Identification and characterization of naturally occurring inhibitors against human carboxylesterase 2 in White Mulberry Root-bark
文献类型：期刊论文
| 作者 | Liang, Xin-Miao2; Liu, Ya-Jing1; Li, Shi-Yang2; Hou, Jie1,3; Liu, Yan-Fang2; Wang, Dan-Dan2; Jiang, Yong-Shan1,4; Ge, Guang-Bo2,3; Yang, Ling2 |
| 刊名 | FITOTERAPIA
 |
| 出版日期 | 2016-12-01 |
| 卷号 | 115页码:57-63 |
| 关键词 | White Mulberry Root-bark Human carboxylesterase 2 (hCE2) Inhibitory effects Sanggenone D Kuwanon G Sanggenone C |
| 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. |
| 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 |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000389113300010 |
| 源URL | [http://cas-ir.dicp.ac.cn/handle/321008/150351]  |
| 专题 | 大连化学物理研究所_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 |
| 推荐引用方式 GB/T 7714 | Liang, Xin-Miao,Liu, Ya-Jing,Li, Shi-Yang,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 | Liang, Xin-Miao.,Liu, Ya-Jing.,Li, Shi-Yang.,Hou, Jie.,Liu, Yan-Fang.,...&Yang, Ling.(2016).Identification and characterization of naturally occurring inhibitors against human carboxylesterase 2 in White Mulberry Root-bark.FITOTERAPIA,115,57-63. |
| MLA | Liang, Xin-Miao,et al."Identification and characterization of naturally occurring inhibitors against human carboxylesterase 2 in White Mulberry Root-bark".FITOTERAPIA 115(2016):57-63. |
入库方式： OAI收割
来源：大连化学物理研究所
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