Guggulsterone |
| رقم الكتالوجGC17658 |
Guggulsterone هو ستيرول نباتي مشتق من صمغ شجرة Commiphora wightiiيمنع Guggulsterone نمو مجموعة متنوعة من الخلايا السرطانية ويحفز موت الخلايا المبرمج من خلال التنظيم السفلي لمنتجات الجينات المضادة للخلايا (IAP1 و xIAP و Bfl-1 / A1 و Bcl-2 و cFLIP و survivin) ، وتعديل بروتينات دورة الخلية (cyclin D1 و c-Myc) ، تفعيل الكاسبيسات و JNK ، تثبيط AktGuggulsterone ، أحد مضادات مستقبلات farnesoid X (FXR) ، يقلل من تنشيط FXR الناجم عن CDCA مع IC50s من 17 و 15 ميكرومتر لـ Z- و E-Guggulsterone ، على التوالي
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 95975-55-6
Sample solution is provided at 25 µL, 10mM.
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Guggulsterone is a plant sterol extracted from the resin of the plant Commiphora wightii. Guggulsterone can inhibit the growth of a wide variety of tumor cells and induce apoptosis through downregulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP, and survivin), modulation of cell cycle proteins (such as Cyclin D1 and c-Myc), activation of caspases, inhibition of Akt, and activation of JNK[1].
In vitro, Guggulsterone (22.28μM; 8 days) inhibits clone-forming potential of liver cancer cells[2]. Guggulsterone (0, 15, 50 and 75µM; 24h) dose-dependently inhibites SGC-7901 cell proliferation[3].
In vivo, Guggulsterone (5 or 10mg/kg; on days 1, 3, and 5 post-infection; i.p.) decreases mortality in dengue virus (DENV) infected ICR suckling mice[4]. In an in vivo xenograft mouse model, Guggulsterone (20 or 40mg/kg; 14 days; oral administration) significantly reduced tumor growth in a dose-dependent manner[5].
References:
[1] Shishodia S, Azu N, Rosenzweig JA, et al. Guggulsterone for Chemoprevention of Cancer. Curr Pharm Des. 2016;22(3):294-306.
[2] Gupta M, Ghufran SM, Kausar T, et al. Z-Guggulsterone Is a Potential Lead Molecule of Dawa-ul-Kurkum against Hepatocellular Carcinoma. Molecules. 2022 Aug 11;27(16):5104.
[3] Lv R, Zhu M, Chen K, et al. Z-Guggulsterone Induces Apoptosis in Gastric Cancer Cells through the Intrinsic Mitochondria-Dependent Pathway. ScientificWorldJournal. 2021 Jan 4;2021:3152304.
[4] Chen WC, Wei CK, Hossen M, et al. (E)-Guggulsterone Inhibits Dengue Virus Replication by Upregulating Antiviral Interferon Responses through the Induction of Heme Oxygenase-1 Expression. Viruses. 2021 Apr 20;13(4):712.
[5] Wu Y, Zhou T, Qian D, et al. Z-Guggulsterone Induces Cell Cycle Arrest and Apoptosis by Targeting the p53/CCNB1/PLK1 Pathway in Triple-Negative Breast Cancer. ACS Omega. 2023 Jan 3;8(2):2780-2792.
| Cell experiment [1]: | |
Cell lines | Huh7 cells |
Preparation Method | Colony Formation Assay Huh7 cells were seeded into 6-well plates at a density of 800 cells per well and incubated for 24h. After 24h, the cells were treated with 22.28μM Guggulsterone or a vehicle alone. The cells were then incubated for an additional 8 days to allow colonies to form. After incubation, the cells were fixed with 100% methanol at room temperature for 30min, and the plates were air-dried. The colonies were stained with 1% Coomassie blue, washed to remove excess dye, and imaged. The data are presented as percentages of the control group. |
Reaction Conditions | 22.28μM; 8 days |
Applications | Guggulsterone inhibits clone-forming potential of liver cancer cells. |
| Animal experiment [2]: | |
Animal models | Six-day-old ICR suckling mice |
Preparation Method | Six-day-old ICR suckling mice were randomly divided into four groups (five mice per group). Group 1 received 60°C heat-inactivated DENV and saline treatment (iDENV); Group 2 received 2.5 × 10⁵ plaque-forming units (PFU) of DENV and saline treatment (DENV); Group 3 received 2.5 × 10⁵ PFU of DENV and intraperitoneal injection of 5mg/kg Guggulsterone on days 1, 3, and 5 post-infection (DENV + Guggulsterone 5mg/kg); Group 4 received 2.5 × 10⁵ PFU of DENV and 10mg/kg Guggulsterone on days 1, 3, and 5 post-infection (DENV + Guggulsterone 10mg/kg). The body weights and mortality rates of the mice in each group were recorded daily for up to 6 days. To determine the viral titer, six-day-old ICR suckling mice were randomly divided into two groups (five mice per group). Group 1 received 2.5 × 10⁵ PFU of DENV and saline treatment (DENV); Group 2 received 2.5 × 10⁵ PFU of DENV and 10mg/kg Guggulsterone on days 1, 3, and 5 post-infection (DENV + Guggulsterone 10mg/kg). The suckling mice were sacrificed by carbon dioxide euthanasia after 6 days. The brain tissues were collected, weighed, and homogenized in 0.5mL RPMI 1640 medium supplemented with 2% fetal bovine serum, and then centrifuged at 8000rpm for 15min at 4°C. Finally, a plaque assay was performed. |
Dosage form | 5 or 10mg/kg; on days 1, 3, and 5 post-infection; i.p. |
Applications | Guggulsterone decreases mortality in dengue virus (DENV) infected ICR suckling mice. |
References: | |
| Cas No. | 95975-55-6 | SDF | |
| Chemical Name | (8S,9R,10R,13R,14S,E)-17-ethylidene-10,13-dimethyl-7,8,9,10,11,12,13,14,15,17-decahydro-1H-cyclopenta[a]phenanthrene-3,16(2H,6H)-dione | ||
| Canonical SMILES | O=C1C[C@H]([C@@](/C1=C\C)(C)CC2)[C@@H](CC3)[C@@H]2[C@](CC4)(C)C3=CC4=O | ||
| Formula | C21H28O2 | M.Wt | 312.45 |
| الذوبان | DMSO: 62 mg/mL (198.43 mM) | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.2005 mL | 16.0026 mL | 32.0051 mL |
| 5 mM | 640.1 μL | 3.2005 mL | 6.401 mL |
| 10 mM | 320.1 μL | 1.6003 mL | 3.2005 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.50%
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Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)
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