Leaves and young pods of Moringa oleifera Lam. are not only used as vegetables, but different parts such as stem, stem barks, gum-resin, root, flower, seed pod, pod husk, seeds, and roots are also used in the traditional system of medicine. Chemical compounds such as alkaloids, phenolics, and terpenoids as excretory or waste products are produced by plants through the metabolic pathways. These chemical compounds have antibiotic, antimicrobial, and anti-insecticidal activity for their self-defense from a wide variety of pathogens. The ethnomedicinal uses and the scientific assessment of M. oleifera Lam. are essential, as it is a traditional food with numerous medicinal properties. Moringa leaves are an excellent nutritional supplement that contains crucial amino acids, minerals, vitamins, proteins, and other bioactive phytochemicals. In particular, the high nutrient content of the leaves benefits pregnant women and infants. It is also an effective diabetic, analgesic, and antimicrobial agent. This review mainly highlights the ancient medicinal uses of different plant parts such as leaves, flowers, fruit pods, seeds, seed oil, stem bark, gums, and roots; its mineral contents, phytochemical composition, and pharmacological potential, especially antidiabetic, antimicrobial, and analgesic activity, emphasizing the molecular mechanisms associated with anti-inflammatory and anti-diabetic activity.