Carissa spinarum L. (Apocynaceae), commonly known as Garna or Jungli Karonda, has a rich history of use in indigenous traditional medicinal systems owing to its tremendous medicinal and nutritional benefits. The present review aims to discuss the traditional uses, ethnopharmacology, bioactive composition, toxicity analysis, and biotechnological applications of Carissa spinarum L. (CS) to identify the gap between current applications and research conducted on this plant. We collected the literature published before December 2022 on the phytochemical composition, pharmacological properties, and biotechnological applications of CS. Literature in English from scientific databases such as Google Scholar, PubMed, ScienceDirect, Springer, and Wiley, along with books on CS, was analyzed and summarized to prepare this review. The plant taxonomy was verified using the “World Flora Online” database (http://www.worldfloraonline.org/). The in vitro and in vivo pharmacological studies on CS revealed its anthelmintic, anticonvulsant, anti-arthritic, anti-inflammatory, antimicrobial, antioxidant, antidiabetic, hepatoprotective, vasorelaxant, antihypertensive, antitumor, wound-healing, anti-venom, and antipyretic effects. Toxicological studies on CS also indicated the absence of any adverse effects even at high doses after oral administration. Although CS showed remarkable therapeutic activities against several diseases—such as diabetes, cancer, inflammation, and hepatitis B virus—there are several drawbacks in previous reports, including the lack of information on the drug dose, standards, controls, and mechanism of action of the extract or the phytocompounds responsible for its activity. Extensive research with proper in vivo or in vitro model systems is required to validate its reported activities.

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