Manufacturer Top Quality Icariin powder

Biological Activity

icariin exhibits inhibitory effects on cgmp-specific phosphodiesterase pde5 and camp-specific phosphodiesterase pde4 activities. phosphodiesterase (pde) is a crucial regulator of camp/pka signaling. pdes are encoded by 21 genes which can be sdivided into 11 families according to the substrate specificities and subcellular localization. pdes are widely expressed in neurons. pde5 has been implicated in regulating some physiological processes such as smooth muscle relaxation and neuronal survival. pde4 has been associated with the darpp-32 signaling pathway and dopaminergic neurotransmission [1].

Biochem/physiol Actions

Icariin is a potent neuroprotective agent in neurodegenerative disorders and other disorders affecting the nervous system. It elicits anti-aging properties in unfertilized oocytes against age-related damage. Icariin exerts anti-inflammatory and antifibrotic properties aiding protection in chronic kidney disease (CKD)-associated renal fibrosis in mouse model. It also serves as an excellent antidiabetic and anti-atherosclerotic agent. Icariin is an excellent anti-cancer agent.

in vitro

icariin inhibited the activity of pde5 and pde4 in a dose- andconcentration-dependent manner. the ic50of icariin on pde5 was 0.43 μm and the ic50 on pde4 was 73.50 μm. icariin showed a selective inhibitory effect on cgmp-specific pde5 compared to camp-specific pde4 [2].icariincould also enhance the osteogenic differentiation of rat primary bone marrow stromal cells [3].

in vivo

in castrated rats, a 4-week oral administration of icariinat 1 mg/kg/day and 5 mg/kg/day improved the erectile function and increased nnos and inos expression [4].icariin also showed its effect on stimulating angiogenesis in human endothelial cells [5].

references

nishi a, kuroiwa m, miller d b, et al. distinct roles of pde4 and pde10a in the regulation of camp/pka signaling in the striatum[j]. the journal of neuroscience, 2008, 28(42): 10460-10471.xin z c, kim e k, lin c s, et al. effects of icariin on cgmp-specific pde5 and camp-specific pde4 activities[j]. asian journal of andrology, 2003, 5(1): 15-18.chen k m, ge b f, ma h p, et al. icariin, a flavonoid from the herb epimedium enhances the osteogenic differentiation of rat primary bone marrow stromal cells[j]. die pharmazie-an international journal of pharmaceutical sciences, 2005, 60(12): 939-942.liu w j, xin z c, xin h, et al. effects of icariin on erectile function and expression of nitric oxide synthase isoforms in castrated rats[j]. asian journal of andrology, 2005, 7(4): 381-388.chung b h, kim j d, kim c k, et al. icariin stimulates angiogenesis by activating the mek/erk-and pi3k/akt/enos-dependent signal pathways in human endothelial cells[j]. biochemical and biophysical research communications, 2008, 376(2): 404-408.

Origin and Sources

Icariin is a prenylated flavonol glycoside isolated from the Epimedium herb. Epimedium is a perennial herb with high medicinal value, and its active ingredient, icariin, is considered the main bioactive component.

Chemical Structure and Properties

Icariin presents a chemical structure belonging to 8-prenyl flavonoid glycosides and appears as a pale yellow powder. It is soluble in ethyl acetate and ethanol but insoluble in chloroform, ether, and benzene.

Pharmacological Activities

Icariin exhibits numerous pharmacological activities, including:
1. Osteoprotective effect: Promotes bone formation and inhibits bone resorption, making it a promising candidate for bone tissue engineering.
2. Neuroprotective effect: Shows potential in disorders of the nervous system such as Alzheimer's disease, Parkinson's disease, and depression.
3. Cardiovascular protective effect: Protects cardiomyocytes and vein endothelium from harmful factors, reducing hypertrophy and apoptosis.
4. Anti-cancer effect: Synergizes with other anti-tumor drugs and radiation therapy, inhibiting tumor growth and inducing apoptosis.
5. Anti-inflammatory effect: Inhibits the production of pro-inflammatory cytokines and reduces inflammation.
6. Immunoprotective effect: Regulates immunocytes and cytokines, contributing to immune modulation.
7. Reproductive function: Enhances reproductive function and anti-aging effects.

Mechanisms of Action

Icariin mediates its pharmacological effects through various mechanisms, including:
Activation of protein kinase B (Akt), peroxisome proliferator-activated receptor (PPAR), and silent mating type information regulation 2 homolog 1 (SIRT1).
Inhibition of nuclear factor-κB (NF-κB) and the production of pro-inflammatory cytokines.
Inhibition of phosphodiesterase-5 (PDE5) and the hypothalamic-pituitary-adrenal (HPA) axis.

Therapeutic Potential

Icariin shows potential therapeutic benefits in various disorders, such as cerebral ischemia, Alzheimer's disease, Parkinson's disease, multiple sclerosis, and depression. It's extensive therapeutic capacities make it a promising agent for disease prevention and therapy, particularly in bone tissue engineering, cardiovascular diseases, and cancer treatment.

Applications

Icariin inhibits the ROS-dependent JNK and p38 pathways.

General Description

Icariin is a prenylated flavonol and the major bioactive compound found in Epimedium herb.