PUBLICATION
PHMH, a diarylheptanoid from Alpinia officinarum attenuates VEGF-induced angiogenesis via inhibition of the VEGFR-2 signaling pathway
- Authors
- Hu, L., Huang, W., Ding, Y., Liu, M., Wang, M., Wang, Y., Zhang, W., Li, Y., Ye, W., Li, M., Liu, Z.
- ID
- ZDB-PUB-190426-2
- Date
- 2019
- Source
- Food & function 10(5): 2605-2617 (Journal)
- Registered Authors
- Keywords
- none
- MeSH Terms
-
- Alpinia
- Vascular Endothelial Growth Factor A/metabolism*
- Mice, Inbred C57BL
- Vascular Endothelial Growth Factor Receptor-2/genetics
- Vascular Endothelial Growth Factor Receptor-2/metabolism*
- Human Umbilical Vein Endothelial Cells/drug effects
- Human Umbilical Vein Endothelial Cells/metabolism
- Cell Movement/drug effects
- Humans
- Male
- Drugs, Chinese Herbal/administration & dosage*
- Drugs, Chinese Herbal/chemistry
- Signal Transduction/drug effects
- Angiogenesis Inhibitors/administration & dosage*
- Angiogenesis Inhibitors/chemistry
- Neovascularization, Pathologic/drug therapy*
- Neovascularization, Pathologic/genetics
- Neovascularization, Pathologic/metabolism
- Neovascularization, Pathologic/physiopathology
- China
- TOR Serine-Threonine Kinases/genetics
- TOR Serine-Threonine Kinases/metabolism
- Female
- Diarylheptanoids/administration & dosage*
- Diarylheptanoids/chemistry
- Animals
- Zebrafish
- PubMed
- 31020299 Full text @ Food Funct
Citation
Hu, L., Huang, W., Ding, Y., Liu, M., Wang, M., Wang, Y., Zhang, W., Li, Y., Ye, W., Li, M., Liu, Z. (2019) PHMH, a diarylheptanoid from Alpinia officinarum attenuates VEGF-induced angiogenesis via inhibition of the VEGFR-2 signaling pathway. Food & function. 10(5):2605-2617.
Abstract
The rhizome of Alpinia officinarum Hance, a popular spice used as a condiment in China and Europe, has various reported bioactivities, including anticancer, anti-inflammatory and antioxidant effects. However, its anti-angiogenic activity has not previously been reported. In this study, a diarylheptanoid was isolated from Alpinia officinarum and identified as 1-phenyl-7-(4-hydroxy-3-methoxyphenyl)-4E-en-3-heptanone (PHMH). We demonstrated that PHMH exerts anti-angiogenic activity both in vitro and in vivo. PHMH inhibited vascular endothelial growth factor (VEGF)-induced viability, migration, invasion and tube formation in human umbilical vein endothelial cells (HUVECs) in vitro, and also suppressed VEGF-induced sprout formation of rat aorta ex vivo. Furthermore, PHMH was found to block VEGF-induced vessel formation in mice and suppress angiogenesis in both zebrafish and chorioallantoic membrane models. Mechanistic studies indicated that PHMH inhibited VEGF-induced VEGF receptor-2 (VEGFR-2) auto-phosphorylation and resulted in the blockage of VEGFR-2-mediated signaling cascades in HUVECs, including the Akt/mTOR, ERK1/2, and FAK pathways. Our findings provide new insights into the potential application of PHMH as a therapeutic agent for anti-angiogenesis.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping