alexa Anti-inflammatory Properties of an Active Sesquiterpene Lactone and its Structure-Activity Relationship | OMICS International | Abstract
ISSN: 2161-0444

Medicinal Chemistry
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Research Article

Anti-inflammatory Properties of an Active Sesquiterpene Lactone and its Structure-Activity Relationship

Yang Hu1, Fei Zhang2, Chaofeng Zhang1* and Mian Zhang1

1State Key Laboratory of Natural Medicines, Research Department of Pharmacognosy, China Pharmaceutical University, Longmian Road 639, Nanjing 211198, PR China

2Jiangsu Simcere Pharmaceutical Group Ltd., Xuanwu Avenue No. 699-18, Nanjing 210042, PR China

*Corresponding Author:
Chaofeng Zhang
State Key Laboratory of Natural Medicines
Research Department of Pharmacognosy
China Pharmaceutical University
Longmian Road 639, Nanjing 211198 PR China
Tel/Fax: (86)-25-86185140
E-mail: [email protected]

Received date: July 01, 2015; Accepted date: August 11, 2015; Published date: August 14, 2015

Citation: Hu Y, Zhang F, Zhang C, Zhang M (2015) Anti-inflammatory Properties of an Active Sesquiterpene Lactone and its Structure-Activity Relationship. Med chem 5:354-360. doi: 10.4172/2161-0444.1000286

Copyright: © 2015 Hu Y, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

Abstract

A sesequiterpenoid, 2α-hydroxyl-3β-angeloylcinnamolide (HAC) was isolated from the Chinese medicinal herb Polygonum jucundum Lindex. (Polygonaceae) with anti-inflammatory activities in vivo. In the present study, we investigated the anti-inflammation effects of HAC on lipopolysaacharide (LPS)-induced murine RAW264.7 cells. As the results, we found that HAC dose-dependently decreased NO over-production with IC50 value of 17.68 μM but showed very weak inhibition on TNF-α release with IC50 value of 98.66 μM. Meanwhile, eight novel derivatives modified at C-2 position of HAC were synthesized to further explore the structure-activity relationships (SARs) of HAC on antiinflammation effects. Compound PJH-1, an acetyl easer of HAC, showed better inhibition on over-production of NO and TNF-α (IC50, 7.31 and 3.38 μM, respectively). Furthermore, we demonstrated that HAC and PJH-1 attenuates the mitogen-activated protein kinases (MAPK) signaling pathways through blocking the phosphorylation of ERK, p38, JNK/MAPK. We also found that the structure of PJH-1 are more stable than that of HAC in cell medium, these finding are useful to develop in vitro molecular mechanism research of HAC. In a conclusion, our studies enhance the understanding of anti-inflammation activities of HAC and lead to the discovery of novel derivatives as potential antiinflammation agents.

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