PUBLICATION
Ligustilide, a major bioactive component of Angelica sinensis, promotes bone formation via the GPR30/EGFR pathway
- Authors
- Yang, F., Lin, Z.W., Huang, T.Y., Chen, T.T., Cui, J., Li, M.Y., Hua, Y.Q.
- ID
- ZDB-PUB-190508-5
- Date
- 2019
- Source
- Scientific Reports 9: 6991 (Journal)
- Registered Authors
- Keywords
- none
- MeSH Terms
-
- 4-Butyrolactone/analogs & derivatives*
- 4-Butyrolactone/pharmacology
- Angelica sinensis/chemistry
- Animals
- Apoptosis/drug effects
- Apoptosis/genetics
- Bone Density Conservation Agents/pharmacology*
- Cell Line
- Disease Models, Animal
- Embryo, Nonmammalian
- Gene Expression Regulation
- Green Fluorescent Proteins/genetics*
- Green Fluorescent Proteins/metabolism
- Larva
- Mesenchymal Stem Cells/cytology
- Mesenchymal Stem Cells/drug effects
- Mesenchymal Stem Cells/metabolism
- Mitogen-Activated Protein Kinase 1/genetics
- Mitogen-Activated Protein Kinase 1/metabolism
- Mitogen-Activated Protein Kinase 3/genetics
- Mitogen-Activated Protein Kinase 3/metabolism
- Osteoblasts/cytology
- Osteoblasts/drug effects*
- Osteoblasts/metabolism
- Osteoporosis/drug therapy*
- Osteoporosis/genetics
- Osteoporosis/metabolism
- Osteoporosis/pathology
- Prednisolone/antagonists & inhibitors
- Prednisolone/pharmacology
- Primary Cell Culture
- Proto-Oncogene Proteins c-bcl-2/genetics
- Proto-Oncogene Proteins c-bcl-2/metabolism
- Rats
- Receptors, G-Protein-Coupled/genetics*
- Receptors, G-Protein-Coupled/metabolism
- Zebrafish
- Zebrafish Proteins/genetics*
- Zebrafish Proteins/metabolism
- PubMed
- 31061445 Full text @ Sci. Rep.
Citation
Yang, F., Lin, Z.W., Huang, T.Y., Chen, T.T., Cui, J., Li, M.Y., Hua, Y.Q. (2019) Ligustilide, a major bioactive component of Angelica sinensis, promotes bone formation via the GPR30/EGFR pathway. Scientific Reports. 9:6991.
Abstract
Angelica sinensis (Oliv.) Diels is a widely-used traditional Chinese herbal medicine in treating osteoporosis. Ligustilide (LIG) is the main component of A. sinensis and is considered to be the most effective biologically active ingredient in this plant. LIG has been found to have multiple pharmacological activities, such as anti-atherosclerosis, neuroprotection, anticancer, anti-inflammatory and analgesic. However, little is known regarding its anti-osteoporotic effects. The aims of this study were to investigate any protective effect of LIG on bone formation. The results showed that LIG significantly ameliorated inhibition of bone formation in zebrafish caused by prednisolone. LIG promoted osteoblast differentiation, including that of the pre-osteoblastic cell line MC3T3-E1 and bone marrow mesenchymal stem cells. LIG greatly improved the viability of MC3T3-E1 cells exposed to H2O2, attenuated H2O2-induced apoptosis and increased the expression of Bcl-2. Furthermore, LIG treatment lead to marked activation of phosphorylated EGFR and ERK1/2. These effects could be obviously inhibited by blocking GPR30 signaling with the specific inhibitor G15. Collectively, the results reveal that GPR30 is a positive switch for LIG to increase bone formation via regulation of EGFR, and these results provide evidence for the potential of LIG to treat osteoporosis.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping