Abstract: | Genipin and geniposide are iridoids from the fruits of Gardenia jasminoides. Both compounds have a methyl acetate (-COOCH3) group at C4 and a hydroxyl (-OH) group at C10. As an iridoid glucoside with a glucose moiety at C1, geniposide is also known as genipin-1-O-β-D-glucoside. Without the glucose moiety, genipin is an iridoid and the aglycone of geniposide. The -OH group at C1 of genipin is responsible for its cytotoxic effects. Geniposide without the -OH group at C1 lacks the cytotoxic effects. There are more publications on the anti-cancer properties of genipin than geniposide. Studies have reported the potentiation of genipin when used in combination with anti-cancer drugs. The anti-cancer properties of geniposide have been investigated using human intestinal microflora that hydrolyzes geniposide to genipin. Both genipin and geniposide exert anti-proliferative and apoptotic activities via different molecular targets and pathways. Other pharmacological properties of genipin and geniposide include antidepressant, antidiabetic, anti-inflammatory, anti-obesity, anti-thrombotic, hepatoprotective, and neuroprotective activities. Future research on genipin and geniposide is suggested. |