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CAS No. : 58-55-9
MCE 国际站:Theophylline
产品活性:Theophylline (1,3-Dimethylxanthine) 是有效的磷酸二酯酶 (PDE) 抑制剂,腺苷受体拮抗剂,和组蛋白脱乙酰酶 (HDAC) 活化剂。Theophylline (1,3-Dimethylxanthine) 抑制 PDE3 活性,放松气道平滑肌。Theophylline (1,3-Dimethylxanthine) 通过增加 IL-10 和抑制 NF-κ B进入细胞核而具有抗炎活性。Theophylline (1,3-Dimethylxanthine) 诱发细胞凋亡 (apoptosis)。Theophylline (1,3-Dimethylxanthine) 可用于哮喘和慢性阻塞性肺疾病 (COPD) 的研究。
研究领域:Metabolic Enzyme/Protease | GPCR/G Protein | Cell Cycle/DNA Damage | Epigenetics | Apoptosis | Immunology/Inflammation
作用靶点:Phosphodiesterase (PDE) | Adenosine Receptor | HDAC | Apoptosis | Interleukin Related | TNF Receptor | Endogenous Metabolite
结构分类:生物碱 | 结构分类
来源:植物 | 山茶科 | 茶
In Vitro: Theophylline (1,3-Dimethylxanthine) (1-1000 µM) inhibits cAMP hydrolysis by PDE in homogenates of bronchial tissue to relax human bronchus and pulmonary arteries.
Theophylline (1,3-Dimethylxanthine) (10 µg/mL; 24 h; eosinophils) induces apoptosis through a reduction in the antiapoptotic protein Bcl-2.
Theophylline (1,3-Dimethylxanthine) (0-500 µM; 2 h; A549 cells) inhibits NF-κB activation, I kappa B alpha (I-κBα) degradation and decreases the level of IL-6 in a concentration-dependent manner.
Theophylline (1,3-Dimethylxanthine) (0-1000 µM; 30 min; A549 cells) induces histone deacetylase activity to decrease inflammatory gene expression.
In Vivo: Theophylline (1,3-Dimethylxanthine) (100 mg/kg; i.p.; daily, for 9 d; male Swiss mice) has anti-inflammatory activity in mice and increases IL-6 and IL-10 levels and inhibits TNF-α and NO.
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