Geniposide is an iridoid glycoside. Geniposide is one of the biologically active ingredients of gardenia fruit. Geniposide exerts protective effects against hepatic steatosis in rats fed with a high fat diet; the underlying mechanism may be associated with its antioxidant actions or regulation of adipocytokine release and expression of peroxisome proliferator-activated receptor-α. Geniposide (10-20 μM) inhibited high glucose (33 mM)-induced adhesion of monocytes to HUVECs in a dose-dependent manner. Geniposide (5-40 μM) also inhibited high glucose-induced expression of VCAM-1 and E-selectin at the gene and protein levels. Furthermore, geniposide (5-20 mM) decreased reactive oxygen species production and prevented IkappaB degradation in the cytoplasm and NF-kappaB translocation from the cytoplasm to the nucleus in HUVECs.
Geniposide exhibits anti-diabetic, antidepressant-like, antioxidative, anti-apoptotic, antiproliferative and neuroprotective activities. Geniposide is an agonist for GLP-1 receptor, it regulates expression of anti-oxidative proteins including HO-1 and Bcl-2 by activating the transcriptor of p90RSK via MAPK signaling pathway in PC12 cells. Geniposide may suppress TGF-β1-induced EMT in hepatic fibrosis by inhibiting the TGFβ/Smad and ERK-mitogen-activated protein kinase (MAPK) signaling pathways.