| 名称 | Butein |
| 描述 | Butein is a cAMP-specific PDE inhibitor, protein tyrosine kinase inhibitor, and SIRT1 activator. It sensitizes HeLa cells to Cisplatin by targeting FoxO3a via the AKT and ERK/p38 MAPK pathways. |
| 细胞实验 | The cells (5× 103/mL) are incubated in triplicate in a 96-well plate in the presence or absence of indicated concentration of Butein in a final volume of 0.2 mL for different time intervals at 37 ℃. Thereafter, 20 μL MTT solution (5 mg/mL in PBS) is added to each well. After a 2-hour incubation at 37 ℃, 0.1 mL lysis buffer (20% SDS, 50% dimethylformamide) is added, incubation is continued overnight at 37 ℃, and then the optical density at 570 nm is measured by plate reader. (Only for Reference) |
| 体外活性 | 方法：用Butein (2’,3,4,4’-tetrahydroxy Chalcone)（10、20，40 μM）和 Cisplatin（10、20，30 μM）处理HeLa细胞，通过MTT法和相互作用指数评估细胞毒性并检测细胞凋亡，探讨Butein (2’,3,4,4’-tetrahydroxy Chalcone)和Cisplatin联合处理的有效性。
结果：单独使用Butein (2’,3,4,4’-tetrahydroxy Chalcone)和Cisplatin治疗以剂量和时间依赖性方式抑制细胞生长；20 μM的 Butein (2’,3,4,4’-tetrahydroxy Chalcone)和20 μM的Cisplatin联合处理48 h，诱导了显著的协同细胞毒性作用；两种药物的组合物可以显着增强细胞凋亡。[3]
方法：用Butein (2’,3,4,4’-tetrahydroxy Chalcone)（20μM）或 Cisplatin （20 μM）处理HeLa 细胞，Western blot分析检测AKT、ERK和p38磷酸化水平。
结果：Butein (2’,3,4,4’-tetrahydroxy Chalcone)显著抑制Cisplatin诱导的ERK和p38磷酸化，但对JNK表达有明显影响；单独使用Cisplatin或Butein (2’,3,4,4’-tetrahydroxy Chalcone)或联合使用可抑制AKT激活。[3] |
| 体内活性 | 方法：用Butein (2’,3,4,4’-tetrahydroxy Chalcone)（2 mg/kg，每两天，腹膜内注射）或Butein (2’,3,4,4’-tetrahydroxy Chalcone)（2 mg/kg，每两天，腹膜内注射）和Cisplatin（2 mg/kg，每2天，腹膜内注射）处理带有Hela细胞模型的裸鼠治疗3周，每隔一天测定小鼠的体重和临床症状；通过免疫组织化学染色进一步评估Butein (2’,3,4,4’-tetrahydroxy Chalcone)对肿瘤组织中FoxO3a表达水平的影响。
结果：联合治疗（Butein (2’,3,4,4’-tetrahydroxy Chalcone)+顺铂）对肿瘤体积的影响最为显着，而对照组小鼠与单独使用 Cisplatin 或两种药物治疗的小鼠在体重上没有观察到明显差异；Butein (2’,3,4,4’-tetrahydroxy Chalcone治疗的小鼠中FoxO3a的表达均显着增加。[3] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 237.5 mg/mL (872.36 mM), Sonication is recommended.
Ethanol : 51 mg/mL (187.33 mM), Sonication is recommended.
10% DMSO+90% Saline : 2.5 mg/mL (9.18 mM), Sonication is recommeded.
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| 关键字 | SIRT1 | PKB | Phosphodiesterase (PDE) | phosphodiesterase | PDE4 | p60c-src | p38 | MAPK | Inhibitor | inhibit | HER1 | HepG2 | HeLa | FoxO3a | ERK | ErbB-1 | Epidermal growth factor receptor | EGFR | cell | Butein | Autophagy | Apoptosis | AKT |
| 相关产品 | Urea | Naringin | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Metronidazole | Hemin | Hydroxychloroquine | Stavudine | Tamoxifen | Paeonol | D(+)-Raffinose pentahydrate |
| 相关库 | 经典已知活性库 | 激酶抑制剂库 | 药食同源库 | 抗癌天然产物库 | 风味天然产物库 | 中药单体化合物库 | 天然产物库 | 免疫/炎症分子化合物库 | 膜蛋白靶向化合物库 | 中药抗炎分子库 | 酪氨酸激酶分子库 | 天然多酚类化合物库 |