Antiproliferative Evaluation of Novel 4-Imidazolidinone Derivatives as Anticancer Agent Which Triggers ROS-Dependent Apoptosis in Colorectal Cancer Cell
机构：[1]College of Pharmacy, National & Local Joint Engineering Research Center of Targeted and Innovative Therapeutics, IATTI, Chongqing University of Arts and Sciences, Chongqing 402160, China.[2]College of Pharmaceutical Sciences, Southwest University, Chongqing 400716, China.[3]Chongqing Academy of Chinese Materia Medica, Chongqing 400065, China.[4]Department of Oncology, Sichuan Cancer Hospital and Institute, Sichuan Cancer Center, School of Medicine, University of Electronic Science and Technology of China, Chengdu 610041, China.四川省人民医院四川省肿瘤医院
Colorectal cancer (CRC) is one of the most common causes of cancer-related death worldwide, and more therapies are needed to treat CRC. To discover novel CRC chemotherapeutic molecules, we used a series of previously synthesized novel imidazolidin-4-one derivatives to study their anticancer role in several cancer cell lines. Among these compounds, compound 9r exhibited the best anticancer activity in CRC cell lines HCT116 and SW620. We further investigated the anticancer molecular mechanism of compound 9r. We found that compound 9r induced mitochondrial pathway apoptosis in HCT116 and SW620 cells by inducing reactive oxygen species (ROS) production. Moreover, the elevated ROS generation activated the c-Jun N-terminal kinase (JNK) pathway, which further accelerated apoptosis. N-acetylcysteine (NAC), an antioxidant reagent, suppressed compound 9r-induced ROS production, JNK pathway activation, and apoptosis. Collectively, this research synthesized a series of imidazolidin-4-one derivatives, evaluated their anticancer activity, and explored the molecular mechanism of compound 9r-induced apoptosis in CRC cells. The present results suggest that compound 9r has a potential therapeutic role in CRC. Hence, it deserves further exploration as a lead compound for CRC treatment.
基金：
Natural Science Foundation of Chongqing, grant number
cstc2020jcyj-msxmX0595; Science and Technology Research Program of Chongqing Municipal Education
Commission, grant number KJQN201901331, KJZD-K202001302, and KJQN202201330; Scientific
Research Foundation of the Chongqing University of Arts and Sciences, grant number P2021YX05.
第一作者机构：[1]College of Pharmacy, National & Local Joint Engineering Research Center of Targeted and Innovative Therapeutics, IATTI, Chongqing University of Arts and Sciences, Chongqing 402160, China.[2]College of Pharmaceutical Sciences, Southwest University, Chongqing 400716, China.[3]Chongqing Academy of Chinese Materia Medica, Chongqing 400065, China.
共同第一作者：
通讯作者：
通讯机构：[1]College of Pharmacy, National & Local Joint Engineering Research Center of Targeted and Innovative Therapeutics, IATTI, Chongqing University of Arts and Sciences, Chongqing 402160, China.[2]College of Pharmaceutical Sciences, Southwest University, Chongqing 400716, China.[4]Department of Oncology, Sichuan Cancer Hospital and Institute, Sichuan Cancer Center, School of Medicine, University of Electronic Science and Technology of China, Chengdu 610041, China.
推荐引用方式(GB/T 7714)：
Huang Jiuhong,Wang Juanli,Song Guiting,et al.Antiproliferative Evaluation of Novel 4-Imidazolidinone Derivatives as Anticancer Agent Which Triggers ROS-Dependent Apoptosis in Colorectal Cancer Cell[J].MOLECULES.2022,27(24):doi:10.3390/molecules27248844.
APA：
Huang Jiuhong,Wang Juanli,Song Guiting,Hu Chunsheng,Xu Zhigang...&Yang Donglin.(2022).Antiproliferative Evaluation of Novel 4-Imidazolidinone Derivatives as Anticancer Agent Which Triggers ROS-Dependent Apoptosis in Colorectal Cancer Cell.MOLECULES,27,(24)
MLA：
Huang Jiuhong,et al."Antiproliferative Evaluation of Novel 4-Imidazolidinone Derivatives as Anticancer Agent Which Triggers ROS-Dependent Apoptosis in Colorectal Cancer Cell".MOLECULES 27..24(2022)
化学