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KMID : 0606920090170010079
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Biomolecules & Therapeutics
2009 Volume.17 No. 1 p.79 ~ p.85
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Structural Features of Polyphenolic Compounds in Their NO Inhibitory Activities
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Kim Byung-Hun
Lee Yong-Gyu
Kim Tae-Woong
Cho Jae-Youl
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Abstract
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Polyphenolic compounds are reported to have various pharmacological activities such as anti-oxidative, anti-cancerous, anti-inflammatory and anti-aging effects. Although numerous papers explore their functional roles in many different cellular actions, not many studies handle their structural features in anti-inflammatory responses. In this study, therefore, we examined structural role of substituted transstilbenes in their NO inhibitory and NF- suppressive activities. Of 10 compounds tested, 4 compounds (cinnamic acid, resveratrol, piceatannol and curcumin) displayed NO inhibitory activities in a dose-dependent manner. Similarly, these compounds blocked LPS-induced cytotoxicity of RAW264.7 cells. All NO inhibitory compounds also inhibited phosphorylation, a hallmark for NF- activation. However, these inhibitory compounds exhibited distinct suppressive pattern in tumor necrosis factor (TNF)-- or phorbol-12-myristate-13-acetate (PMA)-induced NF- and AP-1 activation. According to structure-activity relationship study, polarity and size of ring B seem to be important for diminishing NO production. Therefore, our data suggest that substituted trans-stilbenes can be developed as novel anti-inflammatory drug or further developed as lead compounds for another improvement.
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KEYWORD
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Polyphenolic compounds, Substituted trans-stilbenes, NO production, NF-, Structure-activity relationship study
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