Artemisinin-Qinghaosu-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEArtemisininCat. No.: HY-B0094CAS No.: 63968-64-9Synonyms: Qinghaosu; NSC 369397分式: CHO分量: 282.33作靶点: HCV; Parasite作通路: 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 : 50 mg/mL

2、 (177.10 mM; Need ultrasonic)H2O : 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (8.85 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (8.85 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Artemisinin是从青蒿 (Artemisia annua L.) 植

3、物的地上部分分离的抗疟疾药物。体外研究 Artemisinin (3.125-100 M) concentration-dependently suppresses A25-35 induced cytotoxicity in PC12cells. Artemisinin (25 M) suppresses A25-35-induced LDH release, apoptosis and ROS production,attenuates A-induced mitochondrial membrane potential loss and caspase 3/7 activity incr

4、ease, andstimulates the phosphorylation of ERK1/2 in a time- and concentration-dependent manner in PC12 cell. ERK1/2 pathway mediates the protect effects of artemisinin in PC12 cells 1. Artemisinin shows cytotoxic activityin MCF-7/Dox cell line with IC50 of 3.70.4 g/mL after 24 h treatment. Besides,

5、 Artemisinin treatment ofMCF-7 cells, sensitive and resistant to Dox and DDP, causes a decrease in expression of proteins such asLF, FTH1, and HEP. Artemisinin activates p38 MAPK-kinase cascade regardless of the oxidative stress dueto inhibition of VEGF expression and cell migration 2. Artemisinin (

6、50, 100 or 200 mg) significantly inhibitsisoflurane-induced hippocampal neuronal loss, decreases caspase-3-positive cell counts and also cleavescaspase-3 expression, and modulates the expression of apoptosis pathway proteins. Artemisinin modulatesJNK/ERK 1/2 signalling and histone acetylation 3. Art

7、emisinin inhibits HCV replication in a dose-dependentmanner with EC50 value of 16738 M. Artemisinin and its most potent analogues partially inhibit the in vitroreplication of HCV by induction of reactive oxygen species (ROS) 4. Artemisinin significantly inhibits VSMCproliferation in a dose-dependent

8、 manner. Artemisinin (1mM) for 72h significantly reduces the expression ofproliferating cell nuclear antigen messenger RNA 5.体内研究 Artemisinin (50, 100 or 200 mg/kg b.wt/day, p.o.) prevents isoflurane-induced working memory impairmentsas observed in T-maze test. Artemisinin enhances spatial navigatio

9、n and memory of rats exposed toisoflurane. Artemisinin-treated rats exhibit markedly better performance in comparison with isoflurane-alone-exposed rats 3.PROTOCOLKinase Assay 1 Briefly, PC12 cells are lysed in lysis buffer and centrifuged at 12,500g for 5 min 15 mL of cell lysate isincubated with 5

10、0 mL of 2X substrate working solution at room temperature for 30 min in 96-well plates. Thefluorescence intensity is then determined by Infinite M200 PRO Multimode Microplate at an excitationwavelength of 490 nm and emission at 520 nm. The fluorescence intensity of each sample is normalized tothe pr

11、otein concentration of sample. All values of % caspase 3/7 activities are normalized to the controlgroup.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 2 For this purpose, cells are cultivated in 96-well plates in DMEM, supplemented with ins

12、ulin. The artemisinin,Dox, and DDP are added to media at different concentrations and the cells are cultivated for either 24 or 48h. For this purpose artemisinin is diluted in 0.01% DMSO in media. After this time, 10 L of the MTT dyesolution (5 mg/mL in phosphate buffer saline) is added to the cells

13、; the cells are incubated at the sameconditions for 3 h. After centrifugation (1500 rpm, 5 min) the supernatant is removed. 100 L of dimethylsulfoxide is added to each well, to dissolve formazan. The absorption is measured, using a multi-well2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEspectroph

14、otometer at a wavelength of 540 nm.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Separate group of rat pups (total rat pups 80; n = 16 per group) is administered artemisinin (50, 100 or 200Administration 3 mg/kg body weight) via oral gavage, ev

15、ery day from P2 to P21. On P7, the pups are exposed to isoflurane(0.75% in 30% oxygen or air) for 6 h in a temperature-controlled chamber. Animals that are not exposed toanaesthesia nor given artemisinin served as control group, while rats that receive isoflurane alone aregrouped as anaesthetic-cont

16、rols.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Zeng Z, et al. Artemisinin protects PC12 cells against -amyloid-induced apoptosis through activation of the ERK1/2 signaling pathway.Redox Biol. 2017 Apr 4;12:625-633.2. Chekhun VF, et al

17、. Artemisinin modulating effect on human breast cancer cell lines with different sensitivity to cytostatics. Exp Oncol.2017 Mar;39(1):25-29.3. Xu G, et al. Neuroprotective effects of artemisinin against isoflurane-induced cognitive impairments and neuronal cell death involveJNK/ERK1/2 signalling and

18、 improved hippocampal histone acetylation in neonatal rats. J Pharm Pharmacol. 2017 Mar 12.4. Obeid S, et al. Artemisinin analogues as potent inhibitors of in vitro hepatitis C virus replication. PLoS One. 2013 Dec 11;8(12):e81783.5. Wang HY, et al. The effects of artemisinin on the proliferation and apoptosis