Astilbin _Keap1-Nrf2 Activator - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAstilbinCat. No.: HY-N0509CAS No.: 29838-67-3分式: CHO分量: 450.39作靶點(diǎn): Keap1-Nrf2; TNF Receptor; NF-B作通路: NF-B; Apoptosis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(shí)驗(yàn) DMSO : 60 mg/mL (133.22 mM)* me

2、ans soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.2203 mL 11.1015 mL 22.2030 mL5 mM 0.4441 mL 2.2203 mL 4.4406 mL10 mM 0.2220 mL 1.1101 mL 2.2203 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，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Astilbin種黃酮類化合物，可從 Smilax glabra 根莖中分離。Astilbi

3、n 增強(qiáng) NRF2 活化。Astilbin 還抑制TNF- 表達(dá)和 NF-B 活化。IC50 & Target NRF2 TNF- NF-B體外研究Astilbin is a common dietary flavonoid that can be found in various kinds of herbs and foods such as Smilax1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEGlabra, Sarcandra glabra, grape and red wine. Astilbin markedly inhibi

4、ts cisplatin-induced cell apoptosis andrecovers cell growth. Astilbin significantly decreases reactive oxygen species (ROS) accumulation andalleviates ROS-induced activation of p53, MAPKs and AKT signaling cascades, which in turn attenuatescisplatin-induced HEK-293cell apoptosis. Astilbin effectivel

5、y enhances NRF2 activation and transcription ofits targeting antioxidant genes to reduce ROS accumulation in cisplatin-induced HEK-293cells. Astilbinobviously suppresses tumor necrosis factor alpha (TNF-) expression and NF-B activation, and also inhibitsthe expression of induced nitric oxide synthas

6、e (iNOS) and cyclooxygenase-2 (COX-2). To measure theeffects of Astilbin on the growth of CDDP-treated renal cells, HEK-293cells are treated with CDDP (100M)and/or Astilbin (200M). Astilbin treatment significantly improvescell growth in CDDP-induced HEK-293cells1.體內(nèi)研究 To explore whether Astilbin imp

7、roves CDDP-induced nephrotoxicity in vivo, an acute cisplatin nephrotoxicmouse model is established. Single injection of CDDP with 8mg/kg dose results in notable weight losscompared with control group. However, the phenomenon is significantly alleviated by Astilbin at dose of50mg/kg. The mice fed As

8、tilbin alone do not show any obvious alteration in body weight. Similarly, serumcreatinine (SCr) and blood urea nitrogen (BUN) are higher in CDDP-treated mice than in control group.Treatment with Astilbin also decreases SCr and BUN levels. To examine the protective effect of Astilbin onCDDP-induced

9、renal histopathological damage, the mouse kidney sections are stained with H&E. The micein control group and Astilbin treated group have normal kidney morphology, while kidneys in CDDP groupshow severe damage with tubular degeneration, necrosis and cystic dilatation of the tubules with focalhemorrha

10、ges. Administration of Astilbin mitigated kidney injury, resulting in lower histopathological scorecompared to CDDP group. The apoptosis of renal cells is also detected using TUNEL staining to determinewhether Astilbin treatment decreased renal cell apoptosis in CDDP-induced acute nephrotoxic mice 1

11、.PROTOCOLCell Assay 1 HEK-293cells are seeded into 96-well plate with a density of 5104 cells/well and subsequently treated withCDDP, Astilbin (0, 10, 30, 50, 100, 200 and 300M) or CDDP+Astilbin for 24 h. After treatments, 20 L of 5mg/mL MTT is added to each well. The cells are incubated for additio

12、nal 4 h at 37C. Then cell supernatantis abandoned and 100 L of formanzan is added to each well. The plate is shaken at room temperature for15 min. Spectrophotometric absorbance is measured by Synergy Microplate Reader at 570 nm 1.MCE has not independently confirmed the accuracy of these methods. The

13、y are for reference only.Animal Mice 1Administration 1 Male C57BL/6 mice (20-24 g, 8 weeks of age) are used. After acclimation for one week, the experimentalmice are randomly divided into 4 groups with 10 animals per group: control group, CDDP group,CDDP+Astilbin group and Astilbin group. The contro

14、l group and CDDP group are orally administered salinefor 10 days; the CDDP+Astilbin group and Astilbin group are orally administered 50 mg/kg Astilbin for 10days. The CDDP group and CDDP+Astilbin group receive a single intraperitoneal injection of CDDP on the7th day of the experiment, while control

15、group and Astilbin group receive saline injection on the same day 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. Wang SW, et al. Astilbin ameliorates cisplatin-induced nephrotoxicity through reducing oxidative stress and inflammation. Food ChemTox