OBJECTIVE: To study the metabolism of Z-ligustilide(Z-LIG) in vivo and in vitro in rats and the pharmacological activities of Z-LIG and metabolites in vitro. METHODS: The biotransformation of Z-LIG in rats in vivo was tested. Z-LIG was also incubated with rat liver microsomes in vitro. The incubated product was extracted, separated and identified with high performance liquid chromatography (HPLC), high resolution mass spectrometry, nuclear magnetic resonance spectrum and UV. The effects of Z-LIG and its main metabolites on hydrogen peroxide (H1O2)-induced injuries were examined in cultured PC12 cells. RESULTS: The HPLC analysis of the metabolites of Z-LIG was obtained. Senkyunolide I (SYL) isolated from in vitro incubation was identified as the main metabolite of Z-LIG. Both Z-LIG and SYL showed significant and concentration-dependent protection against H2O2-induced injuries in PC12 cells. CONCLUSION: SYL is the main metabolite of Z-LIG in rats. Z-LIG and SYL exert similar protective effects against oxidative damage in cultured PC12 cells.
OBJECTIVE: To study the metabolism of Z-ligustilide(Z-LIG) in vivo and in vitro in rats and the pharmacological activities of Z-LIG and metabolites in vitro. METHODS: The biotransformation of Z-LIG in rats in vivo was tested. Z-LIG was also incubated with rat liver microsomes in vitro. The incubated product was extracted, separated and identified with high performance liquid chromatography (HPLC), high resolution mass spectrometry, nuclear magnetic resonance spectrum and UV. The effects of Z-LIG and its main metabolites on hydrogen peroxide (H1O2)-induced injuries were examined in cultured PC12 cells. RESULTS: The HPLC analysis of the metabolites of Z-LIG was obtained. Senkyunolide I (SYL) isolated from in vitro incubation was identified as the main metabolite of Z-LIG. Both Z-LIG and SYL showed significant and concentration-dependent protection against H2O2-induced injuries in PC12 cells. CONCLUSION: SYL is the main metabolite of Z-LIG in rats. Z-LIG and SYL exert similar protective effects against oxidative damage in cultured PC12 cells.