Influence of lipophilic structure-modification on lipid-modulating effect of berberine in vivo
AIM: To study the effect of lipophilic structure-modification on Lipid-modulating ability of berberine in vivo. METHODS: With 8-alkyl-berberine homologues ( Ber-n) as model drug and experimental hyperlipidemia rats as animal model, the normal con trol group ( NC) , high fat control group ( FC) and drug groups including berbreine ( Ber-O) group, 8-butyl-berberine ( Ber-4 ) group, 8-octyl-berberine ( Ber-8 ) group, 8-dodecyl-berberine ( Ber-12 ) group and 8-cetyl-berberine(Ber-16) group were set up randomly. During experiment, the basic diet were supplied to NC group and high fat diet to FC group and 5 drug groups, and all drug groups were treated with corresponding drug by dose of 125 mg/kg a day respectively and NC group and FC group with drugs solvent by gavage. The serum indexes including total cholesterol ( TC ) , total glyceride(TG) and high density lipoprotein cholesterol ( HDL-C ) were determined after administration at 10 or 25 d respectively. RESULTS: After administration at 10 d the appreciably repairing effect of all drug groups on serum indexes were observed, and the HDI>-C value of Ber-8 group( 1. 22±0. 19) mmol/L was significantly different than that of FC group (0. 95 ± 0. 19) mmol/L. After administration at 25 d, the serum TC value of Ber-8 group (6. 77 ± 3.26) mmol/L were significantly different (P <0. 05) and that of Ber-12 group(5. 24 ± 2. 45) mmol/L and Ber-16 group(4. 78 ± 2. 67) mmol/L were very significantly different ( P < 0. 01 ) than that of FC group ( 11. 38 ± 3. 41 ) mmol/L, and the serum TG value of Ber-12 group (0. 64 ±0. 25) mmol/L and Ber-16 group(0. 66 ± 0. 23) mmol/L both were significantly different ( P < 0.05 ) than that of FC group( 1.05 ±0.37) mmol/L, and the serum HDL-C value of Ber-8 group ( 1. 34 ±0. 20) mmol/L were significantly different (P < 0. 05 ) and that of Ber-12 group ( 1. 49 ± 0.21) mmol/L and Ber-16 group( 1.48 ±0. 28) mmol/L were very significantly different P < 0. 01 ) than that of FC group ( 1. 11 ± 0.21) mmol/L. CONCLUSION: Overall analysis, the Lipid modulating effects of Ber-re increased as the length of aliphatic chain was elongated. The lipophilic structure-modification on ber berine molecule are beneficial to exerting Lipid-modulating effect in vivo.
NETL
NSTL
万方数据
维普
