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目的:研究川续断皂苷Ⅵ在大鼠体内的代谢。方法:采用高效液相色谱-电喷雾质谱检测大鼠灌胃川续断皂苷Ⅵ后血浆、尿液、胆汁和粪便中的代谢产物。使用Agilent公司Zorbax Extend-C18色谱柱(150 mm×4.6 mm,5!m),以0.05%甲酸乙腈-0.05%甲酸水为流动相梯度洗脱(0～12 min,25%B→27%B;12～30 min,27%B→50%B;30～40 min,50%B→80%B;40～45 min,80%B→90%B;45～50 min,90%B),进行色谱分离,并与电喷雾质谱联用,毛细管电压为2.50 kV,锥孔电压为35 V,干燥气流速为320 L.h-1以及离子源温度为120℃,根据全扫描检测正、负离子模式下获得的准分子离子峰推测化合物的分子量信息及其可能的化学结构。结果:在大鼠血浆、尿液、粪便和胆汁中均检测到原型成分,粪便中检测到川续断皂苷Ⅵ脱去1分子(RM1,RM2)、2分子(RM3,RM4)及全部糖基(RM5)的5个代谢产物,血浆和胆汁中检测出脱去2分子葡萄糖残基的代谢产物(RM4),此外在胆汁中首次发现川续断皂苷Ⅵ的羟基化产物(RM6)。结论:川续断皂苷Ⅵ在大鼠体内的转化主要是在肠道的脱糖基代谢及在肝脏的羟基化反应。
Objective: To study the metabolism of Dipsacus saponins Ⅵ in rats. Methods: The metabolites in plasma, urine, bile and feces of rats after oral administration of Duanchuan saponins Ⅵ were detected by high performance liquid chromatography-electrospray ionization mass spectrometry. The mobile phase was eluted with 0.05% formic acid in acetonitrile-0.05% formic acid water (0-12 min, 25% B → 27% B) using a Zorbax Extend-C18 column (150 mm × 4.6 mm, ; 12-30 min, 27% B → 50% B; 30-40 min, 50% B → 80% B; 40-45 min, 80% B → 90% B; 45-50 min, 90% B) Chromatography and electrospray ionization mass spectrometry were used with a capillary voltage of 2.50 kV, a cone voltage of 35 V, a dry gas flow rate of 320 Lh-1 and an ion source temperature of 120 ° C. The positive and negative ion modes The excimer ion peak obtained presumed the molecular weight of the compound and its possible chemical structure. Results: Prototype components were detected in plasma, urine, feces and bile of rats. One molecule (RM1, RM2), two molecules (RM3, RM4) and all the glycosyl (RM5) five metabolites were detected in the plasma and bile off the two glucose residues metabolites (RM4), in addition to the first discovery in the bile of Sichuan Dipsaccharides Ⅵ hydroxylation product (RM6). CONCLUSION: The transconversion of Daphniphyllum saponins Ⅵ in rats is mainly caused by the de-glycosylation metabolism in the intestine and the hydroxylation reaction in the liver.