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Celastrus paniculatus, a botanically significant and therapeutically versatile medicinal plant, has been extensively utilized in traditional and modern systems of medicine. Its pharmacological applications span centuries, with both crude extracts and purified phytoconstituents being employed in the treatment of diverse pathological conditions. The species exhibits a wide spectrum of biological activities, including but not limited to cognition-enhancing, neuroprotective, antipsychotic, antidepressant, antibacterial, anti-arthritic, anti-malarial, analgesic, anti-inflammatory, antifertility, cardioprotective, anxiolytic, wound healing, antispasmodic, hypolipidemic, anticancer, antioxidant, and iron-chelating effects. These multifaceted properties are attributed to its rich phytochemical profile comprising monoterpenes, sesquiterpene esters, diterpenoids, triterpenoids, alkaloids, fatty acids, steroids, flavonoids, polyols, epoxides, polysaccharides, and ascorbic acid (vitamin C). Rather than the continuous pursuit of novel phytocompounds from unexplored botanical sources, a more pragmatic and cost-effective strategy lies in the rational repurposing of activity-enriched scaffolds from well-established multipotent medicinal plants such as C. paniculatus. This approach not only leverages the intrinsic chemical diversity and established bioavailability of known constituents but also has the potential to significantly reduce time and financial expenditure in drug development. From the standpoint of Ayurvedic medicine, Celastrus paniculatus holds a prominent place in classical compendia. In the Charaka Samhita, it is classified under the category of ?irovirechana Dravyas, indicating its utility in cleansing therapies for disorders of the head and central nervous system. The Sushruta Samhita enumerates it as an Adhobhagahara Dravya, highlighting its purgative action directed toward the lower gastrointestinal tract. Furthermore, traditional Nigha??us include this plant under multiple pharmacological clusters, such as Ark?di Ga?a, Gud?cy?di Varga, and Har?taky?di Varga, underscoring its therapeutic breadth and integrative applications in polyherbal formulations. A comprehensive body of literature spanning from 1990 to 2025 has detailed the ethnopharmacological, phytochemical, and pharmacodynamic profiles of C. paniculatus, affirming its relevance as a model species for translational research and integrative therapeutic development.