首页> 外文期刊>RSC Advances >A UPLC-MS/MS method for simultaneous quantification of pairs of oleanene- and ursane-type triterpenoid saponins and their major metabolites in mice plasma and its application to a comparative pharmacokinetic study
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A UPLC-MS/MS method for simultaneous quantification of pairs of oleanene- and ursane-type triterpenoid saponins and their major metabolites in mice plasma and its application to a comparative pharmacokinetic study

机译:UPLC-MS / MS方法同时定量小鼠血浆中的双萜烯和乌烷型三萜皂苷及其主要代谢物对及其在比较药代动力学研究中的应用

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Ilexhainanoside D (IhD) and Ilexsaponin A _(1) (IsA) are a pair of oleanene- and ursane-type triterpenoid saponins, which are also the main bioactive pharmaceutical ingredients of Ilex hainanensis Merr. with great potential to treat non-alcoholic fatty liver disease (NAFLD). The pharmacokinetics of four representative triterpenoids in mice were investigated in this study, which were IhD, IsA and their major metabolites 3β, 19α-dihydroxyolean-12-ene-24, 28-dioic acid (ID) and Ilexgenin A (IA). A sensitive and accurate UPLC-MS/MS method was developed and validated for the simultaneous quantitative determination of IhD, IsA, ID and IA in control and NAFLD mice plasma after oral administration of the total saponins of I. hainanensis (the contents of IhD and IsA were 41.6% and 54.4%, respectively). The results revealed that the pharmacokinetic behaviors could be changed in NAFLD mice compared with control mice. The area under the plasma drug concentration–time curve and maximum plasma concentrations of IhD and IsA were greatly decreased in the NAFLD mice. However, the main residence time of ID and IA were greatly increased in the NAFLD mice. The results revealed that this method could be used to analyze two pairs of triterpenoid isomers in biological samples.
机译:冬凌草甙D(IhD)和冬凌草皂苷A _(1)(IsA)是一对茄尼型和乌桑烷型三萜皂苷,也是海南冬凌草(Melex hainanensis Merr)的主要生物活性药物成分。具有治疗非酒精性脂肪肝疾病(NAFLD)的巨大潜力。在这项研究中,研究了四种代表性的三萜类化合物在小鼠中的药代动力学,它们分别是IhD,IsA及其主要代谢物3β,19α-二羟基油烯-12-ene-24、28-二酸(ID)和Ilegengenin A(IA)。建立了一种灵敏而准确的UPLC-MS / MS方法,并通过口服海南总皂苷(IhD和IgD的含量)同时测定了对照组和NAFLD小鼠血浆中IhD,IsA,ID和IA的有效性。 IsA分别为41.6%和54.4%)。结果表明,与对照组相比,NAFLD小鼠的药代动力学行为可以改变。在NAFLD小鼠中,血浆药物浓度-时间曲线下的面积以及IhD和IsA的最大血浆浓度大大降低。然而,在NAFLD小鼠中ID和IA的主要停留时间大大增加了。结果表明,该方法可用于分析生物样品中的两对三萜类异构体。

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