology and Applied Sciences 5, no. 10 (2016): 20–26. http://dx.doi.org/10.20546/ijcmas.2016.510.004.

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11

Momin, Munira, Vivek Basudkar, Sankalp Gharat, Anita D. Chando, and Tabassum Khan. "QUANTITATIVE ESTIMATION OF 6-GINGEROL, E-GUGGULSTERONE AND Z-GUGGULSTERONE IN A FIXED DOSE COMBINATION NANOEMULGEL BY RP-HPLC." INDIAN DRUGS 60, no. 07 (2023): 61–69. http://dx.doi.org/10.53879/id.60.07.13722.

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Polyherbal formulations have proved to be efficacious for the therapeutic treatment of various diseases, However, the development of validated robust analytical methods for quantification is a major challenge. The aim of this project was to develop a simple analytical method for the quantification of 6-gingerol (6-GIN), E-guggulsterone (E-GGS) and Z-guggulsterone (Z-GGS) in nanoemulsion based gel using reverse phase high performance liquid chromatography (RP-HPLC). 6-GIN, E-GGS and Z-GGS were quantified using acetonitrile: water: methanol (70:20:10 V/V/V) as the mobile phase at 1.0 mL min-1 flow rate with photodiode array detection. The developed method was validated for linearity, accuracy, precision, specificity and robustness as per ICH Q2 (R1) guidelines. The drug content of the three actives in the developed nanoemulgel was found to be between 90% to 110% w/w. The developed analytical method is simple and can be used for quantification of 6-GIN, E-GGS and Z-GGS in fixed dose product containing these actives.

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12

Tripathi, Y., Pratibha Tripathi, O. Malhotra, and S. Tripathi. "Thyroid Stimulatory Action of (Z)-Guggulsterone: Mechanism of Action." Planta Medica 54, no. 04 (1988): 271–77. http://dx.doi.org/10.1055/s-2006-962431.

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13

Saikumar, Indira, Avinash A. Rasalkar, Bhadravathi M. Shivakumar, Divijendra N. Reddy, and Rajyalakshmi Malempati. "Effect of Guggulsterone on the Expression of Adiponectin in 3T3-L1 Cells." Natural Product Communications 13, no. 3 (2018): 1934578X1801300. http://dx.doi.org/10.1177/1934578x1801300314.

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Obesity is a worldwide threat, affecting both developed and developing countries. Guggulipid obtained from gum guggul is widely prescribed in Ayurveda for various medical conditions including obesity. The present study was designed to investigate the effect of guggulsterone on the expression of adiponectin, the adipokine that regulates glucose and fatty acid metabolism. 3T3-L1 cells were treated with guggulsterone E / Z isomer [(GE) /(GZ)] and mRNA levels of adiponectin as well as PPARγ (a transcription factor that regulates adiponectin expression) were monitored. Treatment of 3T3-L1 cells with GE / GZ during differentiation into adipocytes led to reduced mRNA levels of adiponectin. However, no effect on the mRNA levels of adiponectin was observed when fully differentiated adipocytes were treated with either GE or GZ.

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Kumar, Vijay, Simranjeet Singh, and Ravindra Singh. "Phytochemical Constituents of Guggul and their Biological Qualities." Mini-Reviews in Organic Chemistry 17, no. 3 (2020): 277–88. http://dx.doi.org/10.2174/1570193x16666190129161757.

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: In the herbal drug pharmaceutical industry, guggul is enjoying emergent consumer acceptance around the world. In the Indian market, more than fifty formulations of guggul have been introduced by well-known brands including Himalaya, Patanjali and Baidyanath Pharmaceuticals. Basically, guggul is the gum resin from Commiphora wightii (syn. Commiphora Mukul). It has been used to treat various ailments including obesity, osteoarthritis, arthritis, constipation, liver disorders, inflammation, anemia, diabetes, etc. Including medicinal properties, it is used as a good binding agent and mixed in various herbal formulations. To review the major phytochemical, medicinal properties and analytical methods involved in the detection of guggul by using the exhaustive bibliographic research by means of various scientific engines and databases. Guggul contained approximately 66 phytochemical including gallic acid, quercetin, and guggulsterones E and Z. These phytochemicals have a wide range of pharmacological activities such as antioxidant, antibacterial, antimutagenic, antivenom and antitumor. It has been noticed that the mode of action of guggulsterone has not been fully explored. Pharmacology and toxicological studies are very few. These works have shown huge literature gap, which is to be fulfilled through the detailed in-vivo and in-vitro studies.

