Diseases, such as cancer, peptic ulcers, and diabetes, as well as those caused by drug-resistant infectious agents are examples of some of the world’s major public health problems. Amphipterygium adstringens (Schltdl.) Schiede ex Standl is an endemic tree to Mexico. Its stem bark has been used medicinally since pre-Hispanic times, but in recent decades it has been scientifically proven that it has properties that help counteract some diseases; extracts with organic solvents of the plant are outstanding for their anticancer, gastroprotective, and antimicrobial properties; terpenes and long-chain phenols have been identified as the main active compounds. Currently, overharvesting is causing a sharp reduction in natural populations due to an increase in demand for the stem bark by people seeking to improve their health and by national and transnational companies seeking to market it. Because of the growing interest of the world population and the scientific community, we reviewed recent studies on the bioactive properties of A. adstringens. Through the orderly and critical compendium of the current knowledge of A. adstringens, we provide a reference for future studies aimed at the rational use and protection of this valuable endemic natural resource.