产品
编 号:F482251
分子式:C19H18O6
分子量:342.35
产品类型
结构图
CAS No: 855-97-0
联系客服
产品详情
生物活性:
5,7,3',4'-Tetramethoxyflavone, an orally active polymethoxyflavones (PMFs) that can be isolated from M. exotica, possesses various bioactivities, including anti-fungal, anti-malarial, anti-mycobacterial, and anti-inflammatory activities. 5,7,3',4'-Tetramethoxyflavone exhibits chondroprotective activity by targeting β-catenin signaling.
体内研究:
5,7,3',4'-Tetramethoxyflavone (25-100 mg/kg, 灌胃) 在大鼠体内表现出软骨保护活性。5,7,3',4'-Tetramethoxyflavone (5-20 mg/kg; 静脉注射, 口服) 在大鼠中绝对生物利用度为 14.3 %。1.19药代动力学分析RouteDose (mg/kg)AUC (min μg/mL)AUC/Dose (min/mL)t1/2 (h)Tmax (h)Cmax (ng/mL)Bioavailability (%)
i.v.5161.49 ± 58.78 0.1154 ± 0.042062.85 ± 27.92// 14.3
p.o.50231.43 ± 71.87 0.0165 ± 0.0051 273.76 ± 90.23 190.34 ± 24.500.79 ± 0.30/
Animal Model:Rat knee OA model
Dosage:25-100 mg/kg
Administration:i.g.
Result:Decreased the contents of IL-1b, TNF-a, and PGE2 in a dose-dependent manner.Decreases the expression of the inflammatory cytokines in rat knee osteoarthritis (OA) synovial fluid (SF) lavages.Inhibited chondrocytes hypertrophy and decreased the cartilage thickness.Exhibited down regulation of b-catenin in a dose-dependent manner.
体外研究:
5,7,3',4'-Tetramethoxyflavone (5-20 μg/mL, 24 h) 抑制软骨细胞中 EP2、EP4、bcatenin 和 COX-2 基因的表达。5,7,3',4'-Tetramethoxyflavone (5-20 μg/mL, 48 h) 抑制软骨细胞中 EP/cAMP/PKA 信号通路和 β-catenin 信号通路蛋白的表达。5,7,3',4'-Tetramethoxyflavone (5-20 μg/mL, 4 h) 通过调节IRE1α保护软骨细胞免于凋亡。5,7,3',4'-Tetramethoxyflavone (5-20 μg/mL, 4 h) 可逆转 IRE1α 缺乏导致的内质网 (ER) 应激基因的表达模式。