蟾毒它灵

产品描述生物活性体外研究体内研究蟾毒它灵试剂级价格

蟾毒它灵

CAS号:471-95-4
英文名:Bufotaline
中文名:蟾毒它灵
CBNumber:CB0313399
分子式:C26H36O6
分子量:444.56
MOL File:471-95-4.mol

蟾毒它灵化学性质

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: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 30 mg/ml
形态 :White to off-white solid.
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)

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

蟾毒它灵性质、用途与生产工艺

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.