Hyperoside (quercetin 3-o-β-d-galactopyranoside) is one of the flavonoid glycosides with anti-inflammatory, antidepressant, and anti-cancer effects. The viability and migration capability of Michigan Cancer Foundation-7 (MCF-7) and 4T1 cells were inhibited by hyperoside, while the apoptosis of cells were increased. Tumor volume was significantly decreased in subcutaneous homotransplant mouse model in hyperoside-treated group[3]. Hyp (Hyperoside) inhibited IL-1β-induced expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Additionally, Hyp attenuated IL-1β-induced destruction of the extracellular matrix (ECM) by downregulating the expression of MMPs and ADAMTS5, and meanwhile upregulating the expression of collagen II, aggrecan, and SOX9. Also, Hyp pretreatment reduced IL-1β-induced overproduction of ROS and apoptosis of chondrocytes[4]. Hyperoside treatment ameliorated fibrotic pathological changes and collagen deposition in the lungs of mice with bleomycin-induced pulmonary fibrosis. In addition, hyperoside might inhibit the epithelial-mesenchymal transition (EMT) via the AKT/GSK3β pathway[5]. Hyperoside has potential therapeutic properties against periodontitis via promotion of proliferation and osteogenic differentiation of rBMSCs (rat bone mesenchymal stem cells) via activation of the NF-κB signaling pathway[6].
Hyperoside/金丝桃苷 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Human rheumatoid arthritis fibroblast-like synoviocytes (RA FLSs)
10, 50, 100 µmol/L
48 hours
To investigate the effect of Hyperoside on LPS-induced proliferation and migration of RA FLSs. Results showed that Hyperoside dose-dependently inhibited LPS-induced proliferation and migration of RA FLSs, and reduced the production of TNF-α, IL-6, IL-1β, and MMP-9.
Acta Pharmacol Sin. 2016 May;37(5):674-86.
BV-2 cells
1 μg/ml ctDNA
3-6 hours
To evaluate the inhibitory effect of Hyperoside on the production of pro-inflammatory factors TNF, IL6, and IFNB in ctDNA-stimulated BV-2 cells. Results showed that Hyperoside dose-dependently reduced the levels of these pro-inflammatory factors.
Acta Neuropathol Commun. 2024 May 16;12(1):76.
BV-2 cells
20 ng/ml LPS
12-24 hours
To validate the inhibitory effect of Hyperoside on the production of pro-inflammatory factors TNF, IL6, and CCL2 in LPS-stimulated BV-2 cells. Results showed that Hyperoside dose-dependently reduced the levels of these pro-inflammatory factors.
Acta Neuropathol Commun. 2024 May 16;12(1):76.
HT22 cells
20–80 μM
24 hours
To evaluate the protective effect of HYP on Aβ aggregate-induced cell death, results showed that HYP increased cell viability in a dose-dependent manner.
Redox Biol. 2023 May;61:102637.
Hyperoside/金丝桃苷 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c nude mice
CBRH-7919 tumor xenograft model
Tail vein injection
6.0 mg/kg
Every 2 days for 25 days
To evaluate the antitumor efficacy of DLD/HYP-Lip in vivo. Results showed that DLD/HYP-Lip significantly inhibited tumor growth with a tumor inhibition rate of 88.79%.
APP/PS1 double transgenic Alzheimer’s disease model
Intranasal administration
20, 40, 80 mg/kg
Every 3 days for 8 weeks
To evaluate the improvement of cognitive function and motor ability by HYP, results showed that HYP improved motor deficit, spatial memory and learning ability of APP/PS1 mice, and reduced the level of Aβ plaques and GFAP in the cortex and hippocampus.
Redox Biol. 2023 May;61:102637.
DBA/1 mice
Collagen-induced arthritis (CIA) model
Intraperitoneal injection
25, 50 mg/kg/d
Once daily for 3 weeks
To investigate the therapeutic effect of Hyperoside on CIA mice. Results showed that Hyperoside significantly decreased clinical scores and alleviated synovial hyperplasia, inflammatory cell infiltration, and cartilage damage.
Acta Pharmacol Sin. 2016 May;37(5):674-86.
Balb/c mice
Light damage-induced retinal degeneration model
Intraperitoneal injection
100 mg/kg
Twice daily for 7 days
To evaluate the protective effects of hyperoside on retinal structure and function post-light damage. Results showed that hyperoside partially preserved retinal structure, attenuated functional decline, and reduced neuroinflammatory responses and microglial activation.
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