Isolation of herpetin from Herpetospermum seed and hepatoprotective activity of liposomal herpetin against carbon tetrachloride-induced liver injury in mice.

OBJECTIVE

The aims of this study were to demonstrate the hepatoprotective activity of herpetin (HPT) and the enhanced hepatoprotective efficiency of liposomal herpetin against carbon tetrachloride-induced liver injury in mice.

METHODS

Herpetin was isolated from Herpetospermum seed and identified by ESI-MS and NMR. To enhance liver targeting and improve solubility of HPT, liposomal HPT was prepared with optimal formulation. The intravenous injection safety of the liposomes was then evaluated. Further, the hepatoprotective effects of liposomal HPT on model mice were investigated by the comparison of different liver marker enzymes and histopathological examination.

RESULTS

The prepared HPT liposome showed spherical or ellipsoidal vesicles with the entrapment efficiency of 94.50 ± 2.15% and particle size of 119.2 ± 10.7 nm. After 4 days intravenous administration of liposomal herpetin, no obvious damage could be observed at the injection site of each group. The liposomal HPT has no destructive effect on erythrocytes and little influence on whole blood clotting time. Free HPT exhibited only a weak protective function to model mice, whereas an enhanced hepatoprotective activity was observed using liposomal herpetin for treatment.

CONCLUSION

The hepatoprotective efficiency of herpetin is able to be promoted through pharmaceutical application of liposome and liposomal herpetin is a promising new medicine for hepatoprotection.