氧化苦参碱作用机制 - Medchemexpress - MCE中国

1、Product Data SheetOxymatrineCat. No.: HY-N0158CAS No.: 16837-52-8分式: CHNO分量: 264.36作靶点: TGF-beta/Smad; Influenza Virus作通路: Stem Cell/Wnt; TGF-beta/Smad; Anti-infection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 : 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制备储备液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，-2

3、0C 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: 2.5 mg/mL (9.46 mM); Clear solution此案可获得

4、 2.5 mg/mL (9.46 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 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: 2.5 mg/mL (9.46 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.5 mg/mL (9.46 mM，饱和度未知) 的澄

5、清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (9.46 mM); Clear solution; Need warming此案可获得 2.5 mg/mL (9.46 mM) 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 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTI

6、VITY物活性 Oxymatrine来槐属物种根部的物碱，具有抗炎，抗纤维化和抗肿瘤的作。能抑制iNOS表达和TGF-/Smad通路。Oxymatrine 可抑制博卡病毒 MVC 复制，降低病毒基因表达并减少病毒感染诱导的细胞凋亡 (apoptosis)。体外研究 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.体内研究 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.户使本产品发表的科研献 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