两种新化学成分的代谢物鉴定。Toosendan摘要。调查。UPLC/ESI/qTOF-MS分析

IF 1.3 4区 化学 Q4 BIOCHEMICAL RESEARCH METHODS
Yuan Liu, Ranchen Xu, Siqi Gu, Shuning Li, Ye Fang, Anam Naseem, Yan Liu, Bingyou Yang
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引用次数: 0

摘要

米利亚。toosendan摘要。调查。是一种强效的草药,具有多种治疗特性。作为主要成分,异仙丹素阻断了化疗诱导的培养癌细胞和异种移植肿瘤组织的保护性自噬,显著增强了抗癌活性,而曲辛内酮具有杀虫、抗炎和免疫调节作用。到目前为止,代谢谱仍然未知。本研究采用UPLC/ESI/qTOF-MS分析方法,对大鼠血液、尿液和粪便中的13种异仙丹素代谢物和13种曲辛酮代谢物进行了表征。5种代谢物(F-M3, F-M5, I-M1, I-M5, I-M8)被完全表征。异仙丹素和黄曲霉酮主要参与氢化、乙酰化和甲基化代谢反应。这是首次阐明这两种成分在体内代谢的研究,为今后的药效学和机制研究奠定了基础。深入了解药物活化、失活的过程,合理设计新药,指导新药的研发。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Metabolites Identification of Two Novel Chemical Constituents From Melia. Toosendan Sieb.et Zucc. in Rats by UPLC/ESI/qTOF-MS Analysis

Melia. toosendan Sieb.et Zucc., a potent herbal medicine, boasts diverse therapeutic properties. As the main components, the isotoosendanin blocks protective autophagy in chemotherapy-induced cultured cancer cells and xenograft tumor tissue to significantly enhancing anticancer activity, and the fraxinellone contributes to pesticidal activity, anti-inflammatory and immunomodulatory effects. Until now, the metabolic profiles remained unknown. In the present study, 13 metabolites of isotoosendanin and 13 metabolites of fraxinellone were characterized in the blood, urine, and feces of rats by UPLC/ESI/qTOF-MS analysis. Five metabolites (F-M3, F-M5, I-M1, I-M5, I-M8) were fully characterized. The isotoosendanin and fraxinellone were mainly involved in hydrogenation, acetylation, and methylenation metabolic reactions. This is the first study illuminates the two components in vivo metabolism, laying the foundation for future pharmacodynamic and mechanistic investigations. It is necessary to deeply understand the process of drug activation, and deactivation, rationally design new drugs, and guide the research and development of new drugs.

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来源期刊
Chromatographia
Chromatographia 化学-分析化学
CiteScore
3.40
自引率
5.90%
发文量
103
审稿时长
2.2 months
期刊介绍: Separation sciences, in all their various forms such as chromatography, field-flow fractionation, and electrophoresis, provide some of the most powerful techniques in analytical chemistry and are applied within a number of important application areas, including archaeology, biotechnology, clinical, environmental, food, medical, petroleum, pharmaceutical, polymer and biopolymer research. Beyond serving analytical purposes, separation techniques are also used for preparative and process-scale applications. The scope and power of separation sciences is significantly extended by combination with spectroscopic detection methods (e.g., laser-based approaches, nuclear-magnetic resonance, Raman, chemiluminescence) and particularly, mass spectrometry, to create hyphenated techniques. In addition to exciting new developments in chromatography, such as ultra high-pressure systems, multidimensional separations, and high-temperature approaches, there have also been great advances in hybrid methods combining chromatography and electro-based separations, especially on the micro- and nanoscale. Integrated biological procedures (e.g., enzymatic, immunological, receptor-based assays) can also be part of the overall analytical process.
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