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Metabolite identification and pharmacokinetic study of Lamiophlomis rotata in rats

机译:大鼠鳞叶草旋转液的代谢物鉴定及药代动力学研究

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摘要

An ultra-high performance liquid chromatography coupled with time-of-flight mass spectrometry technique and a subsequent LC-MS/MS method were developed for metabolite profile study of Lamiophlomis rotata extract after its oral administration. Metabolite profile analysis for plasma, bile, urine and feces were performed on a sub-2-μm analytical column, and showed that 39 prototypes and 47 metabolites were identified or tentatively characterized. More than half the metabolites underwent phase II reaction, including sulfate, glucuronide, taurine, glycine, and glutathione conjugation. The targeted and valid LC-MS/MS method, using one-step protein precipitation for rat plasma, was applied for the pharmacokinetic study of shanzhiside methyl ester, 8- O -acetylshanzhiside methyl ester, lamalbid, verbascoside, forsythoside B, and luteolin-7- O -β- D -glucopyranoside. Pharmacokinetics results showed that six bioactive components did not vary significantly in rats after administration of the aerial parts and the whole plant, which was consistent with the metabolite profile comparison between two groups. This article contributes to the understanding of the metabolism of L. rotata , and provides detailed performance analysis and scientific data to support the medicine parts alteration in the Chinese Pharmacopoeia.
机译:耦合与飞行时间质谱技术和随后的LC-MS / MS方法的超高效液相色谱法,用于在其口服给药后的Lamoophlomis Rotata提取物的代谢物剖面研究。对血浆,胆汁,尿液和粪便进行代谢物剖面分析,在亚2μm分析柱上进行,并鉴定或暂时表征了39种原型和47个代谢物。几种以上的代谢物接受了II期反应,包括硫酸盐,葡糖醛酸,牛磺酸,甘氨酸和谷胱甘肽缀合。靶向的和有效的LC-MS / MS方法,使用用于大鼠血浆的一步蛋白质沉淀,用于Shanzhiside甲酯的药代动力学研究,8-O-乙酰辛酰胺甲酯,Lamalbid,术术,连囊化B和曲霉素 - 7-O-β-D-戊醇苷。药代动力学结果表明,在给予航空零部件和整株植物后,大鼠六种生物活性组分在大鼠中没有变化,这与两组之间的代谢物型材比较一致。本文有助于了解L. Rotata的新陈代谢,并提供详细的性能分析和科学数据,以支持中国药典的药物零件改变。

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