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Anti-HBV Activities of Cembranoids from the South China Sea Soft Coral Sinularia pedunculata and Their Structure Activity Relationship

文献类型：期刊论文

作者Huang, Chao4,5; Jin, Yang3,4; Sun, Ruo-Nan1,3,4; Hu, Kong-Ying5; Yao, Li-Gong3; Guo, Yue-Wei3; Yuan, Zheng-Hong2,5; Li, Xu-Wen1,3,4
刊名CHEMISTRY & BIODIVERSITY
出版日期2024-07-17
页码8
关键词Hepatitis B Virus cembranoid anti-HBV activity structure-activity relationship ENI/Xp enhancer/promoter
ISSN号1612-1872
DOI10.1002/cbdv.202401146
通讯作者Guo, Yue-Wei(ywguo@simm.ac.cn) ; Yuan, Zheng-Hong(zhyuan@shmu.edu.cn) ; Li, Xu-Wen(xwli@simm.ac.cn)
英文摘要Hepatitis B Virus (HBV) infection is a global public health challenge that seriously endangers human health. Soft coral, as a major source of terpenoids, contains many structurally novel and highly bioactive compounds. Sixteen cembranoids (1-16), including a new one named sinupedunol B (16), were isolated from the South China Sea Soft coral Sinularia pedunculata. The structure of the sinupedunol B (16) was determined through a combination of spectroscopic analysis and X-ray single-crystal diffraction. In this study, cembranoids isolated from Sinularia pedunculata were found of anti-HBV activity for the first time. Among them, flexilarin D (6) showed significant anti-HBV activity with an IC50 value of 5.57 mu M without cytotoxicity. We then analyzed the structure-activity relationship (SAR). Furthermore, it is demonstrated that flexilarin D (6) can accelerate the formation of capsid, inhibit HBeAg, HBV core particle DNA, HBV total RNA and pregenomic RNA in a dose dependent manner. We also confirmed the anti-HBV activity of 6 in HepG2-NTCP infection system. Finally, we demonstrated the anti-HBV mechanism of these compounds by inhibiting the ENI/Xp enhancer/promoter.
WOS关键词DITERPENOIDS ; STRATEGIES
资助项目National Key Research and Development Program of China[2021YFF0502400] ; National Key Research and Development Program of China[2022YFA1303600] ; National Natural Science Foundation of China[42076099] ; National Natural Science Foundation of China[81991521] ; National Natural Science Foundation of China[U23 A20474] ; Shanghai Municipal Health Commission[GWVI-11.2-XD27] ; Non-profit Central Research Institute Fund of Chinese Academy of Medical Sciences[2023-PT310-02] ; CAMS Innovation Fund for Medical Sciences[2019-12M-5-040] ; Shandong Laboratory Program[SYS202205] ; CAS Youth Interdisciplinary Team ; Taishan Scholars Program[tsqn202312302]
WOS研究方向Biochemistry & Molecular Biology ; Chemistry
语种英语
WOS记录号WOS:001270265700001
出版者WILEY-V C H VERLAG GMBH
源URL[http://119.78.100.183/handle/2S10ELR8/312401]  
专题新药研究国家重点实验室
通讯作者Guo, Yue-Wei; Yuan, Zheng-Hong; Li, Xu-Wen
作者单位1.Univ Chinese Acad Sci, 19 A Yuquan Rd, Beijing 100049, Peoples R China
2.Shanghai Inst Infect Dis & Biosecur, Shanghai 200032, Peoples R China
3.Bohai Rim Adv Res Inst Drug Discovery, Shandong Lab Yantai Drug Discovery, Yantai 264117, Shandong, Peoples R China
4.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Chem Biol, Shanghai 201203, Peoples R China
5.Fudan Univ, Shanghai Med Coll, Shanghai Frontiers Sci Ctr Pathogen Microbes & Inf, Sch Basic Med Sci,Res Unit Cure Chron Hepatitis B, Shanghai 200032, Peoples R China
推荐引用方式
GB/T 7714		 Huang, Chao,Jin, Yang,Sun, Ruo-Nan,et al. Anti-HBV Activities of Cembranoids from the South China Sea Soft Coral Sinularia pedunculata and Their Structure Activity Relationship[J]. CHEMISTRY & BIODIVERSITY,2024:8.
APA Huang, Chao.,Jin, Yang.,Sun, Ruo-Nan.,Hu, Kong-Ying.,Yao, Li-Gong.,...&Li, Xu-Wen.(2024).Anti-HBV Activities of Cembranoids from the South China Sea Soft Coral Sinularia pedunculata and Their Structure Activity Relationship.CHEMISTRY & BIODIVERSITY,8.
MLA Huang, Chao,et al."Anti-HBV Activities of Cembranoids from the South China Sea Soft Coral Sinularia pedunculata and Their Structure Activity Relationship".CHEMISTRY & BIODIVERSITY (2024):8.

入库方式： OAI收割

来源：上海药物研究所

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