丹皮酚作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetPaeonolCat. No.: HY-N0159CAS No.: 552-41-0分式: CHO分量: 166.17作靶點(diǎn): Monoamine Oxidase; Autophagy作通路: Neuronal Signaling; Autophagy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 : 38 mg/mL (228.68 mM)H2O : 0.1 mg/mL (insoluble)* means soluble, but s

2、aturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 6.0179 mL 30.0897 mL 60.1793 mL5 mM 1.2036 mL 6.0179 mL 12.0359 mL10 mM 0.6018 mL 3.0090 mL 6.0179 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

3、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: 2.5 mg/mL (15.04 mM); Suspended solution此案可獲得 2.5 mg/mL (

4、15.04 mM，飽和度未知) 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 25.0 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: 2.5 mg/mL (15.04 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (15.04 mM，飽和度未知

5、) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 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: 2.5 mg/mL (15.04 mM); Clear solution此案可獲得 2.5 mg/mL (15.04 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 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVI

6、TY物活性 Paeonol是牡丹根的活性提取物，Paeonol 抑制 MAO-A 和 MAO-B，IC50 分別為 54.6 M 和 42.5 M。IC & Target IC50: 42.5 M (MAO-B), 54.6 M (MAO-A)1體外研究 Paeonol is found to be inhibitory against MAO A in a dose-dependent manner with IC50 value of 54.6 M. Paeonol isshown to inhibit MAO-B in a dose-dependent manner with the I

7、C50 of 42.5 M. For Paeonol, the Ki is estimated to be51.1 M. The inhibition of Paeonol on MAO B is of competitive type with Ki value of 38.2 M1.體內(nèi)研究 The 200 mg/kg Paeonol+I/R group AN/V (%): 7.62.2, p0.01 and 100 mg/kg Paeonol+I/R group AN/V (%):9.42.8, p0.05 both show lesser extents of no-reflow ar

8、ea in the ventricles compared with the I/R group AN/V (%): 18.22.9. In particular, the 200 mg/kg Paeonol + I/R group experienced markedly alleviated no-reflow in the wholeheart AN/WH (%): 4.61, p0.05 compared with the I/R group AN/WH (%): 10.01.92.PROTOCOLAnimal Mice2Administration 2 Male Wistar rat

9、s (180-220 g, average age of 8 week) are randomly divided into four groups: (1) sham group,thoracotomy without left anterior descending coronary artery (LAD) occlusion or Paeonol pretreatment; (2) I/R group,LAD occlusion (ischemia) for 4 h followed by reperfusion for 8 h; (3) Paeonol (100 mg/kg)+I/R

10、 group, oraladministration of 100 mg/kg Paeonol (1 mL/kg) for 7 days using a intragastric tube prior to I/R procedure; (4)Paeonol (200 mg/kg) + I/R group, oral administration of 200 mg/kg Paeonol (1 mL/kg) for 7 days using a intragastrictube prior to I/R procedure. In addition, rats in the sham and

11、I/R groups received a dosage of DMSO equal to thatwith which the Paeonol was dissolved in for the other two groups. DMSO was also administered intragastrically for 7consecutive days. A minimum of eight rats were assigned to each group. An ischemia group without reperfusion isnot included since our p

12、resent study mainly focuses on the effect of Paeonol on the cardiac injuries after reperfusion,which is closely related to the real-world situation of no-reflow after coronary revascularization. However, futurestudies may include a group subjected only to 4 h of ischemia to differentiate, in terms o

13、f damage to the cardiacfunction, which was due to the ischemia and which was due to the no-reflow.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Kong LD, et al. Inhibition of MAO A and B by some plant-derived alkaloids, phenols and anthraquinones. J Ethnopharmacol. 2004 Apr;91(2-3):351-5.2. Ma L, et al. Paeonol Protects Rat Heart by Improving Regional Blood Perfusion during No-Reflow. Front Physiol. 2016 Jul 21;7:298.Page 2 of 3 www.MedChemEMcePdfHeightCauti