去氧鬼臼脂素

生物活性体外研究体内研究

去氧鬼臼脂素

CAS号:19186-35-7
英文名:Desoxypodophyllotoxin
中文名:去氧鬼臼脂素
CBNumber:CB61267789
分子式:C22H22O7
分子量:398.41
MOL File:19186-35-7.mol

去氧鬼臼脂素化学性质

储存条件 :Store at 2-8°C
溶解度 :Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc.
形态 :Powder
沸点 :564.5±50.0 °C(Predicted)
密度 :1.304±0.06 g/cm3(Predicted)
熔点 :168 °C
颜色 :White to off-white
稳定性 :Hygroscopic

去氧鬼臼脂素性质、用途与生产工艺

生物活性 Deoxypodophyllotoxin (DPT)，鬼臼毒素的衍生物，是一种木酚素，从 Sinopodophullumhexandrum (小檗科)的根茎分离，具有强效抗有丝分裂和抗病毒特性。Deoxypodophyllotoxin 作为靶向微管的药物，不仅抗有丝分裂剂而且作为有效的血管生成抑制剂，在肿瘤学中具有重大影响。Deoxypodophyllotoxin 诱导细胞自噬 (autophagy) 和细胞凋亡 (apoptosis)。 Deoxypodophyllotoxin 引起 DRG 神经元细胞内 Ca2+ 浓度增加。

体外研究

Deoxypodophyllotoxin (25-75 nM; 6-48 hours) increases the percentage of early apoptotic cell population from 2.05 to 5.62 and 18.49% for 24 h and 48 h, respectively. Deoxypodophyllotoxin (25-75 nM; 6-48 hours) treats SGC-7901 cells arrested in G2/M phase in time- and dose- dependent manners. Deoxypodophyllotoxin (25-75 nM; 6-48 hours) results in a remarkably time- and dose-dependent decrease in Cdc2 and Cdc25C expression levels and increases cyclin B1 within 6h, decreases PARP, Bcl-2 and caspase-3 activity.

Apoptosis Analysis

Cell Line:	SGC-7901 cells
Concentration:	25, 50, 75 nM
Incubation Time:	6, 12, 24, 48 hours
Result:	Induced apoptosis in SGC-7901 Cells.

Cell Cycle Analysis

Cell Line:	SGC-7901 cells
Concentration:	25, 50, 75 nM
Incubation Time:	6, 12, 24, 48 hours
Result:	Induced G2/M cell cycle arrest in SGC-7901 Cells

Western Blot Analysis

Cell Line:	SGC-7901 cells
Concentration:	25, 50, 75 nM
Incubation Time:	6, 12, 24, 48 hours
Result:	Altered the expression of cyclin B1, Cdc2,Cdc25C, p-PARP, Bcl-2 and p-caspase-3 proteins.

体内研究

Deoxypodophyllotoxin (intravenously injected; 5, 10, and 20 mg/kg; 3 times a week; 28 days) suppresses the tumors in a dose-dependent manner, the growth of tumors is inhibited by 22.19%, 47.91% and 50.93% with DPT at 5, 10 and 20 mg/kg, respectively.

Animal Model:	Xenograft model of gastric cancer in nude mice with SGC-7901 cells
Dosage:	5, 10, and 20 mg/kg
Administration:	Intravenously injected; 5, 10, and 20 mg/kg; 3 times a week; 28 days
Result:	Inhibited the growth of gastric cancer tumors.