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Angelopoulou, Maria K., Konstantinos Lilakos, Vassilios Salpeas, et al. "Z-Guggulsterone Downregulates Survivin and Induces Cell Death in Large B Cell Lymphoma Cells In Vitro." Blood 108, no. 11 (2006): 4752. http://dx.doi.org/10.1182/blood.v108.11.4752.4752.

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Abstract Introduction: Survivin is a member of the Inhibitor of Apoptosis Proteins and has recently gained attention as a possible therapeutic target in malignancies, due to its dual role both as an antiapoptotic protein and as a cell cycle regulator. It is overexpressed in malignant cells and confers resistance to chemotherapy and other stimuli triggering apoptosis. Z-Guggulsterone (Z-GGS) is a plant sterol, which has been used in inflammatory conditions and has been recognized as a potent NF-kB suppressor. Since Survivin, as well as other antiapoptotic proteins, are under NFkB regulation, we studied the effect of Z-GGS on two B-cell lymphoma cell lines. Methods: DB and HT cell lines were treated with increasing concentrations (10μM, 20μM and 30μM) of Z-GGS, for 24, 48 and 72 hours. Survivin expression was tested with Flow Cytometry and Survivin transcripts were measured with quantitative real time PCR using the Universal Probe Library hydrolysis probes and expressed as Survivin/abl ratio. Cell viability was assessed with the MTT assay. Results: Both cell lines were positive for Survivin at baseline by flow cytometry (66% of total cells for DB and 95% for HT). Treatment of DB cells with 10, 20 and 30μM Z-GGS resulted in a 44%, 49% and 68% reduction of Survivin expression at 24 hours, respectively, whereas the effect on HT was less prominent with a 10% reduction at 24 hours with 30μM Z-GGS. Survivin transcripts decreased as well, with the maximum effect observed at 72 hours with 30μM Z-GGS for both cell lines: Survivin/abl was 0.009 for untreated cells vs 0.0008 with 30μM Z-GGS for DB cells and 0.0135 vs 0.0005 for HT cells. Linearity was observed for increasing concentrations of Z-GGS at 72 hours. Cell viability was practically unaffected at any time point with 10 and 20μM Z-GGS for both cell lines, whereas 30 μM Z-GGS resulted in a 63% and 78% cell death at 48 and 72 hours respectively for DB cells and 67% and 83% for HT cells. Conclusions: The steroid Z-GGS downregulates Survivin expression in B-lymphoma cells in vitro and induces cell death at 30μM concentration. Further experiments will clarify its possible role in the treatment of B-cell malignancies.

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., Pratap B. Pawar, and Sunil A. Nirmal . "Quantitative Estimation of Guggulsterone E and Z in Polyherbal Tablet Formulation by HPLC." Journal of Current Pharma Research 6, no. 3 (2016): 1877–81. http://dx.doi.org/10.33786/jcpr.2016.v06i03.002.

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17

Xu, Yier, Jian Guan, Jianyu Xu, Shuilin Chen, and Guicai Sun. "Z-Guggulsterone attenuates glucocorticoid-induced osteoporosis through activation of Nrf2/HO-1 signaling." Life Sciences 224 (May 2019): 58–66. http://dx.doi.org/10.1016/j.lfs.2019.03.051.

