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KMID : 0043320150380050813
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Archives of Pharmacal Research
2015 Volume.38 No. 5 p.813 ~ p.825
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Validation of cyclooxygenase-2 as a direct anti-inflammatory target of 4-O-methylhonokiol in zymosan-induced animal models
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Kim Hyung-Sook
Ryu Hwa-Sun
Kim Ji-Sung
Kim Yong-Guk
Lee Hong-Kyung
Jung Jae-Kyung
Kwak Young-Shin
Lee Ki-Ho
Seo Seung-Yong
Yun Ji-Eun
Kang Jong-Soon
Hong Jin-Tae
Kim Young-Soo
Han Sang-Bae
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Abstract
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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.
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KEYWORD
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4-O-methylhonokiol, Cyclooxygenase-2, Anti-inflammatory target
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