Chromolaena odorata is a perennial shrub that grows abundantly in Asia and sub-Saharan Africa, where it has been used in the treatment of many ailments and disease conditions such as diabetes, malaria, wounds, inflammation and fever. Several studies have investigated the different biological activities of C. odorata intending to validate its purported medicinal property and identify chemical components of the plants responsible for such properties. Despite the studies carried out on the plant, there is still a dearth of knowl-edge regarding the mechanism by which C. odorata constituents bring about the different biological activity of the plant. The present review collated scientific reports on the antidiabetic, anticancer, anti-inflammatory, antimicrobial, antiparasitic, antinociceptive, antipyretic and wound healing activities of C. odorata from Sco-pus, PubMed, Google Scholar and Web of Science database. Interestingly, findings from these reports suggest that C. odorata contains bioactive compounds such as flavonoids, fatty acids, saponins, and alkaloids, which can act singly or synergistically to mediate different biological properties. Moreover, the bioactive com-pounds act by modulating critical proteins of signalling pathways involved in the different health conditions. The current review discusses the critical aspect of C. odorata biological activity, the likely mechanism involved and possible roadmap for better outcomes in future research. Collectively, the mechanisms covered in this article reveal biochemical pathways that may provide insight into potential targets that could be explored in disease management. (c) 2021 SAAB. Published by Elsevier B.V. All rights reserved.