Kopsia belongs to the family Apocynaceae, which was originally classified as a genus in 1823. Kopsia consists of medicinal plants that can be traditionally used to treat rheumatoid arthritis, pharyngitis, tonsillitis, and dropsy. More than one hundred and twenty-five publications have been documented relating to the phytochemical and pharmacological results, but a systematic review is not available. The goal of this study is to compile almost all of the secondary metabolites from the plants of genus Kopsia, as well as the coverage of their pharmacological research. The document findings were conducted via reliable sources, including Web of Science, Sci-Finder, Science Direct, PubMed, Google Scholar, and publishers, while four words "Kopsia", "monoterpene alkaloids", "Phytochemistry" and "Pharmacology" are key factors to search for references. Most Kopsia secondary metabolites were collected. A total of four hundred and seventy-two, including four hundred and sixty-six monoterpene alkaloids, five triterpenoids, and one sterol, were summarized, along with their resource. Kopsia monoterpene alkaloids presented in various skeletons, but aspidofractinines, eburnamines, and chanofruticosinates are the three major backbones. Mersinines and pauciflorines are new chemical classes of monoterpene alkaloids. With the rich content of monoterpene alkaloids, Kopsia constituents were also the main objects in pharmacological studies since the plant extracts and isolated compounds were proposed for anti-microbial, anti-inflammatory, anti-allergic, anti-diabetic, anti-manic, anti-nociceptive, acetylcholinesterase (AChE) inhibitory, cardiovascular, and vasorelaxant activities, especially cytotoxicity.
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