青蒿酯作用機制 - Medchemexpress - MCE中國

1、Product Data SheetArtesunateCat. No.: HY-N0193CAS No.: 88495-63-0分式: CHO分量: 384.42作靶點: STAT; Ferroptosis; Parasite; Virus Protease作通路: JAK/STAT Signaling; Stem Cell/Wnt; Apoptosis; Anti-infection儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 83.33 mg/mL (216.7

2、7 mM; Need ultrasonic)H2O : 0.1 mg/mL (insoluble)SolventMass1 mg 5 mg 10 mgConcentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存

3、時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.41 mM); Clear

4、 solution此案可獲得 2.08 mg/mL (5.41 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 20.8 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.41 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.08 mg/mL (

5、5.41 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 20.8 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (5.41 mM); Clear solution此案可獲得 2.08 mg/mL (5.41 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 20.8 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOL

6、OGICAL ACTIVITY物活性 ArtesunateSTAT-3 和輸出蛋 1 (EXP1) 的抑制劑。IC & Target Stat-3 EXP1體外研究 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.體內(nèi)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