Synthesis of pyranochalcone derivatives and their inhibitory effect on NF-kappa B activation

doi:10.1016/j.bmcl.2021.128042

	Synthesis of pyranochalcone derivatives and their inhibitory effect on NF-kappa B activation
	Ajiaikebaier, Dilidaer 2,3; Li, Zuopeng 1; Lin, TzuChun 2; Sun, Xinyu 2; Wang, Bianlin 1; Li, Jingya 2,3
刊名	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
	2021-06-15
卷号	42 页码:5
关键词	Pyranochalcone derivatives NF-kappa B inhibitor Anti-inflammatory Inflammatory factor
ISSN号	0960-894X
DOI	10.1016/j.bmcl.2021.128042
通讯作者	Wang, Bianlin(wangbl@ms.xjb.ac.cn) ; Li, Jingya(jyli@simm.ac.cn)
英文摘要	In an effort to identify novel inhibitors of nuclear factor kappa B (NF-kappa B), twenty five pyranochalcone derivatives were synthesized and evaluated for their in vitro activities against TNF-alpha induced NF-kappa B inhibition in HEK293T cells. Among all of these derivatives, several displaying the same acrylate moiety on the B ring exhibited potent inhibition, with IC50 values ranging from 0.29 to 10.46 mu M. A functional study of the most potent of these compounds, designated 6b, revealed that it significantly suppressed the transcriptional expression of inflammatory factor IL-10 in lipopolysaccharide-induced RAW 264.7 macrophages, and also mildly inhibited CCL2, IL6 and TNF-alpha. In addition, compound 6b was found to inhibit IL-10 released in LPS-induced BMDM cells. This study demonstrates that the inhibitory effect of 6b on LPS-stimulated inflammatory mediator production in the mouse macrophage cell line RAW 264.7 correlates with the suppression of the NF-kappa B and MAPK signaling pathways.
资助项目	West Light Foundation of Chinese Academy of Sciences[2016-QNXZ-B-6] ; Central Asian Drug Discovery and Development Center of the Chinese Academy of Sciences[CAM202001] ; One Belt One Road Youth Exchange Program of Shanghai Municipal Committee of Science and Technology[19430742000]
WOS关键词	XANTHOHUMOL ; HOPS ; INFLAMMATION ; APOPTOSIS ; TARGET ; BEER
WOS研究方向	Pharmacology & Pharmacy ; Chemistry
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000655255700003
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/297044]
专题	中国科学院上海药物研究所
通讯作者	Wang, Bianlin; Li, Jingya
作者单位	1.Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, State Key Lab Basis Xinjiang Indigenous Med Plant, Urumqi 830011, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 3.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
推荐引用方式 GB/T 7714	Ajiaikebaier, Dilidaer,Li, Zuopeng,Lin, TzuChun,et al. Synthesis of pyranochalcone derivatives and their inhibitory effect on NF-kappa B activation[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2021,42:5.
APA	Ajiaikebaier, Dilidaer,Li, Zuopeng,Lin, TzuChun,Sun, Xinyu,Wang, Bianlin,&Li, Jingya.(2021).Synthesis of pyranochalcone derivatives and their inhibitory effect on NF-kappa B activation.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,42,5.
MLA	Ajiaikebaier, Dilidaer,et al."Synthesis of pyranochalcone derivatives and their inhibitory effect on NF-kappa B activation".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 42(2021):5.