Moringa oleifera Lam. is a multi-purpose perennial plant belonging to family Moringaceae. Traditionally, it has been used to cure diabetes, anaemia, asthma, typhoid fever, arthritis, malaria and skin disease. M. oleifera is rich in various phytoconstituents such as flavonoids, carotenoids, isothiocyanates, polyphenol, saponins, alkaloid, cardiac glycosides, carbohydrates and glucosinolates. All parts of M. oleifera including seeds, leaves, roots, flowers, stem, pods have traditional medicinal value. Various extracts, fractions and phytoconstituents isolated from various parts of M. oleifera have been studied at molecular level for treatment of various pathological conditions such as cancer, inflammation, diabetes, arthritis, atherosclerosis, and wound healing and atopic dermatitis. These reports indicate that phytoconstituents present in plant parts are responsible for regulation of various biological functions via modulation of various molecular targets. It is used as food fortificant since it isa good source of dietary anti-oxidants; has high content of b-carotene, ascorbic acid, a-tocopherol, iron calcium, iron and potassium and protein content. The purpose of present review is to discuss effect of M. oleifera on various molecular targets such as various cytokines, NF-κB, Nrf-2, HO-1, iNOS, PPAR, COX, MAPK, JNK, ERK, Bax, Caspase 3 and 9, Bcl-2 and understand its role in management of various diseases. Abbreviation: MO- Moringa oleifera, TNF- Tumour Necrosis Factor, BSS- β-sitosterol, IL- Interleukin, LPS- lipopolysaccharide, MSE- Moringa oleifera seed extract, MC- Moringa oleifera concentrate, MIC- Moringa isothiocyanates, VHFD- very high fat diet, DNCB- 2,4-dinitrochlorobenzene, AD- Atopic dermatitis, NF-κB- Nuclear Factor kappa beta, ARE- antioxidant response element, HO- Haem Oxygenase, Nrf- Nuclear factor erythroid 2-related factor, RBITC- 4- (α-L-Rhamnosyloxy)-benzyl isothiocyanate, COX- cyclooxygenase, Bcl2-B-cell lymphoma 2, Bcl-xL- B-cell lymphoma-extra large, EAC- Ehrlich ascites carcinoma, DEN- Diethyl nitrosamine, VEGF- vascular endothelial growth factor, iNOS- inducible nitric oxide synthase, CP- cyclophosphamide, PPAR- Peroxisome proliferator- activated receptors, PARP- poly(ADP-ribose) polymerase, MAPK- Mitogen-activated protein kinase, ERK- Extracellular-signal-regulated kinase, JNK- c-Jun N-terminal kinase, UC- ulcerative colitis, SCI- spinal cord injury, WKY- Wistar Kyoto rats, DNA- deoxyribonucleic acid, ASC- adipose stem cells, MOLEE- Moringa oleifera leaf ethanol extract, TLR4- Toll-like receptor 4, PGE2- Prostaglandin E2, PIK3- Phosphoinositide 3-kinase. © 2020 Taylor & Francis.