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首页> 外文期刊>RSC Advances >Stereoisomerism metabolites found in rats after oral administration of timosaponin B-II using HPLC-Q-TOF-MS and NMR methods
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Stereoisomerism metabolites found in rats after oral administration of timosaponin B-II using HPLC-Q-TOF-MS and NMR methods

机译：使用HPLC-Q-TOF-MS和NMR方法口服给予替莫皂苷B-II后在大鼠中发现的立体异构代谢产物

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摘要

Timosaponin B-II (TB-II), a representative furostanol saponin from Rhizoma Anemarrhenae, has been used to treat diabetes and senile dementia. To better understand the action mechanism of TB-II, it is indispensable to study its metabolism profile in vivo. A HPLC-Q-TOF-MS and NMR methods for the analysis of TB-II and its metabolites in rat urine has been developed. Five derivatives of TB-II including one novel compound (timosaponin BIII-d) were synthesized and used as the reference compounds. In rat urine, a total of 13 metabolites were identified after oral administration of TB-II and eight of them were confirmed by NMR. The metabolic pathways of TB-II were mainly deglycosylation, F-ring isomerization, and even stereoisomerism at C-25. It is important for understanding metabolism of TB-II in rats to clarify its metabolic pathways in vivo, which will also provide useful information and reference for similar study in humans. Moreover, the metabolites could contribute to obtain better compounds than TB-II for the development of new drugs in the future.
机译：Timosaponin B-II（TB-II），是一种来自知母的呋喃固醇皂苷，已被用于治疗糖尿病和老年性痴呆。为了更好地了解TB-II的作用机理，必须在体内研究其代谢情况。已经开发出了用于分析大鼠尿液中TB-II及其代谢物的HPLC-Q-TOF-MS和NMR方法。合成了五种TB-II衍生物，其中包括一种新型化合物（托莫司汀BIII-d），并用作参考化合物。在大鼠尿液中，口服TB-II后共鉴定出13种代谢物，其中8种经NMR确认。 TB-II的代谢途径主要是去糖基化，F环异构化，甚至在C-25处的立体异构。了解大鼠体内TB-II的代谢对于阐明其体内代谢途径非常重要，这也将为人类进行类似研究提供有用的信息和参考。而且，在将来开发新药时，这些代谢物可能有助于获得比TB-II更好的化合物。

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