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Gamit, Kanan G., Niraj Y. Vyas, Nishit D. Patel, and Manan A. Raval. "ESTIMATION OF GUGGULSTERONE-Z IN GOKSHURADI GUGGULU USING REVERSED-PHASE HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY." Asian Journal of Pharmaceutical and Clinical Research 11, no. 11 (2018): 204. http://dx.doi.org/10.22159/ajpcr.2018.v11i11.26894.

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Objective: A study was aimed to estimate guggulsterone-Z (GZ) in Gokshuradi Guggulu (GG).Methods: An analytical method was developed and validated using Waters Alliance high-performance liquid chromatography system (Empower software), equipped with photodiode array detector. Separation was achieved using Phenomenex, C-18 (250 mm×4.6 mm, 5 μ) column. Mobile phase consisted of acetonitrile:water (70:30,v/v). Flow rate was set to 1 ml/min and detection was performed at 251 nm.Results and Discussion: Validation parameters such as linearity, precision, accuracy, limit of detection, limit of quantification, and robustness were performed. Amount of GZ was estimated using linearity equation.Conclusion: GG was found to contain 0.815±0.03 g% w/w GZ. Validated method may be used as one of the parameters to standardize the formulation.

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Shelke, Nitin, Vinodkumar Kuber, Shrinivas Bhope та Ramchandra Jadhav. "Simultaneous HPTLC analysis ofE-guggulsterone,Z-guggulsterone, 11-keto-β-boswellic acid, and 3-acetyl-11-keto-β-boswellic acid in an anti-arthritic formulation". Journal of Planar Chromatography – Modern TLC 24, № 3 (2011): 242–47. http://dx.doi.org/10.1556/jpc.24.2011.3.13.

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Agrawal, P., R. Vegda, and K. Laddha. "Simultaneous Estimation of Withaferin A and Z-Guggulsterone in Marketed Formulation by RP-HPLC." Journal of Chromatographic Science 53, no. 6 (2015): 940–44. http://dx.doi.org/10.1093/chromsci/bmu153.

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Huang, Chao, Jili Wang, Xu Lu та ін. "Z-guggulsterone negatively controls microglia-mediated neuroinflammation via blocking IκB-α–NF-κB signals". Neuroscience Letters 619 (квітень 2016): 34–42. http://dx.doi.org/10.1016/j.neulet.2016.02.021.

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Liu, Minna, Wenjun Wang, Jinhan Wang, Chuntian Fang, and Tianlong Liu. "Z-Guggulsterone alleviates renal fibrosis by mitigating G2/M cycle arrest through Klotho/p53 signaling." Chemico-Biological Interactions 354 (February 2022): 109846. http://dx.doi.org/10.1016/j.cbi.2022.109846.

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Jariwala, JiteshK, ChetanC Anajwala, AjayK Saluja, and SanjayL Dakhara. "Simultaneous estimation of Guggulsterone E & Z and Tinosporaside in Jivitprada vati by HPTLC method." International Journal of Green Pharmacy 5, no. 2 (2011): 113. http://dx.doi.org/10.4103/0973-8258.85168.

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24

Liu, Tianlong, Minna Liu, Tiejun Zhang, et al. "Z-Guggulsterone attenuates astrocytes-mediated neuroinflammation after ischemia by inhibiting toll-like receptor 4 pathway." Journal of Neurochemistry 147, no. 6 (2018): 803–15. http://dx.doi.org/10.1111/jnc.14583.

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25

Liu, Feng-Guo, Wen-Feng Hu, Ji-Li Wang, et al. "Z-Guggulsterone Produces Antidepressant-Like Effects in Mice through Activation of the BDNF Signaling Pathway." International Journal of Neuropsychopharmacology 20, no. 6 (2017): 485–97. http://dx.doi.org/10.1093/ijnp/pyx009.

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Yang, Dongfang, Jian Yang, Deshi Shi, et al. "Hypolipidemic agent Z-guggulsterone: metabolism interplays with induction of carboxylesterase and bile salt export pump." Journal of Lipid Research 53, no. 3 (2012): 529–39. http://dx.doi.org/10.1194/jlr.m014688.

