Abstract： Objective To investigate the therapeutic effect of berberine (BBR) on regulating hyperlipidemia and its possible mechanism. Methods Sixty eight patients with hyperlipidemia were divided into two groups according to the method of treatment: BBR (n=34), simvastatin(n=16)and atorvastain (n=18). Plasma levels of TC,TG,LDL-C and HDL-C were measured before and after therapy. At the same time, expression of LDLR and PPARγ mRNA were analyzed with RT-PCR and Western blot. Results The plasma TC,TG and LDL-C levels decreased by 21.41% , 26.4% and 28.22% respectively , and there were significant differences before and after BBR treatment (P=0.000). The plasma TC level of BBR group was significantly lower than that of simvastatin group (P=0.001). and the plasma TG level of BBR group was lowers than that of atorvastain group. There were the same changes in the plasma LDL-C and HDL-C levels among BBR, simvastatin and atorvastain groups. Berberine accelerated LDLR mRNA transcription, up-regulated LDLR expression and regulated cellular absorption and metabolism of lipid protein. Conclusions Berberine has effective role in lowering plasma TC, TG and LDL-C levels, which may be superior to simvastatin and atorvastain in some aspects. The mechanism of its lowering blood lipid is related to its effect on LDLR expression