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

  • Molecules. 2018 Dec 2;23(12):3177. doi: 10.3390/molecules23123177.
Yun-Chen Tsai  1 ,  Sin-Ling Wang  2 ,  Mei-Yao Wu  3 ,  Chia-Huei Liao  4 ,  Chao-Hsiung Lin  5 ,  Jih-Jung Chen  6  7 ,  Shu-Ling Fu  8
Affiliations
  • 1. Institute of Traditional Medicine, National Yang-Ming University, Taipei 11221, Taiwan. [email protected].
  • 2. School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 80708, Taiwan. [email protected].
  • 3. Research Center for Traditional Chinese Medicine, Department of Medical Research, China Medical University Hospital, Taichung 40402, Taiwan. [email protected].
  • 4. Institute of Traditional Medicine, National Yang-Ming University, Taipei 11221, Taiwan. [email protected].
  • 5. Department of Life Sciences and Institute of Genome Sciences, National Yang-Ming University, Taipei 11221, Taiwan. [email protected].
  • 6. Faculty of Pharmacy, National Yang-Ming University, Taipei 11221, Taiwan. [email protected].
  • 7. Department of Medical Research, China Medical University Hospital, China Medical University, Taichung 40447, Taiwan. [email protected].
  • 8. Institute of Traditional Medicine, National Yang-Ming University, Taipei 11221, Taiwan. [email protected].
PMID: 30513815 DOI: 10.3390/molecules23123177
Abstract

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.

Keywords
Aquilaria sinensis; NF-κB; anti-inflammation; flavonoid; pilloin.
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