Structure determination, bitterness evaluation and hepatic gluconeogenesis inhibitory activity of triterpenoids from the Momordica charantia fruit

Triterpenoids are hypoglycemic substances and flavor components of Momordica charantia L., whether their bitterness correlated with hypoglycemic potential remain unknown. Thus, triterpenoids in M. charantia were isolated by phytochemical methods and identified by spectroscopic analysis. The bitterness levels and hypoglycaemic activity of isolated triterpenoids were evaluated by electronic tongue and hepatic gluconeogenesis assay. Eighteen triterpenoids including two new ones, Momordicoside Y and Z, were identified. Among the six identified bitter triterpenoids, karaviloside III, goyaglycoside C, and momordicoside F2 were bitterer than caffeine (P < 0.05), with caffeine equivalent (CE) values of 289.19, 4.32, and 41.24 mg CE/mg, respectively. Momordicoside Y, charantoside C, momordicoside F1, and momordicoside G could inhibit hepatic gluconeogenesis by 23.9%, 36.2%, 33.4%, 34.4% at 40 μM, respectively. These four compounds could interact with active site of phosphoenolpyruvate carboxykinase in molecular docking simulation. No correlation was observed between hepatic gluconeogenesis inhibitory activity and bitterness of triterpenoids.