In vivo metabolism study of ginsenoside Re in rat using high-performance liquid chromatography coupled with tandem mass spectrometry

• Published in: Analytical and bioanalytical chemistry 2009-11, Vol.395 (5), p.1441-1451
• Main Authors: Yang, Liu, Xu, Shunjun, Liu, Chunjin, Su, Zhijun
• Format: Article
• Language: English
• Subjects: Administration, Oral; Analytical Chemistry; Animals; Biochemistry; Biomedical materials; Characterization and Evaluation of Materials; Chemistry; Chemistry and Materials Science; Chromatographic methods and physical methods associated with chromatography; Chromatography, High Pressure Liquid - methods; Exact sciences and technology; Food Science; Ginsenosides - administration & dosage; Ginsenosides - chemistry; Ginsenosides - urine; Glycosylation; In vivo tests; Injections, Intravenous; Ionization; Laboratory Medicine; Liquid chromatography; Male; Mass spectrometry; Metabolites; Molecular Structure; Monitoring/Environmental Analysis; Original Paper; Other chromatographic methods; Oxidation-Reduction; Rats; Rats, Sprague-Dawley; Spectrometric and optical methods; Spectrometry, Mass, Electrospray Ionization - methods; Surgical implants; Tandem Mass Spectrometry - methods; Urine
• ISSN: 1618-2642; 1618-2650
• DOI: 10.1007/s00216-009-3121-1

Ginsenoside Re is one of the major the bioactive triterpene saponins in ginseng root, a well-known adaptogen in traditional Chinese medicine. It is believed that the lead compound may be further developed into a promising new drug for preventing hypertension and cardiovascular disease. To better understand the pharmacological activities of the component, an investigation of its in vivo metabolism was necessary. In the present study, a high-performance liquid chromatography coupled with electrospray ionization and quadrupole time-of-flight tandem mass spectrometry (HPLC-ESI-TOF-MS/MS) has been applied to discover and identify the metabolites of ginsenoside Re in rat urine following intravenous and oral administration of the component, respectively. The rat urine samples were collected and pretreated through C₁₈ solid-phase extraction cartridges prior to analysis. Negative electrospray ionization mass spectrometry was used to discern ginsenoside Re and its possible metabolites in urine samples. The metabolites were identified and tentatively characterized by means of comparing molecular mass, retention time, and fragmentation pattern of the analytes with those of the parent compound, ginsenoside Re. As a result, eleven and nine metabolites together with Re were detected and identified in rat urine collected after intravenous and oral administration, respectively. A possible metabolic pathway of ginsenoside Re was also investigated and proposed. Oxidation and deglycosylation were found to be the major metabolic processes of the constituent in rat. [graphic removed]