Research progress in phosphodiesterase 4 inhibitors in treatment of inflammatory bowel diseases / 中国药理学与毒理学杂志

ABSTRACT

Inflammatory bowel disease (IBD) is a chronic idiopathic intestinal inflammatory disease that affects all parts of the intestine. Phosphodiesterase 4 (PDE4) is a key enzyme that mediates inflammation, and its inhibitor is useful in many inflammatory diseases. In this review, we summarize the research progress in PDE 4 inhibitors in the treatment of IBD in preclinical studies, such as rolipram, mesopram, roflumilast, tetomilast and apremilast, as well as PDE4 inhibitors in clinical studies, such as apremilast and tetomilast. All PDE4 inhibitors have shown therapeutic effect on IBD, and the mechanisms involve the inhibition of cytokine release, such as tumor necrosis factor-α, lnterleukin-8, suppression thr inflammation in colon, enhancement of the barrier of the intensine, and reduction of the collagen deposition. As a novel drug for IBD therapy, PDE4 inhibitor apremilast might have therapeutic benefit in IBD, and roflumilast, which is yet to enter clinical trial, may have a good therapeutic prospect.