Medicinal plants have been one of the prominent sources of remedies since the inception of human civilization. In rural area herbal medicines are considered to be best healthcare products due to it's easily availability. Globally, demand of herbal based medicines, health products, pharmaceuticals, food supplements, cosmetics, etc. has been intensified in alarming rate.Moringa oleifera belongs to family Moringaecea, native of the Indian subcontinent, where its diverse parts have been employed throughout history as food and medicine. The M. oleifera is extensively used for treating cancer, hyperlipidemic, diabetic, ulcer, analgesic, fertility, convulsant, liver disorder, wound, etc. Dietary consumption of its part is therein promoted as a strategy of personal health preservation and self-medication in various diseases. The phytoconstituents present in this plant are niazirin, niazirinin, flavonoids, anthocyanins, proanthocyanidin, kaempferol-3-O-(6''-malonyl-glucoside), 4-hydroxymellein, β-sitosterone, octacosanic acid, β-sitosterol, etc. These various phytoconstituents contribute for different pharmacological activities. The present review is therefore, an effort to give a detailed overview of the published writings on phytochemistry and pharmacological activities of M. oleifera; this information will be beneficial in developing new formulations, which are more effective and have more therapeutic values.