80% extract of Gamigwaruhaebaekbaekju-Tang (GGHBT), Gagamgwaruhaebaekbaekju-Tang (GGGHBT) and Gamigwaruhaebaekwhanggum-Tang (GGHWT) remarkably showed inhibitory effects on HMG-CoA reductase, lipid peroxidation of rat liver and LDL oxidation, and DPPH free radical scavenging effect in a dose-dependent manner. Especially, GGHWT which is formulated with Trichosanthis Fructus, Pinelliae Tuber, Aurantii Immatures Fructus, Magnoliae Cortex, Allii Macrostemi Bulbus, Cinnamomi Ramulus and Scutellariae Radix on the basis of Gwaruhaebaekbaekiu-Tang listed on the traditional medicinal references showed more effective hypocholesterolemic activities in vitro bioassay than the other prescriptions.