Luteolin, a common flavonoid found in various plants, has been used in traditional Chinese medicine for treating hypertension, inflammatory disorders, and cancer. It exhibits multiple biological effects, including anti-inflammatory, anti-allergic, and anticancer properties. Luteolin functions as both an antioxidant and a pro-oxidant, with its biological effects potentially being functionally related. For instance, its anti-inflammatory activity may be linked to its anticancer function. The anticancer properties of luteolin are associated with apoptosis induction, inhibition of cell proliferation, metastasis, and angiogenesis. Luteolin also sensitizes cancer cells to therapeutic-induced cytotoxicity by suppressing cell survival pathways and stimulating apoptosis pathways. Recent epidemiological studies have attributed a cancer-preventive property to luteolin. This review summarizes recent research on luteolin, focusing on its anticancer role and the underlying molecular mechanisms. Luteolin's anticancer activities include preventing carcinogen metabolic activation, inhibiting cancer cell proliferation, inducing apoptosis, and suppressing angiogenesis and metastasis. In vivo studies in animal models and epidemiological studies in humans support the potential of luteolin as an anticancer agent and chemopreventive agent. However, further preclinical and clinical studies are needed to establish its efficacy and safety.Luteolin, a common flavonoid found in various plants, has been used in traditional Chinese medicine for treating hypertension, inflammatory disorders, and cancer. It exhibits multiple biological effects, including anti-inflammatory, anti-allergic, and anticancer properties. Luteolin functions as both an antioxidant and a pro-oxidant, with its biological effects potentially being functionally related. For instance, its anti-inflammatory activity may be linked to its anticancer function. The anticancer properties of luteolin are associated with apoptosis induction, inhibition of cell proliferation, metastasis, and angiogenesis. Luteolin also sensitizes cancer cells to therapeutic-induced cytotoxicity by suppressing cell survival pathways and stimulating apoptosis pathways. Recent epidemiological studies have attributed a cancer-preventive property to luteolin. This review summarizes recent research on luteolin, focusing on its anticancer role and the underlying molecular mechanisms. Luteolin's anticancer activities include preventing carcinogen metabolic activation, inhibiting cancer cell proliferation, inducing apoptosis, and suppressing angiogenesis and metastasis. In vivo studies in animal models and epidemiological studies in humans support the potential of luteolin as an anticancer agent and chemopreventive agent. However, further preclinical and clinical studies are needed to establish its efficacy and safety.