Icariin is a flavonol glycoside. It inhibits PDE5 and PDE4 activities with IC50s of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator[3]. Icariin was injected in a dose of 50 mg/kg, and significantly reduced paw swelling in carrageenan-injected animals. It also ameliorated carrageenan-induced paw histopathological alterations. Icariin significantly increased paw enzymatic and non-enzymatic antioxidants. It decreased paw lipid peroxidation. Icariin decreased paw levels of inflammatory cytokines and NF-kB[4]. Icariin can prevent the production of amyloid β (1-42) and inhibit the expression of amyloid precursor protein (APP) and β-site APP cleaving enzyme 1 (BACE-1) in animal models of Alzheimer's disease (AD). Icariin also prevents the neurotoxicity induced by hydrogen peroxide (H2O2), endoplasmic reticulum (ER) stress, ibotenic acid, and homocysteine[5]. Icariin selectively inhibited proliferation and triggered apoptosis in breast cancer cells in a concentration- and time-dependent manner, but exhibited little cytotoxicity in normal breast cells. Moreover, icariin induced cell apoptosis via a mitochondria-mediated pathway, as indicated by the upregulated ratio of Bax/Bcl-2 and reactive oxygen species induction. Importantly, icariin impaired the activation of the NF-κB/EMT pathway, as evidenced by upregulation of SIRT6, resulting in inhibition of migration and invasion of breast cancer cells[6]. Icariin protects BMSCs (bone marrow-derived mesenchymal stem cells) against OGD (oxygen, glucose and serum deprivation)-induced apoptosis by inhibiting ERs-mediated (ER Stress) autophagy via MAPK signaling pathway[7].
Icariin/淫羊藿苷 细胞实验
Cell Line
Concentration
Treated Time
Description
References
4T1
20 µM
24 hours
To evaluate the inhibitory effect of icariin on breast cancer cell proliferation, results showed that icariin significantly inhibited the proliferation of 4T1 cells.
Cancer Sci. 2020 Nov;111(11):4242-4256.
MDA-MB-231
10 or 20 µM
24 hours
To evaluate the inhibitory effect of icariin on breast cancer cell proliferation, results showed that icariin significantly inhibited the proliferation of MDA-MB-231 cells.
Cancer Sci. 2020 Nov;111(11):4242-4256.
HMC3 cells
10 μM
24 h
To investigate the effect of ICA on M1/M2 phenotypic polarization in HMC3 cells. Results showed that ICA significantly reduced the expression of M1 markers (TNF-α, COX-2, NO) and increased the expression of M2 markers (ARG1, CD206, IL-10).
Redox Biol. 2022 Jun;52:102297.
primary rat midbrain neuron-enriched cultures
0.1 μM
7 days
To evaluate the protective effect of ICA on 6-OHDA-induced DA neuronal injury, results showed that ICA did not exhibit neuroprotection in neuron-enriched cultures.
J Neuroinflammation. 2019 Apr 22;16(1):92.
primary rat midbrain neuron-glia co-culture
0.1 μM
7 days
To evaluate the protective effect of ICA on 6-OHDA-induced DA neuronal injury, results showed that ICA significantly attenuated 6-OHDA-induced DA neuronal injury in neuron-glia co-cultures.
J Neuroinflammation. 2019 Apr 22;16(1):92.
H9c2 cells
4 μM
2 h
To investigate the protective role of icariin via SIRT1 pathway in H9c2 cells, results demonstrated icariin pretreatment significantly enhanced cell survival and reduced apoptosis and necrosis markers.
Br J Pharmacol. 2018 Nov;175(21):4137-4153.
Neonatal rat ventricular myocytes (NRVMs)
2, 4, 8 μM
12 h
To evaluate the regulatory effect of icariin on SIRT1, results showed icariin significantly increased SIRT1 expression and dose-dependently improved cell viability post-SI/R injury, reducing apoptosis and necrosis.
Br J Pharmacol. 2018 Nov;175(21):4137-4153.
Icariin/淫羊藿苷 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6J mice
Experimental autoimmune uveitis (EAU) model
Intragastric administration
10 mg/kg
Once daily for 7 days
To investigate the effect of ICA on intraocular inflammation in EAU mice. Results showed that ICA significantly reduced conjunctival and ciliary hyperaemia and infiltration of anterior chamber inflammatory cells, decreased retinal folds and inflammatory cells, and improved the integrity of the blood-retinal barrier.
Redox Biol. 2022 Jun;52:102297.
Mice
6-OHDA-induced Parkinson's disease model
Intragastric administration
60 mg/kg
Once daily for 10 consecutive days
To evaluate the protective effect of ICA on 6-OHDA-induced DA neuronal injury, results showed that ICA attenuated 6-OHDA-induced DA neurotoxicity and glial cells-mediated neuroinflammatory response.
J Neuroinflammation. 2019 Apr 22;16(1):92.
C57BL/6 mice
Myocardial ischemia/reperfusion injury model
Oral gavage
60 mg/kg
Twice daily for 2 weeks
To assess the cardioprotective effects of icariin against myocardial I/R injury, results showed icariin significantly improved cardiac function (EF and FS), reduced infarct size and apoptosis, and attenuated oxidative stress markers.
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