Isodon amethystoides (Benth. ) Hara, a traditional folk medicinal plant of the genus Isodon in the Lamiaceae family, is widely distributed across southern and central China. Its stems, leaves and rhizomes are used medicinally, with the effects of clearing heat and promoting diuresis, invigorating blood circulation to resolve stasis, detoxification and detumescence. It is traditionally applied in folk medicine for the treatment of sore throat, wind-damp arthralgia, traumatic injuries, venomous snake bites and other ailments. Notably, Weifuchun Capsules, a proprietary Chinese medicine with its rhizome as the key medicinal ingredient, has been approved for the clinical treatment of gastric precancerous lesions, fully highlighting its prominent medicinal value. Modern phytochemical studies have demonstrated that I. amethystoides contains a diverse array of chemical components, including diterpenoids, triterpenoids, sterols, sesquiterpenoids, lignans and fatty acids. Among them, diterpenoids, as the core characteristic active constituents of this plant, have garnered extensive attention from the academic community. This is attributed to their diverse skeleton types, abundant novel structures, and remarkable pharmacological activities covering antitumor, anti-inflammatory, antibacterial, antiviral and immunomodulatory effects. Herein, we systematically review the research advances in the chemical constituents and pharmacological activities of I. amethystoides, aiming to provide a scientific reference for the further in-depth development and rational utilization of this medicinal plant in the pharmaceutical and healthcare fields.