PUBLICATION
Phenolic Glycoside Monomer from Reed Rhizome Inhibits Melanin Production via PI3K-Akt and Ras-Raf-MEK-ERK Pathways
- Authors
- Pang, M., Yao, H., Bao, K., Xu, R., Xi, R., Peng, R., Zhi, H., Zhang, K., He, R., Du, Y., Su, Y., Liu, X., Ming, D.
- ID
- ZDB-PUB-241001-11
- Date
- 2024
- Source
- Current Medicinal Chemistry : (Journal)
- Registered Authors
- Keywords
- Reed Rhizome extract, anti-melanogenesis, mechanism., tyrosinase, zebrafish model
- MeSH Terms
-
- Animals
- Glycosides*/chemistry
- Glycosides*/isolation & purification
- Glycosides*/pharmacology
- Humans
- MAP Kinase Signaling System/drug effects
- Melanins*/antagonists & inhibitors
- Melanins*/biosynthesis
- Molecular Docking Simulation
- Phenols*/chemistry
- Phenols*/isolation & purification
- Phenols*/pharmacology
- Phosphatidylinositol 3-Kinases/metabolism
- Proto-Oncogene Proteins c-akt/antagonists & inhibitors
- Proto-Oncogene Proteins c-akt/metabolism
- Rhizome*/chemistry
- Signal Transduction/drug effects
- Zebrafish
- raf Kinases/metabolism
- ras Proteins/metabolism
- PubMed
- 39350409 Full text @ Curr. Med. Chem.
Citation
Pang, M., Yao, H., Bao, K., Xu, R., Xi, R., Peng, R., Zhi, H., Zhang, K., He, R., Du, Y., Su, Y., Liu, X., Ming, D. (2024) Phenolic Glycoside Monomer from Reed Rhizome Inhibits Melanin Production via PI3K-Akt and Ras-Raf-MEK-ERK Pathways. Current Medicinal Chemistry. :.
Abstract
Introduction Melanogenesis, the process responsible for melanin production, is a critical determinant of skin pigmentation. Dysregulation of this process can lead to hyperpigmentation disorders.
Method In this study, we identified a novel Reed Rhizome extract, (1'S, 2'S)-syringyl glycerol 3'-O-β-D-glucopyranoside (compound 5), and evaluated its anti-melanogenic potential in zebrafish models and in vitro assays. Compound 5 inhibited melanin synthesis by 36.66% ± 14.00% and tyrosinase in vivo by 48.26% ± 6.94%, surpassing the inhibitory effects of arbutin. Network pharmacological analysis revealed key targets, including HSP90AA1, HRAS, and PIK3R1, potentially involved in the anti-melanogenic effects of compound 5.
Results Molecular docking studies supported the interactions between compound 5 and these targets. Further, gene expression analysis in zebrafish indicated that compound 5 up-regulates hsp90aa1.1, hrasa, and pik3r1, and subsequently down-regulating mitfa, tyr, and tyrp1, critical genes in melanogenesis.
Conclusion These findings suggest that compound 5 inhibits melanin production via PI3K-Akt and Ras-Raf-MEK-ERK signaling pathways, positioning it as a promising candidate for the treatment of hyperpigmentation.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping