氧化苦参碱 T2754

Product Introduction
Bioactivity


英文名: Oxymatrine

描述: Oxymatrine (Oxysophoridine) 是来自槐属物种根部的一种生物碱，具有抗炎，抗纤维化和抗肿瘤的作用。它是一种用于治疗乙型肝炎病毒的中药。它可抑制博卡病毒 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。它还可以抑制 iNOS 的表达和 TGF-β/Smad 通路。

细胞实验: DU145, PC-3 and PNT1B cell lines (3×104 cells/well) are seeded into 96-well plates and incubated overnight at 37°C in 5% 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 37°C for 2 h. Absorbance is measured at a wavelength of 490 nm using a microplate reader[2].

激酶实验: P450 Inhibition Studies: Pooled human liver microsomes (HLM) from at least 15 donors are used for all inhibition assays. For IC50 determinations, the substrate probes are used at their approximate in vitro Km values. All incubations are performed with 100 mM potassium phosphate buffer (pH 7.4) and 1 mM NADPH. For CYP1A2 inhibition study, incubations are performed in a total volume of 0.5 ml, in duplicates with 0.1 mg/ml HLM, 30 μM phenacetin, 1 mM NADPH, and in the presence of avasimibe (0, 0.3, 0.75, 1.5, 3, 7.5, 15, 30, and 40 μM in 50 mM) in a potassium phosphate buffer at pH 7.4. After preincubation at 37 °C for 7 min, NADPH is added to initiate the enzyme reaction. The reaction mixture is quenched with 500 μl of ice-cold 100 ng/ml paracetamol-D4/CH3CN after 25 min. The standards (4-acetamidophenol, singlet) and quality controls (triplicates for low, medium, and high) are prepared at room temperature. After mixing, 0.2 ml of the samples is transferred to another plate and submitted for LC/MS/MS analysis after centrifugation at 3000 rpm for 10 min. A Supelco Discovery Amide C16, 100 × 2.1 mm (5-μm particle size) column (Supelco, Bellefonte, PA) is used. The mobile phase is isocratic, 40:60 [acetonitrile/formic acid, 0.1% (v/v)] at 0.2 ml/min.

体内活性: LD50 in mouse: 521 mg/kg, i.p.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 100 mg/mL (378.27 mM)
H2O : 33.33 mg/ml(126.09 mM)


关键字: TGF-beta/Smad | Inhibitor | inhibit | Transforming growth factor beta | Influenza Virus | Oxymatrine

相关产品: Tofacitinib Citrate | Oseltamivir phosphate | Octyl gallate | Neuraminidase-IN-1 | Elemicin | Chloroxylenol | Camphor | Trifluoperazine | Sophocarpine monohydrate | EBOV-IN-1

相关库: Drug Repurposing Compound Library | FDA-Approved & Pharmacopeia Drug Library | Anti-Cancer Drug Library | Inhibitor Library | Traditional Chinese Medicine Monomer Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | Food as Medicine Compound Library | TGF-beta/Smad Compound Library | Reprogramming Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途