Demethylzeylasteral
(Synonyms: 去甲泽拉木醛) 目录号 : GC38160
Demethylzeylasteral是从传统中药雷公藤中提取的三萜类化合物。
Cas No.:107316-88-1
Sample solution is provided at 25 µL, 10mM.
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Demethylzeylasteral is a triterpenoid compound derived from the traditional Chinese medicine Tripterygium wilfordii [1]. Demethylzeylasteral can inhibit T cell activation, inflammatory factor release, NF-κB and JAK/STAT signaling pathways, and induce tumor cell apoptosis and cell cycle arrest [2-3]. Demethylzeylasteral has significant immunosuppressive, anti-inflammatory and anti-tumor biological activities [4].
In MV3 and A375 cells, Demethylzeylasteral (1μM, 5μM, 10μM, 20μM; 48h) inhibits cell proliferation in melanoma cells [5]. In SW480 cells, Demethylzeylasteral (1μM, 5μM, 10μM, 20μM; 24h, 48h, 72h, 96h) inhibited the colorectal cell malignancy [6]. In MKN-45 cells, Demethylzeylasteral (50nM, 100nM, 500nM, 1µM, 5µM, 10µM, 30µM, 50µM, 100µM; 24h) has cytotoxic effects on human gastric cancer cells [7].
In DSS-induced colitis model, Demethylzeylasteral (5mg/kg, 10mg/kg, 20mg/kg; ip; 9d) exhibited a robust anti-inflammatory activity in vitro [8]. In MRL/lpr mice, treated with Demethylzeylasteral (0.6mg/10g, 1.2mg/10g; ig; 9d) showed a significant improvement in 24h proteinuria and the levels of anti-dsDNA antibody in serum [9]. In the rat kidney transplant model, treated with Demethylzeylasteral (10mg/kg, 20mg/kg; ip; 14d)significantly prolonged the survival of kidney-transplanted rats [10].
References:
[1]. Sun X, Shen B, Yu H, et al. Therapeutic potential of demethylzeylasteral, a triterpenoid of the genus Tripterygium wilfordii. Fitoterapia. 2022 Nov 1; 163: 105333.
[2]. Lv L, Zhou F, Quan Y, et al. Demethylzeylasteral exerts potent efficacy against non-small-cell lung cancer via the P53 signaling pathway. Translational Oncology. 2024 Aug 1; 46: 101989.
[3]. Pan L, Feng F, Wu J, et al. Demethylzeylasteral targets lactate by inhibiting histone lactylation to suppress the tumorigenicity of liver cancer stem cells. Pharmacological research. 2022 Jul 1; 181: 106270.
[4]. Li W, Han F, Tang K, et al. Inhibiting NF-κB-S100A11 signaling and targeting S100A11 for anticancer effects of demethylzeylasteral in human colon cancer. Biomedicine & Pharmacotherapy. 2023 Dec 1; 168: 115725.
[5]. Zhao Y, He J, Li J, et al. Demethylzeylasteral inhibits cell proliferation and induces apoptosis through suppressing MCL1 in melanoma cells. Cell death & disease. 2017 Oct; 8(10): e3133.
[6]. Yang Y, Han J, Ma Y, et al. Demethylzeylasteral inhibits cell proliferation and enhances cell chemosensitivity to 5-fluorouracil in Colorectal Cancer cells. Journal of Cancer. 2020 Aug 19; 11(20): 6059.
[7]. Yang Y, Zhao M, Hu T, et al. Identification of an antitumor effect of demethylzeylasteral on human gastric cancer cells. Oncology Letters. 2021 Jan; 21(1): 49.
[8]. Wen T, Liu T, Chen H, et al. Demethylzeylasteral alleviates inflammation and colitis via dual suppression of NF-κB and STAT3/5 by targeting IKKα/β and JAK2. International Immunopharmacology. 2024 Dec 5; 142: 113260.
[9]. Hu Q, Yang C, Wang Q, et al. Demethylzeylasteral (T-96) treatment ameliorates mice lupus nephritis accompanied by inhibiting activation of NF-κB pathway. PloS one. 2015 Jul 24; 10(7): e0133724.
