紅倍酚作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetPurpurogallinCat. No.: HY-12136CAS No.: 569-77-7分式: CHO分量: 220.18作靶點(diǎn): Xanthine Oxidase作通路: Metabolic Enzyme/Protease儲(chǔ)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(shí)驗(yàn) DMSO : 125 mg/mL (567.72 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制備

2、儲(chǔ)備液1 mM 4.5417 mL 22.7087 mL 45.4174 mL5 mM 0.9083 mL 4.5417 mL 9.0835 mL10 mM 0.4542 mL 2.2709 mL 4.5417 mL請(qǐng)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(chǔ)備液；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍浮Ｒ韵氯芙獍付颊?qǐng)先按照 In Vitro 式配制澄清的儲(chǔ)備液，再依次添加

3、助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (9.45 mM); Clear solution此案可獲得 2.08 mg/mL (9.45 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(chǔ)備液

4、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(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (9.45 mM); Clear solution此案可獲得 2.08 mg/mL (9.45 mM，飽和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液為例，取 100 L 20.8 mg/mL 的澄均勻。DMSO 儲(chǔ)備液加到 900 L 20% 的 SBE-CD 理鹽溶

5、液中，混合BIOLOGICAL ACTIVITY物活性 Purpurogallin是從櫟屬植物中提取的天然酚，具有強(qiáng)的黃嘌呤氧化酶 (Xanthine Oxidase) 抑制活性，其 IC50 為 0.2 M 。Purpurogallin 具有抗氧化和抗炎作。IC & Target IC50: 0.2 M (xanthine oxidase)3體外研究 Purpurogallin (50 or 100 M; 7 or 25 hours; BV2 murine microglial cells) treatment attenuates the production of pro-inflamm

6、atory cytokines, including interleukin-1 (IL-1) and tumor necrosis factor- (TNF-) by suppressing theirmRNA and protein expression in LPS-stimulated BV2 microglial cells1.Purpurogallin (100 M; 75-120 minutes; BV2 murine microglial cells) exhibits anti-inflammatory properties bysuppressing the phospha

7、tidylinositol 3-kinase/Akt and mitogen-activated protein kinase signaling pathways in LPS-stimulated BV2 microglial cells1.RT-PCR1Cell Line: BV2 murine microglial cellsConcentration: 50 or 100 MIncubation Time: 7 or 25 hoursResult: Attenuated the production of pro-inflammatory cytokines, including i

8、nterleukin-1 (IL-1) and tumor necrosis factor- (TNF-) by suppressing their mRNA and proteinexpression.Western Blot Analysis1Cell Line: BV2 murine microglial cellsConcentration: 100 MIncubation Time: 75 minutes, 90 minutes, 120 minutesResult: Suppressed the phosphatidylinositol 3-kinase/Akt and mitog

9、en-activated proteinkinase signaling pathways.體內(nèi)研究Purpurogallin (100-400 g/kg; intraperitoneal injection; for 48 or 72 hours; male Sprague-Dawley rats) exerts itsneuroinflammation effect through the dual effect of inhibiting IL-6 and TNF- mRNA expression and reducingHMGB1 protein and mRNA expression

10、2.Animal Model: Fifty-four male Sprague-Dawley rats (250-350 g) with subarachnoid hemorrhage(SAH)2Dosage: 100 g/kg, 200 g/kg, 400 g/kgAdministration: Intraperitoneal injection; for 48 or 72 hoursResult: Dose-dependently reduced HMGB1 protein expression. High dose reduced TNF-Page 2 of 3 www.MedChemE

11、and HMGB1 mRNA levels.REFERENCES1. Park HY, et al. Purpurogallin exerts antiinflam m atory effects in lipopolysaccharidestim ulated BV2 m icroglial cells through the inactivation of the NFB andMAPK signaling pathways. Int J Mol Med. 2013 Nov;32(5):1171-8.2. Chang CZ, et al. Purpurogallin, a natural

12、phenol, attenuates high-mobility group box 1 in subarachnoid hemorrhage induced vasospasm in a rat model.Int J Vasc Med. 2014;2014:254270.3. Honda S, et al. Conversion to purpurogallin, a key step in the mechanism of the potent xanthine oxidase inhibitory activity of pyrogallol. Free Radic BiolMed. 2017 May;106:228-235.McePdfHeightCaution: Product has not been