Impaired wound healing leads to infection and tissue necrosis. This has spurred the search for wound healing agents derived from natural and non-natural sources. Although natural products are widely used as lead compounds for the design of therapeutic drugs, few studies have looked for potential wound healing compounds in nature. In this review, we briefly discuss each phase of the wound healing process. Examples of natural and non-natural products with wound healing activities are listed, and the structure-activity relationship of fifty one compounds are described. An understanding of how these compounds exert their activities in biological systems is essential for their future development and application as wound healing agents.