CAJ | 학술논문

目的：探讨芹菜素对肺癌细胞氨肽酶N活性的影响及其对肺癌细胞A549生长抑制作用的机制。方法采用酶抑制动力学方法，观察芹菜素对氨肽酶N的抑制作用和延滞时间；进行肺癌细胞A549和肺正常细胞MRC-5生长的抑制试验；通过锌离子螯合实验和分子对接研究芹菜素与氨肽酶N的相互作用机制。结果芹菜素能够对肺癌细胞A549的生长产生抑制作用，对正常细胞MRC-5具有较低的毒性，且是一种可逆的竞争型氨肽酶N抑制剂[半数抑制浓度(IC50)为(71.22±2.43)μmol/L]；锌离子螯合实验和分子模拟结果表明，芹菜素能够优先结合到氨肽酶N的活性中心锌离子附近，并与催化基团His383和Glu350形成氢键。结论芹菜素是一种竞争性的氨肽酶N抑制剂，能够特异性地对肺癌细胞A549的生长起到抑制作用。
목적：탐토근채소대폐암세포안태매N활성적영향급기대폐암세포A549생장억제작용적궤제。방법채용매억제동역학방법，관찰근채소대안태매N적억제작용화연체시간；진행폐암세포A549화폐정상세포MRC-5생장적억제시험；통과자리자오합실험화분자대접연구근채소여안태매N적상호작용궤제。결과근채소능구대폐암세포A549적생장산생억제작용，대정상세포MRC-5구유교저적독성，차시일충가역적경쟁형안태매N억제제[반수억제농도(IC50)위(71.22±2.43)μmol/L]；자리자오합실험화분자모의결과표명，근채소능구우선결합도안태매N적활성중심자리자부근，병여최화기단His383화Glu350형성경건。결론근채소시일충경쟁성적안태매N억제제，능구특이성지대폐암세포A549적생장기도억제작용。
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.