Mangroves are home to various plant species that thrive in challenging environmental conditions, such as high salinity, tidal fluctuations, anaerobic soils, and extreme temperature variations. These stressors may stimulate the production of unique secondary metabolites, which often possess a diverse range of biological activities and potential medicinal applications. Pelliciera rhizophorae(Pellicieraceae) is a mangrove plant endemic to the coasts of Central America. This species has been identified as a prolific producer of bioactive compounds, including pentacyclic triterpenes, flavonols, and dithiolanes. Research has shown that certain pentacyclic triterpenes are potent inhibitors of the enzyme α-glucosidase, exerting their effect through their interaction with the catalytic site, as they are competitive inhibitors of the enzyme, analogous to acarbose (a compound used in the pharmacological market as an α-glucosidase inhibitor). On the other hand, other studies have indicated that these same compounds possess a range of biological activities that are beneficial to human health. Consequently, some bioactive compounds extracted from P. rhizophorae could be useful for generating pharmaceutical and phytopharmaceutical products. This review provides an overview of the bioactive compounds derived from P. rhizophorae, focusing on pentacyclic triterpenes and their significant biological activities related to promoting human health.