DICP OpenIR
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
KeywordWhite Mulberry Root-bark Human Carboxylesterase 2 (Hce2) Inhibitory Effects Sanggenone d Kuwanon g Sanggenone c
Source PublicationFITOTERAPIA
2016-12-01
DOI10.1016/j.fitote.2016.09.022
Volume115Pages:57-63
Indexed BySCI
SubtypeArticle
WOS HeadingsScience & Technology ; Life Sciences & Biomedicine
WOS SubjectChemistry, Medicinal ; Pharmacology & Pharmacy
WOS KeywordHUMAN UDP-GLUCURONOSYLTRANSFERASES ; MORUS-ALBA ; SELECTIVE INHIBITORS ; BIOLOGICAL-ACTIVITY ; IRINOTECAN CPT-11 ; COLORECTAL-CANCER ; FLUORESCENT-PROBE ; NITRIC-OXIDE ; METABOLISM ; POTENT
AbstractWhite 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.
Language英语
WOS IDWOS:000389113300010
Citation statistics
Document Type期刊论文
Identifierhttp://cas-ir.dicp.ac.cn/handle/321008/150351
Collection中国科学院大连化学物理研究所
Affiliation1.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
Recommended Citation
GB/T 7714
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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