Deoxypodophyllotoxin (DPT),鬼臼毒素的衍生物,是一种木酚素,从Anthriscus sylvestris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。
生物活性 | Deoxypodophyllotoxin (DPT), a derivative of podophyllotoxin, is a lignan with potent antimitotic, anti-inflammatory and antiviral properties isolated fromAnthriscus sylvestris. Deoxypodophyllotoxin, targets themicrotubule, has a major impact in oncology not only as anti-mitotics but also as potent inhibitors of angiogenesis[1]. Deoxypodophyllotoxin induces cellautophagyandapoptosis[2]. Deoxypodophyllotoxin evokes increase of intracellular Ca2+concentrations in DRG neurons[3]. |
体外研究 (In Vitro) | 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[1]. Deoxypodophyllotoxin (25-75 nM; 6-48 hours) treats SGC-7901 cells arrested in G2/M phase in time- and dose- dependent manners[1]. 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[1].
Apoptosis Analysis[1] 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[1] 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[1] 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. |
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体内研究 (In Vivo) | 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[1].
Animal Model: | Xenograft model of gastric cancer in nude mice with SGC-7901 cells[1] | 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. |
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来源 | - Plants
- Umbelliferae
- Anthriscus sylvestris
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(251.00 mM;Need ultrasonic) 配制储备液 1 mM | 2.5100 mL | 12.5499 mL | 25.0998 mL | 5 mM | 0.5020 mL | 2.5100 mL | 5.0200 mL | 10 mM | 0.2510 mL | 1.2550 mL | 2.5100 mL |
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此方案可获得 ≥ 2.5 mg/mL (6.27 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (6.27 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.27 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (6.27 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.27 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。
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