Metabolites of injected chlorogenic acid in rats.
- Author:
Cen XIE
1
;
Da-Fang ZHONG
;
Xiao-Yan CHEN
Author Information
1. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
- Publication Type:Journal Article
- MeSH:
Animals;
Bile;
metabolism;
Biotransformation;
Chlorogenic Acid;
administration & dosage;
blood;
pharmacokinetics;
urine;
Chromatography, High Pressure Liquid;
methods;
Cysteine;
metabolism;
Feces;
chemistry;
Glucuronides;
metabolism;
Glutathione;
metabolism;
Injections, Intravenous;
Male;
Protein Binding;
Rats;
Rats, Sprague-Dawley;
Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization;
methods
- From:
Acta Pharmaceutica Sinica
2011;46(1):88-95
- CountryChina
- Language:Chinese
-
Abstract:
Chlorogenic acid (5-CQA) is one of the major components in some Chinese herbal injections. However, the metabolism of 5-CQA in rats after intravenous injection has not been determined. An ultra-high performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC/Q-TOF MS) method was applied to identify the metabolites in bile, urine, feces and plasma after a single intravenous administration of 10 mg x kg(-1) 5-CQA to rats. Using MSE and mass defect filter techniques, a total of 35 metabolites were detected in bile, urine, feces and plasma. The predominant metabolites in bile were glutathione conjugates of O-methyl-5-CQA, accounting for approximately 80% of the metabolites excreted in bile. The major components in urine were parent drug, O-methyl-5-CQA, hydrolyzed metabolites and glucuronide conjugates. The major components in feces were O-methyl-5-CQA and its cysteine conjugates. The major component in plasma was the parent drug. The urinary and fecal excretion pathways were equally important to 5-CQA in rats. These results demonstrate that 5-CQA undergoes extensively metabolism in rats and are highly reactive to nucleophiles such as GSH. This finding indicates that attention should be paid on the injections containing 5-CQA, which may covalently bind to proteins, leading to allergenic drug reactions.