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Vyas, Jayshree, Prakash Itankar, Mohammad Tauqeer, Amruta Kelkar, and Mona Agrawal. "Development of HPTLC method for estimation of piperine, guggulsterone E and Z in polyherbal formulation." Pharmacognosy Journal 5, no. 6 (2013): 259–64. http://dx.doi.org/10.1016/j.phcgj.2013.10.003.

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Yang, Yujia, Xiuting Sun, Chuhang Peng, Jianhe Wei, and Xinquan Yang. "The Genus Commiphora: An Overview of Its Traditional Uses, Phytochemistry, Pharmacology, and Quality Control." Pharmaceuticals 17, no. 11 (2024): 1524. http://dx.doi.org/10.3390/ph17111524.

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Myrrh is the resinous substance secreted by plants of the genus Commiphora. In traditional Chinese medicine, Ayurvedic medicine, and traditional Arabic medicine, myrrh is regarded as an important medicinal material, widely used in the treatment of trauma, arthritis, hyperlipidemia, and other diseases. This review explores the evolving scientific understanding of the genus Commiphora, covering facets of ethnopharmacology, phytochemistry, pharmacology, artificial cultivation, and quality control. In particular, the chemical constituents and pharmacological research are reviewed. More than 300 types of secondary metabolites have been identified through phytochemical studies of this genus. Guggulsterone is a bioactive steroid isolated mainly from Commiphora mukul. The two isomers, Z- and E-guggulsterone, have shown a wide range of in vitro and in vivo pharmacological effects, including anti-proliferation, antioxidant, anti-inflammatory, and antibacterial. However, the current scientific research on quality control of medicinal materials and identification of original plants is insufficient, which limits the reproducibility and accuracy of biological activity evaluation experiments. Therefore, the establishment of analytical protocols and standardization of extracts is an important step before biological evaluation. At the same time, in order to find more bioactive substances, it is necessary to strengthen the research on the stems, barks, and leaves of this genus. The sources used in this study include PubMed, CNKI, Web of Science, Google Scholar, and other databases, as well as multinational pharmacopoeias, ancient books of traditional medicine, herbal classics, and modern monographs.

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Liu, Tianlong, Wenjun Wang, Minna Liu, et al. "Z-Guggulsterone alleviated oxidative stress and inflammation through inhibiting the TXNIP/NLRP3 axis in ischemic stroke." International Immunopharmacology 89 (December 2020): 107094. http://dx.doi.org/10.1016/j.intimp.2020.107094.

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Wang, Jieqin, Yaowei Huang, Xusheng Hou, et al. "Morphologic Damage of Rat Alveolar Epithelial Type II Cells Induced by Bile Acids Could Be Ameliorated by Farnesoid X Receptor Inhibitor Z-Guggulsterone In Vitro." BioMed Research International 2016 (2016): 1–9. http://dx.doi.org/10.1155/2016/9283204.

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Objective. To determine whether bile acids (BAs) affect respiratory functions through the farnesoid X receptor (FXR) expressed in the lungs and to explore the possible mechanisms of BAs-induced respiratory disorder.Methods. Primary cultured alveolar epithelial type II cells (AECIIs) of rat were treated with different concentrations of chenodeoxycholic acid (CDCA) in the presence or absence of FXR inhibitor Z-guggulsterone (GS). Then, expression of FXR in nuclei of AECIIs was assessed by immunofluorescence microscopy. And ultrastructural changes of the cells were observed under transmission electron microscope and analyzed by Image-Pro Plus software.Results. Morphologic damage of AECIIs was exhibited in high BAs group in vitro, with high-level expression of FXR, while FXR inhibitor GS could attenuate the cytotoxicity of BAs to AECIIs.Conclusions. FXR expression was related to the morphologic damage of AECIIs induced by BAs, thus influencing respiratory functions.

