Ardisia Crenata Radix is a traditional Chinese medicinal plant that belongs to the Myrsinaceae family, and its main active components are coumarins, saponins, flavonoids, and volatile oil. Bergenin, ardisicrenoside A, ardisicrenoside B, ardisiacripin A, ardisiacripin B, and embelin were identified as active anticancer compounds in in-depth studies into the anti-tumor effects of Ardisia Crenata Radix. They show high therapeutic potential in oral cancer, nasopharyngeal carcinoma, liver cancer, colon cancer, bladder cancer, cervical cancer, and leukemia, mainly by inducing tumor cell apoptosis, increasing tumor cytotoxicity, inhibiting cell proliferation, inhibiting tumor cell metastasis and migration, and inducing cell regulatory enzyme cascade reactions. However, most preclinical experimental data on cinnabar root’s anti-tumor mechanism have not been verified in high-quality, multi-sample, and repeated randomized controlled trials, and there are a lack of clinical research data on tumor prognosis, pharmacodynamics, and pharmacokinetics. Accurate research experiments and clinical trials should be designed to further explore the pharmacological effects of Ardisia Crenata Radix.