This study investigated effects of the Gynura bicolor (Roxb. and Willd.) DC. ether extract (GBEE) on nitric oxide (NO) and prostaglandin (PG)E_2 production on the lipopolysaccharide (LPS)-induced inflammatory response in RAW 264.7 cells. A composition analysis of GBEE showed that the major compounds were b-carotene, chlorophyll, and quercetin, respectively. Furthermore, NO and PGE_2 levels of 120 μg/ml GBEE-treated cells were 70% and 9.8%, respectively, than those of cells treated with LPS alone. Immunoblots assays showed that the GBEE dose-dependently suppressed LPS-induced inducible NO synthase (iNOS) and cyclooxygenase (COX)-2 protein levels. The GBEE significantly decreased cytosolic phosphorylated (p)-IκBa and nuclear p65 protein expressions. Electrophoresis mobility shift assays indicated that the GBEE effectively inhibited nuclear factor kappa B (NF-κB) activation induced by LPS. These results support a role of the GBEE in suppressing activation of NF-κB to inhibit NO and PGE_2 production in the LPS-induced inflammatory response by RAW 264.7 cells.