大黃素作用機制 - Medchemexpress - MCE中國

1、Product Data SheetEmodinCat. No.: HY-14393CAS No.: 518-82-1分式: CHO分量: 270.24作靶點: Casein Kinase; SARS-CoV; Autophagy作通路: Cell Cycle/DNA Damage; Stem Cell/Wnt; Anti-infection; Autophagy儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 9.4 mg/mL (34.78 mM; Need ultr

2、asonic and warming)H2O : 0.1 mg/mL (insoluble)SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 3.7004 mL 18.5021 mL 37.0041 mL5 mM 0.7401 mL 3.7004 mL 7.4008 mL10 mM 0.3700 mL 1.8502 mL 3.7004 mL請根據產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，避免反復凍融造成的產品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請

3、在 6 個內使，-20C 儲存時，請在 1 個內使。體內實驗請根據您的實驗動物和給藥式選擇適當的溶解案。以下溶解案都請先按照 In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結果的可靠性，澄 的儲備液可以根據儲存條件，適當保存；體內實驗的作液，建議您現現配，當天使； 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沉淀、析出現象，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 90% (20% SBE-CD in saline)Solubility: 1.25 mg/mL (4.63 mM); Suspended solut

4、ion; Need ultrasonic此案可獲得 1.25 mg/mL (4.63 mM) 的均勻懸濁液，懸濁液可于服和腹腔注射。以 1 mL 作液為例，取 100 L 12.5 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。2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 1.25 mg/mL (4.63 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 1.25 mg/mL (4.63 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個

5、以上的實驗。以 1 mL 作液為例，取 100 L 12.5 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Emodin (Frangula emodin) 冠狀病毒 (SARS-CoV)2。種譜抗癌劑。Emodin 抑制蛋激酶 CKII 活性，IC50 為 2 M1。Emodin 抑制 SARSIC & Target CKII2 M (IC50)體外研究 Emodin, an anthraquinone derivative, selectively inhibits casein kinase II(CKII), a Se

6、r/Thr kinase, as a competitiveinhibitor. Emodin inhibits CKII activity with IC50 of 2 M, which is two to three orders of magnitude lower than thoseagainst the other kinases. Enzyme kinetic assays show that Emodin inhibits CKII activity as acompetitive inhibitoragainst ATP with Ki of 7.2 M1. Emodin i

7、s a broad-spectrum inhibitory agent of cancer cells, including leukemia, lungcancer, human tongue squamous cancer, colon cancer, gallbladder cancer, pancreatic cancer, breast cancer, humancervical cancer and hepatic carcinoma cells. Emodin inhibits A549, HepG2, OVCAR-3, HeLa and Madin-Darby CanineKi

8、dney (MDCK) cells with IC50 of 19.54, 12.79, 25.82, 12.14 and 5.81 g/mL. The anticancer mechanisms of Emodin areinvolved in many biological pathways, such as casein kinase II and ERK1/23. Emodin is applied as a Reactive oxygenspecies (ROS) generator in combination with cisplatin in T24 and J82 human

9、 bladder cancer cells. Emodin kills T24and J82 cells in the dose-dependent and time-dependent manner, and it is less toxic to HCV-29 cells. Theconcentration of 20 and 15 M is selected as appropriate doses for investigating chemotherapeutic sensitivity of T24and J82 cells at 24 h, respectively4.體內研究

10、Mice treated with Emodin (50 mg/kg) and Cisplatin (1 mg/kg) have significantly smaller tumors than those from theother groups. In addition, no notable differences on the body weight loss are observed among groups and noobvious necrosis and abnormity are observed in the sections of liver, kidney and

11、heart. These results demonstratethat Emodin/cisplatin co-treatment can significantly suppress tumor growth in vivo with no distinct side effects.Consistent with in vitro experiment, TUNEL assay shows that Emodin/cisplatin combination significantly increased cellapoptosis in xenograft tumors. Emodin/

12、Cisplatin co-treatment group also has lower MRP1 expression than the othergroups4.PROTOCOLCell Assay 4 The T24 human bladder cancer cells, the HCV-29 normal bladder epithelial cells and J82 human bladder cancer cellsare are cultured in RPMI 1640 medium supplemented with 10 % fetal bovine serum at 37

13、C in a humidifiedatmosphere containing 5 % CO2. Cells are seeded in 96-well plates with 2104 cells per well. The cells are incubatedwith Emodin for 24 h at different concentrations (0, 5, 10, 20, 30, 40, 50, 60, 70 M) and chose the criticalconcentration (20 M) treated with cells for 0, 6, 12, 24, 48

14、, 72, 96 h. The cells are incubated with cisplatin for 24 h atdifferent concentrations (0, 0.5, 1.0, 1.5, 2.0, 2.5, 3.0 g/mL). MTT assay is used to analyze the cell viability. Cells aretreated with drugs for 24 h and apoptotic rates are assessed with flow cytometry using AnnexinV-fluoresceinisothioc

15、yanate (AnnexinV-FITC)/propidium iodide (PI) kit. Samples are prepared according to the manufacturersinstruction and analyzed by a flow cytometry (FCM) Calibur4.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice4Administration 4 3106 T24 cells

16、are harvested, washed, and resuspended in serum-free optimum medium and then injectedPage 2 of 3 www.MedChemEsubcutaneously into 6-week old BALB/c-nu/nu mice (n=8 mice per group). Three days after inoculation, the mice areintraperitoneally administered with PBS, Emodin (50 mg/kg), Cisplatin (1 mg/kg

17、), or Emodin/cisplatin every two days.On day 18, every mouse is sacrificed. After body weight measurement, tumors are isolated, weighted and fixed in 4 %paraformaldehyde (PFA). Hearts, livers and kidneys are stained with Hematoxylin & Eosin to determine the systemictoxicity. Terminal deoxynucleotidy

18、l transferase(TdT)-mediated dUTP nick end label (TUNEL) assay is performed onparaformaldehyde-fixed and paraffin-embedded tumor sections.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產品發(fā)表的科研獻 Acta Pharmacol Sin. 2020 May 12. Exp Cell Res. 2020 May

19、3:112054.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Yim H, et al. Emodin, an anthraquinone derivative isolated from the rhizomes of Rheum palmatum, selectively inhibits the activity of casein kinase II as acompetitive inhibitor. Planta Med. 1999 Feb;65(1):9-13.2. Xing JY, et al. Antitumor Effects and Mechanism of Novel Emodin Rhamnoside D