E. Park, Y. Ahn, J. Pyee
May 1, 2005
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Influential Citations
3
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Quality indicators
Journal
Cancer Research
Abstract
748 Pinosylvin (3,5-dihydroxy- trans -stilbene), one of the naturally occurring resveratrol analog found in heartwood and leaves of Pinus species, is a phytoalexin with antioxidant, antifungal, algicidal and nematocidal activities. Based on anti-inflammatory and chemopreventive activities of resveratrol, we have evaluated the effects of pinosylvin on cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) activities in lipopolysaccharide (LPS)-stimulated RAW 264.7 mouse macrophage cells by measuring the production of prostaglandin E 2 (PGE 2 ) and nitric oxide (NO). As a result, pinosylvin exhibited the inhibitory activities in both PGE 2 and NO productions in a dose dependent manner. To elucidate the inhibitory mechanism of pinosylvin on COX-2 and iNOS expression, Western blot analysis and reverse transcription-polymerase chain reaction (RT-PCR) were performed. Pinosylvin suppressed COX-2 and iNOS protein and gene expression. Further study revealed that pinosylvin inhibited NF-κB-DNA binding via the inhibition of IκB-α degradation. In addition, the growth inhibitory effects of pinosylvin against human cancer cells were investigated. Pinosylvin inhibited the growth of HCT116 human colon cancer cells with an IC 50 value of 60 μM by MTT assay at 72 hr incubation. Cell cycle distribution treated by pinosylvin (60 μM) exhibited G 0 /G 1 phase arrest. Checkpoint proteins of cyclin D1, cdk4 and proliferating cell nuclear antigen (PCNA) related to G 0 /G 1 phase were down-regulated by pinosylvin. Taken together, pinosylvin, a natural stilbenoid, might be a new candidate for a potential cancer chemopreventive agent.