Inhibitors of BRD4 protein from the roots of Astilbe grandis stapf ex E.H. Wilson

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(5H)-one (1), caffeic acid...

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Bibliographic Details
Published in:	Natural product research Vol. 35; no. 12; pp. 2044 - 2050
Main Authors:	Shi, Yingying, Zhang, Dongdong, Li, Shupei, Xuan, Xiuxiu, Zhang, Liuqiang, Li, Yiming, Guo, Fujiang
Format:	Journal Article
Language:	English
Published:	England Taylor & Francis 01-06-2021 Taylor & Francis Ltd
Subjects:	Astilbe grandis bromodomain-containing protein 4 Caffeic acid Cytotoxicity monoterpene Proteins Roots Toxicity bromodomain-containing protein 4 cytotoxicity monoterpene
Online Access:	Get full text
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Summary:	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(5H)-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 IC 50 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 IC 50 values ranging from 31.98 to 154.90 µM.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	1478-6419 1478-6427
DOI:	10.1080/14786419.2019.1655414