Abstract: Gynostemma pentaphyllum, a plant of the Cucurbitaceae family, contains saponins, flavonoids, polysaccharides and other bioactive ingredients and has many bioactivities such as inhibiting tumor, reducing blood fat and blood sugar, antiaging, and protecting cells. Gypenoside, a major active ingredient in G. pentaphyllum, has arisen much attention in recent years, because it contains the same mother nucleus of dammarane-type tetracyclic triterpenoids as ginsenoside. In recent years, modification of the glycosidic moiety of gypenoside by bioconversion for derivatives with improved activity has become a research hotspot, and abundant studies on this topic exist in the literature. However, a systematic review is still lacking. In this context, this paper reviews recent advances in research on the structure and classification of gypenosides, the difference and similarity between gypenosides and ginsenosides, and the biotransformation and bioactivity of gypenosides. Finally, directions for future research are put forward. Hopefully, this review will provide insights for gypenosides biotransformation in vitro.

Key words: Gynostemma pentaphyllum, gypenoside, biotransformation, bioactivities