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题名: Determination of Alpinetin Glucuronidation Activities in Liver Microsomes from Different Species Using UFLC-ESI-MS
作者: Wang, Zheng-Hua1;  Hong, Mo2;  Sun, Xiao-Yu2;  He, Gui-Yuan2
关键词: Alpinetin ;  Glucuronidation ;  Species difference ;  UFLC-MS
刊名: LATIN AMERICAN JOURNAL OF PHARMACY
发表日期: 2012-06-01
卷: 31, 期:5, 页:785-789
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine
类目[WOS]: Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy
英文摘要: Alpinetin, a type of novel plant flavonoid derived from Alpinia katsumadai Hayata, has been demonstrated to exhibit multiple biochemical and pharmacological activities. The phenyl hydroxyl group existed in alpinetin is susceptible to the glucuronidation catalyzed by UDP-glucuronosyltransferase (UGT). The aim of the present study is to develop a sensitive and specific ultra-fast liquid chromatography (UFLC)-mass spectrum (MS) method to determine the glucuronidation activity of alpinetin in the liver microsomes obtained from different species, including human liver microsomes (HLMs), rat liver microsomes (RLMs), mice liver microsomes (MLMs), and dog liver microsomes (DLMs). The alpinetin's glucuronide was purified, and the structure was elucidated using H-1-NMR and C-13-NMR. The mass spectrometric detection was performed under selected ion monitoring (SIM) for alpinetin glucuronide at m/z 445 and 4-methylumbelliferyl-beta-glucuronide (I.S.) at m/z 351. The assay exhibited linearity over the range 0.1-60 mu M for alpinetin glucuronide with the correlation coefficient of 0.9991. The intra- and inter-day precision was less than 5.3%, with accuracy in the range 105.1-106.8%. The developed method has been successfully applied to determine the glucuronidation of alpinetin, and the intrinsic clearance was calculated to be 2.51, 1.29, 0.23, and 1.27 mL/min/mg pro for HLM, RLM, MLM and DLM, respectively. The results obtained from this study are helpful to selection of animal models for pre-clinical pharmacokinetic study.
关键词[WOS]: UDP-GLUCURONOSYLTRANSFERASES ;  NOMENCLATURE UPDATE ;  GENE SUPERFAMILY ;  INHIBITION ;  METABOLISM ;  CELLS ;  RATS ;  MICE
语种: 英语
WOS记录号: WOS:000309308100025
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/142962
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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作者单位: 1.Liaoning Med Univ, Affiliated Hosp 1, Liaoning, Peoples R China
2.Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian 116023, Peoples R China

Recommended Citation:
Wang, Zheng-Hua,Hong, Mo,Sun, Xiao-Yu,et al. Determination of Alpinetin Glucuronidation Activities in Liver Microsomes from Different Species Using UFLC-ESI-MS[J]. LATIN AMERICAN JOURNAL OF PHARMACY,2012,31(5):785-789.
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