Saikosaponin-D - STAT 抑制劑 - 生命科學試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESaikosaponin DCat. No.: HY-N0250CAS No.: 20874-52-6分式: CHO分量: 780.98作靶點: STAT; NF-B; Estrogen Receptor/ERR作通路: JAK/STAT Signaling; Stem Cell/Wnt; NF-B; Others儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month

2、溶解性數(shù)據(jù)體外實驗 DMSO : 50 mg/mL (64.02 mM; Need ultrasonic)H2O : 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (3.20 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (3.20 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Saikosaponin D

3、是從柴胡中分離到的三萜皂苷類，具有抗炎，抗菌，抗腫瘤，抗過敏的功效；Saikosaponin D可以抑制 selectin，STAT3 和 NF-kB 的活性，活化 estrogen receptor-。IC50 & Target STAT3 NF-B ER體外研究 Saikosaponin D (Compound 3) is a triterpene saponin, which inhibits E-selectin, L-selectin and P-selectinbinding to THP-1 cells, with IC50s of 1.8 M, 3.0 M and 4.3 M,

4、 and such effects are not due to cytotoxicaction. Saikosaponin D (1, 5, 10 M) dose-dependently inhibits the THP-1 adhesion to the HUVECsmonolayer activated by TNF-. Saikosaponin D (30 M) also inhibits the expression of P-selectin ligand(CD162) in THP-1 cells 1. Saikosaponin D (5 M) suppresses the pr

5、oliferation of HSC-T6 cells induced byH2O2 treatment, reduces the expression levels of -SMA, TGF-1, Hyp, COL1 and TIMP-1, and increasesMMP-1 expressioon, thus inhibiting H2O2-induced excessive extracellular matrix (ECM) formation, withsimilar effects to estradiol (E2), and these effects are blocked

6、by ER antagonists. Saikosaponin D alsoinhibits oxidative stress-induced ROS generation and down reduates MAPK signaling pathway, and theinhibition is also suppressed by ER antagonists 3.體內(nèi)研究 Saikosaponin D (2 mg/kg/day, i.p.) shows a protective effect on overdose of acetaminophen (APAP)-inducedliver

7、 injury of mice. Saikosaponin D affects APAP metabolism, increases GSH levels but does not alter PPAR activation. Saikosaponin D (2 mg/kg/day, i.p.) also suppresses APAP-induced increases in the expressionof STAT3 target genes and pro-inflammatory cytokines and inhibits APAP-induced activation of ST

8、AT3 andNF-kB 2.PROTOCOLCell Assay 1 Cell viability is assessed by morphology and by reduction of the tetrazolium salt (MTT). Briefly, the THP-1cells (2 105 cells/well) and various concentrations of compounds 1-4 (including Saikosaponin D) are addedto the 96-well plates, incubated for 48 h at 37C, an

9、d 5 L of MTT solution (5 mg/mL in PBS) is added toeach well of the 96-well plates. After incubation for 4 h at 37C, the absorbance is measured at 540 nm usinga microplate reader with the reference absorbance at 650 nm 1.MCE has not independently confirmed the accuracy of these methods. They are for

10、reference only.Animal Mice 2Administration 2 Male 6- to 7-week-old C57BL6 mice are randomly divided into four groups, vehicle/control, Saikosaponin D(SSd)/control, vehicle/APAP, and SSd/APAP, and killed 4 h or 24 h after single APAP injection. For overdoseof acetaminophen (APAP) injection, a typical

11、 single dose of 200 mg/kg/day is used. Saikosaponin D, 2 mg/kgonce daily is used as the dosing regimen. Saikosaponin D powder is dissolved in a saline solutionsupplemented with 0.1% Tween 20 and is administered by intraperitoneal injection at a dose of 2 mg/kg/dayonce daily for five days. Saline sol

12、ution containing 0.1% Tween 20 without Saikosaponin D is administeredas a vehicle. APAP is dissolved in warm saline solution (20 mg/mL) and is injected intraperitoneally 30minutes after the last Saikosaponin D injection. Saline is injected to mice in the control groups 2.MCE has not independently co

13、nfirmed the accuracy of these methods. They are for reference only.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEREFERENCES1. Jang MJ, et al. Saikosaponin D isolated from Bupleurum falcatum inhibits selectin-mediated cell adhesion. Molecules. 2014 Dec4;19(12):20340-9.2. Liu A, et al. Saikosaponin

14、 d protects against acetaminophen-induced hepatotoxicity by inhibiting NF-B and STAT3 signaling. Chem BiolInteract. 2014 Nov 5;223:80-6.3. Que R, et al. Estrogen receptor-dependent effects of saikosaponind on the suppression of oxidative stress-induced rat hepatic stellate cellactivation. Int J Mol Med. 2018 Mar;41(3):