Identification and Quantification of 20(S)-Protopanaxatriol and its 20S, 24S-Epoxide in Human Urine with the Treatment of A1kaline Cleavage after the Ingestion of Sanchi Ginseng, the Roots of Panax notoginseng(三七人参)

概要

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The urinary excretion of ginseng saponins having 20(S)-protopanaxatriol (1) and 20(S)-protopanaxadiol (2) as their aglycones was studied in man following the oral administration of Sanchi Ginseng, the roots of Panax notoginseng. After a solid phase extraction of urine on a Sep-Pak Cl8, followed by alkaline cleavage and successive trimethylsilylation, the urinary metabolites were identified by El positive Selective Ion Monitoring (SIM) method using GC-MS. 20(S)-Protopanaxatriol 205,245-epoxide (5) was first identified in human urine with cumulative recoveries in the range of 0.009-0.19% (average: 0.11+0.07%) of the dose among five volunteers, along with 1. The total recoveries of excreted 1 and 5 were between 0.06 and 0.48% (average: 0.29±0.16%) of the dose. Traces of 2 and its 20,24-epoxides were also detected in urine. The maximum excretion of both 1 and S was observed at the period of 15-33 hr, with relative ratios of excreted 5 to 1 in the same volunteer time-dependently increasing until 57 hr after administration. Results of this experiment also indicate that the major urinary metabolites of dammarane saponins of Ginseng are not sapogenins, but instead suggest that they exist primarily in the form of glycosides, or as conjugates of the sapogenins or their glycosides.
日本生薬学会の論文
2002-04-20