高車前素作用機制 - Medchemexpress - MCE中國

1、Product Data SheetHispidulinCat. No.: HY-N1950CAS No.: 1447-88-7分式: CHO分量: 300.26作靶點: Pim作通路: JAK/STAT Signaling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 : 62.5 mg/mL (208.15 mM; Need ultrasonic)H2O : 0.1 mg/mL (insoluble)SolventMass1 mg 5 mg 10 mgConcentra

2、tion制備儲備液1 mM 3.3304 mL 16.6522 mL 33.3045 mL5 mM 0.6661 mL 3.3304 mL 6.6609 mL10 mM 0.3330 mL 1.6652 mL 3.3304 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?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液

3、，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，適當保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)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(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 (6.93 mM); Clear solution此案可獲得 2.08 mg/mL (6.93 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 DM

4、SO 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 (6.93 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.08 mg/mL (6.93 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

5、 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 (6.93 mM); Clear solution此案可獲得 2.08 mg/mL (6.93 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。BIOLOGICAL ACTIVITY物活性 Hispidulin具有泛物活性的天然黃酮。 Hispidulin是Pim-1的抑制劑，IC50值為2.71 M。IC & Tar

6、get IC50: 2.71 M (Pim-1)1體外研究 Hispidulin induces cell death in a dose- and time-dependent manner in HepG2 cells. Hispidulin induces apoptosisthrough mitochondrial dysfunction, which is characterized by decreased Bcl-2/Bax ratio, disrupted mitochondrialmembrane potential and increased release of cyto

7、chrome C and activated capase-32.體內(nèi)研究 Hispidulin shows significant inhibitory effect on mice tumor size2. Hispidulin treatment effectively preventsovariectomy-induced body weight loss and attenuates ovariectomy-induced bone loss. Hispidulin treatment also decreases trabecular spacing in ovariectomy

8、mice3. Intraperitoneally administering hispidulin(10 or 50mg/ kg) to rats30 min before intraperitoneally injecting kainic acid (15mg/kg) increases seizure latency and decreases seizure score.In addition, hispidulin substantially attenuates kainic acid-induced hippocampal neuronal cell death, and thi

9、sprotective effect is accompanied by the suppression of microglial activation and the production of proinflammatorycytokines such as interleukin-1, interleukin-6, and tumor necrosis factor- in the hippocampus4.PROTOCOLCell Assay 2 HepG2 cells are treated with different concentrations of hispidulin (

10、50, 100, 200 M) for 24, 48 and 72 h. Followingtreatment, cells are further incubated with MTT reagents at 37C for 4 h before DMSO is added, to dissolve farmazancrystals, and absorbance is measured at 570 nm in a microplate reader2.MCE has not independently confirmed the accuracy of these methods. Th

11、ey are for reference only.Animal Mice: Tumor are established in mice. Mice are treated with DMSO or Hispidulin at a dosage of 10, 20 or 40Administration 2 mg/kg/day for 35 days. The body weight of tumour-bearing mice is recorded every week and tumour volume iscalculated 2.MCE has not independently c

12、onfirmed the accuracy of these methods. They are for reference only.REFERENCES1. Chao SW, et al. Total Synthesis of Hispidulin and the Structural Basis for Its Inhibition of Proto-oncogene KinasePim-1. J Nat Prod. 2015 Aug28;78(8):1969-76.2. Gao H, et al. Hispidulin induces apoptosis through mitocho

13、ndrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. CellBiochem Biophys. 2014 May;69(1):27-34.3. Zhou R, et al. Hispidulin exerts anti-osteoporotic activity in ovariectomized mice via activating AMPK signaling pathway. Cell Biochem Biophys. 2014Page 2 of 3 www.MedChemEJun;69(2):311-7.4. Lin TY, et al. Protective effect of hispidulin on kainic acid-induced seizures and neurotoxicity in rats. Eur J Pharmacol. 2015 May 15;755:6-15.McePdfHeightCautio