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This study discusses the bioactive composition, supercritical fluid extraction and biological activities of Momordica charantia L. from the last five years. Numerous compounds that have been identified in the extracts of M. charantia, including phytosterols, terpenoids, fatty acids, phenolic compounds, phenolic acids and flavonoids were also discussed. Although, several studies reported the use of organic solvents in the extraction of these compounds, this review emphasized on supercritical fluid extraction (SFE), good selectivity, varied fractions in terms of mass yields and chemical composition obtained, in addition to providing a solvent-free extract. Moreover, the biological effects of M. charantia extracts, including their antidiabetic, neuroprotective, anti-obesogenic, antimalarial, antioxidant, anti-inflammatory, antimicrobial and allelopathic activities, were discussed. These biological effects of the extracts of M. charantia can directly affect human health. The findings of this review are important, as they can guide future studies related to obtaining bioactive compounds from M. charantia and its applications. Key words: Bitter melon, supercritical fluid, bioactive compounds, biological activities.