| 生物活性： |
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.
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| 基本信息： |
CAS：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
规格：1ml ; 1.5ml ; 0.5ml ; 0.3ml ; 0.1ml
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.
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| 靶点： |
STAT3;exported protein 1 (EXP1) |
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