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采用液相色谱-质谱法从五加科植物刺五加叶中分离得到天然皂甙——杠柳苷 B,对其口服代谢产物进行了结构表征。

Structural characterization of the metabolites of orally ingested hederasaponin B, a natural saponin that is isolated from Acanthopanax senticosus leaves by liquid chromatography-mass spectrometry.

机构信息

Key Laboratory of Chinese Materia Medica (Heilongjiang University of Chinese Medicine), Ministry of Education, 24 Heping Road, Harbin, 150040, PR China.

Key Laboratory of Chinese Materia Medica (Heilongjiang University of Chinese Medicine), Ministry of Education, 24 Heping Road, Harbin, 150040, PR China.

出版信息

J Pharm Biomed Anal. 2021 Apr 15;197:113929. doi: 10.1016/j.jpba.2021.113929. Epub 2021 Jan 29.

Abstract

Plant saponins are important natural product with biologically active. However, the metabolism of these compounds has rarely been studied due to their low bioavailability and the complexity of their metabolite structures. In this study, ultra-performance liquid chromatography/Fusion Lumos Orbitrap mass spectrometry was used to analyze the metabolites of hederasaponin B in vivo, and its possible metabolic pathways were proposed. After oral administration of the parent drug, a total of 47 metabolites are identified in rat feces (42), urine (11), and plasma (9) samples. These metabolites resulted from the metabolic processes in phases I and II reactions involved in deglycosylation, hydroxylation, acetylation, oxidation, gluconalciation and glycosylations. Deglycosylation is the main metabolic pathway (accounts for 52.46 % of all metabolites in feces samples). Among the identified metabolites, four were glycosylated (deprotonated precursors at m/z = 1335.7, 1365.7, 1467.9, and 1379.6) with higher molecular weight than the parent drug . These glycosylated compounds account for 11.55 % of the metabolites in rat feces according to the semi-quantitative chromatographic peak areas. To sum up, the results of this study provide a basis for further understanding the metabolism of plant saponins in vivo.

摘要

植物皂苷是具有生物活性的重要天然产物。然而,由于其生物利用度低和代谢产物结构复杂,这些化合物的代谢很少被研究。在这项研究中,采用超高效液相色谱/融合 Lumos Orbitrap 质谱法分析了熊果酸 B 在体内的代谢产物,并提出了其可能的代谢途径。在口服给药母体药物后,在大鼠粪便(42 个)、尿液(11 个)和血浆(9 个)样品中鉴定出 47 种代谢物。这些代谢物来源于涉及去糖基化、羟化、乙酰化、氧化、葡萄糖醛酸化和糖基化的 I 相和 II 相反应的代谢过程。去糖基化是主要的代谢途径(占粪便样品中所有代谢物的 52.46%)。在鉴定出的代谢物中,有四个是糖基化的(m/z=1335.7、1365.7、1467.9 和 1379.6 的去质子前体),分子量比母体药物高。根据半定量色谱峰面积,这些糖基化化合物占大鼠粪便中代谢物的 11.55%。总之,本研究结果为进一步了解植物皂苷在体内的代谢提供了依据。

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