蟾毒它灵
| 中文名称 | 蟾毒它灵 |
|---|---|
| 中文同义词 | 蟾毒它灵;Γ-日蟾毒配质;蟾蜍皂素;蟾毒他灵;蟾蜍他灵;蟾蜍皂素,蟾蜍他灵,蟾毒他灵;蟾毒它灵(蟾蜍皂素,蟾蜍他灵,蟾毒他灵);蟾毒它灵, 蟾蜍他灵 |
| 英文名称 | Bufotaline |
| 英文同义词 | 3-BETA-14,16-BETA-TRIHYDROXY-5BETA-BUFA-20,22-DIENOLIDE SULFATE;16-(Acetyloxy)-3,14-dihydroxybufa-20,22-dienolide;22-dienolide,3-beta,14,16-beta-trihydroxy-5-beta-bufa-216-acetate;5beta-Bufa-20,22-dienolide, 3beta,14,16beta-trihydroxy-, 16-acetate;Bufa-20,22-dienolide, 16-(acetyloxy)-3,14-dihydroxy-, (3beta,5beta,16beta)-;Bufotaline;BUFOTALIN SULFATE;GAMMA-BUFOTALIN |
| CAS号 | 471-95-4 |
| 分子式 | C26H36O6 |
| 分子量 | 444.56 |
| EINECS号 | |
| 相关类别 | 中药对照品;标准品;植物提取物;中草药成分;对照品;Miscellaneous Natural Products;标准品-对照品;标准品 -中药标准品;其它萜类;分析试剂-对照品;20版药典新增;标准品，对照品 |
| Mol文件 | 471-95-4.mol |
| 结构式 |  |
蟾毒它灵 性质
| 熔点 | 223°C (rough estimate) |
|---|---|
| 沸点 | 474.53°C (rough estimate) |
| 比旋光度 | D20 +5.4° (c = 0.5 in chloroform) |
| 密度 | 1.0942 (rough estimate) |
| 折射率 | 1.4593 (estimate) |
| 储存条件 | Store at -20°C |
| 溶解度 | DMF：30mg/mL； DMSO：30mg/mL；乙醇：30mg/mL |
| 形态 | 白色至类白色固体。 |
| 酸度系数(pKa) | 14.44±0.70(Predicted) |
| CAS 数据库 | 471-95-4 |
| NIST化学物质信息 | Bufotalin(471-95-4) |
Bufotalin (0.1-2.5 μM; 12-96 hours) treatment dose- and time-dependently inhibits MG-63 osteoblastoma cell survival.
Bufotalin (0.5-2.5 μM; 48 hours) treatment dose-dependently increases the percentage of Annexin V positive cells (apoptotic cells) and caspase-12 activity in MG-63 cells. Bufotalin-induced osteoblastoma cell apoptosis is associated with caspase-12 activation.
Bufotalin (0.5-2.5 μM; 12 hours) treatment dose-dependently induces C/EBP homologous protein (CHOP) expression as well as PERK and IRE1 phosphorylation in MG-63 cells. Bufotalin induces endoplasmic reticulum (ER) stress activation in cells.
Bufotalin treatment induces cell cycle arrest at G2/M phase through down-regulation of Aurora A, CDC25, CDK1, cyclin A and cyclin B1, as well as up-regulation of p53 and p21 in HepG2 cells. Bufotalin treatment also induces apoptosis which was accompanied by decrease in mitochondrial membrane potential, increases in intracellular calcium level and reactive oxygen species production, activations of caspase-9 and -3, cleavage of poly ADP-ribose polymerase (PARP) as well as changes in the expressions of bcl-2 and bax.
Cell Viability Assay
| Cell Line: | MG-63 osteoblastoma cells |
| Concentration: | 0.1 μM, 0.5 μM, 1 μM, 2.5 μM |
| Incubation Time: | 12 hours, 24 hours, 48 hours, 72 hours, 96 hours |
| Result: | Inhibited MG-63 osteoblastoma cell survival. |
Apoptosis Analysis
| Cell Line: | MG-63 cells |
| Concentration: | 0.5 μM, 1 μM, 2.5 μM |
| Incubation Time: | 48 hours |
| Result: | Dose-dependently increased the percentage of Annexin V positive cells (apoptotic cells) and caspase-12 activity in MG-63 cells. |
Western Blot Analysis
| Cell Line: | MG-63 cells |
| Concentration: | 0.5 μM, 1 μM, 2.5 μM |
| Incubation Time: | 12 hours |
| Result: | Dose-dependently induced CHOP expression as well as PERK and IRE1 phosphorylation in MG-63 cells. |
Bufotalin (0.5-1 mg/kg; intraperitoneal injection; twice daily; for 7 days) treatment shows a significantly reduced tumor growth in mice.
| Animal Model: | SCID male mice (4-6 weeks old) injected with U2OS cells |
| Dosage: | 0.5 mg/kg, 1 mg/kg |
| Administration: | Intraperitoneal injection; twice daily; for 7 days |
| Result: | Inhibited U2OS osteoblastoma cell growth in mice. |
安全信息
| 危险品运输编号 | 3172 |
|---|---|
| 危险等级 | 6.1(a) |
| 包装类别 | II |
| 海关编码 | 29329990 |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-N0878 | Bufotalin | 1 mg | 411元 | |
| 2024/01/25 | HY-N0878 | 蟾毒它灵 Bufotalin | 471-95-4 | 5mg | 900元 |