18β-甘草次酸作用機制 - Medchemexpress - MCE中國

1、Product Data Sheet18-Glycyrrhetinic acidCat. No.: HY-N0180CAS No.: 471-53-4分式: CHO分量: 470.68作靶點: Endogenous Metabolite作通路: Metabolic Enzyme/Protease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 : 250 mg/mL (531.15 mM)* means soluble, but saturation unknown.Solv

2、entMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 2.1246 mL 10.6229 mL 21.2459 mL5 mM 0.4249 mL 2.1246 mL 4.2492 mL10 mM 0.2125 mL 1.0623 mL 2.1246 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?shù)娜芙?/p>

3、案。以下溶解案都請先按照 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)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使； 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: 2.17 mg/mL (4.61 mM); Clear solution此案可獲得 2.17 mg/mL (4.61 mM，飽和度未知) 的澄清溶液。以 1 m

4、L 作液為例，取 100 L 21.7 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 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% corn oilSolubility: 2.17 mg/mL (4.61 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.17 mg/mL (4.61 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 21.7 mg

5、/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 18-Glycyrrhetinic acid草的主 物活性成分，具有抗?jié)?，抗炎和抗增殖的特性。IC & Target Human Endogenous Metabolite體外研究 18-Glycyrrhetinic acid is the major bioactive component of Glycyrrhizae Radix and possesses anti-ulcerative, anti-inflammatory and antiproliferative prop

6、erties. MTS assay demonstrates that 24 h treatment of 18-Glycyrrhetinic acidsuppresses cell proliferation in both cell lines in a dose-dependent manner. 18-Glycyrrhetinic acid at 160 Msignificantly decreases the percentage of viable cells to around 40.510.5% in A549 and 38.34.6% in NCI-H460(p0.01 re

7、spectively). When the cells are treated with 320 M 18-Glycyrrhetinic acid, a greater inhibitory effects oncell proliferation is shown, as the percentage of viable cells is below 30% compare with untreated controls (p0.001).Treatment with 18-Glycyrrhetinic acid at 160 M and 320 M decreases the levels

8、 of full-length PARP and increasesthe levels of cleaved-PARP1.體內(nèi)研究 Rats in 18-Glycyrrhetinic acid+Triptolide (TP) group which receive low-dose 18-Glycyrrhetinic acid (50 mg/kg) havesignificant reductions in the three serum parameters when compare with TP rats. Rats in 18-Glycyrrhetinic acid+TP group

9、 which receive the high-dose 18-Glycyrrhetinic acid (100 mg/kg) have slightly lowered the levels of three liverenzymes, the reductions do not reach statistical significance compare with TP group. Contrastingly, preadministrationof low-dose 18-Glycyrrhetinic acid protects animals from TP-induced hepa

10、tic lesions. On the contrary, low-dose 18-Glycyrrhetinic acid (50 mg/kg) markedly suppresses the release of the four cytokines above3.PROTOCOLCell Assay 2 Primary microglia cultures are used in this study. For treatment assay, microglia are incubated with complete DMEMand stimulated with or without

11、100 ng/mL IFN- in the presence or absence of 18-Glycyrrhetinic acid (25 M and50 M) at 37C in a humidified incubator with 5% CO2. For cell migration assay, the isolated primary microglia thatseeded in complete DMEM medium are stimulated with or without IFN- (100 ng/mL), and treated with differentdose

12、s of 18-Glycyrrhetinic acid, 24 h later, the microglia culture supernatants are collected and added to the lowerchambers of Transwell inserts2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Healthy Wistar rats (male, 20020 g) are used and divide

13、d into five groups with 10 individuals for each groupAdministration 3 randomly. Animals in normal control (NC) group receive distilled water for 6 days and 0.5% CMC-Na for the last 3days. Rats in Triptolide model group (TP), 18-Glycyrrhetinic acid low-dose group (GAL+TP), and 18-Glycyrrhetinicacid h

14、igh-dose group (GAH+TP) receive distilled water, 18-Glycyrrhetinic acid (50 mg/kg, p.o., dissolved in distilledwater), or 18-Glycyrrhetinic acid (100 mg/kg, p.o., dissolved in distilled water) for consecutive 6 days, respectively,and liver injury is induced by TP (2.4 mg/kg, p.o., suspended in 0.5%

15、CMC-Na) for the last 3 days. Animals in theabove three groups receive TP 6 hours after distilled water or 18-Glycyrrhetinic acid treatment on the last 3 days3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCESPage 2 of 3 www.MedChemE1. Huang RY,

16、 et al. 18-Glycyrrhetinic acid suppresses cell proliferation through inhibiting thromboxane synthase in non-small cell lung cancer. PLoS One.2014 Apr 2;9(4):e93690.2. Zhou J, et al. 18-glycyrrhetinic acid suppresses experimental autoimmune encephalomyelitis through inhibition of microglia activation and promotionof remyelination. Sci Rep. 2015 Sep 2;5:13713.3. Yang G, et al. Protective Effect of 18-Glycyrrhetinic Acid against Triptolide-Induced Hepatotoxicity in Rats. Evid Based Complement Al