| 内容提要: |
Inflammation underlies the pathogenesis of various human diseases, which affect a certain population worldwide and posses extremely complicated pathogenic mechanisms. To date, targeting cyclic nucleotide phosphodiesterase type 4 (PDE4) has been verified as an effective therapeutic strategy. lavonoids are widely distributed in many fruits and plants, and it has been shown that most flavonoids have anti-inflammatory activity. We therefore focus on a series of flavonoids because of their related structure—featured with an unsaturated benzo-g-pyrone (A and C Rings) displaced to a phenyl (B-ring) and hydroxyl groups in the C3-position or C3’-position. They showed to exhibit inhibitory effects against PDE4 enzymes in different degrees. And, molecular docking calculations were also applied to complement the inhibitory activity studies and to predict the binding model of the flavonoids to the three-dimensional structure of PDE4. |