Characterization of in vitro metabolites of irisflorentin by rat liver microsomes using high-performance liquid chromatography coupled with tandem mass spectrometry
文献类型：期刊论文
| 作者 | Liao, X; Liao, X (reprint author), Chinese Acad Sci, Chengdu Inst Biol, Chengdu 610041, Peoples R China.; Jia, YW; Zeng, ZQ; Shi, HL; Liang, J; Liu, YM; Tang, YX |
| 刊名 | BIOMEDICAL CHROMATOGRAPHY
 |
| 出版日期 | 2016 |
| 卷号 | 30期号:9页码:1363-1370 |
| 关键词 | Liver Microsomes Metabolites Kinetics Irisflorentin Anticancer Activity |
| DOI | 10.1002/bmc.3692 |
| 产权排序 | 1 |
| 文献子类 | Article |
| 英文摘要 | Belamcanda chinensis has been extensively used as antibechic, expectorant and anti-inflammatory agent in traditional medicine. Irisflorentin is one of the major active ingredients. However, little is known about the metabolism of irisflorentin so far. In this work, rat liver microsomes (RLMs) were used to investigate the metabolism of this compound for the first time. Seven metabolites were detected. Five of them were identified as 6,7-dihydroxy-5,3,4,5-tetramethoxy isoflavone (M1), irigenin (M2), 5,7,4-trihydroxy-6,3,5-trimethoxy isoflavone (M3), 6,7,4-trihydroxy-5,3,5-trimethoxy isoflavone (M4) and 6,7,5-trihydroxy-5,3,4-trimethoxy isoflavone (M5) by means of NMR and/or HPLC-ESI-MS. The structures of M6 and M7 were not elucidated because they produced no MS signals. The predominant metabolite M1 was noted to be a new compound. Interestingly, it was found to possess anticancer activity much higher than the parent compound. The enzymatic kinetic parameters of M1 revealed a sigmoidal profile, with V-max = 12.02 m/mg protein/min, K-m = 37.24 m, CLint = 0.32 L/mg protein/min and h = 1.48, indicating the positive cooperation. For the first time in this work, a new metabolite of irisflorentin was found to demonstrate a much higher biological activity than its parent compound, suggesting a new avenue for the development of drugs from B. chinensis, which was also applicable for other herbal plants. Copyright (c) 2016 John Wiley & Sons, Ltd. |
| 学科主题 | Biochemistry & Molecular Biology ; Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| 资助机构 | National Natural Science Foundation of China [21072184, 81173536] ; National Natural Science Foundation of China [21072184, 81173536] ; State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Biology, Chinese Academy of Sciences [P2015-KF12] ; State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Biology, Chinese Academy of Sciences [P2015-KF12] ; National Natural Science Foundation of China [21072184, 81173536] ; National Natural Science Foundation of China [21072184, 81173536] ; State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Biology, Chinese Academy of Sciences [P2015-KF12] ; State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Biology, Chinese Academy of Sciences [P2015-KF12] |
| 源URL | [http://210.75.237.14/handle/351003/28182]  |
| 专题 | 成都生物研究所_天然产物研究 |
| 通讯作者 | Liao, X (reprint author), Chinese Acad Sci, Chengdu Inst Biol, Chengdu 610041, Peoples R China. |
| 推荐引用方式 GB/T 7714 | Liao, X,Liao, X ,Jia, YW,et al. Characterization of in vitro metabolites of irisflorentin by rat liver microsomes using high-performance liquid chromatography coupled with tandem mass spectrometry[J]. BIOMEDICAL CHROMATOGRAPHY,2016,30(9):1363-1370. |
| APA | Liao, X.,Liao, X .,Jia, YW.,Zeng, ZQ.,Shi, HL.,...&Tang, YX.(2016).Characterization of in vitro metabolites of irisflorentin by rat liver microsomes using high-performance liquid chromatography coupled with tandem mass spectrometry.BIOMEDICAL CHROMATOGRAPHY,30(9),1363-1370. |
| MLA | Liao, X,et al."Characterization of in vitro metabolites of irisflorentin by rat liver microsomes using high-performance liquid chromatography coupled with tandem mass spectrometry".BIOMEDICAL CHROMATOGRAPHY 30.9(2016):1363-1370. |
入库方式： OAI收割
来源：成都生物研究所
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