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<i>Codonopsis</i>, in the family Campanulaceae, is a genus containing 42 species of dicotyledonous herbaceous perennial plants, predominantly found in Central, East and South Asia. Several <i>Codonopsis</i> species are widely used in traditional medicine and are considered to have multiple medicinal properties. Among the <i>Codonopsis</i> species, <i>Codonopsis pilosula</i> (Franch.) Nannf. and <i>C. lanceolata</i> (Sieb. et Zucc.) Benth. & Hook. f. ex Trautv. are more popular than others according to the findings, especially phytochemical and bioactive studies. Phytochemical research shows that <i>Codonopsis</i> species contain mainly polyacetylenes, phenylpropanoids, alkaloids, triterpenoids and polysaccharides, which contribute to multiple bioactivities. However, the mechanisms of their bioactivities need to be further elucidated. The less popular <i>Codonopsis</i> species remain to be studied and exploited. In addition, although a series of methods for the quality evaluation of <i>Codonopsis</i> species have been developed, a feasible and reliable approach to the efficacious and safe use of various <i>Codonopsis</i> species is still needed, with considering botanical origin, chemical constituents and bioactive effects. This review aims to provide up-to-date and comprehensive information on the phytochemistry, bioactivity and quality control of medicinal plants in the genus <i>Codonopsis</i> and to highlight current gaps in knowledge, which is useful for the wider development of the <i>Codonopsis</i> genus.