Anti-angiogenic and anticancer effects of baicalein derivatives based on transgenic zebrafish model |
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| Authors: | Xueyang Jiang Junting Zhou Qinghua Lin Guiyi Gong Haopeng Sun Wenyuan Liu Qinglong Guo Feng Feng Wei Qu |
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| Institution: | 1. Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China;2. Key Laboratory of Biomedical Functional Materials, China Pharmaceutical University, Nanjing 210009, China;3. Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009, China;4. Key Laboratory of Drug Quality Control and Pharmacovigilance (China Pharmaceutical University), Ministry of Education, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China;5. Jiangsu Key Laboratory of Carcinogenesis and Intervention, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China;6. Jiangsu Food & Pharmaceutical Science College, Huaian 223003, China |
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| Abstract: | Angiogenesis leads to tumor neovascularization by promoting tumor growth and metastatic spread, therefore, angiogenesis is considered as an attractive target for potential small molecule anticancer drug discovery. Herein, we report the structural modification and biological evaluation of baicalein derivatives, among which compound 42 had potent in vivo anti-angiogenic activity and wide security treatment window in transgenic zebrafish model. Further, 42 exhibited the most potent inhibitory activity on HUVEC proliferation, migration and tube formation in vitro. Moreover, 42 significantly inhibited growth of human lung cancer A549 cells and weak influence on human normal fibroblast L929 cells. The present research demonstrated that the significant anti-angiogenic and anticancer effects, which provided the supportive evidence for 42 could be used as a potential compound of cancer therapy. |
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| Keywords: | Baicalein derivatives Anti-angiogenesis Transgenic zebrafish model Anticancer |
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