: Gynura procumbens (Lour.) Merr. is a well-known plant used in the folkloric medicine in tropical Asian countries. The plant is prevalently employed by traditional healers in the treatment of diabetes, cancer, hypertension, inflammation, fever and skin disorders. Several scientific studies reported that, Gynura procumbens possesses considerable therapeutic value for the development of emerging treatment options. The diverse pharmacological effects of this plant are attributed to its vast phytoconstituent content. Different chemical classes including alkaloids, flavonoids, phenolics, steroids, proteins and polysaccharides have been isolated from this plant. In this review, we tried to explore the different aspects of Gynura procumbens as an established medicinal plant. The data gathered here give an indication that the plant Gynura procumbens is a good natural source of chemical compounds with different types of pharmacological actions and these chemical compounds can be used as model for the development of de novo therapeutic agents.