Wogonin possesses potent inhibitory activities against cancer cell growth in vitro and in vivo and has attractive safety profiles.A highly sensitive liquid chromatography coupled with tandem mass spectrometry method w...Wogonin possesses potent inhibitory activities against cancer cell growth in vitro and in vivo and has attractive safety profiles.A highly sensitive liquid chromatography coupled with tandem mass spectrometry method was developed for the identification of major metabolites in mice liver after intravenous administration of wogonin.Five metabolites were identified and biotransformation pathways were elucidated as well.Furthermore,a method was developed and validated for the simultaneous quantitatively determination of wogonin and wogonin-7-O-glucuronide in mice liver.After liquid-liquid extraction by ethyl acetate,the analytes were separated on a C_（18）column with a mobile phase of methanol-10 mM ammonium acetate water （80：20,v/v）.The detection was operated with negative selected reaction monitoring mode using electrospray ionization technique. The linear response range was 0.2-40μg/g for both wogonin and wogonin-7-O-glucuronide in mice liver.The developed quantification method was suitable for distribution study after intravenous infusion of wogonin injection in animals.展开更多
Edaravone glucuronate and edaravone sulfate,two metabolites of edaravone,were synthesized in improved yields. Edaravone glucuronate was synthesized by conjugation of edaravone with glucuronolactone through a series of...Edaravone glucuronate and edaravone sulfate,two metabolites of edaravone,were synthesized in improved yields. Edaravone glucuronate was synthesized by conjugation of edaravone with glucuronolactone through a series of reactions.Edaravone sulfate was synthesized through sulfonation of edaravone.Compared with the reported methods in the literature,the yields of both metabolites with the improved methods were much higher.展开更多
基金China National Key Hi-Tech Innovation Project for the R&D of Novel Drugs(Grant No.2009zx09102-032).
文摘Wogonin possesses potent inhibitory activities against cancer cell growth in vitro and in vivo and has attractive safety profiles.A highly sensitive liquid chromatography coupled with tandem mass spectrometry method was developed for the identification of major metabolites in mice liver after intravenous administration of wogonin.Five metabolites were identified and biotransformation pathways were elucidated as well.Furthermore,a method was developed and validated for the simultaneous quantitatively determination of wogonin and wogonin-7-O-glucuronide in mice liver.After liquid-liquid extraction by ethyl acetate,the analytes were separated on a C_（18）column with a mobile phase of methanol-10 mM ammonium acetate water （80：20,v/v）.The detection was operated with negative selected reaction monitoring mode using electrospray ionization technique. The linear response range was 0.2-40μg/g for both wogonin and wogonin-7-O-glucuronide in mice liver.The developed quantification method was suitable for distribution study after intravenous infusion of wogonin injection in animals.
基金Jiangsu Key Laboratory of Molecular Targeted Antitumor Drug Research Foundation(Grant No.BM2008201)
文摘Edaravone glucuronate and edaravone sulfate,two metabolites of edaravone,were synthesized in improved yields. Edaravone glucuronate was synthesized by conjugation of edaravone with glucuronolactone through a series of reactions.Edaravone sulfate was synthesized through sulfonation of edaravone.Compared with the reported methods in the literature,the yields of both metabolites with the improved methods were much higher.
