Theophylline (1,3-Dimethylxanthine) sodium glycinate is a potent phosphodiesterase (PDE) inhibitor that targets PDE3 to relax airway smooth muscle and is used in asthma and chronic obstructive pulmonary disease (COPD) research. It also functions as an adenosine receptor antagonist, histone deacetylase (HDAC) activator, and exhibits anti-inflammatory activity by increasing IL-10 levels and inhibiting NF-κB nuclear import, while inducing 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].