Icariin, an Anti-atherosclerotic Drug from Chinese Medicinal Herb Horny Goat Weed

Jian Fang, Yongjun Zhang, Jian Fang, Yongjun Zhang

Abstract

Icariin is a major bioactive pharmaceutical constituent isolated from Chinese medicine Horny Goat Weed (Ying Yang Huo) with potent cardiovascular protective functions. Emerging evidence in the past decade has shown that Icariin possesses multiple atheroprotective functions, through multiple mechanisms, including attenuating DNA damage, correcting endothelial dysfunction, inhibiting the proliferation and migration of smooth muscle cells, repressing macrophage-derived foam cell formation and inflammatory responses, as well as preventing platelet activation. All of these protective effects, combined with its lipid-modulatory effects, contribute to the broad atheroprotective effects of Icariin. In this review, we will summarize the anti-atherosclerotic properties of Icariin and highlight future perspectives in developing Icariin as a promising anti-atherosclerotic drug.

Keywords: atherosclerosis; endothelial function; foam cell; icariin; smooth muscle cell.

Figures

FIGURE 1
FIGURE 1
Anti-atherosclerotic effects of Icariin. EC, endothelial cell; VSMC, vascular smooth muscle cell; Mφ, macrophage. (A) The chemical structure of Icariin obtained from PubChem database. (B) Atheroprotective effects of Icariin.
FIGURE 2
FIGURE 2
Potential molecular targets of Icariin. Nrf2, eNOS, endothelial nitric oxide synthase; NO, nitric oxide; AR, androgen receptor; ADMA, asymmetric dimethylarginine; DDAH, dimethylarginine dimethylaminohydrolase; CD36, cluster of differentiation 36; SR-BI, scavenger receptor B1; COX2, cyclooxygenase 2; iNOS, inducible NO synthase; NF-κB, nuclear factor-kappa B; CX3CR1, SREBP, sterol regulatory element-binding protein; GRP78, glucose regulated protein 78; PCNA, proliferating cell nuclear antigen; PAI-1, plasminogen activator inhibitor-1; t-PA, tissue-type plasminogen activator.

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