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Paeonol, a naturally existing compound found in Chinese traditional medicinal herb Cortex Moutan, the root bark of Paeonia suffruticosa Andr., has shown anticancer, antiinflammatory and anti-cardiovascular disease activities. These biological activities largely rely on the mechanisms underlying. It has been shown that these biological activities of paeonol are largely related to the inflammatory NF-ΚB cell signaling pathways. In this minireview, we are the first to summarize biological activities and associated pathways of paeonol.