Abstract: Oleocanthal(OC) is a secondary metabolite of olive oil. Currently, it has become one of the research hotspots in abroad, while domestic attention is less. The relevant research foundation is weaker in China, and the big gap with foreign countries is obvious. As an important active ingredient discovered in recent years, OC has a stronger anti-inflammatory activity than that of ibuprofen, and it had preventive and therapeutic effects on various diseases originating from inflammation, such as rheumatic diseases, cancer, cardiovascular diseases, diabetes, etc. At the same time, its excellent neuroprotective function also promote OC to inhibit the occurrence of neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease. This review focuses on an in-depth introduction to the biological activities including anti-inflammatory activity and anticancer activity(including melanoma, multiple myeloma, breast and colon cancer), neuroprotection, cardiovascular protection, and the prevention and therapeutic effects of diabetes, and the current efficient extraction and separation methods of OC were also analyzed, including liquid-liquid extraction separation method, high performance countercurrent chromatography extraction method, high vacuum assisted extraction method and centrifugal partition chromatography method. Meanwhile, different factors affecting OC contents were comprehensively discussed, and its research progress in bioavailability was explored. Finally, the future research of OC was prospected.