Despite the several uses of drugs from natural compounds in the pharmaceutical industry, new molecules have been discovered and associated with pharmacological activities over the years. Hecogenin, a steroidal saponin, has been the subject of several studies due to reports of pharmacological activities. This study combines the articles published to date that show the pharmacological activity and the mechanism of action of hecogenin, its acetate, and its derivates. This compilation shows that the compounds can act in different pathologies that affect many systems of the human body. They showed pharmacological properties in inflammation, mediating cytokines, cells, and environment. Also, it participated in tumoral processes by pathways like PPGARγ, ERK½, and MMP-2 and showed antimicrobial effects against organisms like Candida and Aedes aegypti’s larvae. This review indicates that continuing studies with these molecules are essential once they have the potential to be a future drug.