| CAS |
No.88495-63-0 |
| 中文名称 |
青蒿琥酯(10mM in DMSO,无菌） |
| 英文名称 |
Artesunate(10mM in DMSO，Sterile） |
| 分子式 |
C19H28O8 |
| 分子量 |
384.42 |
| 溶解性 |
请根据自己的实验要求使用。 |
| 外观(性状) |
无菌溶液 |
| 储存条件 |
Stroe at -20℃，6 months. |
| 靶点 |
STAT3;exported protein 1 (EXP1) |
| 通路 |
JAK/STAT Signaling |
| 背景说明 |
Artesunate是 STAT-3 和EXP1 的抑制剂。 |
| 生物活性 |
Artesunate is an inhibitor of both STAT-3 and exported protein 1 (EXP1).[1-3] |
| In Vitro |
Artesunate is an inhibitor of both STAT-3[1] and exported protein 1 (EXP1)[2]. Artesunate treatment for 24 h causes a significant increase in the levels of reactive oxygen species (ROS) in a dose-dependent manner in both cell lines. Moreover， Western blotting shows that the levels ofγ-H2AX are significantly elevated when cancer cells are treated with Artesunate in the higher dose range for 24 h. Artesunate also shows a time-dependent effect on the level of RAD51 in A2780 and HO8910 cells. In two types of non-malignant cells， normal human fibroblasts and immortalized epithelial cells， FTE-187， the level of RAD51 is not altered by Artesunate. In A2780 cells， the level of RAD51 mRNA is indeed decreased by the addition of Artesunate， in a dose-dependent manner. Correspondingly， the promoter activity of RAD51 is significantly inhibited by Artesunate. In contrast， the RAD51 mRNA level in H8910 cells is not affected by Artesunate[3]. |
| In Vivo |
Tumor growth is significantly reduced in the group receiving combined treatment of Artesunate and cisplatin (P[3]. |
| 细胞实验 |
A2780 and HO8910 cells are cultured in RPMI 1640， Normal human fibroblasts (NHF) in DMEM， and FTE-187 in M199， supplemented with 10% fetal bovine serum， 100 units/mL penicillin， and 100 mg/mL streptomycin. All the cells are incubated in a humidified atmosphere of 95% air and 5% CO2. Artesunate is applied to the cultured cells at the concentration of 0， 5， 10， 25， or 50 μg/mL for various periods. The reactive oxygen species (ROS) production following Artesunate treatment is determined. Briefly， cells are loaded with 5 μM of CM-H2DCFDA and incubated at 37°C for 20 min after treatment with Artesunate. Cells are resuspended using preserving fluid and analyzed with a FACSCanto II. The peak excitation wavelength for oxidized CM-H2DCFDA is 490 nm and emission is 530 nm[3]. |
| 动物实验 |
Four to six weeks old female athymic nude mice (BALB/c， nu/nu) are used. A2780 and HO8910 cells are harvested and resuspended in 0.1 ml of PBS， 5×106 cells/0.2 mL are injected subcutaneously into the left inguinal area of the mice. Two weeks later， mice bearing tumors (~70 mm3 for A2780 and HO8910) are randomly divided into 4 groups. Artesunate is administered daily via i.p. injection at doses of 50 mg/kg alone for 16 days. The tumor growth is monitored every other day. Tumor volume is determined by the formula 1/2a×b2 where a is the long diameter (mm) and b is the short diameter (mm)[3]. |
| 激酶实验 |
After treatment with Artesunate for 24 h， cells are harvested and lysed in 1×cell lysis buffer. Total proteins of 15 to 25 μg are separated by SDS-PAGE and transferred to polyvinylidenedifluoride (PVDF) membranes. Membranes are blocked with 5% non-fat milk for 1 to 2 h at room temperature and then probed with primary antibodies and incubated at 4°C overnight. After extensive washing with TBS-T， membranes are incubated with appropriate HRP-conjugated secondary antibody for 1 h at room temperature， and then are detected by Western ECL-enhanced luminol reagent [3]. |
| 数据来源文献 |
[1]. Ilamathi M， et al. Artesunate as an Anti-Cancer Agent Targets Stat-3 and Favorably Suppresses Hepatocellular Carcinoma. Curr Top Med Chem. 2016;16(22):2453-63.
[2]. Lisewski AM， et al. Supergenomic network compression and the discovery of EXP1 as a glutathione transferase inhibited by artesunate. Cell. 2014 Aug 14;158(4):916-928.
[3]. Wang B， et al. Artesunate sensitizes ovarian cancer cells to cisplatin by downregulating RAD51. Cancer Biol Ther. 2015;16(10):1548-56. |
| 规格 |
0.1ml 0.3ml 0.5ml 1ml 1.5ml |
| 单位 |
瓶 |
中文
英语
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