Open AccessBrassinin, a brassica‐derived phytochemical, regulates monocyte‐to‐macrophage differentiation and inflammatory responses in human monocytes and murine macrophages
Author(s) -
Kang Bobin,
Hwang Jisu,
Choi HyeonSon
Publication year - 2020
Publication title -
journal of pharmacy and pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.745
H-Index - 118
eISSN - 2042-7158
pISSN - 0022-3573
DOI - 10.1111/jphp.13291
Subject(s) - monocyte , lipopolysaccharide , phorbol , macrophage , cd36 , nitric oxide synthase , microbiology and biotechnology , nitric oxide , reactive oxygen species , thp1 cell line , tumor necrosis factor alpha , biology , chemistry , biochemistry , signal transduction , cell culture , immunology , in vitro , protein kinase c , endocrinology , genetics , receptor
Objectives The effects and molecular mechanisms of brassinin (BR), an indole phytoalexin from cruciferous vegetables, on monocyte‐to‐macrophage differentiation and inflammatory responses were investigated in this study. Methods Inflammatory responses from RAW264.7 cells and THP‐1 were stimulated by lipopolysaccharide (1 µg/ml), and monocyte‐to‐macrophage differentiation of THP‐1 was induced by phorbol myristate acetate (50 ng/ml). The production of inflammatory mediators was determined by ELISA, Western blot or real‐time PCR. Reactive oxygen species were examined by DCFH‐DA assay. Key findings Brassinin at 50 µm suppressed lipopolysaccharide‐induced production of nitric oxide synthase, cyclooxygenase‐2, prostaglandin E2 and reactive oxygen species by 90%, 69%, 52% and 41%, respectively, in RAW264.7 cells. In THP‐1 cells, BR inhibited phorbol myristate acetate‐induced monocyte‐to‐macrophage differentiation by suppressing cluster of differentiation molecule β and CD36. In addition, BR suppressed translocation of nuclear factor ‘kappa‐light‐chain‐enhancer’ of activated B cells (NF‐κB) into the nucleus. However, BR activated the nuclear factor erythroid‐derived 2‐like 2 (Nrf2) and its target molecules hemoxygenase‐1 (HO‐1) and NAD(P)H: quinone oxidoreductase 1 (NQO1), with an increase in nuclear translocation of Nrf2. Conclusions Brassinin suppressed monocyte‐to‐macrophage differentiation and inflammatory responses by differentially regulating Nrf2 and NF‐κB signallings.