Kinase Assay: |
Science China Chemistry,2009, 52(3):332-7. | Screening and docking studies of natural phenolic inhibitors of carbonic anhydrase II.[Reference: WebLink] | Carbonic anhydrase II (CA II) is an important enzyme complex with Zn2+, which is involved in many physiological and pathological processes, such as calcification, glaucoma and tumorigenicity.
METHODS AND RESULTS:
In order to search for novel inhibitors of CA II, inhibition assay of carbonic anhydrase II was performed, by which seven natural phenolic compounds, including four phenolics (grifolin, 4-O-methyl-Grifolic acid, Grifolic acid, and isovanillic acid) and three flavones (eriodictyol, quercetin and puerin A), showed inhibitory activities against CA II with IC50s in the range of 6.37–71.73 μmol/L. Grifolic acid is the most active one with IC50 of 6.37 μmol/L. These seven phenolic compounds were proved to be novel natural carbonic anhydrase II inhibitors, which were obtained in flexible docking study with GOLD 3.0 software.
CONCLUSIONS:
Results indicated that the aliphatic chain and polar groups of hydroxyl and carboxyl are important to their inhibitory activities, providing a new insight into study on CA II potent inhibitors. |
|