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采用超高效液相色谱/四极杆飞行时间质谱法,结合血浆药物化学和微透析技术,筛选知母皂苷提取物中的潜在生物活性成分及其代谢产物。

Plasma pharmacochemistry combined with microdialysis to screen potential bioactive components and their metabolites in Anemarrhena asphodeloides saponin extract using ultrahigh-performance liquid chromatography/quadrupole-time-of-flight mass spectrometry.

机构信息

School of Pharmacy, Second Military Medical University, Shanghai, PR China.

出版信息

J Sep Sci. 2013 May;36(9-10):1659-66. doi: 10.1002/jssc.201201116.

Abstract

Although various techniques have been employed to analyze drug metabolites, the metabolism of multicomponent herbal medicine has seldom been fully addressed. In contrast to chemical drugs, a number of compounds in herbal medicine could get into circulation and then be metabolized. Metabolism study on active constituents in herbal medicine is a good way for us to explain and predict a variety of events related to the efficacy and toxicity of herbal medicine. The present work aims to elucidate the multicomponent metabolic characteristics of a herbal medicine by the combination of plasma pharmacochemistry and microdialysis sampling. Anemarrhena asphodeloides, a well-known traditional Chinese medicine, was chosen as a model. After oral administration of A. asphodeloides saponin extract to rats, microdialysis samples were collected continuously in the jugular vein and analyzed by ultrahigh-performance LC/quadrupole-TOF MS. The identification of compounds in biosamples was achieved by accurate mass measurement and detailed fragmentation pathway analysis. The results showed that unbound constituents in blood circulation of the rat included seven parent saponins and six metabolites, which might be the potential active components in vivo. Among which, three metabolites have not been previously reported and were identified in this study. It is the first report on systemic metabolism of total saponins of A. asphodeloides in mammalian plasma.

摘要

尽管已经采用了各种技术来分析药物代谢物,但对复方草药的代谢研究却很少得到充分的关注。与化学药物不同,草药中的许多化合物可以进入循环并被代谢。对草药中活性成分的代谢研究是一种很好的方法,可以帮助我们解释和预测与草药的功效和毒性相关的各种事件。本工作旨在通过血浆药物化学和微透析采样相结合的方法阐明草药的多成分代谢特征。知母是一种著名的中药,被选为模型药物。在大鼠口服知母皂苷提取物后,连续从颈静脉采集微透析样品,并通过超高效液相色谱/四极杆飞行时间质谱进行分析。通过精确质量测量和详细的碎片途径分析来鉴定生物样品中的化合物。结果表明,大鼠血液循环中的游离成分包括七种母皂苷和六种代谢物,它们可能是体内潜在的活性成分。其中三种代谢物以前没有报道过,是在本研究中鉴定出来的。这是知母总皂苷在哺乳动物血浆中系统代谢的首次报道。

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