Structural Features of Polyphenolic Compounds in Their NO Inhibitory Activities

초록

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 trans-stilbenes in their NO inhibitory and NF-kappa B 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 LIPS-induced cytotoxicity of RAW264.7 cells. All NO inhibitory compounds also inhibited I kappa B alpha phosphorylation, a hallmark for NF-kappa B activation. However, these inhibitory compounds exhibited distinct suppressive pattern in tumor necrosis factor (TNF)-alpha- or phorbol-12-myristate-13-acetate (PMA)-induced NF-kappa B 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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