Objective To investigate the effect of Apigenin on the Aminopeptidase N (APN) activity of lung cancer cells and inhibitory mechanisms for mouse hepatitis virus A549 (A549) growth. Methods The inhibition effect and lag time of Apigenin on APN were analyzed using enzyme inhibition and kinetic method. The inhibitory tests of the growth of lung cancer cell A549 and lung normal cell MRC-5 were performed, and the interaction mechanisms of Apigenin on APN was performed by zinc chelation experiment and molecular docking. Results Apigenin had the inhibitory effect on the growth of lung cancer cell A549 and little toxicity to normal lung cell MRC-5, and it was a reversible and competi-tive inhibitor [inhibitory concentration 50 (IC50):(71. 22 ± 2. 43)μmol/L]; zinc chelation experiment and molecular docking showed that Apigenin combined with Zn ions in APN active center preferentially, and formed hydrogen bonds with catalytic groups of His383 and Glu350. Conclusion Apigenin is a competitive APN inhibitor, and it has a special inhibitory effect on the growth of lung cancer cells A549.
ApigeninLung cancer cells A549Aminopeptidase NInhibitory effectMolecular mimicry
国家科技期刊平台
NSTL
维普
万方数据
