Plants are important source of traditional medicine that can be used to aid many type of illness. Gynura procumbens is one of the plants that are often used by Indonesian people as traditional medicine. Gynura procumbens exhibits antibacterial, anticancer, anti-hyperglycemic, antihypertensive, anti-inflammatory, antioxidant, cardioprotective, fertility enhancement, organ protective activity. This review aims to provide an overview on the relatedness of the identified bioactive compounds with the reported biological activities of Gynura procumbens leave and on the herbal therapy with leave of Gynura procumbens. Literature search is carried out with the help of two searching engines: PubMed and Science Direct. The searching was carried out with keyword: Gynura procumbens. From PubMed and Science Direct, 42 and 94 results were obtained respectively. There were 45 full text articles that meet systematic review criteria. The relevant information is compiled to illustrate that leave of Gynura procumbens is a potential natural source of compounds with various pharmacological actions. Polar, semi and nonpolar solvent can be used to extract the bioactive compounds from the leave of Gynura procumbens. The identified bioactive compounds belong to phenolic, flavonoid, coumaric acids, essential oils, carbohydrates and proteins. Most of the extracts show potent antioxidative activity. The bioactivities of the leave extract are associated with many diseases, such as diabetes, hypertension, cancer, obesity, etc. The herbal therapy with leave of Gynura procumbens can be appropriately applied in oral administration and topical application. Leave of Gynura procumbens is good resource for oral or topical herbal medicine/ingredient.