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Spiroarborin, an ent-Clerodane Homodimer from Callicarpa arborea as an Inhibitor of the Eleven-Nineteen Leukemia (ENL) Protein by the YEATS Domain

文献类型：期刊论文

作者Pu, De-Bing2; Guo, Si-Qi3,4; Ni, Dong-Xuan2; Lin, Jing2; Gao, Jun-Bo5; Li, Xiao-Ning1; Zhang, Rui-Han2; Li, Xiao-Li2; Luo, Cheng3,6; Chen, Shi-Jie3,6
刊名JOURNAL OF NATURAL PRODUCTS
出版日期2022-02-25
卷号85期号:2页码:317-326
ISSN号0163-3864
DOI10.1021/acs.jnatprod.1c00775
通讯作者Chen, Shi-Jie(shijiechen@simm.ac.cn) ; Xiao, Wei-Lie(xiaoweilie@ynu.edu.cn)
英文摘要A spiro ent-clerodane homodimer with a rare 6/6/6/6/6-fused pentacyclic scaffold, spiroarborin (1), together with four new monomeric analogues (2-5), were isolated from Callicarpa arborea. Their structures were elucidated by comprehensive spectroscopic data analysis, quantum-chemical calculations, and X-ray diffraction. A plausible biosynthetic pathway of 1 was proposed, and a biomimetic synthesis of its derivative was accomplished. Compound 1 showed a potent inhibitory effect by directly binding to the YEATS domain of the 11-19 leukemia (ENL) protein with an IC50 value of 7.3 mu M. This gave a K-D value of 5.0 mu M, as recorded by a surface plasmon resonance binding assay.
WOS关键词DITERPENOIDS ; CONSTITUENTS
资助项目Yunnan Applicative and Basic Research Program[2018FY001] ; Yunnan Applicative and Basic Research Program[2018FA048] ; NSFC[81903541] ; NSFC[21762048] ; NSFC[81703415] ; NSFC[21820102008] ; Postdoctoral Science Foundation of China[2018M633428] ; Program for Changjiang Scholars and Innovative Research Team in University[IRT-17R94] ; Science and Technology Commission of Shanghai Municipality[21ZR1474700] ; Projects of Yunling Scholar and Innovative Team of Yunnan Province ; High-Performance Comput-ing Center of Yunnan University
WOS研究方向Plant Sciences ; Pharmacology & Pharmacy
语种英语
出版者AMER CHEMICAL SOC
WOS记录号WOS:000762347300001
源URL[http://119.78.100.183/handle/2S10ELR8/300242]  
专题新药研究国家重点实验室
通讯作者Chen, Shi-Jie; Xiao, Wei-Lie
作者单位1.Yunnan Univ Chinese Med, Sch Pharmaceut Sci, Kunming 650500, Yunnan, Peoples R China
2.Yunnan Univ, Yunnan Res & Dev Ctr Nat Prod, Sch Chem Sci & Technol, Key Lab Med Chem Nat Resources,Minist Educ, Kunming 650091, Yunnan, Peoples R China
3.Chinese Acad Sci, Ctr Chem Biol, Drug Discovery & Design Ctr, Shanghai Inst Mat Med,State Key Lab Drug Res, Shanghai 201203, Peoples R China
4.Nanchang Univ, Sch Pharm, Nanchang 330006, Jiangxi, Peoples R China
5.Zhejiang Univ, State Key Lab CAD&CG, Hangzhou 310058, Peoples R China
6.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
推荐引用方式
GB/T 7714		 Pu, De-Bing,Guo, Si-Qi,Ni, Dong-Xuan,et al. Spiroarborin, an ent-Clerodane Homodimer from Callicarpa arborea as an Inhibitor of the Eleven-Nineteen Leukemia (ENL) Protein by the YEATS Domain[J]. JOURNAL OF NATURAL PRODUCTS,2022,85(2):317-326.
APA Pu, De-Bing.,Guo, Si-Qi.,Ni, Dong-Xuan.,Lin, Jing.,Gao, Jun-Bo.,...&Xiao, Wei-Lie.(2022).Spiroarborin, an ent-Clerodane Homodimer from Callicarpa arborea as an Inhibitor of the Eleven-Nineteen Leukemia (ENL) Protein by the YEATS Domain.JOURNAL OF NATURAL PRODUCTS,85(2),317-326.
MLA Pu, De-Bing,et al."Spiroarborin, an ent-Clerodane Homodimer from Callicarpa arborea as an Inhibitor of the Eleven-Nineteen Leukemia (ENL) Protein by the YEATS Domain".JOURNAL OF NATURAL PRODUCTS 85.2(2022):317-326.

入库方式： OAI收割

来源：上海药物研究所

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