去氧鬼臼脂素
生物活性体外研究体内研究
| 中文名称 | 去氧鬼臼脂素 |
|---|---|
| 中文同义词 | 去氧鬼臼脂素;去氧鬼臼毒素,去氧鬼臼脂素;脱氧鬼臼毒素,脱氧鬼臼脂素;去氧鬼臼毒素标准品;去氧鬼臼毒素对照品;脱氧鬼臼毒素;鬼臼毒素杂质5;(5R,5AR,8AR)-5-(3,4,5-三甲氧基苯基)-5,8,8A,9-四氢呋喃并[3',4':6,7]萘并[2,3-D][1,3]二氧戊环-6(5AH)-酮 |
| 英文名称 | Desoxypodophyllotoxin |
| 英文同义词 | Desoxypodophyllotoxin;anthric;Anthricin/Deoxypodophyllotoxin;4-Deoxypodophyllotoxin;Furo[3',4':6,7]naphtho[2,3-D]-1,3-dioxol-6(5ah)-one, 5,8,8A,9-tetrahydro-5-(3,4,5-trimethoxyphenyl)-,(5R,5ar,8ar)-;Nsc403148;Deoxypodophyllotoxin, deoxypodophyllotoxin;Podophyllotoxin 9-Desoxy Impurity |
| CAS号 | 19186-35-7 |
| 分子式 | C22H22O7 |
| 分子量 | 398.41 |
| EINECS号 | |
| 相关类别 | 对照品;标准品;植物提取物;标准品 -对照药材;木脂素 |
| Mol文件 | 19186-35-7.mol |
| 结构式 | ![]() |
去氧鬼臼脂素 性质
| 储存条件 | Store at 2-8°C |
|---|---|
| 溶解度 | 溶于氯仿、二氯甲烷、乙酸乙酯、DMSO、丙酮等。 |
| 形态 | 粉末 |
| 沸点 | 564.5±50.0 °C(Predicted) |
| 密度 | 1.304±0.06 g/cm3(Predicted) |
| 熔点 | 168 °C |
| 颜色 | 白色至米白色 |
| 稳定性 | 吸湿性 |
去氧鬼臼脂素 用途与合成方法
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. |
化学性质
无色棱柱状结晶(无水乙醇),可溶于甲醇、乙醇、DMSO等有机溶剂,来源于桃儿七Sinopodophyllum hexandrum (Royle) Ying;八角莲Dysosma versipellis (Hance) M. Cheng ex Ying的根茎。
用途
去氧鬼臼毒素具有抗肿瘤活性。



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