青蒿酯作用机制 - Medchemexpress - MCE中国

1、Product Data SheetArtesunateCat. No.: HY-N0193CAS No.: 88495-63-0分式: CHO分量: 384.42作靶点: STAT; Ferroptosis; Parasite; Virus Protease作通路: JAK/STAT Signaling; Stem Cell/Wnt; Apoptosis; Anti-infection储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 83.33 mg/mL (216.7

2、7 mM; Need ultrasonic)H2O : 0.1 mg/mL (insoluble)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 2.6013 mL 13.0066 mL 26.0132 mL5 mM 0.5203 mL 2.6013 mL 5.2026 mL10 mM 0.2601 mL 1.3007 mL 2.6013 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存

3、时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.41 mM); Clear

4、 solution此案可获得 2.08 mg/mL (5.41 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 20.8 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.41 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.08 mg/mL (

5、5.41 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 20.8 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (5.41 mM); Clear solution此案可获得 2.08 mg/mL (5.41 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 20.8 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOL

6、OGICAL ACTIVITY物活性 ArtesunateSTAT-3 和输出蛋 1 (EXP1) 的抑制剂。IC & Target Stat-3 EXP1体外研究 Artesunate is an inhibitor of both STAT-31 and exported protein 1 (EXP1)2. Artesunate treatment for 24 h causes asignificant increase in the levels of reactive oxygen species (ROS) in a dose-dependent manner in both c

7、ell lines.Moreover, Western blotting shows that the levels of-H2AX are significantly elevated when cancer cells are treatedwith Artesunate in the higher dose range for 24 h. Artesunate also shows a time-dependent effect on the level ofRAD51 in A2780 and HO8910 cells. In two types of non-malignant ce

8、lls, normal human fibroblasts and immortalizedepithelial cells, FTE-187, the level of RAD51 is not altered by Artesunate. In A2780 cells, the level of RAD51 mRNA isindeed decreased by the addition of Artesunate, in a dose-dependent manner. Correspondingly, the promoter activityof RAD51 is significan

9、tly inhibited by Artesunate. In contrast, the RAD51 mRNA level in H8910 cells is not affected byArtesunate3.体内研究 Tumor growth is significantly reduced in the group receiving combined treatment of Artesunate and cisplatin(P0.01). In comparison, Artesunate alone has no significant effect on the growth

10、 of tumor xenografts for both celllines3.PROTOCOLKinase Assay 3 After treatment with Artesunate for 24 h, cells are harvested and lysed in 1cell lysis buffer. Total proteins of 15 to 25g are separated by SDSand transferred to polyvinylidenedifluoride (PVDF) membranes. Membranes areblocked with 5% no

11、n-fat milk for 1 to 2 h at room temperature and then probed with primary antibodies andincubated at 4C 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-enhancedl

12、uminol reagent 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 3 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

13、, and 100 mg/mL streptomycin. All the cells areincubated in a humidified atmosphere of 95% air and 5% CO2. Artesunate is applied to the cultured cells at theconcentration of 0, 5, 10, 25, or 50 g/mL for various periods. The reactive oxygen species (ROS) production followingArtesunate treatment is de

14、termined. Briefly, cells are loaded with 5 M of CM-H2DCFDA and incubated at 37C for 20min 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 nm3.MCE has no

15、t independently confirmed the accuracy of these methods. They are for reference only.Page 2 of 3 www.MedChemEAnimal Four to six weeks old female athymic nude mice (BALB/c, nu/nu) are used. A2780 and HO8910 cells are harvested andAdministration 3 resuspended in 0.1 ml of PBS, 5106 cells/0.2 mL are in

16、jected 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 ismonitored every other day

17、. Tumor volume is determined by the formula 1/2ab2 where a is the long diameter (mm)and b is the short diameter (mm)3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Ilamathi M, et al. Artesunate as an Anti-Cancer Agent Targets Stat-3 and F

18、avorably 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 Aug14;158(4):916-928.3. Wang B, et al. Artesunate sensitizes ovarian cancer cells to cisplatin by downreg