Prostaglandins (PGs) are a group of 20-carbon unsaturated fatty acids derived from arachidonic acid, one of the key components of phospholipids in animal cell membranes. Although PGs were originally named and discovered in the prostate gland of man and sheep, current evidence suggests that PGs are synthesized by nearly all mammalian cells. The biological and pathological functions of these compounds are extremely varied and complicated. This paper will first review the biosynthesis, metabolism, biological and pathological effects, and clinical applications of these naturally occurring substances in living organisms. The possibility that these compounds may mediate the pathophysiological functions of oral diseases is then discussed in detail. Prostaglandins have been demonstrated to be related to the pathogenesis of periodontal diseases, dental cyst, pulpal and periapical pathologies, wound healing, tooth movement, and oral cancers. Studies have shown that anti-inflammatory drugs block the synthesis of PGs, and antagonists competitively inhibit the action of these compounds in the body. The application of PG inhibitors and PG antagonists or analogues for prevention and treatment of oral diseases might thus be a promising research field for future development.