In an attempt to identify compounds with antihepatotoxic activity, car
bon tetrachloride-induced cytotoxicity in primary cultured rat hepatoc
ytes has been adopted as a screening system. Using this screening syst
em, an antihepatotoxic compound from the aerial parts of Epimedium kor
eanum has been isolated. This compound, icariin, is a flavonol glycosi
de. Its antihepatotoxic activity was first evaluated by measuring the
release of glutamic pyruvic transaminase and sorbitol dehydrogenase ho
m CCl4-intoxicated rat hepatocytes into the culture medium. Icariin si
gnificantly reduced the level of glutamic pyruvic transaminase and sor
bitol dehydrogenase released resulting in a 76% protection from toxici
ty at concentration ranges from 1 mu M to 20 mu M. 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.