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Fused-ring alpha-pyrones from intramolecular C-H activation and their lipids-lowering activity associated with LXR-IDOL-LDLR axis regulation

文献类型：期刊论文

作者Mao, Yingle1,4,5,6; Li, Jiaomeng4,6; Tang, Chunping1,6; Ma, Biao2; Xu, Zhijian3; Ke, Changqiang1,6; Feng, Lu1,6; Zhang, Haiyan2,4; Yao, Sheng1,4,6; Dai, Hui-Xiong4,6
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
出版日期2022-12-15
卷号244页码:11
ISSN号0223-5234
关键词C-H activation One-pot intramolecular cyclization ?-Pyrone derivatives LDL uptaking LXR-IDOL-LDLR axis In vivo lipids-lowering effect
DOI10.1016/j.ejmech.2022.114866
通讯作者Yao, Sheng(yaosheng@simm.ac.cn) ; Dai, Hui-Xiong(hxdai@simm.ac.cn) ; Ye, Yang()
英文摘要Lipids-lowering is considered as the most effective approach to decrease the risk of Atherosclerotic cardiovas-cular disease (ASCVD), of which atherosclerosis is the most common cause. Natural products containing a unique type of alpha-pyrone was reported to suppress atherosclerosis in which alpha-pyrone might be considered as an important pharmacore. In this study, an efficient one-pot intramolecular C-H activation strategy was applied to the syn-thesis of potentially bioactive alpha-pyrone derivatives. As the result, three different scaffolds were quickly and conveniently generated, including thiophenes, pyrrole and indole derivatives. Among of them, eight alpha-pyrone derivatives showed potential effects to promote the uptake of LDL in HepG2 cells. Active unique alpha-pyrones compounds exhibiting potent in vitro and in vivo lipids-lowering effects, and a novel mechanism associated with the regulation of LXR-IDOL-LDLR axis, the new pathway targeted pharmacologically to control plasma choles-terol levels, were disclosed firstly in this study.
WOS关键词BENZOIC-ACIDS ; ANNULATION ; ALKYNES ; RECEPTORS
资助项目National Natural Science Foundation of China ; [81573305] ; [81673327]
WOS研究方向Pharmacology & Pharmacy
语种英语
出版者ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
WOS记录号WOS:000891313800001
源URL[http://119.78.100.183/handle/2S10ELR8/304386]  
专题新药研究国家重点实验室
通讯作者Yao, Sheng; Dai, Hui-Xiong; Ye, Yang
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Nat Prod Chem Dept, Shanghai 201203, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China
3.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, Shanghai 201203, Peoples R China
4.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
5.Shanghai Tech Univ, Sch Life Sci & Technol, Shanghai 201210, Peoples R China
6.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Mao, Yingle,Li, Jiaomeng,Tang, Chunping,et al. Fused-ring alpha-pyrones from intramolecular C-H activation and their lipids-lowering activity associated with LXR-IDOL-LDLR axis regulation[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2022,244:11.
APA Mao, Yingle.,Li, Jiaomeng.,Tang, Chunping.,Ma, Biao.,Xu, Zhijian.,...&Ye, Yang.(2022).Fused-ring alpha-pyrones from intramolecular C-H activation and their lipids-lowering activity associated with LXR-IDOL-LDLR axis regulation.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,244,11.
MLA Mao, Yingle,et al."Fused-ring alpha-pyrones from intramolecular C-H activation and their lipids-lowering activity associated with LXR-IDOL-LDLR axis regulation".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 244(2022):11.

入库方式： OAI收割

来源：上海药物研究所

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