蟾毒它灵|471-95-4|出售|厂家|价格|009生物|灵灵九

英文名：Bufotaline

外观：

纯度：请咨询卖家

分子式：C26H36O6

分子量：444.56

最小起售量：10g/20g/100g/1kg

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;BUFOTALIN SULFATE

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;标准品-对照品;Miscellaneous Natural Products;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

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)

酸度系数(pKa)

14.44±0.70(Predicted)

形态

White to off-white solid.

CAS 数据库

471-95-4

NIST化学物质信息

Bufotalin(471-95-4)

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.

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.

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.

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.

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.

化学性质

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。

用途

橙花叔醇具有抗炎，行咳的作用。