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Identification and characterization of naturally occurring inhibitors against human carboxylesterase 2 in White Mulberry Root-bark
Liu, Ya-Jing1; Li, Shi-Yang2; Hou, Jie1,3; Liu, Yan-Fang2; Wang, Dan-Dan2; Jiang, Yong-Shan1,4; Ge, Guang-Bo2,3; Liang, Xin-Miao2; Yang, Ling2
关键词White Mulberry Root-bark Human Carboxylesterase 2 (Hce2) Inhibitory Effects Sanggenone d Kuwanon g Sanggenone c
刊名FITOTERAPIA
2016-12-01
DOI10.1016/j.fitote.2016.09.022
115页:57-63
收录类别SCI
文章类型Article
WOS标题词Science & Technology ; Life Sciences & Biomedicine
类目[WOS]Chemistry, Medicinal ; Pharmacology & Pharmacy
关键词[WOS]HUMAN UDP-GLUCURONOSYLTRANSFERASES ; MORUS-ALBA ; SELECTIVE INHIBITORS ; BIOLOGICAL-ACTIVITY ; IRINOTECAN CPT-11 ; COLORECTAL-CANCER ; FLUORESCENT-PROBE ; NITRIC-OXIDE ; METABOLISM ; POTENT
英文摘要White Mulberry Root-bark (WMR) is an edible Chinese herbal used for the treatment of inflammation, nephritis and asthma. This study aimed to investigate the inhibitory effects of ethanol extract from WMR against human carboxylesterase 2 (hCE2), as well as to identity and character natural hCE2 inhibitors in this herbal. Our results demonstrated that the ethanol extract of WMR displayed potent inhibitory effects against hCE2, while three major bioactive constitutes in WMR were identified on the basis of LC fingerprinting combined with activity based screening of LC fractions. Three bioactive compounds including SD, KG and SC were efficiently identified by comparison of LC retention times, UV and MS spectral data, with the help of authentic standards. The inhibition potentials and inhibition types of these natural compounds against hCE2 were further investigated in human liver microsomes. The results demonstrated that these bioactive compounds are potent non-competitive inhibitors against hCE2, with the K-i values ranging from 0.76 mu M to 1.09 mu M. All these findings suggested that three abundant natural compounds in WMR displayed potent inhibitory effects against hCE2, which could be used as lead compounds to develop more potent hCE2 inhibitors for the alleviation of hCE2-mediated severe delayed onset diarrhea. (C) 2016 Published by Elsevier B.V.
语种英语
WOS记录号WOS:000389113300010
引用统计
文献类型期刊论文
条目标识符http://cas-ir.dicp.ac.cn/handle/321008/150351
专题中国科学院大连化学物理研究所
作者单位1.Dalian Med Univ, Dalian 116044, Peoples R China
2.Chinese Acad Sci, Dalian Inst Chem Phys, Dalian 116023, Peoples R China
3.Dalian Univ Technol, State Key Lab Fine Chem, Dalian 116024, Peoples R China
4.Dalian Med Univ, Affiliated Hosp 1, Dalian 116011, Peoples R China
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Liu, Ya-Jing,Li, Shi-Yang,Hou, Jie,et al. Identification and characterization of naturally occurring inhibitors against human carboxylesterase 2 in White Mulberry Root-bark[J]. FITOTERAPIA,2016,115:57-63.
APA Liu, Ya-Jing.,Li, Shi-Yang.,Hou, Jie.,Liu, Yan-Fang.,Wang, Dan-Dan.,...&Yang, Ling.(2016).Identification and characterization of naturally occurring inhibitors against human carboxylesterase 2 in White Mulberry Root-bark.FITOTERAPIA,115,57-63.
MLA Liu, Ya-Jing,et al."Identification and characterization of naturally occurring inhibitors against human carboxylesterase 2 in White Mulberry Root-bark".FITOTERAPIA 115(2016):57-63.
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