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Identification of Dihydrobenzofuran Neolignans as Novel PDE4 Inhibitors and Evaluation of Antiatopic Dermatitis Efficacy in DNCB-Induced Mice Model

文献类型：期刊论文

作者Gu, Chenming6; Liu, Jiayuan5; Qian, Fei4; Yu, Wenchao6; Huang, Doudou6; Shen, Jingshan5; Feng, Chenguo3; Chen, Kaixian6; Li, Yiming6; Jiang, Xiangrui5
刊名JOURNAL OF MEDICINAL CHEMISTRY
出版日期2024-03-15
卷号67期号:6页码:4855-4869
ISSN号0022-2623
DOI10.1021/acs.jmedchem.3c02424
通讯作者Jiang, Xiangrui(jiangxiangrui@simm.ac.cn) ; Xu, Yechun(ycxu@simm.ac.cn) ; Zhang, Liuqiang(04100217@163.com)
英文摘要Atopic dermatitis is a chronic relapsing skin disease characterized by recurrent, pruritic, localized eczema, while PDE4 inhibitors have been reported to be effective as antiatopic dermatitis agents. 3 ',4-O-dimethylcedrusin (DCN) is a natural dihydrobenzofuran neolignan isolated from Magnolia biondii with moderate potency against PDE4 (IC50 = 3.26 +/- 0.28 mu M) and a binding mode similar to that of apremilast, an approved PDE4 inhibitor for the treatment of psoriasis. The structure-based optimization of DCN led to the identification of 7b-1 that showed high inhibitory potency on PDE4 (IC50 = 0.17 +/- 0.02 mu M), good anti-TNF-alpha activity (EC50 = 0.19 +/- 0.10 mu M), remarkable selectivity profile, and good skin permeability. The topical treatment of 7b-1 resulted in the significant benefits of pharmacological intervention in a DNCB-induced atopic dermatitis-like mice model, demonstrating its potential for the development of novel antiatopic dermatitis agents.
WOS关键词ATOPIC-DERMATITIS ; IN-VITRO ; PHOSPHODIESTERASE-4 ; APREMILAST ; MANAGEMENT ; RESOLUTION ; CAMP
资助项目National Key Science and Technology Infrastructure (Shanghai) Translational Medicine Open Program[TMSK-2021-404] ; National Key Science and Technology Infrastructure (Shanghai) Translational Medicine Open Program[23S11900700] ; National Key Science and Technology Infrastructure (Shanghai) Translational Medicine Open Program[TM202101H003] ; Shanghai Scientific and Technological Innovation Program[2022] ; SIMM-SHUTCM Joint Innovation Research Program
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:001186377200001
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/310187]  
专题新药研究国家重点实验室
通讯作者Jiang, Xiangrui; Xu, Yechun; Zhang, Liuqiang
作者单位1.Univ Chinese Acad Sci, Hangzhou Inst Adv Study, Sch Pharmaceut Sci & Technol, Hangzhou 310024, Peoples R China
2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
3.Shanghai Univ Tradit Chinese Med, Innovat Res Inst Tradit Chinese Med, Res Ctr Chiral Drugs, Shanghai 201203, Peoples R China
4.Shanghai Univ Tradit Chinese Med, Inst Interdisciplinary Integrat Med Res, Shanghai 201203, Peoples R China
5.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
6.Shanghai Univ Tradit Chinese Med, Sch Pharm, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Gu, Chenming,Liu, Jiayuan,Qian, Fei,et al. Identification of Dihydrobenzofuran Neolignans as Novel PDE4 Inhibitors and Evaluation of Antiatopic Dermatitis Efficacy in DNCB-Induced Mice Model[J]. JOURNAL OF MEDICINAL CHEMISTRY,2024,67(6):4855-4869.
APA Gu, Chenming.,Liu, Jiayuan.,Qian, Fei.,Yu, Wenchao.,Huang, Doudou.,...&Zhang, Liuqiang.(2024).Identification of Dihydrobenzofuran Neolignans as Novel PDE4 Inhibitors and Evaluation of Antiatopic Dermatitis Efficacy in DNCB-Induced Mice Model.JOURNAL OF MEDICINAL CHEMISTRY,67(6),4855-4869.
MLA Gu, Chenming,et al."Identification of Dihydrobenzofuran Neolignans as Novel PDE4 Inhibitors and Evaluation of Antiatopic Dermatitis Efficacy in DNCB-Induced Mice Model".JOURNAL OF MEDICINAL CHEMISTRY 67.6(2024):4855-4869.

入库方式： OAI收割

来源：上海药物研究所

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