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

Peng，Xing Rong1; Wang，Qian1,2; Wang，Hui Rong3; Hu，Kun1; Xiong，Wen Yong1; Qiu，Ming Hua1

2021-11-01

10.1016/j.bioorg.2021.105338

BIOORGANIC CHEMISTRY   影响因子和分区

0045-2068

1090-2120

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, C 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 IC value of 7.93 μM. In addition, compared to the positive control LiCl (20 mM), 4 showed comparable anti-lipogenesis activity at the concentration of 20 μM. Meanwhile, 4 can suppress the protein levels of peroxisome proliferators-activated receptor-γ (PPAR-γ), CCAAT/enhancer-binding protein-β (C/EBP-β), 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.

Anti-lipogenesis FPR2-based inflammation Ganoderma applanatum Meroterpenoid dimers Molecular docking

SCI

英语

其他

National Natural Science Foundation of China[21702209] ; Youth Innovation Promotion Association[2019383] ; Basic Research Project of Yunnan Province[202001AT070070] ; Fund of State Key Laboratory of Phytochemistry and Plant Resources in West China[P2020-KF02]

Biochemistry & Molecular Biology ; Chemistry

Biochemistry & Molecular Biology ; Chemistry, Organic

WOS:000702879500011

ACADEMIC PRESS INC ELSEVIER SCIENCE

BIOLOGY & BIOCHEMISTRY

2-s2.0-85114830480

Scopus

1.State Key Laboratory of Phytochemistry and Plant Resources in West China,Kunming Institute of Botany,Chinese Academy of Science,Kunming,650201,China
2.University of the Chinese Academy of Science,Beijing,100049,China
3.Department of Biology,Southern University of Science and Technology,Shenzhen,China

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.

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.

Peng，Xing Rong,et al."FPR2-based anti-inflammatory and anti-lipogenesis activities of novel meroterpenoid dimers from Ganoderma".BIOORGANIC CHEMISTRY 116(2021).