Abstract: Plant alkaloids are a set of nitrogen-containing organic compounds, which exhibit a wide range of biological activities, including anticancer, neuromodulation and antidiabetes, making them highly valuable for drug development. The natural yields of many high-value alkaloids however are very low, and their chemical synthesis is highly cost and environmentally polluting, greatly limiting their development and utilization. Currently, bio-regulatory and biosynthetic strategies for alkaloid production are attracting incresing attention. This paper reviews recent advances in alkaloids classification, biological activities and potential applications, and current status and future directions. This review also analyzes the key challenges in their development and utilization, highlights the promoting role of synthetic biology in enhancing alkaloid biosynthesis efficiency, and provides perspectives on their scaled production and industrial prospects.