甘草素作用机制 - Medchemexpress - MCE中国

1、Product Data SheetLiquiritigeninCat. No.: HY-N0377CAS No.: 578-86-9分式: CHO分量: 256.25作靶点: Estrogen Receptor/ERR作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 125 mg/mL (487.80 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 3.902

2、4 mL 19.5122 mL 39.0244 mL5 mM 0.7805 mL 3.9024 mL 7.8049 mL10 mM 0.3902 mL 1.9512 mL 3.9024 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可

3、靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.42 mg/mL (9.44 mM); Clear solution此案可获得 2.42 mg/mL (9.44 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 24.2 mg/mL 的澄 DMSO 储备液加到 400 L PEG3

4、00 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.42 mg/mL (9.44 mM); Clear solution此案可获得 2.42 mg/mL (9.44 mM，饱和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液为例，取 100 L 24.2 mg/mL 的澄均匀。DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合3. 请依序添加

5、每种溶剂： 10% DMSO 90% corn oilSolubility: 2.42 mg/mL (9.44 mM); Clear solution此案可获得 2.42 mg/mL (9.44 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 24.2 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Liquiritigenin 从草中分离出的 EC50 值为36.5 nM。烷酮，它 种度选择性的雌激素受体 (ER) 激动剂，于活化ERE tk-Luc的IC & Ta

6、rget EC50: 36.5 nM (activation of the ERE tk-Luc)1体外研究 Liquiritigenin produces a dose-response activation of ERE tk-Luc in the U2OS cells transfected with ER, but not ER.Liquiritigenin produces a dose-dependent activation and a time-dependent increase of the CECR6, NKG2E and NKDwith ER but not with

7、ER. The ER-selectivity of liquiritigenin is due to the selective recruitment of the coactivatorsteroid receptor coactivator-2 to target genes. Liquiritigenin exhibits similar binding affinities for ER and ER, andcauses the recruitment of SRC-2 to target genes selectively in ER cells1. Pretreatment o

8、f MC3T3-E1 cells withliquiritigenin prevents the MG-induced cell death and production of protein adduct, intracellular reactive oxygenspecies, mitochondrial superoxide, cardiolipin peroxidation, and TNF- in osteoblastic MC3T3-E1 cells2.体内研究 In a mouse xenograph model, liquiritigenin does not stimula

9、te uterine size or tumorigenesis of MCF-7 breast cancercells1. Treatment with liquiritigenin significantly reduces the concentrations of pro-inflammatory cytokines includinginterleukin (IL)-6, IL-1 and tumor necrosis factor (TNF)- in serum and hippocampus3.PROTOCOLKinase Assay 1 The relative binding

10、 affinity of liquiritigenin to pure full-length ER and ER is determined using ER and ERcompetitor assay kits. Fluorescence polarization of the fluorophore-tagged estrogen bound to ER and ER in thepresence of increasing amounts of competitor ligand or extract is determined using the GENios Pro microp

11、latereader with fluorescein excitation (485 nM) and emission (530 nM) filters1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: MCF-7 (250,000) cells are grafted under the kidney capsule of nude mice. Five mice per group are treated withAdmi

12、nistration 1 a continuous infusion using osmotic pumps containing vehicle, E2 (0.4 mg) or liquiritigenin (2 mg) that infused 2.5 L/h for 1 month. After one month of treatment, the tumors and uteri are removed and analyzed1.MCE has not independently confirmed the accuracy of these methods. They are f

13、or reference only.REFERENCES1. Mersereau JE, et al. Liquiritigenin is a plant-derived highly selective estrogen receptor beta agonist. Mol Cell Endocrinol. 2008 Feb 13;283(1-2):49-57.2. Suh KS, et al. Protective effect of liquiritigenin against methylglyoxal cytotoxicity in osteoblastic MC3T3-E1 cells. Food Funct. 2014 Jul 25;5(7):1432-40.3. Tao W, et al. Liquiritigenin reverses depression-like behavior in unpredictable chronic mild stress-induced mice by regulating PI3K/Akt/mTOR mediatedPage 2 of 3 www.MedChemEBDNF/TrkB pathway. Behav Brain Res. 2016 Jul 15;308:177-86.McePdfHeightC