Abstract:Objective: Reveal the composition of bitter substance and its biological activity of Schisandra chinensis. Method: Using organic solvent extraction and silica gel separation to prepare bitter substances from Schisandra chinensis, HPLC were applied for qualitative and quantitative analysis. Meanwhile, observed the biological activity of bitter substance. Result: The bitterness substances mainly contains lignans, the total amount of six lignans were approximately 42.5%.The bitterness substances in high dose group had significant inhibitory effect on the spontaneous activity of mice(P<0.05) and also could significantly prolong the sleeping time of mice with pentobarbital sodium(P<0.001); and there has no obvious effect on the swimming time of mice, but can prolong the normobaric hypoxia tolerance time(P<0.05); high and low groups bitter substance can reduce total cholesterol in hyperlipidemic rats (TC)(P<0.01), elevated low density lipoprotein(LDL)and high density lipoprotein(HDL)content, and high dose group was stronger than the low dose group. Conclusion: Bitter substance of S. chinensis is the Pharmacodynamic substance with sedative, hypnotic, antihypoxia and hypolipidemic effect.