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Ahmad, Md Afroz, Mohd Mujeeb, Mohd Akhtar, Mohd Khushtar, Mohd Arif, and Md Rafiul Haque. "Guggulipid: A Promising Multi-Purpose Herbal Medicinal Agent." Drug Research 70, no. 04 (2020): 123–30. http://dx.doi.org/10.1055/a-1115-4669.

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Herbal medicines therapy is appreciated by many research works because herbal drugs have relatively high therapeutic window, lower side effects and more cost effective. Guggulipid is an ethyl acetate extract of resin known as guggul from the tree Commiphora wightii / mukul (Arn.) Bhandari. Chemical analysis revealed that the compounds responsible for the major activities of gum guggul are the isomers E- and Z-guggulsterone. Guggul has been used for thousands of years in the treatment of arthritis, inflammation, obesity, cardiac protection, anti-ulcer, anti-epileptic and disorders of lipid metabolism. This review is an assortment of available information reported on its chemical, pharmacological and toxicological properties in various research studies. The available therapeutic properties of guggulipid make it suitable natural product for the treatment of various disorders like inflammation, pain, wounds, liver disorder and Acne etc. Graphical Abstract Graphical Abstract.

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Samudio, Ismael, Marina Konopleva, Stephen Safe, and Michael Andreeff. "Guggulsterones Induce Apoptosis and Differentiation in AML: Identification of Isomer-Specific Antileukemic Activities of the Pregnanedienedione Structure." Blood 106, no. 11 (2005): 4466. http://dx.doi.org/10.1182/blood.v106.11.4466.4466.

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Abstract The gum resin from the guggul tree, commiphora mukul, has been used in Ayurvedic medicine for centuries to treat inflammatory and lipid disorders, and an ethylacetate extract of the resin, termed guggulipid, has been reported to have an anti-obesity and antilipidemic effect in clinical trials with no significant toxicity. In this study, we investigate the antileukemic effects of the active components in guggulipid, namely cis- and trans-guggulsterone (cGS and tGS, respectively), and compare their effects to those of the unrelated structural isomer 16-dehyroprogesterone (P). Our results demonstrate that all three compounds inhibited the proliferation of HL60 and U937 cells with IC50 values ranging from 3.6 - 10.9 μM after treatment for 6 days. These growth inhibitory effects correlated with externalization of phosphatidyl serine (PS) and loss of mitochondrial membrane potential (ΔψM) suggesting that these isomeric steroids induce apoptosis in leukemia cells. Z-VAD-fmk prevented PS externalization, but not ΔψM loss indicating that mitochondrial dysfunction occurred in the absence of caspase activation. Interestingly, while all three compounds increased the generation of reactive oxygen species and decreased phosphorylation of ERK, only cGS induced a rapid depletion of reduced glutathione levels and oxidation of the mitochondrial phospholipid cardiolipin. Curiously, the potent antioxidant n-acetylcysteine (NAC) only reversed the cytotoxicity of P suggesting that this structural isomer induces a different cytotoxic response from that of cGS and tGS. P and tGS induced differentiation of HL60 and NB4 cells as evidenced by increased surface expression of CD11b and/or CD14, and all three steroids rapidly induced mitochondrial dysfunction and PS externalization of CD34-positive blasts from primary leukemic samples. This study is the first to demonstrate that guggulsterones and 16-dehydroprogesterone exert antileukemic effects via the induction of apoptosis and differentiation, and more importantly, identifies the pregnadienedione structure as a potential chemotherapeutic scaffold for the development of novel antileukemic agents.

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Mogal, Nitin. "Simultaneous Determination of Diosgenin and Guggulsterone-Z in gokshuradi guggulu tablet by High-Performance Thin-Layer Chromatography." Asian Journal of Biomedical and Pharmaceutical Sciences 05, no. 48 (2015): 32–34. http://dx.doi.org/10.15272/ajbps.v5i48.735.

