Ageratina adenophora is an invasive weed with widespread distribution. During the last several decades, many biologically active secondary metabolites have been isolated and characterized from A. adenophora, some of them having inspired the research and development of new therapeutic agents. This review mainly focuses on biological properties of A. adenophora, including the toxicity, antibacterial, antifungal, insecticidal, antiviral activities and others. In addition, the current limits and potentials of A. adenophora and its extracts are also discussed.