机构：[1] Guangzhou Univ Chinese Med, Clin Med Coll 2, Guangzhou 510006, Guangdong, Peoples R China[2] Guangzhou Univ Chinese Med, Guangdong Prov Key Lab Chinese Med Prevent & Trea, Guangzhou 510006, Peoples R China[3] Guizhou Med Univ, State Key Lab Funct & Applicat Med Plants, Guiyang 550014, Peoples R China[4] Guangzhou Key Lab Chiral Res Act Components Tradi, Guangzhou 510006, Peoples R China[5] Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Res Ctr Modernizat Tradit Chinese Med, Natl Engn Lab TCM Standardizat Technol, Shanghai 201203, Peoples R China[6] Guangzhou Univ Chinese Med, Guangdong Hong Kong Macau Joint Lab Chinese Med &, Guangzhou 510006, Peoples R China
Background: Caesalpinia sappan L. is a traditional medicinal plant that is used to promote blood circulation and treat stroke in China. Protosappanin B (PTB) is a unique homoisoflavone compound isolated from Sappan Lignum (the heartwood of Caesalpinia sappan L). In a previous study, the metabolic fate of PTB remained unknown. Objective: To explore whether PTB is extensively metabolized, the metabolites of PTB in bile, plasma, urine, feces, and intestinal bacteria samples in rats were investigated. Methods: The biosamples were investigated by ultraperformance liquid chromatography combined with time-offlight mass spectrometry (UPLC-TOF-MS/MS) with MetabolitePilot software. Results: 28 metabolites were identified in the biosamples: 18 metabolites in rat bile, 8 in plasma, 20 in feces, 7 in urine and 2 in intestinal bacteria samples. Both phase I and phase II metabolites were observed. Metabolite conversion occurred via 9 proposed pathways: sulfate conjugation, glucuronide conjugation, bis-glucuronide conjugation, glucose conjugation, dehydration, oxidation, hydrolysis, methylation and hydroxymethylene loss. The metabolic pathways differed among biosamples and exhibited different distributions. Among these pathways, the most important was sulfate and glucuronide conjugation. Conclusion: The results showed that the small intestinal and biliary routes play an important role in the clearance and excretion of PTB. The main sites of metabolism in the PTB chemical structure were the phenolic hydroxyl and the side-chains on the eight-element ring.
基金：
Research Project of Traditional Chinese Medicine Bureau of Guangdong Province [20211186]; National Key Research and Development Program of China [2018YFC1707900]; National Natural Science Foundation of China (NSFC) [81202398, 81703379]; special foundation of Guangzhou Key Laboratory [202002010004]
第一作者机构：[1] Guangzhou Univ Chinese Med, Clin Med Coll 2, Guangzhou 510006, Guangdong, Peoples R China[2] Guangzhou Univ Chinese Med, Guangdong Prov Key Lab Chinese Med Prevent & Trea, Guangzhou 510006, Peoples R China
通讯作者：
通讯机构：[1] Guangzhou Univ Chinese Med, Clin Med Coll 2, Guangzhou 510006, Guangdong, Peoples R China[*1]Guangzhou Univ Chinese Med, Clin Med Coll 2, Guangzhou 510006, Guangdong, Peoples R China[2] Guangzhou Univ Chinese Med, Guangdong Prov Key Lab Chinese Med Prevent & Trea, Guangzhou 510006, Peoples R China[*2]Guangzhou Univ Chinese Med, Guangdong Prov Key Lab Chinese Med Prevent & Trea, Guangzhou 510006, Peoples R China[*3]Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Res Ctr Modernizat Tradit Chinese Med, Natl Engn Lab TCM Standardizat Technol, Shanghai 201203, Peoples R China[*4]Guangzhou Univ Chinese Med, Guangdong Hong Kong Macau Joint Lab Chinese Med &, Guangzhou 510006, Peoples R China[5] Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Res Ctr Modernizat Tradit Chinese Med, Natl Engn Lab TCM Standardizat Technol, Shanghai 201203, Peoples R China[6] Guangzhou Univ Chinese Med, Guangdong Hong Kong Macau Joint Lab Chinese Med &, Guangzhou 510006, Peoples R China
推荐引用方式(GB/T 7714)：
Chen Wei-Ying,Liang Guang-Yan,Zheng Zuo-Liang,等.UPLC-ESI-Q-TOF/MS Based Metabolic Profiling of Protosappanin B in Rat Plasma, Bile, Feces, Urine and Intestinal Bacteria Samples[J].CURRENT DRUG METABOLISM.2021,22(6):491-499.
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