The aim of this review is to highlight the biological potential of the aporphine class of alkaloids, crebanine, oxocrebanine and dehydrocrebanine and their molecular mechanisms, in order to understand their therapeutic potential in medicine. Using the phrases herbal medicine, aporphine, crebanine, oxocrebanine, dehydrocrebanine, and phytochemical, all of the scientific data on crebanine, oxocrebanine, and dehydrocrebanine used in this review was gathered from Google, Google Scholar, PubMed, Scopus, and Science Direct. Nevertheless, analytical techniques for the isolation, separation, and identification of crebanine, oxocrebanine, and dehydrocrebanine are also covered in this study. Present review describes the biological potential of crebanine against cerebral ischemia, human cancer, hepatocellular carcinoma, human lung adenocarcinoma, memory and cognition, and cardiac tissues with their anti-inflammatory, anti-bacterial, cytotoxic potential and anti-invasion effect. Additionally, oxocrebanine biological potential against breast cancer, inflammatory disorders, and acute lung injury is explained by scientific research. Nonetheless, the biological effects of dehydrocrebanine on malaria, cancer, and ulcerative colitis are also discussed in this article. In order to understand the potential for health promotion in human illnesses, this review also discussed the molecular mechanisms behind the pharmacological effects of crebanine, oxocrebanine, and dehydrocrebanine. For the isolation, separation, and identification of crebanine, oxocrebanine, and dehydrocrebanine in biological and non-biological substances, the analytical data showed the significance of various analytical techniques. The biological potential of crebanine, oxocrebanine, and dehydrocrebanine is discussed in the current review along with its various molecular mechanisms, pharmacokinetics, and analytical features. To claim their therapeutic applicability in human illnesses, however, the scientific community needs clinical data.