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Xiao, Dong, and Shivendra V. Singh. "z-Guggulsterone, a constituent of Ayurvedic medicinal plant Commiphora mukul, inhibits angiogenesis in vitro and in vivo." Molecular Cancer Therapeutics 7, no. 1 (2008): 171–80. http://dx.doi.org/10.1158/1535-7163.mct-07-0491.

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Chhonker, Yashpal S., Hardik Chandasana, Veenu Bala, et al. "In-vitro metabolism, CYP profiling and metabolite identification of E- and Z- guggulsterone, a potent hypolipidmic agent." Journal of Pharmaceutical and Biomedical Analysis 160 (October 2018): 202–11. http://dx.doi.org/10.1016/j.jpba.2018.06.047.

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Xu, Hong-Bin, Jing Yu, Lu-Zhong Xu, and Jun Fu. "Regulation of P-glycoprotein efflux activity by Z-guggulsterone of Commiphora mukul at the blood-brain barrier." Journal of the Neurological Sciences 363 (April 2016): 147–52. http://dx.doi.org/10.1016/j.jns.2016.02.046.

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Prajapati, Disha, Madhavi Patel, and Abhay Dharamsi. "Development and Evaluation of a Polyherbal Tablet for Polycystic Ovarian Syndrome (PCOS)." Journal of Natural Remedies 22, no. 2 (2022): 161. http://dx.doi.org/10.18311/jnr/2022/28557.

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The main objective of the present study was to develop and evaluate polyherbal tablet for the treatment of Polycystic Ovarian Syndrome (PCOS). For the formulation of tablet, the herbs were selected based on the concepts of pathophysiology and Ayurvedic perspective of the disease. The extracts of <em>T. foenum graceum, C. longa, B. aristata, S. asoka, B. variegata</em> and Guggul purified in cow’s urine was used for the preparation of polyherbal tablet. The physicochemical, phytochemical evaluation and quantification of markers by HPTLC of crude drugs and extracts were performed. The guggul was used as binder in different proportion for the preparation of tablet. Pre-formulation study of the powder blend and post compression evaluation of tablet was done by various parameters like weight variation, friability, hardness, thickness, diameter, disintegration time, in-vitro dissolution and accelerated stability study. The physicochemical evaluations of crude drugs yielded results which were in accordance with the monograph’s standard values. The phytochemical analysis of the extracts revealed the presence of variety of phytoconstituents. From the results of HPTLC quantification the amount of curcumin (7.14%) in <em>C. longa</em>, diosgenin (40.6%) in <em>T. foenum graceum ,T. foenum graceum</em>, berberine hydrochloride (4.83%) in <em>B. aristata</em>, catechin (3.48%) in S. asoka, lupeol (0.11%) in <em>B. variegata</em> and Z-guggulsterone (0.140%) and E-guggulsterone (0.146%) in purified guggul was found. The micrometrics of the powder blend of all the formulations showed good flow properties. Formulation F3 showed better results compared to other formulations in post compression evaluation. Accelerated stability study showed that the formulation F3 was stable during the course of study.

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Guan, Baoxiang, Ashraful Hoque, and Xiaochun Xu. "Amiloride and guggulsterone suppression of esophageal cancer cell growth in vitro and in nude mouse xenografts." Frontiers in Biology 9, no. 1 (2014): 75–81. http://dx.doi.org/10.1007/s11515-014-1289-z.

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Sairkar, PramodKumar, and Anjana Sharma. "Estimation of guggulsterone E and Z in the guggul-based commercial formulations using high-performance thin-layer chromatography." Journal of Pharmacy And Bioallied Sciences 9, no. 1 (2017): 1. http://dx.doi.org/10.4103/0975-7406.206225.

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Liu, Jing, Ye Lin, Yang Yang, et al. "Z-Guggulsterone attenuates cognitive defects and decreases neuroinflammation in APPswe/PS1dE9 mice through inhibiting the TLR4 signaling pathway." Biochemical Pharmacology 202 (August 2022): 115149. http://dx.doi.org/10.1016/j.bcp.2022.115149.

