From traditional herb to modern therapeutics: phytochemistry, pharmacology, toxicology, and clinical translation challenges of Cyperus rotundus L

Cyperus rotundus L. (C. rotundus.), widely distributed in tropical and temperate regions, is a perennial herb with a long history of application in traditional medical systems for treating emotional disturbances, digestive disorders, and gynecological diseases. Despite its extensive traditional use, a systematic integration of its modern phytochemistry and pharmacology is essential for its further development. This review summarizes the research progress over the past decade regarding the chemical constituents, pharmacological mechanisms, and toxicological profile of C. rotundus. Phytochemical investigations have revealed a diverse array of bioactive compounds, primarily volatile oils (e.g., α-cyperone, cyperotundone) and non-volatile constituents such as flavonoids and phenolic acids. Pharmacological studies have corroborated its broad therapeutic potential, demonstrating significant antitumor, antidepressant, anti-inflammatory, antioxidant, and reproductive-regulating activities. Toxicological assessments indicate that aqueous and ethanolic extracts possess a favorable safety profile with high LD50 values, although systematic clinical safety data remain limited. Finally, future perspectives are proposed to facilitate the clinical translation of this herb, emphasizing the importance of standardized quality control, structure-activity relationship (SAR) elucidation, nanotechnology-based delivery, and rigorous randomized controlled trials (RCTs).