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471-95-4

中文名称 蟾毒它灵
英文名称 Bufotaline
CAS 471-95-4
分子式 C26H36O6
分子量 444.56
MOL 文件 471-95-4.mol
更新日期 2024/05/13 10:59:08
471-95-4 结构式 471-95-4 结构式

基本信息

中文别名
蟾毒它灵
蟾蜍他灵
蟾毒他灵
蟾蜍皂素
蟾毒它灵对照品
Γ-日蟾毒配质
蟾毒它灵(标准品)
蟾毒它灵, 蟾蜍他灵
蟾蜍皂素,蟾蜍他灵,蟾毒他灵
蟾蜍皂素、蟾蜍他灵、蟾毒他灵、日蟾毒配质
英文别名
BUFOTALIN
Bufotaline
BUFOTALIN(SH)
Bufotalin std.
GAMMA-BUFOTALIN
Bufotaline ,98%
BUFOTALIN SULFATE
Bufotalin Standard
Bufotaline cas no. 471-95-4
16-(Acetyloxy)-3,14-dihydroxybufa-20,22-dienolide
所属类别
化学试剂:其他酯类化合物

物理化学性质

外观性状无色液体,可溶于甲醇、乙醇、DMSO等有机溶剂,来源于石菖蒲,蔷薇科植物枇杷叶。
熔点223°C (rough estimate)
比旋光度D20 +5.4° (c = 0.5 in chloroform)
沸点474.53°C (rough estimate)
密度1.0942 (rough estimate)
折射率1.4593 (estimate)
储存条件-20°C储存
溶解度DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 30 mg/ml
酸度系数(pKa)14.44±0.70(Predicted)
形态白色至类白色固体
CAS 数据库471-95-4
NIST化学物质信息Bufotalin(471-95-4)

应用领域

用途1
橙花叔醇具有抗炎,行咳的作用。

安全数据

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

常见问题列表

产品描述
蟾毒它灵是蟾酥中的主要化合物之一。众多的研究发现蟾毒它灵具有良好的抗肿瘤活性,具有很大的药物应用开发前景。目前含有蟾毒它灵的口服液、片剂已应用于临床,对肝癌、肺癌、胃癌等具有较好的疗效。
生物活性
Bufotalin 是一种从 Venenum Bufonis 分离的类固醇内酯,具有强大的抗肿瘤活性。Bufotalin 诱导癌细胞凋亡 (apoptosis),也诱导内质网应激激活。
体外研究

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.
体内研究

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.
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