| Summary: | 碩士 === 高雄醫學大學 === 醫學研究所碩士班 === 93 === Glyceryl Nonivamide (GLNVA) was a nonpungent and antinociceptive capsaicin derivative. GLNVA has reported for several pharmacological effects including antihypertension, calcitonin gene related peptide (CGRP) and substance P releasing, enhancement of renal function and prevention subarachnoid hemorrhage-induced cerebral vasospasm. In this study, the effects of GLNVA on protein expressions related to inflammation were investigated in murine macrophage RAW264.7 and immortalized microglia cell line BV-2. Pretreatment of cells with GLNVA diminished lipopolysaccharide (LPS)-induced nitric oxide (NO) production in a concentration-dependent manner. GLNVA inhibition of LPS-induced NO production accompanied by suppression of inducible NO synthase (iNOS) expression. ERK1/2 phosphorylation and I�羠��/I�羠�� degradation were also inhibited by GLNVA in RAW264.7 and BV-2. Although COX-2 was slightly inhibited by GLNVA, LPS-induced PGE2 level was lowered by GLNVA in dose -dependent manners. The potency for ERK inhibition and I�羠��/I�羠�� degradation displayed relative correlations with their inhibitory effects on translocation into nucleus and DNA binding affinity of NF-�羠 and NO production. GLNVA also decreases pro-inflammatory cytokines-TNF-�� and IL-1β release and increases anti-inflammatory cytokine-IL-10 production. LPS could not induce ERK1/2 phosphorylation in BV-2 and it might be the reason that there are different effects of GLNVA in LPS-activated two cell lines. Taken together, GLNVA exerts its anti-inflammatory effect by inhibiting LPS-induced pro-inflammatory mediators, and thus could be used as a potential agent for anti-inflammation.
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