Pharmacological effects and pharmacokinetic properties of icariin, the major bioactive component in Herba Epimedii

Life Sci. 2015 Apr 1;126:57-68. doi: 10.1016/j.lfs.2015.01.006. Epub 2015 Jan 26.


Herba Epimedii is an important medicinal plant which has been used in various traditional Chinese formulations for thousands of years as well as in modern proprietary traditional Chinese medicine products. It has extensive clinical indications, especially for the treatment of sexual dysfunction and osteoporosis. There have been more than 260 chemical moieties identified in the genus Epimedium most of which belong to flavonoids. Icariin is the most abundant constituent in Herba Epimedii. Icariin is pharmacologically bioactive and demonstrates extensive therapeutic capacities such as osteoprotective effect, neuroprotective effect, cardiovascular protective effect, anti-cancer effect, anti-inflammation effect, immunoprotective effect and reproductive function. Particularly, the significant osteogenic effect of icariin made it a promising drug candidate in bone tissue engineering. The current review paper aims to summarize the literatures reporting the pharmacological effects of icariin. The pharmacokinetic properties of bioactive ingredients in Herba Epimedii have also been discussed.

Keywords: Herba Epimedii; Icariin; Icaritin; Pharmacokinetic; Pharmacological effects.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacokinetics
  • Anti-Inflammatory Agents / pharmacology
  • Drugs, Chinese Herbal* / chemistry
  • Drugs, Chinese Herbal* / pharmacokinetics
  • Drugs, Chinese Herbal* / therapeutic use
  • Flavonoids / chemistry
  • Flavonoids / pharmacokinetics
  • Flavonoids / therapeutic use
  • Humans
  • Medicine, Chinese Traditional*
  • Osteoporosis / drug therapy*
  • Plants, Medicinal / chemistry*
  • Sexual Dysfunction, Physiological / drug therapy*


  • Anti-Inflammatory Agents
  • Drugs, Chinese Herbal
  • Flavonoids
  • icariin