[10]. Xu W, Lin Z, Yang C, et al. Immunosuppressive effects of demethylzeylasteral in a rat kidney transplantation model. International immunopharmacology. 2009 Jul 1; 9(7-8): 996-1001.
Demethylzeylasteral是从传统中药雷公藤中提取的三萜类化合物 [1]。Demethylzeylasteral能够抑制T细胞活化、炎症因子释放、NF-κB和JAK/STAT信号通路，并诱导肿瘤细胞凋亡和细胞周期阻滞 [2-3]。Demethylzeylasteral具有显著的免疫抑制、抗炎和抗肿瘤生物活性 [4]。
在MV3和A375细胞中，Demethylzeylasteral（1μM、5μM、10μM、20μM；48h）可抑制黑色素瘤细胞的增殖 [5]。在SW480细胞中，Demethylzeylasteral（1μM、5μM、10μM、20μM；24h、48h、72h、96h）可抑制结肠直肠细胞恶性肿瘤 [6]。在MKN-45细胞中，Demethylzeylasteral（50nM、100nM、500nM、1µM、5µM、10µM、30µM、50µM、100µM；24h）对人胃癌细胞具有细胞毒作用 [7]。
在DSS诱发的结肠炎模型中，Demethylzeylasteral（5mg/kg、10mg/kg、20mg/kg；ip；9d）表现出强大的体外抗炎活性 [8]。在MRL/lpr小鼠中，Demethylzeylasteral（0.6mg/10g、1.2mg/10g；ig；9d）治疗后，24小时蛋白尿和血清抗双链DNA抗体水平显著改善 [9]。在大鼠肾移植模型中，用Demethylzeylasteral（10mg/kg，20mg/kg；ip；14d）治疗可显著延长肾移植大鼠的存活期 [10]。
| Cell experiment [1]: | |
Cell lines | MV3 and A375 cells |
Preparation Method | Demethylzeylasteral was dissolved in DMSO as 40mM stock solution. Demethylzeylasteral was then used to treat melanoma cell lines, MV3 and A375 with different concentration (1μM, 5μM, 10μM, 20μM), DMSO was used as control. |
Reaction Conditions | 1μM, 5μM, 10μM, 20μM; 48h |
Applications | Demethylzeylasteral inhibits cell proliferation in melanoma cells. |
| Animal experiment [2]: | |
Animal models | DSS-induced colitis model |
Preparation Method | Based on body weight, mice were randomly divided into six groups, including control group, DSS group, DSS + SASP (Sulfasalazine, 50mg/kg, positive control) group, DSS + Demethylzeylasteral (5mg/kg, low dose) group, DSS + Demethylzeylasteral (10mg/kg, middle dose) group, DSS + Demethylzeylasteral (20mg/kg, high dose) group. Mice were injected intraperitoneally with Demethylzeylasteral, SASP, or vehicle (5% DMSO, 30% PEG400, and 65% normal saline) for 9 days. Then, mice were orally administered with 4% DSS solution to induce colitis at the 2th to 9th day of drug administration. During the experiment, loose and bloody stools as well as body weight of mice were daily recorded. |
Dosage form | 5mg/kg, 10mg/kg, 20mg/kg; ip; 9d |
Applications | Demethylzeylasteral exhibited a robust anti-inflammatory activity in vitro. |
References: | |
| Cas No. | 107316-88-1 | SDF | |
| 别名 | 去甲泽拉木醛 | ||
| Canonical SMILES | C[C@](C1=CC2=O)(CC[C@]3(C)[C@@]4([H])C[C@@](C(O)=O)(C)CC3)[C@]4(CC[C@]1(C5=C2C(C=O)=C(O)C(O)=C5)C)C | ||
| 分子式 | C29H36O6 | 分子量 | 480.59 |
| 溶解度 | DMSO: 250 mg/mL (520.19 mM) | 储存条件 | Store at 2-8°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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0808 mL | 10.4039 mL | 20.8078 mL |
| 5 mM | 0.4162 mL | 2.0808 mL | 4.1616 mL |
| 10 mM | 0.2081 mL | 1.0404 mL | 2.0808 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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