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Development of a novel nitric oxide (NO) production inhibitor with potential therapeutic effect on chronic inflammation.

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资源类型：
Pubmed体系：
作者：
Youzhe Yang[a,b,c,*2] * ; Zhe Wei[b] * ; Alexander Tobias Teichmann[a] ; Frank Heinrich Wieland[a] ; Amu Wang[d] ; Xiangui Lei[d] ; Yue Zhu[d] ; Jinxiang Yin[d] ; Tiantian Fan[c] ; Li Zhou[c] ; Chao Wang[c] ; Lijuan Chen[b,*1] ;
机构： [a]Sichuan Provincial Center for Gynaecology and Breast Diseases, The Affiliated Hospital of Southwest Medical University, Luzhou, 646000, PR China [b]State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University and Collaborative Innovation Center, Chengdu, 610041, PR China [c]Natural Products Research Center, Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu, 610041, PR China [d]School of Science, Xihua University, Chengdu, 610039, PR China
出处：
DOI： 10.1016/j.ejmech.2020.112216
ISSN：

关键词： Inflammation Nitric oxide (NO) Kava chalcones Inducible nitric oxide synthase (iNOS) Structure-activity relationship (SAR)

摘要：
Inflammation is a complex biological response to stimuli. Activated macrophages induced excessively release of pro-inflammatory cytokines and mediators such as endogenous radical nitric oxide (NO) play a significant role in the progression of multiple inflammatory diseases. Both natural and synthetic chalcones possess a wide range of bioactivities. In this work, thirty-nine chalcones and three related compounds, including several novel ones, based on bioactive kava chalcones were designed, synthesized and their inhibitory effects on NO production in RAW 264.7 cells were evaluated. The novel compound (E)-1-(2'-hydroxy-4',6'-dimethoxyphenyl)-3-(3-methoxy-4-(3-morpholinopropoxy)phenyl)prop-2-en-1-one (53) exhibited a better inhibitory activity (84.0%) on NO production at 10 μM (IC50 = 6.4 μM) with the lowest cytotoxicity (IC50 > 80 μM) among the tested compounds. Besides, western blot analysis indicated that compound 53 was a potent down-regulator of inducible nitric oxide synthase (iNOS) protein. Docking study revealed that compound 53 also can dock into the active site of iNOS. Furthermore, at the dose of 10 mg/kg/day, compound 53 could both significantly suppress the progression of inflammation on collagen-induced arthritis (CIA) and adjuvant-induced arthritis (AIA) models. In addition, the structure-activity relationship (SAR) of the kava chalcones based analogs was also depicted. Copyright © 2020 Elsevier Masson SAS. All rights reserved.

基金：
This research was funded by the National Natural Science Foundation of China (81702900) and the Doctoral Research Initiation Fund of the Affiliated Hospital of Southwest Medical University (Project No.: 18061).
语种：
外文
PubmedID：
中科院(CAS)分区：
出版当年[2020]版：
大类 | 1 区 医学
小类 | 1 区 药物化学
最新[2023]版：
大类 | 2 区 医学
小类 | 1 区 药物化学
第一作者：
第一作者机构： [a]Sichuan Provincial Center for Gynaecology and Breast Diseases, The Affiliated Hospital of Southwest Medical University, Luzhou, 646000, PR China [b]State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University and Collaborative Innovation Center, Chengdu, 610041, PR China [c]Natural Products Research Center, Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu, 610041, PR China [*2]Sichuan Provincial Center for Gynaecology and Breast Diseases, the Affiliated Hospital of Southwest Medical University, Luzhou, 646000, PR China.
共同第一作者：
通讯作者：
通讯机构： [a]Sichuan Provincial Center for Gynaecology and Breast Diseases, The Affiliated Hospital of Southwest Medical University, Luzhou, 646000, PR China [b]State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University and Collaborative Innovation Center, Chengdu, 610041, PR China [c]Natural Products Research Center, Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu, 610041, PR China [*1]Lab of Natural Product Drugs, State Key Laboratory of Biotherapy and Cancer Center, West China Medical School, West China Hospital, Sichuan University, Chengdu, 610041, PR China. [*2]Sichuan Provincial Center for Gynaecology and Breast Diseases, the Affiliated Hospital of Southwest Medical University, Luzhou, 646000, PR China.
推荐引用方式(GB/T 7714)：
Youzhe Yang,Zhe Wei,Alexander Tobias Teichmann,et al.Development of a novel nitric oxide (NO) production inhibitor with potential therapeutic effect on chronic inflammation.[J].European journal of medicinal chemistry.2020,193:112216.doi:10.1016/j.ejmech.2020.112216.
APA：
Youzhe Yang,Zhe Wei,Alexander Tobias Teichmann,Frank Heinrich Wieland,Amu Wang...&Lijuan Chen.(2020).Development of a novel nitric oxide (NO) production inhibitor with potential therapeutic effect on chronic inflammation..European journal of medicinal chemistry,193,
MLA：
Youzhe Yang,et al."Development of a novel nitric oxide (NO) production inhibitor with potential therapeutic effect on chronic inflammation.".European journal of medicinal chemistry 193.(2020):112216

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