Pharmacokinetic study and metabolite identification of the bidesmosidic triterpenoid saponin BTS-1 in rat plasma

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• 作者：Jianguang Luo ; Chan Zhou ; Wei Zhang ; Lingyi Kong ; ^{cpu_lykong@126.com}
• 关键词：Triterpenoid saponin ; BTS-1 ; HPLC ; LC&ndash ; MSn ; Pharmacokinetic study ; Metabolite identification ; Rat plasma
• 刊名：Acta Pharmaceutica Sinica B
• 出版年：2013
• 出版时间：May, 2013
• 年：2013
• 卷：3
• 期：3
• 页码：174-179
• 全文大小：364 K

文摘

Assays based on high-performance liquid chromatography (HPLC) and liquid chromatography tandem mass spectrometry (LC-MSⁿ) have been developed and validated for the determination and metabolite identification of the bidesmosidic triterpenoid saponin, BTS-1 (3-O-¦Â-d-galactopyranosyl-(1¡ú2)-[¦Â-d-xylopyranosyl-(1¡ú3)]-¦Â-d-glucuronopyranosyl gypsogenin 28-O-¦Á-l-arabinopyranosyl-(1¡ú3)-¦Â-d-xylopyranosyl-(1¡ú4)-¦Á-l-rhamnopyranosyl-(1¡ú2)-¦Â-d-fucopyranoside), in rat plasma. The assay was successfully applied to a pharmacokinetic study in rats given a single oral dose of BTS-1 (400 mg/kg). The results indicated that the compound was rapidly absorbed (T_max=1.28¡À0.29 h, C_max=37.4¡À5.6 ¦Ìg/mL) and slowly eliminated (t_1/2=13.2¡À6.6 h). In addition, secondary glycosides and aglycones of BTS-1 were detected and identified. Since these metabolites are known to be active ¦Á-glucosidase inhibitors, they probably play an important role in mediating the pharmacological effects of the saponin.