甘草素作用機制 - Medchemexpress - MCE中國

1、Product Data SheetLiquiritigeninCat. No.: HY-N0377CAS No.: 578-86-9分式: CHO分量: 256.25作靶點: Estrogen Receptor/ERR作通路: Others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 DMSO : 125 mg/mL (487.80 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制備儲備液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；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍浮Ｒ韵氯芙獍付颊埾劝凑?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可

3、靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.42 mg/mL (9.44 mM); Clear solution此案可獲得 2.42 mg/mL (9.44 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 24.2 mg/mL 的澄 DMSO 儲備液加到 400 L PEG3

4、00 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.42 mg/mL (9.44 mM); Clear solution此案可獲得 2.42 mg/mL (9.44 mM，飽和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液為例，取 100 L 24.2 mg/mL 的澄均勻。DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合3. 請依序添加

5、每種溶劑： 10% DMSO 90% corn oilSolubility: 2.42 mg/mL (9.44 mM); Clear solution此案可獲得 2.42 mg/mL (9.44 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 24.2 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Liquiritigenin 從草中分離出的 EC50 值為36.5 nM。烷酮，它 種度選擇性的雌激素受體 (ER) 激動劑，于活化ERE tk-Luc的IC & Ta

6、rget EC50: 36.5 nM (activation of the ERE tk-Luc)1體外研究 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.體內(nèi)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