Discovery of novel jaspine B analogues as autophagy inducer |
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| Authors: | En Zhang Shang Wang Li-Li Li Yong-Gang Hua Jing-Fei Yue Jin-Feng Li Cheng-Yun Jin |
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| Institution: | 1. School of Pharmaceutical Sciences, Institute of Drug Discovery and Development, Key Laboratory of Advanced Pharmaceutical Technology, Ministry of Education of China, Zhengzhou University, Zhengzhou 450001, PR China;2. Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, Zhengzhou 450001, PR China;3. Kidney Transplantation, The First Affiliated Hospital of Zhengzhou University, No. 1 Jianshe Road, Zhengzhou 450001, PR China |
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| Abstract: | A series of 2-alkylaminomethyl jaspine B analogues were synthesized and evaluated for their cytotoxic effects on human lung adenocarcinoma, breast cancer, and prostate cancer cell lines and a mouse melanoma cell line. Most of the compounds exhibited moderate to good activity against the cancer cell lines. Compound 7f showed the best overall cytotoxicity on PC-3 cells (IC50?=?0.85?μM). Further mechanistic studies revealed that compound 7f induced marked changes in PC-3 cell morphology, disrupted the mitochondrial membrane potential, and increased expression of the autophagy proteins beclin-1, LC3, and P62. |
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| Keywords: | Jaspine B Pachastrissamine Anti-tumor Anti-proliferative Autophagy |
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