氧化苦參堿作用機制 - Medchemexpress - MCE中國

1、Product Data SheetOxymatrineCat. No.: HY-N0158CAS No.: 16837-52-8分式: CHNO分量: 264.36作靶點: TGF-beta/Smad; Influenza Virus作通路: Stem Cell/Wnt; TGF-beta/Smad; Anti-infection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 : 100 mg/mL (378.27 mM; Need ultrasonic)H2O : 10

2、0 mg/mL (378.27 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 3.7827 mL 18.9136 mL 37.8272 mL5 mM 0.7565 mL 3.7827 mL 7.5654 mL10 mM 0.3783 mL 1.8914 mL 3.7827 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 個內使，-2

3、0C 儲存時，請在 1 個內使。體內實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?。以下溶解案都請先按?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: 2.5 mg/mL (9.46 mM); Clear solution此案可獲得

4、 2.5 mg/mL (9.46 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 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% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (9.46 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (9.46 mM，飽和度未知) 的澄

5、清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (9.46 mM); Clear solution; Need warming此案可獲得 2.5 mg/mL (9.46 mM) 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 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTI

6、VITY物活性 Oxymatrine來槐屬物種根部的物堿，具有抗炎，抗纖維化和抗腫瘤的作。能抑制iNOS表達和TGF-/Smad通路。Oxymatrine 可抑制博卡病毒 MVC 復制，降低病毒基因表達并減少病毒感染誘導的細胞凋亡 (apoptosis)。體外研究 Oxymatrine, an alkaloid component extracted from the roots of Sophora species, has been shown to haveantiinflammatory, antifibrosis, and antitumor effects and the abil

7、ity to protect against myocardial damage, etc. Thepotential signaling pathways involved in the clinical application of oxymatrine might include the TGF-/Smad, tolllikereceptor 4/nuclear factor kappa-light-chain-enhancer of activated B cells, toll-like receptor9/TRAF6, Januskinase/signal transduction

8、 and activator of transcription, phosphatidylinositol-3 kinase/Akt, delta-opioidreceptorarrestinl-Bcl-2, CD40, epidermal growth factor receptor, nuclear factor erythroid-2-related factor2/hemeoxygenase-1 signaling pathways, and dimethylarginine dimethylaminohydrolase/asymmetric dimethylargininemetab

9、olism pathway1. Oxymatrine significantly inhibits the proliferation of DU145 and PC-3 cell lines in a time- anddose-dependent manner. By contrast, following treatment with oxymatrine, PNT1B healthy human prostate cellproliferation is not inhibited2.體內研究 The volume and weight of tumors in mice signif

10、icantly decreased in a dose-dependent manner. Oxymatrine mayreduce prostate cancer cell growth by promoting cell apoptosis in vivo2. Oxymatrine is effective in reducing the production and deposition of collagen in the liver tissue of experimental rats. Oxymatrine could promote theexpression of Smad

11、7 and inhibit the expression of Smad 3 and CBP in CCl4-induced hepatic fibrosis in SD rats, couldmodulate the fibrogenic signal transduction of TGF-Smad pathway3.PROTOCOLCell Assay 2 DU145, PC-3 and PNT1B cell lines (3104 cells/well) are seeded into 96-well plates and incubated overnight at 37Cin 5%

12、 CO2. Subsequently, the cells are incubated with different concentrations of oxymatrine (0, 2, 4, 6 and 8 mg/mL).MTT (10 mL; 5 mg/mL) is added and the mixture is incubated in darkness at 37C for 2 h. Absorbance is measured ata wavelength of 490 nm using a microplate reader2.MCE has not independently

13、 confirmed the accuracy of these methods. They are for reference only.Animal Rats: One hundred healthy male SD rats (weight 140-160 g) are used in the study. All 100 rats are randomLy dividedAdministration 23 into three groups: Control (n=20), Treatment (n=40) and Model group (n=40). For the model g

14、roup, 300 g/L CCl4soluted in liquid paraffin is injected subcutaneously at a dosage of 3 mL/kg twice per week6. The treated ratsreceive Oxymatrine celiac injections at 10 mg/kg twice a week besides the injection of CCl43.Mice: BALB/c homozygous (nu/nu) nude mice are used in the study. 24 tumor-beari

15、ng mice are randomLy dividedinto three groups: The control group is treated with PBS, and two groups are treated with different concentrations ofoxymatrine (50 mg/kg and 100 mg/kg body weight). Oxymatrine is administered to the mice, using dailyPage 2 of 3 www.MedChemEintraperitoneal injections2.MCE

16、 has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 J Med Chem. 2019 Sep 12;62(17):7961-7975. Front Physiol. 2020 May.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Lu ML, et al. Potential Signaling Pathways Involv

17、ed in the Clinical Application of Oxymatrine. Phytother Res. 2016 Jul;30(7):1104-12.2. Wu C, et al. Oxymatrine inhibits the proliferation of prostate cancer cells in vitro and in vivo. Mol Med Rep. 2015 Jun;11(6):4129-34.3. Wu XL, et al. Effect of Oxymatrine on the TGFbeta-Smad signaling pathway in rats with CCl4-induced hepatic fibrosis. World J Gastroenterol. 2008 Apr7;14(13):2100-5.4. Ding Y, et al. Oxymatrine Inhibits Bocavirus MVC Replication, Reduces Viral Gene Expression and Decreases Apoptosis Induced by Vi