<p><i>Gymnosporia senegalensis</i> (<i>G. senegalensis</i>) belongs from Celastraceae family. It is a well-known medicinal plant that has long been used in Ayurveda and India’s ancient healthcare system, to treat a variety of ailments. It is a vital source of a wide range of bioactive compounds having a diverse range of chemical structures, and potential therapeutic uses that gained very little attention. The plant extracts have been reported to possess multifaceted biological activities including antibacterial, antifungal, cytotoxic, anti-mycobacterial, antioxidant, anti-inflammatory, antimalarial, antiedematogenic, and antinociceptive activities. Several bioactive compounds pristimerin, β-sitosterol, maytenoic acid, β-amyrin, and lupenone, etc., have been already isolated from this plant. As a result, more research is needed to fully unlock their health benefits to combat human illness, for a more therapeutic utilization, and cost-effective medical benefit. <i>G. senegalensis</i> associated biological activities are collected and presented for the first time in this review. This information is useful to support and validate the large use of various plant parts in folklore medicine. Further knowledge and lay the groundwork for the creation of herbal formulations associated with <i>G. senegalensis</i> that may help combat a variety of illnesses, including cancer.</p>