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Molecules 2018, 23(12), 3177; https://doi.org/10.3390/molecules23123177

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

1
Institute of Traditional Medicine, National Yang-Ming University, Taipei 11221, Taiwan
2
School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 80708, Taiwan
3
Research Center for Traditional Chinese Medicine, Department of Medical Research, China Medical University Hospital, Taichung 40402, Taiwan
4
Department of Life Sciences and Institute of Genome Sciences, National Yang-Ming University, Taipei 11221, Taiwan
5
Faculty of Pharmacy, National Yang-Ming University, Taipei 11221, Taiwan
6
Department of Medical Research, China Medical University Hospital, China Medical University, Taichung 40447, Taiwan
*
Authors to whom correspondence should be addressed.
Received: 3 November 2018 / Revised: 28 November 2018 / Accepted: 30 November 2018 / Published: 2 December 2018
(This article belongs to the Special Issue Anti-Inflammatory Activity of Natural Products)
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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. View Full-Text
Keywords: pilloin; flavonoid; Aquilaria sinensis; anti-inflammation; NF-κB pilloin; flavonoid; Aquilaria sinensis; anti-inflammation; NF-κB
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Tsai, Y.-C.; Wang, S.-L.; Wu, M.-Y.; Liao, C.-H.; Lin, C.-H.; Chen, J.-J.; Fu, S.-L. Pilloin, A Flavonoid Isolated from Aquilaria sinensis, Exhibits Anti-Inflammatory Activity In Vitro and In Vivo. Molecules 2018, 23, 3177.

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