[Description]:
Theophylline (1,3-Dimethylxanthine) monohydrate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) monohydrate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) monohydrate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) monohydrate induces apoptosis. Theophylline (1,3-Dimethylxanthine) monohydrate can be used for asthma and chronic obstructive pulmonary disease (COPD) research[1][2][3][4][5].
[Related Catalog]:
[Target]
Human Endogenous Metabolite
[In Vitro]
Theophylline (1,3-Dimethylxanthine) monohydrate (1-1000 µM) inhibits cAMP hydrolysis by PDE in homogenates of bronchial tissue to relax human bronchus and pulmonary arteries[1]. Theophylline (1,3-Dimethylxanthine) monohydrate (10 µg/mL; 24 h; eosinophils) induces apoptosis through a reduction in the antiapoptotic protein Bcl-2[2]. Theophylline (1,3-Dimethylxanthine) monohydrate (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[3]. Theophylline (1,3-Dimethylxanthine) monohydrate (0-1000 µM; 30 min; A549 cells) induces histone deacetylase activity to decrease inflammatory gene expression[4]. Western Blot Analysis[3] Cell Line: A549 cells Concentration: 0, 20, 100 and 500 µM Incubation Time: 2 hours Result: Decreased the expression of NF-κB p65 and I-κBα degradation in a concentration-dependent manner. Western Blot Analysis[2] Cell Line: Eosinophils Concentration: 10 µg/mL Incubation Time: 24 hours Result: Decreased the expression of Bcl-2.
[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[1]. Animal Model: Male Swiss mice[1] Dosage: 100 mg/kg Administration: Intraperitoneal injection; daily, for 9 days Result: Increased IL-6 and IL-10 levels and inhibited TNF-α and NO.
[References]
[1]. Rabe KF, et, al. Theophylline and selective PDE inhibitors as bronchodilators and smooth muscle relaxants. Eur Respir J. 1995 Apr;8(4):637-42.
[2]. Chung IY, et, al. The downregulation of Bcl-2 expression is necessary for theophylline-induced apoptosis of eosinophil. Cell Immunol. 2000 Aug 1;203(2):95-102.
[3]. Ichiyama T, et, al. Theophylline inhibits NF-kappa B activation and I kappa B alpha degradation in human pulmonary epithelial cells. Naunyn Schmiedebergs Arch Pharmacol. 2001 Dec;364(6):558-61.
[4]. Ito K, et, al, Adcock IM, Barnes PJ. A molecular mechanism of action of theophylline: Induction of histone deacetylase activity to decrease inflammatory gene expression. Proc Natl Acad Sci U S A. 2002 Jun 25;99(13):8921-6.
[5]. Barnes PJ. Theophylline. Am J Respir Crit Care Med. 2013 Oct 15;188(8):901-6.