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Parthenolide ((-)-Parthenolide) 属于天然倍半萜内酯,是一种 NF-κB 抑制剂,也可特异性抑制 HDAC1 蛋白,对其他 I/II 类 HDAC 无活性。Parthenolide 具有抗炎、抗肿瘤、抗病毒等活性。
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Parthenolide ((-)-Parthenolide) 属于天然倍半萜内酯,是一种 NF-κB 抑制剂,也可特异性抑制 HDAC1 蛋白,对其他 I/II 类 HDAC 无活性。Parthenolide 具有抗炎、抗肿瘤、抗病毒等活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
25 mg | ¥ 298 | 现货 | |
50 mg | ¥ 418 | 现货 | |
100 mg | ¥ 587 | 现货 | |
200 mg | ¥ 925 | 现货 | |
500 mg | ¥ 1,569 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 270 | 现货 |
产品描述 | Parthenolide ((-)-Parthenolide) is a natural sesquiterpene lactone that is an NF-κB inhibitor and also specifically inhibits HDAC1 protein, but is inactive against other class I/II HDACs. Parthenolide has anti-inflammatory, anti-tumor, and anti-viral activities. |
体外活性 | 方法: 人乳腺癌细胞 MDA-MB231 用 Parthenolide (4-100 µM) 处理 4-24 h,通过 MTT assay 检测细胞活力。 结果: Parthenolide 以剂量和时间依赖的方式抑制了 MDA-MB231 细胞的存活率。在 25 µM Parthenolide 处理 16 h 后,细胞存活率降低了 64%。[1] 方法: 人膀胱癌 5637 细胞用 Parthenolide (2.5-10 µM) 处理 48 h,再用 H2O2 (20 mM) 处理 20 min,通过 Hoechst 33342 核染色检测细胞凋亡。 结果: 高浓度的 Parthenolide 处理导致显着的染色质凝缩或断裂,这与凋亡的发生有关。通过计算染色质浓缩的细胞比例来计算凋亡程度,表明用 PTL 处理 5637 细胞会导致剂量依赖性的凋亡诱导。[2] |
体内活性 | 方法: 为研究对代谢功能障碍相关脂肪肝 (MAFLD) 的作用,用 Parthenolide (2-6 mg/kg) 腹腔注射给 MAFLD 模型小鼠,每周三次,持续八周。 结果: Parthenolide 对患有 MAFLD 的小鼠的肝损伤、脂质代谢、纤维化、炎症和氧化应激产生了有益影响,这是由 HIPPO 途径的激活介导的。[3] |
细胞实验 | Parthenolide (PTL) is dissolved in DMSO and diluted with appropriate media[2]. Cells are seeded in 96-well plates and treated on the second day with the given concentration of Parthenolide (0, 5, 10, 20 μM) for another 48 hours and then subjected to SRB or MTT assay. For SRB assay, live cell number is estimated as described earlier. After treatment, the medium is discarded firstly. In order to fix the adherent cells, 100 μL of cold trichloroacetic acid (10% (w/v)) are adding to each well and incubating at 4°C for at least 1 hour. The plates are then washed five times with deionized water and dried in the air. Each well are then added with 50 μL of SRB solution (0.4% w/v in 1% acetic acid) and incubated for 5 min at room temperature. The plates are washed five times with 1% acetic acid to remove unbound SRB and then air dried. The residual bound SRB is solubilized with 100 μL of 10 mM Tris base buffer (pH 10.5), and then read using a microtiter plate reader at 495 nm. The MTT assay is executed. 20 μL MTT (5 mg/mL) are added to each sample and incubate at 37°C for 4 h, then 100 μL solubilization solution are added. Cell viability is determined at 595 nm[2]. |
别名 | 小白菊内酯, (-)-Parthenolide |
分子量 | 248.32 |
分子式 | C15H20O3 |
CAS No. | 20554-84-1 |
Smiles | C\C1=C/CC[C@@]2(C)O[C@H]2[C@H]2OC(=O)C(=C)[C@@H]2CC1 |
密度 | 1.13 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
溶解度信息 | DMSO: 55 mg/mL (221.49 mM) 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4.9 mg/mL (19.73 mM), In vivo: Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. Ethanol: 50 mg/mL (201.35 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||
Ethanol/DMSO
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中药材名称 | 中药材拉丁名 | 性 | 味 | 归经 |
---|---|---|---|---|
长叶天名精 | Carpesium longifolium Chen et C. M. Hu | |||
黄缅桂 | Michelia champaca L. | 凉 | 苦 | |
雷公藤 | Tripterygium wilfordii Hook. f. | 凉 | 辛, 苦 | 心, 肝 |
云南含笑 | Michelia yunnanensis Franch. ex Finet et Gagnep. | |||
皱叶木兰 | Magnolia praecocissima Koidz. |
中成药名称 | 处方组成 | 中成药类型 |
---|---|---|
雷公藤片 | 雷公藤 | 清热药 |
金关片 | 雷公藤,续断,山药,细辛,制附子,茯苓,桑枝,桂枝,鹿角霜,秦艽,丹参,枸杞子,牛膝,鸡血藤,黄精,淫羊藿,薏苡仁,黄芪 | 扶正药 |
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