Plants of genus Paeonia have both medicinal and edible value for a long history. Albiflorin (AF), one of the characteristic monoterpenoid glycosides of Paeonia L. plants, has extensive protective effects in nervous system, cardiovascular and cerebrovascular system, digestive system, endocrine system, skeletal system, and other diseases. AF has demonstrated favorable outcomes in the treatment of depression, neurodegenerative diseases inflammation, oxidative stress, and other related disorders. The aforementioned effects of AF are primarily mediated by the antioxidant activity, modulation of mitochondrial autophagy, regulation of the gut microbiota, and involvement in cell signaling pathways including NF-κB, AMPK, PI3K/Akt, Wnt/β-catenin, and so on. Based on studies over the past several decades, this review systematically summarizes the pharmacological effects of AF to provide an overall understanding of the pharmacological functions of AF and propose valuable insights for future research of AF on food and medicine applications.