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Title 

Validation of cyclooxygenase-2 as a direct anti-inflammatory target of 4-O-methylhonokiol in zymosan-induced animal models

Authors 

H S KimH S RyuJ S KimY G KimH K LeeJ K JungY S KwakK LeeS Y SeoJi Eun YunJong Soon KangJ T HongY KimS B Han

Publisher 

Pharmaceutical Society of Korea

Issue Date 

2015

Citation 

Archives of Pharmacal Research, vol. 38, no. 5, pp. 813-825

Keywords 

4-O-methylhonokiolAnti-inflammatory targetCyclooxygenase-2

Abstract 

4-O-methylhonokiol (MH) is known to inhibit inflammation by partially understood mechanisms. Here, the anti-inflammatory mechanisms of MH were examined using enzymatic, cellular, and animal assays. In enzymatic assays, MH inhibited COX-2 activity with an IC50 of 0.062 μM, and also COX-1 with an IC50 of 2.4 μM. In cellular assays, MH was immunotoxic above 10 μM. At non-toxic concentrations (below 3 μM), MH strongly inhibited COX-2-mediated prostaglandin production with an IC50 of 0.1 μM, whereas did not or slightly affect other functions of B cells, T cells, dendritic cells, and macrophages. In an animal model, MH inhibited the increase in footpad thickness and popliteal lymph node weight in zymosan-injected mice. When analyzed the draining pLNs of zymosan-injected mice on day 5, MH inhibited the overall inflammatory responses. However, MH inhibited cyclooxygenase (COX)-2-mediated prostaglandin production without affecting tumor necrosis factor-α production in inflamed tissues within 6 h after zymosan injection. In summary, our data suggest that COX-2 may be a direct anti-inflammatory target of MH in vitro and in vivo.

ISSN 

0253-6269

Link 

http://dx.doi.org/10.1007/s12272-014-0456-8

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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