FPR2-based anti-inflammatory and anti-lipogenesis activities of novel meroterpenoid dimers from Ganoderma

doi:10.1016/j.bioorg.2021.105338

KIB OpenIR

	FPR2-based anti-inflammatory and anti-lipogenesis activities of novel meroterpenoid dimers from Ganoderma
	Peng,Xing-Rong ; Wang,Qian ; Wang,Hui-Rong ; Hu,Kun; Xiong,Wen-Yong; Qiu,Ming-Hua
	2021
发表期刊	BIOORGANIC CHEMISTRY
ISSN	0045-2068
卷号	116 页码:105338
摘要	Four pairs of novel meroterpenoid dimers, (+/-)-applandimeric acids A-D (1-4) with an unprecedented spiro[furo [3,2-b]benzofuran-3,2 '-indene] core were isolated from the fruiting bodies of Ganoderma applanatum. Their planar structures were unambiguously determined via extensive spectroscopic analysis. Their relative and absolute configurations were confirmed through calculated internuclear distance, coupling constant, 13C NMR with DP4 + analysis and electronic circular dichroism (ECD). Furthermore, the molecular docking-based method was used to evaluate their interaction with formyl peptide receptor 2 (FPR2) associated with inflammation. Interestingly, (+/-)-applandimeric acid D (4) can bond with FPR2 by some key hydrogen bonds. Furthermore, an in vitro bioassay verified that 4 can inhibit the expression of FPR2 with IC50 value of 7.93 mu M. In addition, compared to the positive control LiCl (20 mM), 4 showed comparable anti-lipogenesis activity at the concentration of 20 mu M. Meanwhile, 4 can suppress the protein levels of peroxisome proliferators-activated receptor-gamma (PPAR-gamma), CCAAT/ enhancer-binding protein-fl (C/EBP-fl), adipocyte fatty acid-binding protein 4 (FABP4), and fatty acid synthase (FAS) through activating AMP-activated protein kinase (AMPK) signaling pathway. Thus, our findings indicate that compound 4 could be a lead compound to treat obesity and obesity-related diseases by inhibiting lipid accumulation in adipocyte and alleviating inflammation.
关键词	Ganoderma applanatum Meroterpenoid dimers Molecular docking Anti-lipogenesis FPR2-based inflammation INDUCED INSULIN-RESISTANCE ADIPOCYTE DIFFERENTIATION OBESITY INFLAMMATION DEFICIENCY MACROPHAGES ACTIVATION EXPRESSION LIGAND MICE
DOI	10.1016/j.bioorg.2021.105338
WOS记录号	WOS:000702879500011
引用统计
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/73187
专题	中国科学院昆明植物研究所
作者单位	1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Yunnan, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 3.Southern Univ Sci & Technol, Dept Biol, Shenzhen, Peoples R China
推荐引用方式 GB/T 7714	Peng,Xing-Rong,Wang,Qian,Wang,Hui-Rong,et al. FPR2-based anti-inflammatory and anti-lipogenesis activities of novel meroterpenoid dimers from Ganoderma[J]. BIOORGANIC CHEMISTRY,2021,116:105338.
APA	Peng,Xing-Rong,Wang,Qian,Wang,Hui-Rong,Hu,Kun,Xiong,Wen-Yong,&Qiu,Ming-Hua.(2021).FPR2-based anti-inflammatory and anti-lipogenesis activities of novel meroterpenoid dimers from Ganoderma.BIOORGANIC CHEMISTRY,116,105338.
MLA	Peng,Xing-Rong,et al."FPR2-based anti-inflammatory and anti-lipogenesis activities of novel meroterpenoid dimers from Ganoderma".BIOORGANIC CHEMISTRY 116(2021):105338.

条目包含的文件		下载所有文件
文件名称/大小	文献类型	版本类型	开放类型	使用许可
045-D06-162-彭-BC.pdf（7004KB）	期刊论文	出版稿	开放获取	CC BY-NC-SA	浏览下载