Monika Anna Olszewska

Gaultheria procumbens L. is a medicinal plant whose aerial parts (leaves, stems, and fruits) and methyl salicylate-rich essential oil (wintergreen oil) are used in phytotherapy to treat inflammation, muscular pain, and infection-related disorders. This overview summarises the current knowledge about ethnobotany, phytochemistry, pharmacology, molecular mechanisms, biocompatibility, and traditional use of G. procumbens and the wintergreen oil distilled from different plant organs. Over 70 hydrophilic compounds, including methyl salicylate glycosides, flavonoids, procyanidins, free catechins, caffeoylquinic acids, and simple phenolic acids, have been identified in G. procumbens plant parts. Moreover, aliphatic compounds, triterpene acids, and sterols have been revealed in lipophilic fractions. Furthermore, over 130 volatile compounds have been detected in wintergreen oil with dominating methyl salicylate (96.9–100%). The accumulated research indicates that mainly hydrophilic non-volatiles are responsible for the pharmacological effects of G. procumbens, primarily its potent anti-inflammatory, antioxidant, and photoprotective activity, with mechanisms verified in vitro and ex vivo in cellular and cell-free assays. The biological effectiveness of the dominant methyl salicylate glycoside—gaultherin—has also been confirmed in animals. Wintergreen oil is reported as a potent anti-inflammatory agent exhibiting moderate antioxidant and antimicrobial activity in vitro and significant insecticidal and larvicidal capacity. Together, G. procumbens accumulate a diverse fraction of polyphenols, triterpenes, and volatiles with validated in vitro and ex vivo biological activity but with the absence of in vivo studies, especially clinical trials concerning effective dose determination and toxicological verification and technological research, including drug formulation.