Tangeretin is a polymethoxy flavonoid found in citrus fruits. This compound exhibits a wide variety of health-related benefits, including anti-inflammatory, anti-allergic, anti-diabetic, anti-osteoporotic, and anticancer activities. In an in vivo model of skin-based allergic reaction, administration of tangeretin inhibits expression of IL-4 and TNF-α as well as inhibiting activation of NF-kB, AP-1, and p38. In both in vitro and in vivo models of diabetes mellitus, tangeretin increases AMPK phosphorylation and glucose uptake and alters secretion of adipocytokines such as leptin, adiponectin, resistin, IL-6, and MCP-1. Additionally, this compound induces cell cycle arrest and inhibited proliferation of breast cancer and colon cancer cells. Tangeretin also inhibits osteoclast formation, suggesting potential benefit as a treatment for bone diseases.