Genipin 1-beta-gentiobioside, an iridoid glucoside, is one of the major components in gardenia fruit (“Zhizi” in Chinese) that constitutes several edible pigments. Genipin 1-beta-gentiobioside is also widely applied in many classical compound prescriptions for thousand years in Asia, such as Zhizi-Dahuang decoction for reducing icterus and relaxing bowels, Zhizi-Chi decoction for depression treatment, and Yinchen-Hao decoction for the therapies on jaundice with damp-heat pathogen. As one of the major pharmacodynamic substances, Genipin 1-beta-gentiobioside has valuable biological activities, such as resisting heart failure induced by pentobarbital sodium through enhancing heart inotropy and lowering the preload of heart; attenuating melanogenesis, and releasing cytotoxicities. Moreover, Genipin 1-beta-gentiobioside is also a promising candidate for the treatment of memory dysfunction because of its excellent anti-acetylcholine activity in vitro and antiamnesic effect via increasing the acetylcholine levels in brain.