Sarsasapogenin-Parigenin-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESarsasapogeninCat. No.: HY-N0073CAS No.: 126-19-2Synonyms: Parigenin; Sarsagenin分式: CHO分量: 416.64作靶點: NF-B作通路: NF-B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 Ethanol : 1 mg/mL (2.40 mM; Need

2、ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.4002 mL 12.0008 mL 24.0015 mL5 mM - - -10 mM - - -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 Sarsasapogenin是從中草藥知母中分離到的甾體皂苷元，具有抗糖尿病、抗氧化、抗癌、抗炎等多種功效。IC50 & Target NF-B體外研究Sarsasapogenin (20-80 M) induces apoptosis

3、via caspase-dependent mitochondrial pathway in heLa cells.Sarsasapogenin also induces apoptosis via the caspase-dependent mitochondrial apoptotic pathway.1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESarsasapogenin (60 M)-induced ROS generation triggers ER stress and mitochondrial dysfunction 1.S

4、arsasapogenin potently inhibits NF-B and MAPK activation, as well as IRAK1, TAK1, and IBphosphorylation in LPS-stimulated macrophages. Moreover, Sarsasapogenin inhibits the binding of LPS tomacrophage Toll-like receptor 4, and polarization of M2 to M1 macrophages 3.體內(nèi)研究 Sarsasapogenin (20 and 40 mg/

5、kg) significantly restores the sucrose preference deficit induced by olfactorybulbectomy (OB), and increases locomotor activity. Sarsasapogenin groups (20 and 40 mg/kg) havesignificantly lower immobility times, higher AChE protein expression levels than the OB group. Furthermore,Sarsasapogenin (20 a

6、nd 40 mg/kg) groups have significantly higher 7-nAChR protein expression, andincreases higher 4-nAChR protein expression levels compared to rats in the OB group 2. Sarsasapogenin(5 or 10 mg/kg, p.o.) inhibits TNBS-induced colon shortening and myeloperoxidase activity in mice, reducingNF-B activation

7、 and interleukin (IL)-1, tumor necrosis factor (TNF)-, and IL-6 levels, while simultaneouslyincreasing IL-10 3.PROTOCOLCell Assay 1 The effect of Sarsasapogenin on cell viability is measured by the MTT assay method. After exposure toSarsasapogenin in the absence or presence of Z-VAD-FMK pretreatment

8、 for the indicated time, cells in 96-well plates are incubated with MTT. The formazan precipitate is dissolved in 200 L of dimethyl sulfoxide,and the absorbance at 570 nm is measured using a Benchmark microplate reader.MCE has not independently confirmed the accuracy of these methods. They are for r

9、eference only.Animal The mice are randomly divided into 7 groups: normal control, TNBS-induced colitic control groups treatedAdministration 3 with vehicle, timosaponin AIII (5 or 10 mg/kg), Sarsasapogenin (5 or 10 mg/kg) or sulfasalazine (50 mg/kg).Each group consists of 6 mice. The colitis is induc

10、ed by the intrarectal injection of 2.5% (w/v) TNBS solution(100 L, dissolved in 50% ethanol) into the colon of anesthetized mice using a thin round-tip needle equippedwith a syringe. The normal group is treated with vehicle alone instead of TNBS and test agents. If the injectedTNBS solution is excre

11、ted, the mouse is excluded from the experiment. Timosaponin AIII or Sarsasapogenin(5 or 10 mg/kg) or sulfasalazine (50 mg/kg) dissolved in 2% tween 80 are orally administered once a day for3 days after treatment with TNBS. The mice are killed 18 h after the final administration of test agents. Theco

12、lon is quickly removed, opened longitudinally, and gently washed by PBS. Macroscopic evaluation of thecolitis grade is scored (0, no ulcer and no inflammation; 1, no ulceration and local hyperemia; 2, ulcerationwith hyperemia; 3, ulceration and inflammation at one site only; 4, two or more sites of

13、ulceration andinflammation; 5, ulceration extending more than 2 cm). The colons are stored at 80C until used in theexperiment for ELISA and immunoblotting.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Shen S, et al. Sarsasapogenin induces

14、 apoptosis via the reactive oxygen species-mediated mitochondrial pathway and ER stresspathway in HeLa cells. Biochem Biophys Res Commun. 2013 Oct 26.2. Feng B, et al. Sarsasapogenin reverses depressive-like behaviors and nicotinic acetylcholine receptors induced by olfactory bulbectomy.Neurosci Lett. 2017 Feb 3;639:173-178.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. Lim SM, et al. Timosaponin AIII and its metabolite sarsasapogenin ameliorate colitis in mice by inhibiting NF-B and MAPK activationand restoring Th17/Treg cell balance. Int Immunopharmacol.