Originating in China, tea and tea planting have spread throughout the world since the middle of the Tang dynasty. Now people from 160 countries in the world are accustomed to tea drinking. A brief history of tea's medicinal role in China and its spread to the world are introduced. The effectiveness of tea active components and tea drinking on major human diseases, including cancer, metabolic syndrome, cardiovascular disease, and neurodegenerative diseases, is discussed. Also presented are some related issues, such as the bioavailability of tea active components, the new formulations of tea polyphenols, and the safety for consumers of dietary supplements containing tea polyphenols.