Inhibitors of BRD4 protein from the roots of Astilbe grandis stapf ex E.H. Wilson. Issue 12 (31st May 2021)

• Record Type: Journal Article
• Authors: Shi, Yingying; Zhang, Dongdong; Li, Shupei; Xuan, Xiuxiu; Zhang, Liuqiang; Li, Yiming; Guo, Fujiang
• Is Part Of: Natural product research. Volume 35:Issue 12(2021)
• Page Start: 2044
• Page End: 2050
• Publication Date: 2021-05-31
• Subjects: Astilbe grandis -- monoterpene -- bromodomain-containing protein 4 -- cytotoxicity; Natural products -- Periodicals; Natural products -- Research -- Periodicals; Biological Factors -- Periodicals; Biological Products -- Periodicals; 547
• DOI: 10.1080/14786419.2019.1655414
• Languages: English
• ISSNs: 1478-6419

Abstract

Abstract: A new monoterpene (1 ) along with eight known compounds were isolated from the roots of Astilbe grandis Stapf ex E.H. Wilson. Their structures were determined by extensive spectroscopic analysis and ECD experiments as ( S )-3-(2-hydroxyethyl)-5-(2-methylprop-1-en-1-yl)furan-2(5 H )-one (1 ), caffeic acid (2 ), mandelic acid (3 ), sonchifolinin B (4 ), α -viniferin (5 ), euscaphic acid (6 ), cianidanol (7 ), β -sitosterol (8 ), and stigmasterol (9 ), respectively. Compounds 5 and 6 exhibited inhibitory effects against BRD4 protein with IC50 values of 13.20 and 17.39 µM, respectively. In vitro, compounds 5 and 6 showed moderate cytotoxicity to A549 cells, HCC827 cells and Hela cells with IC50 values ranging from 31.98 to 154.90 µM. GRAPHICAL ABSTRACT: