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Camellia nitidissima
C.W. Chi, honored as “the Queen of Camellia”, has attracted considerable attention as a rare and famous ornamental species characterized by yellow waxy petals. Its flowers and leaves have been used in Chinese folk herbal medicine to treat dysentery, hypertension, diarrhea, faucitis, hepatitis with jaundice, liver cirrhosis, sores, malignant tumors, and irregular menstruation. In recent years, a great number of phytochemical, pharmacological, and toxicity studies on
C. nitidissima
have been carried out, primarily in China. Phytochemical investigations have shown that the plant contains a rich source of bioactive constituents, including flavonoids, polysaccharides, saponins, volatile compounds, and other components such as mineral elements and amino acids. Both in vitro and in vivo pharmacological studies have demonstrated that
C. nitidissima
possesses anticancer, antioxidant, hypolipidemic, hypoglycemic, antiallergic, immunomodulatory, antibacterial, anxiolytic, and antidepressant properties. The present paper presents an up-to-date and comprehensive overview of the botany, processing, chemical constituents, pharmacological effects, and toxicity of
C. nitidissima
in order to provide scientific credence for this traditional medicine while exploring the potential of this plant for drug development.