PUBLICATION
Anti-angiogenic and anticancer effects of baicalein derivatives based on transgenic zebrafish model
- Authors
- Jiang, X., Zhou, J., Lin, Q., Gong, G., Sun, H., Liu, W., Guo, Q., Feng, F., Qu, W.
- ID
- ZDB-PUB-180814-5
- Date
- 2018
- Source
- Bioorganic & Medicinal Chemistry 26(15): 4481-4492 (Journal)
- Registered Authors
- Keywords
- Anti-angiogenesis, Anticancer, Baicalein derivatives, Transgenic zebrafish model
- MeSH Terms
-
- Angiogenesis Inhibitors/chemistry*
- Angiogenesis Inhibitors/pharmacology
- Animals
- Animals, Genetically Modified
- Antineoplastic Agents/chemistry*
- Antineoplastic Agents/pharmacology
- Apoptosis/drug effects
- Cell Line
- Cell Movement/drug effects
- Cell Proliferation/drug effects
- Embryo, Nonmammalian/blood supply
- Embryo, Nonmammalian/drug effects
- Flavanones/chemistry*
- Flavanones/pharmacology
- Human Umbilical Vein Endothelial Cells
- Humans
- Neovascularization, Physiologic/drug effects
- Structure-Activity Relationship
- Zebrafish
- PubMed
- 30098912 Full text @ Bioorg. Med. Chem.
Citation
Jiang, X., Zhou, J., Lin, Q., Gong, G., Sun, H., Liu, W., Guo, Q., Feng, F., Qu, W. (2018) Anti-angiogenic and anticancer effects of baicalein derivatives based on transgenic zebrafish model. Bioorganic & Medicinal Chemistry. 26(15):4481-4492.
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.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping