Persimmon is a delicious fruit, and its leaves are considered a valuable ingredient in food, beverage, pharmaceutical, and cosmetic sectors. Traditionally, persimmon leaves (PL) are used as a functional tea in Asian culture to cure different ailments, and are also incorporated into various food and cosmeceutical products as a functional ingredient. PL mainly contain flavonoids, terpenoids, and polysaccharides, along with other constituents such as carotenoids, organic acids, chlorophylls, vitamin C, and minerals. The major phenolic compounds in PL are proanthocyanidins, quercetin, isoquercetin, catechin, flavonol glucosides, and kaempferol. Meanwhile, ursolic acid, rotungenic acid, barbinervic acid, and uvaol are the principal terpenoids. These compounds demonstrate a wide range of pharmacological activities, including antioxidant, anticancer, antihypertensive, antidiabetic, anti-obesity, anti-tyrosinase, antiallergic, and antiglaucoma properties. This review summarizes the latest information on PL, mainly distribution, traditional uses, industrial potential, and bioactive compounds, as well as their potential action mechanisms in exhibiting biological activities. In addition, the effect of seasonality and geographical locations on the content and function of these biomolecules are discussed.