Humans experience different kinds of stress as a part of the day to day activity. The manifestation of stress will aggravate based on the physical conditions of individuals and due to their socio-economic situation of living. Herbal extracts have long been used in the traditional systems of medicine for the treatment of various ailments because of their potent antioxidant activity and lesser or no side-effects. Recently, there is a surge of interest toward the search of natural substances with diverse pharmacological activities, that can scavenge free radicals and protect cells from oxidative damage and apoptosis because of the adverse effects associated with the use of conventional medicines. Celastrus paniculatus is an endangered medicinal plant used from years in the traditional Ayurvedic system of medicine. The review presents the diverse chemical constituents of C. paniculatus and their pharmacological actions such as neuroprotective, memory-enhancing, anti-depressant, anxiolytic, anti-aging, hypolipidemic, anticancerous, analgesic, anti-inflammatory, antioxidant, anti-apoptotic, gastroprotective, anti-ulcerative properties at the cellular and molecular level based on the pre-clinical and clinical reports available. In the present review, we gathered the information from sources such as Google Scholar, Science direct, PUBMED, and reviewed with a special focus on the mode of action of C. paniculatus at molecular biology from the data on animal and preclinical experiments to cure various ailments. These diverse medicinal values of C. paniculatus demonstrates its value as traditional medicine as a cure for multiple maladies.