Drug intelligence / Profile preview

hyperoside

Development stage
Preclinical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Topical
01

Overview

Hyperoside is a naturally occurring flavonol glycoside, specifically the 3-O-galactoside of quercetin, with the molecular formula C21H20O12 and a molecular weight of 464.40 g/mol[4][6][8][11]. It is commonly extracted from various fruits, vegetables, and medicinal plants, and is known for its wide spectrum of biological activities, including antioxidant, anti-inflammatory, antitumor, neuroprotective, vasoprotective, and hepatoprotective effects[1][3][5][7]. Mechanistically, hyperoside exerts its effects by modulating multiple cellular signaling pathways, such as PI3K/AKT, MAPK, AMPK, NF-κB, Wnt/β-catenin, and TLR4[1][3][9]. It induces apoptosis, inhibits cell proliferation, blocks angiogenesis, and sensitizes cancer cells to chemotherapy[1][3]. Hyperoside has demonstrated therapeutic potential in preclinical models for cancer, diabetes, Alzheimer’s disease, Parkinson’s disease, pulmonary fibrosis, and liver diseases[1][3][5][7]. It is not approved as a pharmaceutical drug; it is primarily experimented with in laboratory and preclinical models.

Other names
quercetin-3-O-galactosidequercetin3-O-galactosidequercetin 3-O-galactosidequercetin 3-O-β-D-galactopyranosidequercetin-3-galactosidequercetin3-galactosidequercetin 3-galactosidequercetin-3-D-galactosidequercetin3-D-galactosidequercetin 3-D-galactoside3-O-β-D-galactopyranosyl-quercetinhyperasidhyperozideactoside
02

Targets

EGFR (Epidermal growth factor receptor)AKT (RAC-alpha serine/threonine-protein kinase)AMPK (Adenosine monophosphate–activated protein kinase)BCL-2 (BCL-2 family)FOXO1 (Forkhead box protein O1)HMOX1 (Heme oxygenase 1)MAPK3 (Mitogen-activated protein kinase 1)MMP2 (Matrix metalloproteinase-2)MMP9 (Matrix metalloproteinase-9)NF-κBCD274 (Programmed cell death protein 1 ligand 1)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)SIRT1 (NAD-dependent protein deacetylase sirtuin-1)TLR4 (Toll-like receptor 4)MYC (MYC proto-oncogene protein)mTOR (Mammalian target of rapamycin kinase)

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