| Summary: | The <i>Agastache</i> genus is part of the <i>Lamiaceae</i> family and is native to North America, while one species, <i>Agastache rugosa</i> (<i>A. rugosa</i>), is native to East Asia. A review on the phytochemistry and bioactivity of <i>Agastache</i> genus was last performed in 2014. Since then, a lot of progress has been made on the characterization of the phytochemical and pharmacological profiles of <i>Agastache</i> species. Thus, the purpose of this paper is to present a summary of the findings on the phytochemistry and biological effects of several <i>Agastache</i> species, including both extracts and essential oil characterization. We performed a comprehensive search using PubMed and Scopus databases, following PRISMA criteria regarding the study selection process. The available data is focused mainly on the description of the chemical composition and bioactivity of <i>A. rugosa</i>, with fewer reports referring to <i>Agastache mexicana</i> (<i>A. mexicana</i>) and <i>Agastache foeniculum</i> (<i>A. foeniculum</i>). <i>Agastache</i> species are characterized by the dominance of flavonoids and phenolic acids, as well as volatile compounds, particularly phenylpropanoids and monoterpenes. Moreover, a series of pharmacological effects, including antioxidant, cytotoxic, antimicrobial, anti-atherosclerotic, and cardioprotective properties, have been reported for species from the <i>Agastache</i> genus.
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