A variety of bioactivities induding papaya alkaloids, rutin, benzyl isothiocyanate, carotenoids in Papaya (Carica Papaya L.) were investigated in this study. Some of these compounds exhibited a broad array of pharmacological activities in gastrointestinal protection, hepatoprotective effect, anti-inflammatory, weight loss and beauty, anti-cancer, anti-bactericidal and antioxidation properties. This review summarizes the research progress of main bioactive substances, anticancer functions in different parts of papaya, and its wide application prospects in food industry, pharmaceutical industry and health care industry were proposed.