Monotropitoside (gaultherin) is a natural plant-extracted salicylate derivative that can be used as a natural aspirin substitute. Gaultherin is the major constituent of salicylate derivatives fraction (SDF) isolated from Gaultheria yunnanensis, medicinal plant widely used in Chinese traditional medicine for the treatments of rheumatoid arthritis, swellings, pain, trauma, chronic tracheitis, cold and vertigo. In animal studies gaultherin showed to be a potent inhibitor of pain and acute inflammation like non-steroidal anti-inflammatory drugs (NSAIDs). Gaultherin demonstrated analgesic and anti-inflammatory effects in rodents lacking gastric ulcerogenic effect compared to aspirin exhibiting the peripheral analgesic properties rather than central analgesic effects. The study of gaultherin metabolism in mice and rats indicated that gaultherin could be metabolically converted to salicylate, which produced the pharmacological effects, and provided effective concentrations for an extended period. In vitro metabolism experiments demonstrated that gaultherin was metabolized by beta-glycosidase produced by human intestinal bacteria and esterases in intestine, blood and liver successively to release salicylate. Gaultherin, has a similar chemical structure to aspirin which suggests that gaultherin or some active metabolites could inhibit cyclooxygenase activity.