[Study on the metabolites of guanfu base A hydrochloride in rat urine by high performance liquid chromatograph-mass spectrum].
OBJECTIVE
To study the metabolites of guanfu base A hydrochloride (GFA) in rat urine.


METHODS
Rat urine was collected after i.v. injection of GFA. Phase I metabolites were identified by HPLC/MS and by comparison with authentic standards. Phase II conjugates were treated with either glucuronidase or sulfatase in presence or absence of glucuronidase specific inhibitor D-saccharic acid beta-1,4-lactone. The aglycones were identified by HPLC/MS.


RESULTS
Phase I metabolites guanfu base I (GFI) and guanfu alcohol-amine (AA) were separated and identified in rat urine by comparison with authentic standards. Phase II conjugates, for which no authentic standards were available, GFA glucuronide and sulfate conjugates, GFI glucuronide and sulfate were separated and tentatively identified by hydrolysis with glucuronidase or sulfatase, the aglycones, GFA and GFI, were identified in rat urine.


CONCLUSIONS
After i.v. injection of GFA, GFA is metabolized into GFI, AA, GFA glucuronide and sulfate conjugates, GFI glucuronide and sulfate conjugates in rat urine. The polarity of the metabolites is increased, and the effectiveness of them is lower than the parent drug.
A
Ji-ye
JY
Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing 210009, China. ajiye@public1.ptt.js.cn
Wang
Guang-ji
GJ
Liu
Xiao-quan
XQ
Jiang
Dan-yun
DY
Liu
Jing-han
JH
D031841:Aconitum / Q000737:chemistry; D000470:Alkaloids / Q000302:isolation & purification / Q000378:metabolism* / Q000652:urine; D000818:Animals; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D008401:Gas Chromatography-Mass Spectrometry; D006576:Heterocyclic Compounds, 4 or More Rings; D008297:Male; D010946:Plants, Medicinal / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar
D000470:Alkaloids; D006576:Heterocyclic Compounds, 4 or More Rings; C040615:Guan-fu base A