Pedunculagin is a widely abundant ellagitannin found in the plant kingdom, with a chemical structure featuring two hexahydroxydiphenoyl units linked to a glucose core. It has demonstrated various biological activities, including anti-cancer, anti-inflammatory, and anti-bacterial effects. This review aims to summarize the bioactivities, chemistry, and health-promoting properties of pedunculagin and plant preparations containing it. It is the first comprehensive summary covering pedunculagin’s chemistry, sources, metabolism, and other relevant research. The search databases were Google Scholar, EBSCO Discovery Service, REAXYS Database, SCILIT, SCOPUS, PubMed, MEDLINE, Web of Science, Wiley Online Library, Science Direct/ELSEVIER, WordCat, and Taylor and Francis Online. All the databases were methodically searched for data published from 1911 until 2024. Various biological effects were proven in vitro for pedunculagin; however, due to the limited availability of the isolated compound, they have not been so far directly confirmed on more advanced in vivo and clinical models. However, its bioactivity can be deduced from studies conducted for plant preparations containing this ellagitannin as a dominant constituent, consequently indicating beneficial health effects. Further studies are needed to determine the molecular mechanism of action following topical application as well as the contribution of gut microbiota postbiotic metabolites– urolithins–being formed following the oral ingestion of preparations containing pedunculagin.