**Abstract**

Nature is full of poisons as well as life-saving entities. Extracts of natural products in medicinal plants have been used for thousands of years in traditional medicine throughout the World. Bitter melon (*Momordica charantia)* is a member of Cucurbitaceae family, widely distributed in tropical regions of the World, that has been used in folk medicine for the treatment of diabetes mellitus, and its fruit has been used as a vegetable for thousands of years. It contains phytochemicals, flavonoids, triterpenes, saponins, ascorbic acid, steroids, proteins, and polysaccharides. This plant is a traditional herbal medicine, possesses various biological, medicinal activities and pharmacological functions, namely antidiabetic, anthelmintic, contraceptive, antimalarial, laxative, antihyperglycemic, antimutagenic, antiulcer, antilipolytic, antifertility, hepatoprotective, anticancer, antibacterial, antiviral, antitumor, immunomodulation, antioxidant, antidiabetic, and anti-inflammatory activities of *M. charantia* have been reported. Its fruit has a special bitter taste, parts of *M. charantia,* such as fruits, vines, leaves and even roots have been used as folk medicine for the remedy of diseases like toothache, diarrhea, and diabetes. It is also used for the treatment of eczema, gout, jaundice, pneumonia, psoriasis, and rheumatism. These beneficial effects are attributed to the various bioactive components of *M. charantia*, which are important sources of phytoconstituents used to treat various diseases since ancient times. This chapter reviews various aspects of the results of investigations involving *M. charantia* in the recent years, providing a comprehensive overview of the phytochemical application of *M. charantia* to attract more attention to their biological activities for better utilization of *M. charantia*; focusing on the review of benefits that bitter melon offers in terms of its potential as a source of bioactive compounds and its role in the control of different diseases.

**Keywords:** Bitter melon, medicinal, biologicl, bioactive compounds, phytochemicals
