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The present paper aims to provide an up-to-date review at the advancements of the investigations on the ethnopharmacology, phytochemistry, pharmacological effect and toxicity of Fuzi.Besides, the possible tendency and perspective for future research of this plant are discussed, as well.All available information on Fuzi was collected via electronic search (using Elsevier, PubMed, ACS, CNKI, Google Scholar, Baidu Scholar, and Web of Science), books and classic works about Chinese herb.122 chemical constituents, among which C19-diterpenoid alkaloids and C20-diterpenoid alkaloids are the predominant groups, have been isolated and identified from Fuzi.Fuzi with its active compounds is possessed of wide-reaching biological activities, including effects on cardiovascular system, anti-inflammation and analgesic action, anti-tumor activity, effect on the immune system, hypoglycemic and hypolipidemic effects, anti-aging effect, effect of protecting kidney and effect on energy metabolism.Nearly all of compounds were found from the roots of the plant, so further phytochemical studies should focus more on the other parts of the plant, such as the leaves, flowers or stems.Besides, a majority of the pharmacological studies were carried out using crude and poorly characterized extracts.Thus, more bioactive components particularly cardiotonic and analgesic compounds should be identified through bioactivity-guided isolation strategies.Moreover, investigations on how to develop Fuzi's new clinical usage on the basis of its pharmacological effects are in requirement.