人參皂苷 Rb1作用機制 - Medchemexpress - MCE中國

1、Product Data SheetGinsenoside Rb1Cat. No.: HY-N0039CAS No.: 41753-43-9分式: CHO分量: 1109.29作靶點: Na+/K+ ATPase; IRAK; NF-B; Autophagy; Mitophagy; HSV作通路: Membrane Transporter/Ion Channel; NF-B; Autophagy; Anti-infection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

2、: 100 mg/mL (90.15 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 0.9015 mL 4.5074 mL 9.0148 mL5 mM 0.1803 mL 0.9015 mL 1.8030 mL10 mM 0.0901 mL 0.4507 mL 0.9015 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，-

3、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(dāng)?shù)娜芙獍浮Ｒ韵氯芙獍付颊埾劝凑?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 (2.25 mM); Clear solution此案可獲

4、得 2.5 mg/mL (2.25 mM，飽和度未知) 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 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 (2.25 mM); Clear solution此案可獲得 2.5 mg/mL (2.25 mM，飽和度未知) 的澄清溶液。Page 1 of 2 www.Med

5、ChemE以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄均勻。DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (2.25 mM); Clear solution此案可獲得 2.5 mg/mL (2.25 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 ACTIVITY物活性

6、Ginsenoside Rb1是中藥 Panax ginseng 的成分。Ginsenoside 抑制 Na+, K+-ATPase 活性，IC50 為 6.31.0 M。 Ginsenoside Rb1 也抑制 IRAK-1 激活及 NF-B p65 的磷酸化。IC & Target IRAK-1 p65 Na+, K+-ATPase Autophagy6.3 M (IC50)Mitophagy體外研究 Rat brain microsomal Na+, K+-ATPase activity is inhibited significantly and rapidly by Ginsenos

7、ide Rb1. The IC50 ofGinsenoside Rb1 for Na+,K+-ATPase is 6.31.0 M. The inhibition is enhanced with increasing the concentration ofGinsenoside Rb1 or decreasing that of Na+ and K+. Kinetic analysis reveals that Ginsenoside is an uncompetitiveinhibitor with respect to ATP1.Ginsenoside Rb1 significantl

8、y inhibits the activation of interleukin-1 receptor-associated kinase-1 (IRAK-1), IKK-, NF-B, and MAP kinases (ERK, JNK, and p-38); however, interaction between LPSand Toll-like receptor-4, IRAK-4 activation and IRAK-2 activation are unaffected2. Ginsenoside Rb1 is an ingredient ofa Chinese medicine

9、 Panax ginseng. Ginsenoside Rb1 is a major bioactive compound in the regulating pregnane Xreceptor (PXR)/NF-B signaling. Ginsenoside Rb1 is the compound with potent anti-inflammatory activity in ginsengsaponin extract (GSE). The concentration for Ginsenoside Rb1 (10 M) is optimized from a preliminar

10、y study to ensuresufficient anti-inflammatory activity and without apparent cytotoxicity. Ginsenoside Rb1 significantly reduces TNF-induced upregulation of IL-1 and iNOS mRNA levels, and restores the mRNA levels of PXR and CYP3A4 in LS174Tcells. TNF- causes a significant reduction in PXR protein lev

11、els and increase in the ratio of phosphorylated to totalNF-B p65, both of which are significantly abrogated by Ginsenoside Rb13.體內(nèi)研究 Ginsenoside Rb1 at the both doses of 30 mg/kg and 60 mg/kg significantly attenuates the histological lung injury.Ginsenoside Rb1 at the dose of 30 mg/kg and 60 mg/kg b

12、oth significantly attenuates the histological intestine injury4. Ginsenoside Rb1 (Rb1), an ingredient of a Chinese medicine Panax ginseng, has beneficial effects on mesenterymicrovascular hyperpermeability induced by Lipopolysaccharide (LPS) and the underlying mechanisms. In some rats,Ginsenoside Rb

13、1 (5 mg/kg per hour) is administrated through the left jugular vein 30 min after LPS infusion.Ginsenoside Rb1 decreases caveolae number in endothelial cells of microvessels. Ginsenoside Rb1 amelioratesmicrovascular hyperpermeability after the onset of endotoxemia and improves intestinal edema throug

14、h inhibitingcaveolae formation and junction disruption, which is correlated to suppression of NF-B and Src activation5.PROTOCOLCell Assay 3 LS174T cells are seeded in cell imaging dish. After overnight incubation, cells are treated with GSE (100 g/mL),Ginsenoside Rb1 (10 M), or CK (10 M) for 3 hours, followed by an additional incubation with or without TNF- (20ng/ml) for 6 hours. At the end of the incubation, cells are harvested and fixed with 4% paraformaldehyde solution at20C for 20 minutes. Af