Harpagoside is isolated from Harpagophytum procumbens (Hp). Harpagoside has inhibitory effects on COX-1 and COX-2 activity and inhibits NO production. The highest concentration of harpagoside inhibited indistinctively COX-1 and COX-2 (37.2 and 29.5% respectively) activity and greatly inhibited NO production (66%)[3]. Harpagoside exerts a significant anti-inflammatory effect by inhibiting the inflammatory stimuli mediated by suppressing c-FOS/AP-1 activity in OA (osteoarthritis) chondrocytes under pathological conditions[4]. With the use of chronic cerebral hypoperfusion rats, a well-known VaD (Vascular dementia) model, we demonstrated that chronic administration (two months) of harpagoside was able to restore both the spatial learning/memory and fear memory impairments. Harpagoside suppressed the overactivation of PTEN induced by CCH by enhancing PTEN phosphorylation. Furthermore, harpagoside elevated the activity of Akt and inhibited the activity of GSK-3β, downstream effectors of PTEN[5].
Harpagoside/哈巴俄苷 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Primary spinal cord neurons
50, 100, 200 µg/mL
24 hours
To evaluate the effect of HAS on neuronal survival and axonal growth after FeSO4 injury. Results showed HAS significantly promoted neuronal survival and axonal growth at concentrations of 50-200 µg/mL.
Cells. 2023 Sep 15;12(18):2281
Human primary synoviocytes (FLSs)
100 μg/mL
24 hours
HPE H2O and HPE DMSO were able to enhance CB2 receptor expression and to downregulate PI-PLC β2 in synovial membranes.
Nutrients. 2020 Aug 23;12(9):2545
H9C2 cells
25 μM
24 hours
HAR significantly improved the viability and proliferation of H9C2 cells and alleviated DOX-induced apoptosis.
Front Cell Dev Biol. 2022 Feb 10;10:813370
Osteoblast-macrophage co-culture
75 μM
3 days
To assess the anti-inflammatory effect of HR in an inflammation model. Results showed that HR 75 μM significantly reduced LPS-induced IL-1β levels, indicating its anti-inflammatory properties.
Nanomaterials (Basel). 2020 Sep 3;10(9):1743
Human primary synoviocytes (FLSs)
0.1 mg/mL
5 min to 48 h
HPE DMSO was able to inhibit cAMP production and reduce cAMP levels even under forskolin stimulation.
Pharmaceuticals (Basel). 2022 Apr 9;15(4):457
bone marrow-derived macrophages (BMMs)
50 μg/mL, 100 μg/mL, 200 μg/mL
4 days
Inhibited TRAP-positive cell formation and bone resorption in a dose-dependent manner
Plants (Basel). 2020 Nov 26;9(12):1656
Vero E6 cells
100 μM
6 h
To evaluate the effect of Harpagoside on SARS-CoV-2 infection, results showed that Harpagoside dramatically reduced the viral RNA.
Cell Metab. 2022 Mar 1;34(3):424-440. e7
HUVECs
100 μM
16 h
To evaluate the effect of Harpagoside on ACE2 enzymatic activity, results showed that Harpagoside significantly elevated the enzymatic activity of ACE2.
Cell Metab. 2022 Mar 1;34(3):424-440. e7
Human osteoblasts
50–100 μM
21 days
To evaluate the effect of HR on osteoblast proliferation and differentiation. Results showed that HR 75 μM significantly increased osteoblast proliferation and induced the highest alkaline phosphatase (ALP) expression at days 3 and 7, indicating enhanced early osteogenic differentiation.
Nanomaterials (Basel). 2020 Sep 3;10(9):1743
Harpagoside/哈巴俄苷 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Diet-induced insulin-resistant mice
Gavage
100 mg/kg
Once daily for 4 weeks
To evaluate the effect of Harpagoside on metabolic defects and viral entry, results showed that Harpagoside improved metabolic defects and inhibited viral entry.
Cell Metab. 2022 Mar 1;34(3):424-440. e7
Sprague-Dawley rats
Lumbar spinal stenosis (LSS) model
Epidural injection
100 and 200 µg/kg
Once daily for 4 weeks
To evaluate the effect of epidural HAS administration on inflammatory responses and pain relief in LSS rats. Results showed HAS significantly reduced inflammatory cell infiltration, decreased iNOS expression, and downregulated pro-inflammatory cytokines.
Cells. 2023 Sep 15;12(18):2281
Zebrafish
DOX-induced cardiotoxicity model
Water bath
25 μM
Assessed after 1 day
HAR significantly improved DOX-induced cardiac dysfunction and myocardial structural lesions, and reduced mitochondrial oxidative damage and restored mitophagy flux.
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