Tripterygium hypoglaucum (Levl.) Hutch (THH) is the source plant of a traditional Chinese medicine named Kunmingshanhaitang, which was first recorded in Compendium of Materia Medica. Like Tripterygium wilfordii Hook f. (TWH), THH is also widely used in the treatment of various autoimmune diseases, such as systemic lupus erythematosus, rheumatoid arthritis and psoriasis. The therapeutic effect of THH is closely related to its special compound composition. By now, about 300 compounds have been isolated and identified from THH, including sesquiterpenoids, diterpenoids, triterpenoids, flavonoids, lignans, alkaloids, fatty acids, steroids and others. Further studies found that many compounds originated from THH showed a wide range of biological activities, such as immunosuppression, anti-inflammatory, antitumor, neuroprotection and the others. It is worth noting that THH belongs to the toxic traditional Chinese medicine, commonly known as gut-break grass. Although there have been a lot of studies on the toxic doses of some extracts or isolated compounds of THH, their mechanism remains unclear. Further study on the structure and function relationship of each active and/or toxic compound, analysis of their unique mechanism of action or toxicity mechanism, and exploration of its detoxification methods and new clinical uses will contribute to its better use for human health. In order to better explore the pharmaceutical potential of THH, this paper systematically reviewed its traditional uses, botany, phytochemistry, pharmacology, pharmacokinetics, toxicology and detoxification, which is convenient for further understanding and research.

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