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Chen, Zhuo, Chao Huang, and Wenbin Ding. "Z-Guggulsterone Improves the Scopolamine-Induced Memory Impairments Through Enhancement of the BDNF Signal in C57BL/6J Mice." Neurochemical Research 41, no. 12 (2016): 3322–32. http://dx.doi.org/10.1007/s11064-016-2064-0.

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Sultana, Nighat, and Sarwat Jahan. "Studies on the Constituents of Commiphora mukul." Zeitschrift für Naturforschung B 60, no. 11 (2005): 1202–6. http://dx.doi.org/10.1515/znb-2005-1114.

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Studies on ommiphora mukul (Hook, ex stock) Engl. have led to the isolation of a new lignan (+)-commiphorin (1), a new fatty acid ester, (+)-commiphotetrol (2) along with (-)- hydroxyisohopane (3) [1], which is the first report of this compound from Commiphora mukul of Pakistan origin, Z and E-guggulsterones, cholesterol and guggulsterol-II (4). Of these complete 1H and 13C NMR data of guggulsterol-II (4) is assigned for the first time [2]. The structures of the compounds were elucidated with the help of extensive spectroscopic studies [3, 4]. Compound 1 have shown antibacterial activity against a number of bacteria. Amoxicillin (H2O)3, Ampicilin and Cefuroxime were used as positive control (Table 2).

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Mayuree, Patel, Macwan Carol, B. N. Suhagia, and Sanjeev R. Acharya. "Qualitative and Quantitative Estimation of Guggulsterone E and Z in Different Sodhit Guggul by LC-MS and HPLC Method." JOURNAL OF NATURAL REMEDIES 17, no. 3 (2017): 1–18. http://dx.doi.org/10.18311/jnr/2017/18928.

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Dang, Sha-Jie, Wen-Bo Wei, Rui-Li Li, Can-Xu Song, and Jin Xu. "Z-Guggulsterone Relieves Neuropathic Pain by Inhibiting the Expression of Astrocytes and Proinflammatory Cytokines in the Spinal Dorsal Horn." Journal of Pain Research Volume 15 (May 2022): 1315–24. http://dx.doi.org/10.2147/jpr.s360126.

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Xu, Hong-Bin, Zhao-Qi Tang, Juan Wang, and Ping-shi Kong. "Z-guggulsterone regulates MDR1 expression mainly through the pregnane X receptor-dependent manner in human brain microvessel endothelial cells." European Journal of Pharmacology 874 (May 2020): 173023. http://dx.doi.org/10.1016/j.ejphar.2020.173023.

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Chander, Ramesh, Farhan Rizvi, A. K. Khanna, and Ram Pratap. "Cardioprotective activity of synthetic guggulsterone (E and Z-isomers) in isoproterenol induced myocardial ischemia in rats: A comparative study." Indian Journal of Clinical Biochemistry 18, no. 2 (2003): 71–79. http://dx.doi.org/10.1007/bf02867370.

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Chang, Shiun, Darwin C. Chang, Rachel V. Jimenez, Rosa A. Sierra-Mondragon, Julio A. Vazquez Martinez, and Paulo C. Rodriguez. "Abstract 6137: Inhibition of FXR signaling in tumor-associated myeloid cells protects against melanoma progression." Cancer Research 85, no. 8_Supplement_1 (2025): 6137. https://doi.org/10.1158/1538-7445.am2025-6137.

