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

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Front. Pharmacol., 12 October 2017
Sec. Cardiovascular and Smooth Muscle Pharmacology

Jian Fang1* and Yongjun Zhang2

  • 1Department of Pharmacy, Huadu District People’s Hospital, Southern Medical University, Guangzhou, China
  • 2Department of Gastroenterology, Huadu District People’s Hospital, Southern Medical University, Guangzhou, China

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.

Introduction

Cardiovascular diseases (CVDs) represent one of the leading causes of death in the modern society worldwide (Benjamin et al., 2017). At present, due to the complexity of the pathogenesis of atherosclerosis, therapeutic drugs that can prevent or treat atherosclerosis remain very limited (Orekhov et al., 2015). Currently, in light of the fact that atherosclerosis is a lipid disorder; lipid-lowering statins are the main category of anti-atherosclerotic drugs. Recently, several new therapeutic options are showing promising prospect in treating atherosclerosis, such as PCSK9 monoclonal antibodies (Pedersen, 2016). Despite the wide application of statins, the mortality rate of CVD remains very high, suggesting the need to develop new drugs that can treat atherosclerosis.

Numerous studies have shown that atherosclerosis is a chronic inflammatory disease with the characteristics of persistent inflammatory response, inflammasome activation, and impaired inflammation resolution (Ross, 1993Rader and Daugherty, 2008Libby et al., 2011Tabas et al., 2015). Many vascular cells, including endothelial cells, smooth muscle cells, monocytes, macrophages, and platelets are involved in the inflammatory responses of vessel wall in response to pro-atherogenic stimuli (Rader and Daugherty, 2008). It has been reported that the current “gold standard” anti-atherosclerotic drugs such as statins can also produce anti-inflammatory effects independent of lipid-lowering effects (Rosenson, 2004). Therefore, anti-inflammatory therapy is a good strategy for the prevention and treatment of atherosclerosis. As we are entering a golden era of developing drugs from natural products (Shen, 2015), natural products especially Chinese medicinal herbs emerges as important sources of cardiovascular protective medicine that target multiple cellular processes of atherosclerosis. These natural products would probably translate into effective novel cardiovascular therapeutics (Amirkia and Heinrich, 2015Fang et al., 2017).

Horny Goat Weed, an eminent Chinese herbal medicine (also known as Epimedii Herba or Ying Yang Huo), is widely used to treat various diseases such as coronary heart disease, impotence and osteoporosis, and rheumatism (Ye and Chen, 2001). Among the pharmacologically active constituents, Icariin (Figure 1A) is a major bioactive pharmaceutical constituent that has been reported to treat multiple CVDs (He et al., 1995Xu and Huang, 2007) via anti-oxidant, anti-inflammatory, and lipid-modulatory effects. The excellent cardiovascular protective profiles of Icariin make it an excellent drug candidate for cardiovascular therapeutics. In the following sections, we will present an overview of the cardiovascular protective effects and molecular mechanisms of Icariin in atherosclerosis.

Reference:

https://www.frontiersin.org/articles/10.3389/fphar.2017.00734/full

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