The plant Rubus species (Rosaceae) mainly contains 19α-hydroxyurane-type triterpenoids (19α-HUT) as bioactive components. Available functional food includes blackberry (the fruit of thornless Rubus sp.), red raspberry (R. idaeus) and black raspberry (R. occidentalis). However, the fruit of R. coreanus, which is used in Korea as a functional food, substitutes black raspberry. Rubi Fructus, which has been traditionally used as an oriental medicinal drug, designates only unripe fruit of R. coreanus but not its ripe fruit which indicates that it needs high content of 19α-HUT as a crude drug. Throughout our experiment, we found that ripe fruits contain very little amount of 19α-HUT when compared to unripe fruits. In addition, various and rich 19α-HUT has been reported from Rubus species. The most common structure of 19α-HUT of Rubus species, euscaphic acid or tormentic acid with 3α-OH or 3β-OH, respectively, can be glycosylated or oxidized to produce a number of 19α-HUTs as euscaphic acid and tormentic acid derivatives and even esterified to form dimeric triterpenoids. In this review, the bioactivity and biosynthetic pathway and chemical characterization of 19α-HUTs found in Rubus species are discussed.