| Summary: | The species <i>Fissistigma oldhamii</i> (Hemsl.) Merr. (Annonaceae) has long been used as a traditional herbal medicine in China to treat diverse human diseases. Decoctions from the roots of the plant (Guā Fù Mù) are used to treat body pain and inflammatory pathologies, such as rheumatic syndromes, sciatica, and osteoarthritis. The phytochemical content of the plant and the associated pharmacological activities have been analyzed. Seventy natural products were identified in the different parts of the plants, namely, the roots, stems, leaves, fruits, and seeds. The compounds comprise many tri- and tetracyclic alkaloids (aporphine-type), anthraquinones, terpenoids, flavonoids, and others. The pharmacological properties of these molecules were analyzed to point out the anti-inflammatory, antioxidant, anticancer, and/or antimicrobial effects, together with the underlying modulated pathways and molecular targets in some cases. The panel of phytoconstituents present in <i>F. oldhamii</i> extracts is large, with the majority of bioactive products identified in the roots and stems. Multiple molecules can contribute to the anti-inflammatory properties of the extracts. Network pharmacology analyses of the phytoconstituents are needed to better delineate the effective components and their targets.
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