Antihepatotoxic activity of icariin, a major constituent of Epimedium koreanum

Lee MK, Choi YJ, Sung SH, Shin DI, Kim JW, Kim YC.
College of Pharmacy, Seoul National University, Korea.

In an attempt to identify compounds with antihepatotoxic activity, carbon tetrachloride-induced cytotoxicity in primary cultured rat hepatocytes has been adopted as a screening system. Using this screening system, an antihepatotoxic compound from the aerial parts of Epimedium koreanum has been isolated. This compound, icariin, is a flavonol glycoside. Its antihepatotoxic activity was first evaluated by measuring the release of glutamic pyruvic transaminase and sorbitol dehydrogenase from CCl4-intoxicated rat hepatocytes into the culture medium. Icariin significantly reduced the level of glutamic pyruvic transaminase and sorbitol dehydrogenase released resulting in a 76% protection from toxicity at concentration ranges from 1 microM to 20 microM. The antihepatotoxic activity of icariin was also estimated by the determination of total cytochrome P-450 content and glutathione-S-transferase activity in the CCl4-intoxicated hepatocytes.