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We show that the crude extract of Plectranthus Amboinicus (PA) has anti-inflammatory effects and can inhibit AP-1 binding in vitro. The incubation of HUVEC cells with PA crude extract results in significant inhibition of the LPS-induced expression of IL-6, IL-12, MCP-1, and RANTES. After the crude extract being further fractionated with a preparative HPLC, the active components can server as a novel leads for potential AP-1 inhibitors. We also identify that in vitro AP-1 binding activity can be inhibited by some fractionats from actinomycetes fermentation broth. These fractions have inhibitory effects on AP-1activity and are useful as preventive or therapeutic agents for diseases in which excessive expression or activities of AP-1 are involved.