Abstract: AimTo study the different biological activities of the enantiomers of the anti-hepatitis drug (±)-bicyclol, the (±)-bicyclol was resolved. MethodsBy being treated with optically active alkaloid, the two diastereoisomers alkaloid salts of the compound could be obtained, separately. After decomposing and methylating, they were transformed separately into (-)-bicyclol and (+)-bicyclol. ResultsThe two enantiomers of bicyclol were determined by melting point, ［α］D, ¹H NMR, MS and chiral column HPLC. ConclusionComparison of hepatoprotective action of racemic bicyclol and (-)-, (+)-bicyclol on experimental liver injury, the effect of (-)-bicyclol was two times more potent than that of racemic bicyclol and the potency of (+)-bicyclol was much less than that of the racemate.