Cyperaceae are a plant family of grass‐like monocots, comprising 5600 species with a cosmopolitan distribution in temperate and tropical regions. Phytochemically,Cyperusis one of the most promising health supplementing genera of the Cyperaceae family, housing ≈950 species, withCyperus rotundusL. being the most reported species in pharmacological studies. The traditional uses ofCyperusspp. have been reported against various diseases,viz., gastrointestinal and respiratory affections, blood disorders, menstrual irregularities, and inflammatory diseases.Cyperusspp. are known to contain a plethora of bioactive compounds such asα‐cyperone,α‐corymbolol,α‐pinene, caryophyllene oxide, cyperotundone, germacrene D, mustakone, and zierone, which impart pharmacological properties to its extract. Therefore,Cyperussp. extracts were preclinically studied and reported to possess antioxidant, anti‐inflammatory, antimicrobial, anticancer, neuroprotective, antidepressive, antiarthritic, antiobesity, vasodilator, spasmolytic, bronchodilator, and estrogenic biofunctionalities. Nonetheless, conclusive evidence is still sparse regarding its clinical applications on human diseases. Further studies focused on toxicity data and risk assessment are needed to elucidate its safe and effective application. Moreover, detailed structure‐activity studies also need time to explore the candidature ofCyperus‐derived phytochemicals as upcoming drugs in pharmaceuticals.