摘要
该研究运用药物分子片段原理及拼合原理,开发了一种新的芒柄花素三氮唑衍生物,采用MTT法对5种癌细胞进行了活性筛选,选取抗肿瘤活性最强的化合物及其对应的细胞株进行进一步的抗肿瘤活性研究。通过检测化合物对肿瘤细胞增殖、迁移、周期、凋亡、自噬等方面的影响,综合评价化合物的抗肿瘤活性,并通过分子对接实验预测相关通路,对相关蛋白进行检测。结果表明7-[7-(2H-1,2,3-三氮唑-2-基)庚基]芒柄花素醚(FN.12)对人胃癌细胞HGC-27的活性较为突出,IC50值达到8.52μmol/L。此外FN.12对HGC-27细胞有较强的增殖、迁移抑制作用,能阻滞HGC-27细胞于S期,还可诱导HGC-27细胞的凋亡和自噬,且这些影响可能是通过PI3K/Akt/mTOR信号通路实现的。
In this study,a new triazole derivative of formononetin was developed based on the principle of drug molecular fragments and combination.Five kinds of cancer cells were screened by MTT method,and the compounds with the strongest anti-tumor activity and their corresponding cell lines were selected for further anti-tumor activity study.By detecting the effects of the compounds on tumor cell proliferation,migration,cycle,apoptosis and autophagy,the anti-tumor activity of the compounds was comprehensively evaluated,and the related pathways were predicted by molecular docking experiments,and the related proteins were detected.The results showed that the activity of 7-[7-(2H-1,2,3-triazole-2-yl)heptyl]formononetin ether(FN.12)on human gastric cancer cell line HGC27 was prominent,and the IC50 value was 8.52μmol/L.Besides,FN.12 can inhibit the proliferation and migration of HGC-27 cells,block HGC-27 cells in S phase,induce apoptosis and autophagy of HGC-27 cells,and these effects may be achieved through PI3K/Akt/mTOR signal pathway.
作者
崔焕杰
唐泽
赵岩
韩佳宏
蔡恩博
CUI Huanjie;TANG Ze;ZHAO Yan;HAN Jiahong;CAI Enbo(College of Traditional Chinese Medicine,Jilin Agricultural University,Changchun 130118,China;Department of Thoracic Surgery,the First Hospital of Jilin University,Changchun 130021,China)
出处
《中国细胞生物学学报》
CAS
CSCD
2024年第6期1112-1120,共9页
Chinese Journal of Cell Biology
基金
吉林省科技发展计划(批准号:20210101234JC)资助的课题。
