鸦胆子苦醇 TQ0211

Product Introduction
Bioactivity


英文名: Brusatol

描述: Brusatol (NSC-172924) 是一种从鸦胆子植物中分离出来的天然产物，抑制Nrf2通路，可使多种癌细胞对 Cisplatin 和其他化疗药物敏感。它可开发为辅助化疗化合物，可增加细胞凋亡。

细胞实验: CT-26 cells in logarithmic growth are seeded onto a 96-well plate at a density of 4×10^3 cells/well. After 24 h of incubation at 37°C, fresh medium containing a series of concentrations of Brusatol (0.05, 0.15, 0.45, 1.35, 4.05 and 12.15 μg/mL) and CDDP (0.05, 0.15, 0.45, 1.35, 4.05 and 12.15 μg/mL) is added at 100 μL/well; each concentration is used to treat six replicate wells. After 48 h of incubation at 37°C, the cells are further incubated with MTT (10 mg/mL) at 37°C for 4 h. The supernatant is then removed and the precipitate is dissolved with 100 μL DMSO. Absorbance is measured using a microplate reader at a wavelength of 490 nm. Cytotoxicity is expressed as the concentration of Brusatol and CDDP that inhibit cell growth by 50% (IC50 value). The inhibitory rate is calculated. The possible synergistic effect of Brusatol combined with CDDP is investigated by exposing CT-26 cells to various concentrations of each agent alone or in combination for 48 h [2].

动物实验: Athymic nude mice are used. Mice 4-6 wk old are injected with A549 cells. Once the tumors reached 80 mm3 (for the two times five-time Cisplatin treatment regimen) or 280 mm3 (for the single five-time Cisplatin treatment regime), mice are randomly allocated into four groups and treated i.p. with DMSO, Cisplatin (2 mg/kg), Brusatol (2 mg/kg), or in combination every other day for a total of five times. After the initial five-time Cisplatin treatment regimen, treatment stops for 1 wk to allow mice to recover before the second five-time Cisplatin treatment regimen is repeated [3].

体外活性: Brusatol 通过一种不依赖于 Keap1、蛋白酶体和自噬蛋白降解系统的机制，引发 Nrf2 的消耗。在小鼠 Hepa-1c1c7 肝癌细胞中，Brusatol 通过一种转录后机制迅速且短暂地引起 Nrf2 蛋白的消耗。Brusatol 也能抑制新鲜分离的原代人肝细胞中的 Nrf2 [1]。CT-26 细胞分别单独或联合应用不同浓度的 Brusatol（0.05、0.15、0.45、1.35、4.05 和 12.15 μg/mL）和 CDDP（0.05、0.15、0.45、1.35、4.05 和 12.15 μg/mL）处理 48 小时。经 Brusatol 和 CDDP 处理 48 小时后，CT-26 细胞的存活率呈剂量依赖性降低，其 IC50 值分别为 0.27±0.01 和 1.44±0.22 μg/mL。当 Brusatol 与 CDDP 以 1:1 的恒定浓度比联合应用时，细胞生长抑制明显增强，合用治疗的 IC50 值为 0.19±0.02 μg/mL [2]。

体内活性: 裸鼠被注射A549细胞以诱导肿瘤生长，随后进行一次每千克体重2 mg的Brusatol腹腔注射。在注射后24小时或48小时，将肿瘤组织分离出来。发现Nrf2蛋白水平在注射后24小时或48小时显著降低，表明Brusatol能够达到肿瘤组织并抑制Nrf2途径。在第一次实验中，一旦肿瘤体积达到平均230 mm3，将DMSO、Brusatol（每千克体重2 mg）、Cisplatin（每千克体重2 mg）或Cisplatin（每千克体重2 mg）与Brusatol（每千克体重2 mg）联合治疗通过腹腔注射，每隔一天一次，共五次。Cisplatin或Brusatol单独使用未能显著抑制肿瘤生长，而在联合治疗组中，肿瘤体积显著减小[3]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : Insoluble
DMSO : 90 mg/mL (172.9 mM)


关键字: Nrf2 | oxygen | CT-26 | defense | stress | Keap1-Nrf2 | Brusatol | chemosensitization | Toxicity | NSC-172924 | species | radicals | reactive | Chemical | response | cisplatin | synergistic effect | Hepatocyte | Keap1 | antioxidant | Cell | Free | Inhibitor | inhibit | NSC172924 | Apoptosis

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途