异荭草素作用机制 - Medchemexpress - MCE中国

1、Product Data SheetIsoorientinCat. No.: HY-N0767CAS No.: 4261-42-1分式: CHO分量: 448.38作靶点: COX作通路: Immunology/Inflammation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 : 100 mg/mL (223.03 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentr

2、ation制备储备液1 mM 2.2303 mL 11.1513 mL 22.3025 mL5 mM 0.4461 mL 2.2303 mL 4.4605 mL10 mM 0.2230 mL 1.1151 mL 2.2303 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

3、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: 2.5 mg/mL (5.58 mM); Clear solution此案可获得 2.5 mg/mL (5.58 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMS

4、O 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: 2.5 mg/mL (5.58 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.5 mg/mL (5.58 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐

5、溶液中，混合均匀。BIOLOGICAL ACTIVITY物活性 Isoorientin种有效的 COX-2 抑制剂，IC50 值为 39 M。IC & Target COX-239 M (IC50)体外研究 Isoorientin is a Selective Inhibitor of Cyclooxygenase-2 (COX-2) from the Tubers of Pueraria tuberosa1. PANC-1 andPATU-8988 cells are grown for 24 hours in the presence of Isoorientin (0, 20, 40,

6、80, and 160 M), and a CCK8solution is added. The cell viability decreases significantly at the concentrations of 20, 40, 80, and 160 M. After thecells are cultured with Isoorientin (0, 20, 40, 80, and 160 M for PANC-1; 0, 20, 40, 80, 160, and 320 M for PATU-8988) for 24 hours, the expression of p-AM

7、PK and AMPK is assessed by Western blotting. After the Isoorientintreatment, the p-AMPK expression is increased. Then, in the shRNA group, the concentration of 80 M is used todetect the effects of Isoorientin. The expression levels of AMPK and p-AMPK are much lower in the shRNA group thanin the wild

8、-type PC cells (WT) and the group that is transfected with a negative control lentivirus (NC)2.体内研究 Animals treated with Isoorientin at 10 mg/kg and 20 mg/kg body weight have a statistically significant reduction inpaw edema, with a mean peak thickness of 1.190.05 mm and 1.080.04 mm, respectively. T

9、his indicated thatIsoorientin significantly attenuates paw edema compared with the control group3.PROTOCOLCell Assay 2 PANC-1 and PATU-8988 cells are plated onto 96-well plates. Each well contain 5,000 cells and 200 L of themedium with 10% FBS. When the cells of each well reach 70% confluency, the m

10、edium is changed, and FBS-freemedium with different concentrations of Isoorientin is added. After 24 hours, the cells are washed with PBS once, themedium containing Isoorientin is discarded, and 100 L of FBS-free medium with 10 L of the Cell Counting Kit 8(CCK8) reagent are added. The cells are incu

11、bated for another 1-2 hours at 37C, and the absorbance of each well isdetected using an ELISA reader at 490 nm. Cell viability is expressed as the fold change of absorbance2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice3Administration 3 In

12、 the case of paw edema model the Isoorientin or Celecoxib is given intraperitoneally and Carrageenan is injectedinto the paw directly one hour later. In air pouch model all the treatments are given along with Carrageenan directlyinto the pouch cavity. Isoorientin is injected three hours earlier than

13、 injection of Carrageenan into the pouch cavity.Isoorientin and Celecoxib are administered into the mice air pouch. The stock solutions of Isoorientin (100 mg/mL)and Celecoxib (100 mg/mL) are prepared in DMSO and further dilutions are made at the time of treatments. Animalsare divided, into 5 differ

14、ent groups as follows: control (DMSO treated); Carrageenan (0.5 mL of 1.5% (w/v)Carrageenan in saline) treated; Carrageenan+Celecoxib (20 mg/kg body weight) treated; Carrageenan+Isoorientin (10mg/Kg body weight) treated; Carrageenan+Isoorientin (20 mg/Kg body weight) treated.MCE has not independentl

15、y confirmed the accuracy of these methods. They are for reference only.REFERENCESPage 2 of 3 www.MedChemE1. Sumalatha M, et al. Isoorientin, a Selective Inhibitor of Cyclooxygenase-2 (COX-2) from the Tubers of Pueraria tuberosa. Nat Prod Commun. 2015Oct;10(10):1703-4.2. Ye T, et al. Isoorientin indu

16、ces apoptosis, decreases invasiveness, and downregulates VEGF secretion by activating AMPK signaling in pancreatic cancercells. Onco Targets Ther. 2016 Dec 12;9:7481-7492.3. Anilkumar K, et al. Evaluation of Anti-Inflammatory Properties of Isoorientin Isolated from Tubers of Pueraria tuberosa. Oxid Med Cell Longe