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Kansui, the root of Euphorbia kansui T.N. Liou ex T.P. Wang, is a well-known traditional Chinese medicine. This paper reviews advances in investigations of the botany, the phytochemistry, the analytical method, the pharmacology and the toxicology of kansui. Nearly 100 compounds have been isolated from kansui and identified, and diterpenes and triterpenes are considered to be the characteristic and bio-active constituents of kansui. They possess multiple pharmacological activities, including diuretic, purgation, and antitumor effects. However, they also have a degree of toxicity, and can cause skin, oral, and gastrointestinal irritation. In this paper, the toxicity-efficacy relationship, attenuation and incompatibility of kansui are further discussed. Several future investigations of kansui are also proposed, all of which would improve the identification of kansui and other toxic herbs, as well as further their utilization.