A 3D screening approach identifies the compound epitajixanthone hydrate as a new inhibitor of cancer cell growth and invasion
| Autor: | Jing-Fang Xiao, Xiao-Long Yang, Ze-Diao Huang, Ye-Miao Chen, Xiang Li, Ting-Kai Liu, Sheng-Xiang Yang |
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| Rok vydání: | 2020 |
| Předmět: |
0301 basic medicine
Cancer Research Epithelial-Mesenchymal Transition Cell Survival Xanthones Antineoplastic Agents Cell Growth Processes Small Molecule Libraries 03 medical and health sciences 0302 clinical medicine Imaging Three-Dimensional Cell Movement Cell Line Tumor Neoplasms Humans Pharmacology (medical) Neoplasm Invasiveness Pharmacology Virtual screening Biological Products biology Drug discovery Chemistry biology.organism_classification HCT116 Cells Small molecule 030104 developmental biology Oncology Colony formation Biochemistry Taxus A549 Cells 030220 oncology & carcinogenesis Cancer cell Drug Screening Assays Antitumor Hydrate |
| Zdroj: | Anti-cancer drugs. 31(9) |
| ISSN: | 1473-5741 |
| Popis: | With unique advantages, the small-molecule anticancer drugs have recently gained growing attention. Particular strategies, exemplified by high-throughput screening, fragment-based drug discovery, virtual screening and knowledge-based design, have been developed to identify active compounds. However, such screens generally rely on sophisticated and expensive instrumentations. Herein, we developed a simple spheroids 3D culture system to enable direct screening of small molecules with reliable results. Using this system, we screened 27 fungal natural products and three fungal crude extracts for their inhibitory effects on cancer cell growth, and invasion. We identified that the compound M23 (epitajixanthone hydrate, a derivative of prenylxanthone) and the crude extracts (MPT-191) from the fungi Taxus chinensis showed potential anticancer activity. The effect of epitajixanthone hydrate on cancer cell growth and invasion were further confirmed by the assays of cells viability, trans-well migration and invasion, colony formation and cells reattachment. Overall, Epitajixanthone hydrate was identified as an effective inhibitor of cancer cell growth and invasion by our simple and fast screening platform. |
| Databáze: | OpenAIRE |
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