Guggulsterone
(Synonyms: 香胶甾酮; Z/E-Guggulsterone) 目录号 : GC17658
Guggulsterone是一种从植物Commiphora wightii的树脂中提取的植物甾醇。Guggulsterone可以抑制多种肿瘤细胞的生长，并通过下调抗凋亡基因产物（IAP1、xIAP、Bfl-1/A1、Bcl-2、cFLIP和survivin）、调节细胞周期蛋白（如Cyclin D1和c-Myc）、激活半胱氨酸蛋白酶、抑制Akt以及激活JNK来诱导细胞凋亡。
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.
Guggulsterone是一种从植物Commiphora wightii的树脂中提取的植物甾醇。Guggulsterone可以抑制多种肿瘤细胞的生长，并通过下调抗凋亡基因产物（IAP1、xIAP、Bfl-1/A1、Bcl-2、cFLIP和survivin）、调节细胞周期蛋白（如Cyclin D1和c-Myc）、激活半胱氨酸蛋白酶、抑制Akt以及激活JNK来诱导细胞凋亡[1]。
在体外实验中，Guggulsterone（22.28μM; 8天）抑制肝癌细胞的克隆形成能力[2]。Guggulsterone（0, 15, 50和75µM; 24小时）剂量依赖性地抑制SGC-7901细胞增殖[3]。
在体内实验中，Guggulsterone（5或10mg/kg; 感染后第1, 3和5天; 腹腔注射）降低了感染登革热病毒（DENV）的ICR乳鼠的死亡率[4]。在体内异种移植小鼠模型中，Guggulsterone（20或40mg/kg；14天；口服）以剂量依赖性方式显著减少了肿瘤生长[5]。
| 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 | |
| 别名 | 香胶甾酮; Z/E-Guggulsterone | ||
| 化学名 | (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 | ||
| 分子式 | C21H28O2 | 分子量 | 312.45 |
| 溶解度 | DMSO: 62 mg/mL (198.43 mM) | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50%
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