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, at concentrations ranging from 1-1000 μM, effectively inhibits cyclic AMP (cAMP) hydrolysis by phosphodiesterase (PDE) in bronchial tissue homogenates, consequently relaxing human bronchus and pulmonary arteries [1]. At a specific concentration of 10 μg/mL for 24 hours, it promotes apoptosis by reducing levels of the antiapoptotic protein Bcl-2 in eosinophils [2]. Additionally, within the range of 0-500 μM over 2 hours, this compound suppresses NF-κB activation, I kappa B alpha (I-κBα) degradation, and lowers IL-6 concentration in a concentration-dependent manner [3]. Furthermore, when applied to A549 cells at 0-1000 μM for 30 minutes, it activates histone deacetylase, leading to a reduction in inflammatory gene expression [4]. Western Blot Analysis on A549 cells, using concentrations of 0, 20, 100, and 500 μM for 2 hours, confirms a dose-dependent decrease in the expression of NF-κB p65 and I-κBα degradation [3].

Theophylline sodium glycinate, administered via intraperitoneal injection at a dosage of (100 mg/kg; i.p.; daily, for 9 d), exhibits anti-inflammatory effects in male Swiss mice by elevating IL-6 and IL-10 concentrations while suppressing TNF-α and NO levels [1].