Theophylline (1,3-Dimethylxanthine) sodium glycinate is a potent inhibitor of phosphodiesterase (PDE) that inhibits PDE3 activity to relax airway smooth muscle. Theophylline sodium glycinate can be used for the research of asthma and chronic obstructive pulmonary disease (COPD). Theophylline sodium glycinate is also an adenosine receptor antagonist and histone deacetylase (HDAC) activator. Theophylline sodium glycinate has anti-inflammatory activity by increasing IL-10 and inhibiting NF-κB nucleus import. Theophylline sodium glycinate induces apoptosis [1] [2] [3] [4] [5].

Theophylline sodium glycinate (1-1000 μM) inhibits cAMP hydrolysis by PDE in homogenates of bronchial tissue to relax human bronchus and pulmonary arteries [1]. Theophylline sodium glycinate (10 μg/mL; 24 h) induces apoptosis through a reduction in the antiapoptotic protein Bcl-2 in eosinophils [2]. Theophylline sodium glycinate (0-500 μM; 2 h) 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 sodium glycinate (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 dose-dependent manner.

Theophylline sodium glycinate (100 mg/kg; i.p.; daily, for 9 d) has anti-inflammatory activity in mice and increases IL-6 and IL-10 levels and inhibits TNF-α and NO in male Swiss mice [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.