Melatonin (N-acetyl-5-methoxy-tryptamine) is a hormone taking place in many biological and physiological processes, such as reproduction, sleep, antioxidant effect, and circadian rhythm (biological clock), and is a multifunctional indolamine compound synthesized mainly from the metabolism of tryptophan via serotonin in the pineal gland. Melatonin, which is a hormone synthesized from the essential amino acid tryptophan, is substantially secreted from the pineal gland between the cerebral hemispheres found in the mammalian brain. In addition to this, it is also produced in the cells and tissues, such as the gastrointestinal system, gall, epithelial hair follicles, skin, retina, spleen, testis, salivary glands, bone marrow, leukocytes, placenta, and thrombocytes. It plays a role in many physiological events, such as synchronizing circadian rhythms, reproduction, fattening, molting, hibernation, and change of pigment granules, preserving the integrity of the gastrointestinal system with an anti-ulcerative effect in tissues and organs from which it is produced. Melatonin is also a powerful antioxidant and anti-apoptotic agent that prevents oxidative and nitrosative damage to all macromolecules due to its ability to form in metabolic activities, directly excrete toxic oxygen derivatives, and reduce the formation of reactive oxygen and nitrogen species. In this book chapter, we will explain the structure, synthesis, metabolism, and antioxidant effects of the melatonin hormone.