期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 39, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2021.127912
关键词
Antitumor; Novel artemisinin ester derivatives; Apoptosis; ??m; ROS
资金
- Scientific Research Project of Education Department in Hunan Province [17C0973]
- Natural Science Foundation of Changsha [KQ2014081]
- National Natural Science Foundation of China [81874212]
- Key Laboratory of Study and Discovery of Small Targeted Molecules of Hunan Province, Hunan Normal University [2017TP1020]
- Huxiang High-Level Talent Innovation Team [2018RS3072]
- Major Scientific and Technological Projects for Collaborative Prevention and Control of Birth Defect in Hunan Province [2019SK1012]
- Key Grant of Research and Development in Hunan Province [2020DK2002]
Novel artemisinin ester derivatives were synthesized and compound 2c showed the most potent anti-proliferative activity against OVCAR3 cells with low cytotoxicity, likely through targeting mitochondria and inducing cell apoptosis. These findings suggest compound 2c may be a promising candidate for further investigation against ovarian cancer.
A series of novel artemisinin ester derivatives were designed and synthesized for targeting mitochondria. Cytotoxicity against SMMC-7721, HepG2, OVCAR3, A549 and J82 cancer cell lines was evaluated. Compound 2c (IC50 = 3.0 ?M) was the most potent anti-proliferative molecule against the OVCAR3 cells with low cytotoxicity in normal HUVEC cells. The mechanism of action of compound 2c was further investigated by analyzing cell apoptosis, mitochondrial membrane potential (??m) and intracellular ROS generation. The results indicated that compound 2c targeted mitochondria and induced cell apoptosis. ROS and heme attributed to the cytotoxicity and cell apoptosis of compound 2c. These promising findings indicated the compound 2c could serve as a great candidate against ovarian cancer for further investigation.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据