Hypolipidemic Berberine Derivatives with a Reduced Aromatic Ring C

A series of aromatic and reduced berberine derivatives were synthesized. Their hypocholesterolemic activity was studied in vitro and in vivo . As a rule, berberine derivatives containing a reduced ring C were more capable of increasing the LDL receptor gene expression than the corresponding aromatic derivatives. Tests using a Triton WR1339-induced hypercholesterolemia model showed that 9- O -tosyltetrahydroberberine and 12-bromotetrahydroberberine possessed pronounced hypocholesterolemic activity and reduced the total cholesterol level by 33 and 27%; the triglyceride level, by 25 and 26%, respectively.