Aims: To critically summarize and provide update knowledge on phytochemistry and pharmacological activities of Moringa oleifera with a view to provide baseline data for medicinal food fortification formulation.Study Design: Multidisciplinary advanced bibliographic surveys, utilization of ChemBioDraw software package and dissemination of the resulted knowledge.Place and Duration of Study: Faculty of Science, University of Kinshasa, Department ofEnvironmental Science, University of Gbadolite and Faculty of Science, University of Kisangani, the Democratic Republic of the Congo, between March and June 2018.Methodology: A deep literature search was carried out to obtain information about the phytochemistry and pharmacognosy of M. oleifera from various established scientific databases such as PubMed, PubMed Central, Science Direct and Google scholar. The scientific name of this plant species was used as a keyword for the search, along with the terms phytochemistry and bioactivity or pharmacognosy. The chemical structures of the M. oleifera naturally occurring compounds were drawn using ChemBioDraw Ultra 12.0 software package.Results: Comparative analysis of the literature revealed that Moringa oleifera is traditionally used to treat several ailments. This plant is reported to possess various pharmacological properties such as antioxidant, antibacterial, anti-inflammatory, antidiabetic, antifungal, antispasmodic, anticancer, antipyretic, anti-proliferative, wound healing, and antidyslipidemic, CNS effects as well as it is efficient against infertility. These properties are due to the presence of numerous naturally occurring phytochemicals like tannins, alkaloids, phenols, glycosides, flavonoids and steroids while its proximate composition makes it very relevant in daily life as nutraceutical.Conclusion: The present review can, therefore, help inform future scientific research towards the development of novel drugs of relevance from M. oleifera to improve human health and wellbeing. Especially, M. oleifera could serves as drug candidates for Sickle cell anemia treatment and others ailments of relevance in developing world like Democratic Republic of the Congo.