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Molecules 2017, 22(10), 1605; doi:10.3390/molecules22101605

Evaluation of LPS-Induced Acute Lung Injury Attenuation in Rats by Aminothiazole-Paeonol Derivatives

1
Department of Critical Care Medicine, Taichung Veterans General Hospital, Taichung 40705, Taiwan
2
Department of Biotechnology, Hungkuang University, Taichung 43302, Taiwan
3
School of Chinese Medicine, China Medical University, Taichung 40447, Taiwan
4
Animal Technology Laboratory, Agriculture Technology Research Institute, Miaoli 35053, Taiwan
5
Institute of Biomedical Engineering and Nanomedicine, National Health Research Institutes, Miaoli 35053, Taiwan
6
Department of Medical Research, Tungs’ Taichung MetroHarbor Hospital, Taichung 43503, Taiwan
7
Department of Chemistry, National Tsing Hua University, Hsinchu 30013, Taiwan
8
Department of Chemistry, National Changhua University of Education, Changhua County 50007, Taiwan
9
Graduate Institute of Life Sciences, National Defense Medical Center, Taipei 11490, Taiwan
10
School of Dentistry, National Defense Medical Center, Taipei 11490, Taiwan
*
Author to whom correspondence should be addressed.
Received: 1 September 2017 / Revised: 20 September 2017 / Accepted: 21 September 2017 / Published: 25 September 2017
(This article belongs to the Special Issue Focusing on Sulfur in Medicinal Chemistry)
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Abstract

Paeonol is a key phenolic compound in the root bark of Moutan Cortex Radicis that has been used in traditional Chinese Medicine to ameliorate inflammation. A series of aminothiazole-paeonol derivatives (APDs) were synthesized in this work and subjected to preliminary evaluation in cells followed by verification in animals. Quantification of monocyte chemotactic protein-1 (MCP-1) and interleukin-6 (IL-6) in culture media of LPS-activated A549 cells, a lung epithelial adenocarcinoma cell line, were used to investigate the anti-inflammatory capability of APDs. ALI-bearing rats were employed to verify therapeutic efficacy of APDs according to observations of total cells, protein amounts, MCP-1 and IL-6 in bronchoalveolar lavage fluid (BALF). Histopathological examinations of lung tissues were consequently applied for validation of APDs. Among these compounds, 2-(2-aminothiazol-4-yl)-5-methoxyphenol (4) had the most potent activity, showing comparable inhibition of MCP-1/IL-6 and superior elimination of neutrophil infiltration and protein exudation in lungs compared to others as well as dexamethasone. This study demonstrated a comprehensive strategy to evaluate APDs through integration of cell-based screening and animal-based verification. In order to fulfill unmet needs of treating acute lung injury (ALI) and acute respiratory distress syndrome (ARDS), APDs introduced in this work could be promising lead compounds to develop high potent anti-inflammation agents. View Full-Text
Keywords: paeonol; aminothiazole-paeonol derivatives; Moutan Cortex Radicis; anti-inflammation agents; acute lung injury; acute respiratory distress syndrome paeonol; aminothiazole-paeonol derivatives; Moutan Cortex Radicis; anti-inflammation agents; acute lung injury; acute respiratory distress syndrome
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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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Fu, P.-K.; Yang, C.-Y.; Huang, S.-C.; Hung, Y.-W.; Jeng, K.-C.; Huang, Y.-P.; Chuang, H.; Huang, N.-C.; Li, J.-P.; Hsu, M.-H.; Chen, J.-K. Evaluation of LPS-Induced Acute Lung Injury Attenuation in Rats by Aminothiazole-Paeonol Derivatives. Molecules 2017, 22, 1605.

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