Simultaneous determination of flavonol glycoside and its major metabolites by LC-MS/MS in rat plasma
文献类型：期刊论文
| 作者 | Dong Lei4; Liu Jinqiu6; Li Liang6 ; Chen Xiaoyan6; Shan Weiguang5; Zhong Dafang4
|
| 刊名 | Acta Pharmaceutica Sinica
 |
| 出版日期 | 2018 |
| 卷号 | 53期号:8页码:1344-1350 |
| ISSN号 | 0513-4870 |
| 关键词 | LC-MS/MS flavonol glycoside glucuronide conjugate pharmacokinetics |
| 其他题名 | LC-MS/MS法测定大鼠血浆中黄酮醇糖苷及其主要代谢物 |
| 文献子类 | Article |
| 英文摘要 | Flavonol glycoside is in clinical trials for treatment of hyperlipidemia. An accurate and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the simultaneous determination of flavonol glycoside (M0), aglycone (M1) and glucuronide conjugate (M2) in rat plasma. d_6-Flavonol glycoside was used as internal standard (IS). After extraction from the plasma by protein precipitation, the analytes and internal standard were separated on a XDB C_(18) column (50 mm * 4.6 mm, 1.8 mum) using a gradient elution procedure. The mobile phase consisted of methanol and water (0.2% formic acid) at a flow rate of 0.6 mL·min~(-1). The total run time was 4.5 min. Positive electrospray ionization was performed using multiple reaction monitoring (MRM) with transitions of m/z 461.3 m/z 299.1 for M0, m/z 299.1 m/z 283.1 for M1, m/z 475.0 m/z 299.1 for M2, and m/z 467.3 m/z 305.1 for d_6-flavonol glycoside. The method was validated and successfully applied to the pharmacokinetics study of flavonol glycoside in SD rats which were given flavonol glycoside (30 mg·kg~(-1)) by gavage. The C_(max) of M0 is (341 106) ng·mL~(-1) and AUC_(0-t) is (1 960 725) h·ng·mL~(-1), while the C_(max) of M2 is (1 720 843) ng·mL~(-1)and AUC_(0-t) is (8 510 2 920) h·ng·mL~(-1). The results suggest that flavonol glycoside existed mainly in the form of M0 and M2 in rats. After flavonol glycoside being hydrolyzed by the intestinal flora, it was absorbed in the form of aglycone and further metabolized to M2 after the first-pass effect. In this paper, the main metabolites of flavonol glycoside in rat plasma were determined for the first time, which provided a basis for the design of clinical pharmacokinetic experiment. |
| WOS研究方向 | Pharmacology & Pharmacy (provided by Clarivate Analytics) |
| 语种 | 中文 |
| CSCD记录号 | CSCD:6301237 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/269164]  |
| 专题 | 上海药物代谢研究中心 |
| 通讯作者 | Zhong Dafang |
| 作者单位 | 1.; 2.Hangzhou; 3.Chinese Academy of Sciences,; 4.College of Pharmaceutical Science, Zhejiang University of Technology; 5.College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou, Zhejiang 310014, China. 6.Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.; |
| 推荐引用方式 GB/T 7714 | Dong Lei,Liu Jinqiu,Li Liang,et al. Simultaneous determination of flavonol glycoside and its major metabolites by LC-MS/MS in rat plasma[J]. Acta Pharmaceutica Sinica,2018,53(8):1344-1350. |
| APA | Dong Lei,Liu Jinqiu,Li Liang,Chen Xiaoyan,Shan Weiguang,&Zhong Dafang.(2018).Simultaneous determination of flavonol glycoside and its major metabolites by LC-MS/MS in rat plasma.Acta Pharmaceutica Sinica,53(8),1344-1350. |
| MLA | Dong Lei,et al."Simultaneous determination of flavonol glycoside and its major metabolites by LC-MS/MS in rat plasma".Acta Pharmaceutica Sinica 53.8(2018):1344-1350. |
入库方式： OAI收割
来源：上海药物研究所
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