Discovery and evaluation of novel anti-inflammatory derivatives of natural bioactive curcumin

doi:10.2147/DDDT.S69914

科研成果详情

题名	Discovery and evaluation of novel anti-inflammatory derivatives of natural bioactive curcumin
作者	Zhang, Yali1; Jiang, Xin 2; Peng, Kesong1; Chen, Chengwei3; Fu, Lili1; Wang, Zhe1; Feng, Jianpeng1; Liu, Zhiguo1,4; Zhang, Huajie1; Liang, Guang1; Pan, Zheer 4
发表日期	2014-12-31
发表期刊	DRUG DESIGN DEVELOPMENT AND THERAPY 影响因子和分区
语种	英语
原始文献类型	Article
关键词	curcumin anti-inflammation sepsis macrophage cytokine
其他关键词	MONO-CARBONYL ANALOGS ; NF-KAPPA-B ; IN-VITRO ; SEPSIS ; INTERLEUKIN-6 ; MECHANISMS ; CYTOKINES ; RESPONSES ; PROTEIN ; LPS
摘要	Curcumin is a natural active product that has various pharmacological activities such as anti-inflammatory effects. Here, we report the synthesis and evaluation of 34 monocarbonyl curcumin analogs as novel anti-inflammatory agents. Among the analogs, the symmetrical heterocyclic type displayed the strongest inhibition of lipopolysaccharide (LPS)-stimulated expression of pro-inflammatory cytokines in macrophages. Analogs S1-S5 and AS29 reduced tumor necrosis factor-alpha (TNF-alpha) and interleukin-6 (IL-6) production in a dose-dependent manner and also displayed excellent stability and low cytotoxicity in vitro. In addition, analog S1 dose-dependently inhibited LPS-induced extracellular signal-regulated kinase (ERK) phosphorylation. Furthermore, analogs S1 and S4 displayed a significant protective effect on LPS-induced septic death in mouse models, with 40% and 50% survival rates, respectively. These data demonstrate that the heterocyclic monocarbonyl curcumin analogs have potential therapeutic effects in acute inflammatory diseases.
资助项目	National Natural Science Fund of ChinaNational Natural Science Foundation of China (NSFC) [21272179, 81272462, 81202462]; Project of Zhejiang Provincial Key Constructive Subject (Traditional Chinese Medicine) [2012-XK-A28]; Qianjiang Talent Project of Zhejiang Province [2013R10020]; Zhejiang Key Group Project in Scientific Innovation [2010R50042]
出版者	DOVE MEDICAL PRESS LTD
出版地	ALBANY
ISSN	1177-8881
EISSN	1177-8881
卷号	8 页码:2161-2171
DOI	10.2147/DDDT.S69914
页数	11
WOS类目	Chemistry, Medicinal ; Pharmacology & Pharmacy
WOS研究方向	Pharmacology & Pharmacy
WOS记录号	WOS:000344068500001
收录类别	SCIE ; PUBMED ; SCOPUS
URL	查看原文
PubMed ID	25395833
PMC记录号	PMC4226458
SCOPUSEID	2-s2.0-84908514410
通讯作者地址	[Pan, Zheer]Department of Orthopedic Surgery, The First Affiliated Hospital, Wenzhou Medical University,Wenzhou,325035,China
Scopus学科分类	Pharmacology;Pharmaceutical Science;Drug Discovery
引用统计	被引频次：21[WOS] [WOS记录] [WOS相关记录]
文献类型	期刊论文
条目标识符	https://kms.wmu.edu.cn/handle/3ETUA0LF/6132
专题	药学院（分析测试中心）附属第一医院第一临床医学院（信息与工程学院）、附属第一医院_外科学_整形外科
通讯作者	Pan, Zheer
作者单位	1.Chemical Biology Research Center, School of Pharmaceutical Sciences, Wenzhou Medical University,Wenzhou,325035,China; 2.The Children’s Hospital, Zhejiang University School of Medicine,Hangzhou,China; 3.Department of Orthopedic Surgery, The First Affiliated Hospital, Wenzhou Medical University,Wenzhou,China; 4.Wenzhou Undersun Biotchnology Co. Ltd,Wenzhou,China
第一作者单位	药学院（分析测试中心）; 生物有机与药物化学研究中心
通讯作者单位	附属第一医院
第一作者的第一单位	药学院（分析测试中心）
推荐引用方式 GB/T 7714	Zhang, Yali,Jiang, Xin,Peng, Kesong,et al. Discovery and evaluation of novel anti-inflammatory derivatives of natural bioactive curcumin[J]. DRUG DESIGN DEVELOPMENT AND THERAPY,2014,8:2161-2171.
APA	Zhang, Yali., Jiang, Xin., Peng, Kesong., Chen, Chengwei., Fu, Lili., ... & Pan, Zheer. (2014). Discovery and evaluation of novel anti-inflammatory derivatives of natural bioactive curcumin. DRUG DESIGN DEVELOPMENT AND THERAPY, 8, 2161-2171.
MLA	Zhang, Yali,et al."Discovery and evaluation of novel anti-inflammatory derivatives of natural bioactive curcumin".DRUG DESIGN DEVELOPMENT AND THERAPY 8(2014):2161-2171.