[Pharmacological activities of Z-ligustilide and metabolites in rats].
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.


CONCLUSIONS
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.
Tang
Jing
J
Department of Pharmacology & Biopharmaceutics, West China School of Pharmacy, Sichuan University, Chengdu, China.
Chen
Chu
C
Yu
Yan
Y
Du
Jun-Rong
JR
Yang
Wen
W
Wang
Cheng-Yuan
CY
D015107:4-Butyrolactone / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D001572:Benzofurans / Q000302:isolation & purification / Q000494:pharmacology*; D001711:Biotransformation; D006861:Hydrogen Peroxide; D008297:Male; D008862:Microsomes, Liver / Q000187:drug effects; D018384:Oxidative Stress / Q000187:drug effects*; D016716:PC12 Cells; D020011:Protective Agents / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley
D001572:Benzofurans; D020011:Protective Agents; C027820:ligustilide; C045855:3-N-butyl-4,5-dihydrophthalide; D006861:Hydrogen Peroxide; D015107:4-Butyrolactone