Journal Article

Pilloin, A Flavonoid Isolated from Aquilaria sinensis, Exhibits Anti-Inflammatory Activity In Vitro and In Vivo

Wu, Mei-Yao, Chen, Jih-Jung, Fu, Shu-Ling, Tsai, Yun-Chen, Liao, Chia-Huei, Lin, Chao-Hsiung, Wang, Sin-Ling

2018

Overview

Flavonoids, widely present in medicinal plants and fruits, are known to exhibit multiple pharmacological activities. In this study, we isolated a flavonoid compound, pilloin, from Aquilaria sinensis and investigated its anti-inflammatory activity in bacterial lipopolysaccharide-induced RAW 264.7 macrophages and septic mice. Pilloin inhibited NF-κB activation and reduced the phosphorylation of IκB in LPS-stimulated macrophages. Moreover, pilloin significantly suppressed the production of pro-inflammatory molecules, such as TNF-α, IL-6, COX-2 and iNOS, in LPS-treated RAW 264.7 macrophages. Additionally, pilloin suppressed LPS-induced morphological alterations, phagocytic activity and ROS elevation in RAW 264.7 macrophages. The mitogen-activated protein kinase-mediated signalling pathways (including JNK, ERK, p38) were also inhibited by pilloin. Furthermore, pilloin reduced serum levels of TNF-α (from 123.3 ± 7 to 46.6 ± 5.4 ng/mL) and IL-6 levels (from 1.4 ± 0.1 to 0.7 ± 0.1 ng/mL) in multiple organs of LPS-induced septic mice (liver: from 71.8 ± 3.2 to 36.7 ± 4.3; lung: from 118.6 ± 10.6 to 75.8 ± 11.9; spleen: from 185.9 ± 23.4 to 109.6 ± 18.4; kidney: from 160.3 ± 11.8 to 75 ± 10.8 pg/mL). In summary, our results demonstrate the anti-inflammatory potential of pilloin and reveal its underlying molecular mechanism of action.

• Publisher: MDPI AG,MDPI
• Subject: Animals / anti-inflammation / Anti-Inflammatory Agents - pharmacology / Aquilaria sinensis / Bacterial infections / Cyclooxygenase 2 - metabolism / Cytokines / Cytokines - metabolism / Cytotoxicity / flavonoid / Flavonoids / Flavonoids - chemistry / Flavonoids - isolation & purification / Flavonoids - pharmacology / Herbal medicine / Inflammation / Inflammation Mediators - metabolism / Kinases / Lipopolysaccharides - pharmacology / Macrophages - drug effects / Macrophages - metabolism / MAP Kinase Signaling System - drug effects / Mice / Morphology / NF-kappa B - metabolism / NF-κB / Nitric oxide / Nitric Oxide - metabolism / Nitric Oxide Synthase Type II - metabolism / Pathogens / Phagocytosis - drug effects / Phosphorylation / pilloin / RAW 264.7 Cells / Reactive Oxygen Species - metabolism / Sepsis / Sepsis - pathology / Thymelaeaceae - chemistry / Tumor necrosis factor-TNF