Abstract

To study the antihyperlipidemic effect of 8-alkyl-berberine derivatives (8-BBR-C_n). The experimental hyperlipidemia rabbits were prepared by feeding with high cholesterol and high fat (HCHF) diet. Then the effects of 8-alkyl-BBR on the serum levels of total cholesterol (TC), triglyceride (TG), (HDL-C), low density lipoprotein-cholesterol (LDL-C) and highdensity lipoprotein-cholesterol (HDL-C) in rabbit blood were measured and those on hepatic and kidney function were observed. 8-BBR-C_n effectively decreased the serum content of TC, TG, LDL-C and increased HDL-C level in hyperlipidemic rabbits, compared with berberine. The antihyperlipidemic effect was increased with elongating the alkyl chain of 8-BBR-C_n. Among all synthesized derivatives, 8-cetyl-berberine (8-BBR-C₁₆) showed the highest antihyperlipidemic effect, which was a dose-effect relationship on blood lipid. Pathological examination indicated that 8-BBR-C₁₆ could recover the liver tissue of rabbits damaged by high lipid diet. 8-BBR-C₁₆ showed a strong antihyperlipidemia effect with low toxicity, thus it might be a promising drug of antihyperlipidemic.

Key words: Berberine (BBR), 8-alkyl-berberine derivatives (8-BBR-C_n), antihyperlipidemic effect.