The genus (Asteraceae/Compositae) comprises 24 species worldwide and has long been utilized in traditional medicine for clearing heat, detoxification, relieving intestinal colic, and treating rheumatoid arthritis, neurasthenia, kidney deficiency, lumbago, and gastrointestinal disorders. Modern pharmacological studies have revealed its diverse bioactivities, including antihypertensive, hypolipidemic, immunomodulatory, neuroprotective, antitumor, hepatoprotective, cardioprotective, anti-inflammatory and anti-influenza effects. However, a comprehensive systematic review integrating its traditional uses, phytochemical metabolites and pharmacological activities is still lacking, which hinders its further development and rational utilization. This study aims to fill the existing research gap by systematically collating and summarizing the traditional medicinal applications, phytochemical compositions, and proven pharmacological activities of species, thereby laying a solid theoretical foundation for the subsequent development, utilization, and in-depth research of this genus. This review aims to systematically summarize the traditional applications, phytochemical profiles, and pharmacological activities of species, provide a theoretical basis for their future development and utilization, and highlight the necessity of further investigations into this valuable genus. This study was primarily conducted through comprehensive literature search and screening. The retrieval sources included ethnobotanical textbooks, peer-reviewed journals, and scientific databases such as PubMed, Web of Science, Scifinder, and Google Scholar. The search terms encompassed the genus , its representative species (e.g., ). Literature screening was based solely on relevance to the focus of the review, with the past 4 decades. species have a centuries-old history of folk medicinal use, with different ethnic groups utilizing various medicinal parts to treat diverse diseases. A total of 217 metabolites have been isolated and identified from Rhaponticum, covering steroids, flavonoids, sesquiterpenoids, thiophenes, triterpenoids, and other classes. Consistent with traditional uses, modern pharmacological studies have confirmed their antihypertensive, hypolipidemic, antitumor, neuroprotective, anti-inflammatory, cardioprotective, hepatoprotective, antimicrobial, and anti-influenza activities. Despite 24 documented species, research has predominantly focused on a limited number of Asian species. The material basis, mechanism of action, and therapeutic efficacy of many species remain unclear, and systematic studies on the bioactive metabolites, pharmacological effects, and toxicological profiles of understudied species are insufficient. Given its traditional medicinal value and proven pharmacological activities, further investigations into understudied species, clarification of the molecular mechanisms of core bioactivities, and supplementation of toxicological data are warranted. This review systematically collates the traditional applications, phytochemical compositions, and modern pharmacological value of , providing a valuable reference for its further development and rational utilization.