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Abstract Our study delves into the complex interplay between the tumor microenvironment and immune cell regulation, with a particular focus on myeloid-derived suppressor cells (MDSCs). A key discovery of our research is the accumulation of bile acids (BAs) within the tumor microenvironment and tumor-infiltrating myeloid cells. BAs significantly enhance the suppressive function of MDSCs and M2 macrophages via activation of Farnesoid X Receptor (FXR).Using melanoma as our primary model. We demonstrate that modulation of MDSCs' suppressive function can be achieved through the targeting FXR using specific agents like GW4064 and z-Guggulsterone (z-GS). Myeloid-specific elimination of FXR via Lysozyme M Cre led to a significant delay in tumor progression. This was accompanied by the reduction of PMN-MDSC and an increased infiltration of CD45 positive immune cells and a surge in the presence of anti-tumor specific T cells. Administration of FXR inhibitor, z-GS, through oral gavage also reduced tumor size in vivo. Additionally, targeting FXR by z-GS or myeloid specific genetic ablation enhances adoptive T cells transfer therapy efficacy. MDSCs with impaired FXR signaling result in reduced mitochondria activity and downregulation of Arg1. Furthermore, an enhanced antigen presentation function is observed in MDSCs and dendritic cells treated with z-GS. Our research presents a compelling case for targeting FXR signaling in myeloid cells as a novel therapeutic strategy and open new pathways for enhancing anti-tumoral immunity. Citation Format: Shiun Chang, Darwin C. Chang, Rachel V. Jimenez, Rosa A. Sierra-Mondragon, Julio A. Vazquez Martinez, Paulo C. Rodriguez. Inhibition of FXR signaling in tumor-associated myeloid cells protects against melanoma progression [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2025; Part 1 (Regular Abstracts); 2025 Apr 25-30; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2025;85(8_Suppl_1):Abstract nr 6137.

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Akhade, MeenakshiS, PoonamA Agrawal, and KS Laddha. "Development and validation of RP-HPLC method for simultaneous estimation of picroside I, plumbagin, and Z-guggulsterone in tablet formulation." Indian Journal of Pharmaceutical Sciences 75, no. 4 (2013): 476. http://dx.doi.org/10.4103/0250-474x.119835.

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Meyer, Udo, Gabriele Costantino, Antonio Macchiarulo, and Roberto Pellicciari. "Is Antagonism ofE/Z-Guggulsterone at the Farnesoid X Receptor Mediated by a Noncanonical Binding Site? A Molecular Modeling Study." Journal of Medicinal Chemistry 48, no. 22 (2005): 6948–55. http://dx.doi.org/10.1021/jm0505056.

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Narasimhaji, Cheemalapati Venkata, Gokul Marimuthu, Ajay K. Meena, et al. "Marker-based HPTLC profiling and HPLC method for estimating Guggulsterone-Z in Commiphora wightii (Arn.) Bhandari resin and polyherbal Ayurveda formulation (PHAF)." Journal of Drug Research in Ayurvedic Sciences 10, no. 1 (2025): 48–55. https://doi.org/10.4103/jdras.jdras_50_24.

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Abstract BACKGROUND: The Indian herbal medicine system Ayurveda has a rich history associated with use of gum Guggulu (Commiphora wightii (Arn.) Bhandari; CM) for its therapeutic properties. In the present study, CM resin and Guggulu-based polyherbal Ayurvedic formulation (PHAF; having Guggulu as one of the major components) were evaluated for the estimation of Guggulsterone-Z (GZ) using high-performance planar and liquid chromatography techniques. METHODS: In HPTLC analysis, the identification of GZ was carried out in the CM and PHAF extract using a silica gel-coated aluminum plate as the stationary phase and toluene: acetone (90:10% v/v) as the mobile phase. The developed HPTLC chromatograms were scanned at 254 nm and 366 nm, whereas the chromatogram after derivatization with the vanillin-sulfuric acid reagent was scanned at 540 nm. The mobile phase used in HPLC analysis included water (with 1% KH2PO4 buffer) and acetonitrile (20:80% v/v). HPLC analysis was performed at a UV wavelength of 245 nm. RESULTS: The chromatograms and respective retention times indicated the presence of GZ in CM and PHAF, and the quantity of GZ within the samples was 0.5020% and 0.2994%, respectively. CONCLUSION: The HPLC and HPTLC fingerprints can be used to identify and quantify GZ. Furthermore, these methods will be beneficial in determining GZ in the polyherbal formulation PHAF as well as detecting adulteration for CM resin.

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