Icariin is believed to have cardiovascular protective properties. Sourced from Horny Goat Weed, Icariin is known to have potent atheroprotective function. The ancient Chinese medicine has proven to be effective in treating cardiovascular ailments, degenerative diseases, and osteoporosis. Besides, it is believed to improve sexual and neurological function.[1]

Anti-inflammatory therapy is touted to help prevent and treat atherosclerosis. Statins and similar anti-atherosclerotic drugs can have potent anti-inflammatory effects in the prevention and treatment of atherosclerosis. However, drugs developed from natural products are believed to have potent cardiovascular protective properties. These are known to target a range of cellular processes of atherosclerosis.

Emerging evidence suggests the potent role of Icariin in attenuating DNA damage, preventing platelet activation, inhibiting the proliferation of muscle cells, correcting endothelial dysfunction, and repressing inflammatory responses. Icariin’s lipid-modulatory effects are known to contribute to its atheroprotective properties and emphasize its role as a promising anti-atherosclerotic drug.

The ancient Chinese herbal medicine has been in use in China for the treatment of coronary heart disease, rheumatism, osteoporosis, and impotence. It is known to have anti-inflammatory response, apart from its anti-oxidant and lipid-modulatory effects that enhance its cardiovascular protective profile. Therefore, it is touted to be an excellent drug for cardiovascular ailments.

Anti-DNA Damage Effects

Research backs the polyphenol structure of Icariin that has same antioxidative effects as other polyphenols. A study observed the role of Icariin in protecting the body against peroxidation in erythrocytes, which is induced by free radicals. The study found that Icariin was effective in reducing AAPH-induced DNA damage.[2]

Protects endothelial cells

Endothelium is the direct type of cell responsible for keeping blood vessels healthy. It also helps regulate vascular tone. Endothelium is responsible for anti-inflammatory, antioxidative, and anti-thrombotic function. But the functioning could be impaired by pathological stimuli, resulting in dysfunction and development of atherosclerosis.

Endothelial injury is believed to result in the migration of vascular smooth muscle cells to the sub-endothelial space, where they can proliferate quickly. As a result, neointima is formed. This is the early form of atherosclerosis-linked vascular remodeling.

Icariin or horny goat weed is a kind of flavonoid that exhibits antioxidative, immunoregulatory, and antitumorigenic effects. A study investigated the role of Icariin on endothelial cells after treatment with oxidized low‑density lipoprotein. The study concluded that Icariin prevented injury and apoptosis in human vascular endothelial cells after ox‑LDL treatment.[3]

Icariin treatment arrests cell cycle in the early stage (S and G2/M phase).

So it may be concluded that Icariin has anti-proliferative effects and protects endothelial cell damage.

Platelet activation inhibition

Research claims that Icariin has lipid-lowering properties and could play a role in the treatment and prevention of thrombosis. Platelet activation and thrombus formation are related to atherosclerosis. Icariin seems promising in the treatment of atherosclerosis by inhibiting platelet activation in hypercholesterolemia.[4]

Lipid metabolism

Icariin is believed to play an effective role in the treatment of hyperlipidemia. A study reveals that Icariin regulates the level of enzymes and proteins responsible for activating lipid metabolism. The research concludes that this could be a basis for the lipid-lowering effects of Icariin and its potential role in preventing against the risk of diabetes.[5]

Conclusion

Also known as Yin Yang Huo, Icariin is a flavonoid sourced from plants. Its extracts have been in use in Chinese herbal medicine since ages. More research is under way to further look into the protective role of Icariin against atherosclerosis. Further research is exploring the role of Icariin as an anti-inflammatory, antioxidant, anti-tumor, and neuro-protector.

References

[1] Fang, J., & Zhang, Y. (2017). Icariin, an Anti-atherosclerotic Drug from Chinese Medicinal Herb Horny Goat Weed. Frontiers in pharmacology, 8, 734. doi:10.3389/fphar.2017.00734

[2] Fang, J., & Zhang, Y. (2017). Icariin, an Anti-atherosclerotic Drug from Chinese Medicinal Herb Horny Goat Weed. Frontiers in pharmacology, 8, 734. doi:10.3389/fphar.2017.00734

[3] Hu, Y.1. (2018). Protective effects of Icariin on human vascular endothelial cells induced by oxidized low-density lipoprotein via modulating caspase-3 and Bcl-2.Molecular Medicine Reports. doi: 10.3892/mmr.2018.8717. Epub 2018 Mar 9.

[4] Fang, J., & Zhang, Y. (2017). Icariin, an Anti-atherosclerotic Drug from Chinese Medicinal Herb Horny Goat Weed. Frontiers in pharmacology, 8, 734. doi:10.3389/fphar.2017.00734

[5] Lu, Yuan-Fu & Xu, Yun-Yan & Jin, Feng & Wu, Qin & Chan, Neolignan & Liu, Jie. (2014). Icariin Is A PPAR alpha Activator Inducing Lipid Metabolic Gene Expression in Mice. Molecules (Basel, Switzerland). 19. 18179-18191. 10.3390/molecules191118179.