DL-Borneol-racemic-Borneol-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDL-BorneolCat. No.: HY-N1368CAS No.: 507-70-0Synonyms: ()-Borneol分式: CHO分量: 154.25作靶点: GABA Receptor作通路: Membrane Transporter/Ion Channel; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶

2、解性数据体外实验 DMSO : 100 mg/mL (648.30 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (16.21 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (16.21 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% cor

3、n oilSolubility: 2.5 mg/mL (16.21 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 DL-BorneolD-Borneol和L-Borneol的外消旋混合物。DL-Borneol在中国泛于管和脑管疾病的治疗。体外研究 DL-Borneol increases intracellular accumulation of Rho123, and enhances P-gp substrates across the BBBin vitro, and also depresses mdr1a mRNA and P-gp expres

4、sion. Furthermore, DL-Borneol could activate NF-B and inhibition of NF-B with MG132 and SN50 obscures the P-gp decreases induced by DL-Borneol. 10 g/mL and 20 g/mL DL-Borneol significantly increase phosphorylation of IB expression at 30 min aftertreatment transiently. DL-Borneol treatment decreases

5、P-gp expression in BMECs 1.体内研究 DL-Borneol significantly suppresses the process of epileptogenesis in PTZ-kindled mice. The biochemicalalterations induced by PTZ kindling are ameliorated in DL-Borneol-treated animals which is indicated bydecreased LPO and increased SOD, GSH, CAT levels. The distinct

6、 neuronal damage observed in thekindled group is counteracted by DL-Borneol. Furthermore, it decreases the levels of GFAP which ismanifested by reduced immunostaining 2. The pathological damages of ischemia-reperfusion have asignificant impact on the pharmacokinetic traits of DL-Borneol and that the

7、re are some components inXingnaojing inhibiting the absorption of DL-Borneol 3.PROTOCOLCell Assay 1 Rho123 efflux assay is used to measure the activity of P-gp in BMECs according to previous methods.BMECs grown to confluency in 24-well plates are treated with 5 g/mL, 10 g/mL and 20 g/mL DL-Borneol,D

8、MSO, CsA for 2 h, or with 10 g/mL and 20 g/mL DL-Borneol for different times (30 min, 1 h, 2 h, and 4 h).Then BMECs are exposed to 5 mol/L Rho123 in DMEM for 90 min. After incubation with Rho123, BMECsare washed with ice-cold PBS and solubilized in 1% NaOH. Fluorescence of Rho123 is measured withemi

9、ssion wavelength at 535 nm and excitation wavelength at 485 nm using a fluorescencespectrophotometer 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats: The pharmacokinetic study is performed 24 h after reperfusion in the model groups, i.e.,

10、26 h afterAdministration 23 operation in the SO group. The XNJ subgroup rats are orally administered with XNJ decoction dissolved in0.7% CMC-Na aqueous solution (10.00 ml/kg body weight (BW). The pure DL-Borneol subgroup alsoreceives gavages of DL-Borneol suspension (10.00 ml/kg BW). DL-Borneol and

11、XNJ suspensions areadministrated respectively at a dosage of 162.0 mg/kg of DL-Borneol. Then 0.5 ml plasma samples arecollected into heparinized tubes by the puncture of the retro-orbital sinus at 5, 10, 20, 30, 45, 60, 90, 120,180, 240, and 360 min separately following oral administration. After ce

12、ntrifugation at 6000 r/min for 10 min,plasma samples are stored at 20 C and analyzed within one week 3.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEMice: Repeated administration of a subconvulsive dose of PTZ (35 mg/kg, i.p.) on every alternate day for 4weeks produces kindling in mice. DL-Borneo

13、l (5, 10, and 25 mg/kg, i.p.) and diazepam (1 mg/kg, i.p.) aregiven as a pretreatment prior to each PTZ injection during the progression of kindling. Oxidative stressparameters such as superoxide dismutase (SOD), reduced glutathione (GSH), catalase (CAT), and lipidperoxidation (LPO) are assessed at

14、the end of the study. Neuronal damage is assessed by hematoxylin andeosin staining technique. GFAP is also evaluated in the hippocampus region of the brain by usingimmunohistochemistry 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Fan X

15、, et al. Borneol Depresses P-Glycoprotein Function by a NF-B Signaling Mediated Mechanism in a Blood Brain Barrier in VitroModel. Int J Mol Sci. 2015 Nov 18;16(11):27576-88.2. Tambe R, et al. Antiepileptogenic effects of borneol in pentylenetetrazole-induced kindling in mice. Naunyn Schmiedebergs ArchPharmacol. 2016 May;389(5):467-75.3. Xu P, et al. Comparative pharmacokinetics of borneol in cerebral ischemia-reperfusion and sham-operated rats. J Zhejiang