期刊论文详细信息
Journal of Enzyme Inhibition and Medicinal Chemistry
Antiproliferative chromone derivatives induce K562 cell death through endogenous and exogenous pathways
Runwei Jiao1  Dahong Li1  Haonan Li1  Zhanlin Li1  Huiming Hua1  Xiaofang Huang1  Hao Cao2  Linghe Zang2  Weiwei Liu3  Fanxing Xu3 
[1]Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University
[2]School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University
[3]Wuya College of Innovation, Shenyang Pharmaceutical University
关键词: chromone;    nitric oxide;    antiproliferative;    selectivity;    apoptosis;   
DOI  :  10.1080/14756366.2020.1740696
来源: DOAJ
【 摘 要 】
A series of furoxan derivatives of chromone were prepared. The antiproliferative activities were tested against five cancer cell lines HepG2, MCF-7, HCT-116, B16, and K562, and two normal human cell lines L-02 and PBMCs. Among them, compound 15a exhibited the most potent antiproliferative activity. It was also found 15a produced more than 8 µM of NO at the peak time of 45 min by Griess assay. Generally, antiproliferative activity is positively related to NO release to some extent. Further in-depth studies on apoptosis-related mechanisms showed that 15a caused S-phase cell cycle arrest in a concentration-dependent manner and induced apoptosis significantly through mitochondria-related pathways. Human apoptosis protein array assay also demonstrated 15a increased the expression levels of pro-apoptotic Bax, Bad, HtrA2 and Trail R2/DR5. The expression of catalase and cell cycle blocker claspin were similarly up-regulated. In balance, 15a induced K562 cells death through both endogenous and exogenous pathways.
【 授权许可】

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