Ginsenoside-Rb3-Gypenoside-IV-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGinsenoside Rb3Cat. No.: HY-N0041CAS No.: 68406-26-8Synonyms: Gypenoside IV分式: CHO分量: 1079.27作靶点: NF-B; COX; NO Synthase作通路: NF-B; Immunology/Inflammation储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 monthBIOL

2、OGICAL ACTIVITY物活性 Ginsenoside Rb3是从 Panax notoginseng 中提取的。在 293T 细胞系中 Ginsenoside Rb3 抑制 TNF 诱导的NF-B 转录活性，IC50 为 8.2 M。Ginsenoside Rb3 还抑制 COX-2 和 iNOS mRNA的诱导。IC50 & Target NF-B COX-2 iNOS8.2 M (IC50, in 293T cell lines)体外研究 Ginsenoside Rb3 (0.1-10 M) is tested for inhibition of tumor necrosis fa

3、ctor- (TNF)-induced nuclear factorkappa-light-chain-enhancer of activated B cells (NF-B) luciferase reporter activity using a human kidney293T cell-based assay. Ginsenoside Rb3 shows the significant activity with an IC50 of 8.2 M. GinsenosideRb3 also inhibits the induction of cyclooxygenase-2 (COX-2

4、) and inducible nitric oxide synthase (iNOS)messenger Ribonucleic acid (mRNA) in a dose-dependent manner after HepG2 cells have been treated withTNF- (10 ng/mL) 1. Ginsenoside Rb3 (0.1-10 M) significantly increases cell viability and inhibits lactatedehydrogenase (LDH) release in a dose-dependent ma

5、nner. PC12 cell viability as determined by MTTreduction is also markedly decreased after the cell is exposed to oxygen and glucose deprivation(OGD)/OGD-Rep. But, when the cells are pretreated with Ginsenoside Rb3 (0.1, 1, and 10 M), OGD/OGD-Rep induced cell toxicity is significantly attenuated, whic

6、h is concentration-dependently attenuated byGinsenoside Rb3 treatment. The viabilities are raised to 52.8%5.6%, 64.6%5.7%, and 76.4%8.8%,respectively, compared with the control group 2.1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE体内研究 Ginsenosides Rb3 is a major compound isolated from Gynostemma

7、 pentaphyllum that holistically improvesgut microenvironment and induces anti-polyposis in ApcMin/+ mice. Six-weeks-old mice are subjected to Rb3treatment, before the appearance of the intestinal polyps. All the mice are monitored for food intake, waterconsumption, and weight changes. Throughout the

8、 experiment, no Rb3/Rd-associated weight loss in mice isobserved. In addition, none of the treated mice show variations in food and water consumption. Whereas, thenumber and size of the polyps are effectively reduced by Rb3 treatments 3.PROTOCOLKinase Assay 1 HepG2 cells are seeded at a concentratio

9、n of 1105 cells/mL (1.5 mL) in a 12-well plate and grown for 24 h.All cells are then transfected with Pnf-B-luc plasmid (0.5 g/well). Transfection are performed by thelipofectamine LTX. After 23 h of transfection, medium is changed to assay medium. After 24 h of transfection,cells are treated with t

10、est compounds (e.g., Ginsenoside Rb3; 0.1, 1 and 10 uM) for another 24 hours. After25 h of transfection, cells are treated with 10 ng/mL of TNF- for another 23 hours. The luciferase activity ofcell lysates is assayed with 100 L of by luciferase assay kit using an LB 953 Autolumat. Transfections arep

11、erformed in triplicate, and activation is normalized against -galactosidase activity 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 2 NGF-differentiated PC12 cells are plated at a density of 1.0105 cells/mL 2 days before each experiment. T

12、oinitiate OGD, the cell culture medium is removed and replaced with the glucose-free DMEM, then the cellsare incubated at 37C in an oxygen-free chamber (95% N2 and 5% CO2) for 4 h (OGD), and the change inoxygen levels of the culture medium are monitored during incubation in oxygen-free chamber. Foll

13、owingOGD, glucose is added to normal levels (final concentration: 4.5 mg/mL) and cells are incubated undernormal growth conditions (95% air and 5% CO2) for additional 24 h as OGD-reperfusion (OGD-Rep).Ginsenoside Rb3 (0.1, 1, 10 M) is added to the culture 24 h before OGD treatment and throughout the

14、 OGDreperfusion. The control culture is always maintained in normal DMEM and put in the incubator under normalconditions 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 3Administration 3 Heterozygous male ApcMin/+ (C57BL/6J-ApcMin/+) mice

15、are used. Total 32 male ApcMin/+ mice (aged 6weeks) are divided into three groups; 10 mice in the control group and 22 mice equally divided for Rb3 andRd treatments. The mice are daily gavage with a single dose of Ginsenoside Rb3 or Rd at 20mg/kg, orsolvent control. The treatments are carried out fo

16、r 8 consecutive weeks.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. He F, et al. Antitumor effects of dammarane-type saponins from steamed Notoginseng. Pharmacogn Mag. 2014 Jul;10(39):314-7.2. Zhu JR, et al. Protective effects of ginsenos

17、ide Rb(3) on oxygen and glucose deprivation-induced ischemic injury in PC12 cells. ActaPharmacol Sin. 2010 Mar;31(3):273-80.3. Huang G, et al. Ginsenosides Rb3 and Rd reduce polyps formation while reinstate the dysbiotic gut microbiota and the intestinalmicroenvironment in ApcMin/+ mice. Sci Rep. 2017 Oct 2;7(1