绿僵菌素B, 来源于绿僵菌属
| 中文名称 | 绿僵菌素B, 来源于绿僵菌属 |
|---|---|
| 中文同义词 | 绿僵菌素B, 来源于绿僵菌属;绿僵菌素B;黑僵菌素 B;腐败菌素B |
| 英文名称 | destruxin B |
| 英文同义词 | destruxin B;N-[N-[(2R)-1-Oxo-2-hydroxy-4-methylpentyl]-L-Pro-L-Ile-N-methyl-L-Val-N-methyl-L-Ala-]-β-alanine lactone;N-[N-[(R)-2-Hydroxy-4-methyl-1-oxopentyl]-L-Pro-L-Ile-N-methyl-L-Val-N-methyl-L-Ala-]-β-alanine lactone;Destruxin B, 97.5%, from Metarrhizium anisopliae;Destruxin B from Metarhizium anisopliae;Cyclo[N-methyl-L-alanyl-β-alanyl-(2R)-2-hydroxy-4-methylpentanoyl-L-prolyl-L-isoleucyl-N-methyl-L-valyl];Destruxin B, from Metarrhizium anisopliae;Cyclo[N-methyl-L-alanyl-β-alanyl-(2R)-2-hydroxy-4-methylpentanoyl-L-prolyl-L-isoleucyl-N-methyl-L-valyl |
| CAS号 | 2503-26-6 |
| 分子式 | C30H51N5O7 |
| 分子量 | 593.761 |
| EINECS号 | |
| 相关类别 | 医药原料 |
| Mol文件 | 2503-26-6.mol |
| 结构式 |  |
绿僵菌素B, 来源于绿僵菌属 性质
| 熔点 | 234 °C |
|---|---|
| 沸点 | 875.0±65.0 °C(Predicted) |
| 密度 | 1.17±0.1 g/cm3(Predicted) |
| 储存条件 | -20°C |
| 溶解度 | 溶于DMSO（高达10mg/ml） |
| 形态 | 固体 |
| 酸度系数(pKa) | 13.54±0.70(Predicted) |
| 颜色 | 白色 |
| 稳定性 | 可在-20°C下的DMSO溶液保存长达1个月。 |
|
Bcl-2
|
Caspase-3
|
Destruxin B (1-30 μM; 48 hours) inhibits cell proliferation of H1299 cells and A549 cells, with IC
50
s of 4.1 μM and 4.9 μM, respectively.
Activation of mitochondria-dependent caspase cascade plays an important role in Destruxin B (1-30 μM; 48 hours) induced apoptotic cell death in A549 cells.
Destruxin B (1.25-20.00 μM; 72 hours) treatment significantly inhibits HT-29 human colorectal cancer cells viability in time- and dose-dependent manners.
Destruxin B (10 or 20 μM; 12 and 24 hours) treatment markedly increases levels of the proapoptotic protein PUMA and reduces levels of antiapoptotic proteins Mcl-1 of A549 cells in a concentration- and time-dependent manner .
Cell Proliferation Assay
| Cell Line: | H1299 cells |
| Concentration: | 1, 5, 10, 20, 30 μM |
| Incubation Time: | 48 hours |
| Result: | Inhibited H1299 cells proliferation of H1299 cells with an IC 50 of 4.1 μM. |
Apoptosis Analysis
| Cell Line: | Lung adenocarcinoma A549 cells |
| Concentration: | 1, 5, 10, 20, 30 μM |
| Incubation Time: | 48 hours |
| Result: | Induces caspase-dependent Lung adenocarcinoma A549 cells death. |
Cell Viability Assay
| Cell Line: | HT-29 human colorectal cancer cells |
| Concentration: | 1.25, 2.50, 5.00, 10.00 and 20.00 μM |
| Incubation Time: | 72 hours |
| Result: | The IC 50 s at 24 h, 48 h and 72h were determined as 14.97, 2.00 and 0.67 μM, respectively. |
Western Blot Analysis
| Cell Line: | A549 cells |
| Concentration: | 10 or 20 μM |
| Incubation Time: | 12 and 24 hours |
| Result: | Regulates Mcl-1 and PUMA. |
Destruxin B (DB) ( injection; 0.6-15 mg/kg/day for 6 weeks) attenuates the tumor growth in time- and dose-dependent manners.
| Animal Model: | Athymic female nude mice (BALB/cAnN.Cg-Foxn1nu/CrlNarl), approximately 4-5 weeks old on arrival |
| Dosage: | Low dose (0.6 mg/kg), medium dose (3 mg/kg), high dose (15 mg/kg) |
| Administration: | Injection; daily; for 6 weeks |
| Result: | Low dose, medium dose and high dose indicated a reduction of 23.9%, 33.4% and 55.8% in mean tumor size, respectively. |
安全信息
| 海关编码 | 2933790090 |
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