Review Article

Diverse Pharmacological Activities and Potential Medicinal Benefits of Geniposide

Table 1

Summary of the in vitro and in vivo evidence for the biological activities of geniposide.

Pharmacological effectIn vitro evidenceIn vivo evidence

Anti-Alzheimer’s disease activity [217](i) Neuroprotective effects in neuroblastoma SH-SY5Y cells, N2a neuroblastoma cells, primary hippocampal neurons, BV2 microglia cells, primary cortical neurons, and PC12 cells(i) Inhibits RAGE-mediated signaling, enhances leptin receptor expression, reduces tau phosphorylation, mitochondrial dysfunction and cerebral Aβ peptide level in mice
(ii) Reduced STZ-induced spatial learning deficit, tau phosphorylation, GSK-3β hyperactivity, and neural pathology in rats

Antidiabetic activity and inhibition of diabetic complications [10, 1833](i) Regulates GSIS, antagonizes cell injury, and counteracts lipotoxicity in INS-1 cells
(ii) Regulates GSIS in primary pancreatic β-cells
(iii) Promotes β-cell survival in cultured mouse islets
(iv) Prevents cytotoxicity in INS-1E cells
(v) Suppresses hepatic glucose level in HepG2 cells
(vi) Inhibits cell adhesion in HUVECs
(i) Promotes β-cell regeneration and prevents metabolic disease status in mice
(ii) Modulates blood glucose, insulin, total cholesterol and triglyceride, decreases cerebral Aβ peptide level, and reduces development of diabetic nephropathy in rats

Anti-Parkinson’s disease activity [34, 35](i) Prevents α-synuclein expression in SH-SY5Y cells(i) Enhances growth factor signaling, reduces apoptosis, and inhibits α-synuclein expression in mice

Inhibition of ischemia and reperfusion injury [3643](i) Attenuates inflammatory responses in rat microglial cells and brain microvascular endothelial cells
(ii) Attenuates neuronal cell death in rat hippocampal slice culture
(iii) Increases rat primary cortical neuron viability
(iv) Inhibits myocardial apoptosis in H9c2 cells
(i) Improves learning and memory ability, attenuates postischaemic neurovascular injury, and prevents hepatic injury and microglial cells activation in rats

Hepatoprotective activity [4452](i) Enhances lysosomal activity in HepG2 cells
(ii) Suppresses epithelial-mesenchymal transition in AML12 cells
(i) Prevents liver damage and cholestasis in mice
(ii) Attenuates hepatic steatosis and cholestasis in rats

Anti-inflammatory activity [5368](i) Inhibits inflammation in primary mouse mammary epithelial cells, Caco-2 cells, THP-1 cells, primary mouse macrophages, HEK293 cells, N9 microglial cells, RAW264.7 cells, and HUVECs(i) Inhibits inflammation in rats and mice

Antidepressant-like activity [69, 70](i) Alleviates depression-like behavior in rats and mice

Antioxidant activity [71, 72](i) Increases HO-1 expression in primary hippocampal neurons and PC12 cells

Anti-apoptotic activity [7375](i) Inhibits apoptosis in chondrocytes, primary mouse mammary epithelial cells, and PC12 cells(i) Inhibits apoptosis in mice

Immune-regulatory activity [76, 77](i) Induces regression of atherosclerosis in mice

Antisepsis activity [78, 79](i) Binds and neutralizes LPS in RAW264.7 cells(i) Protects mice challenge with lethal heat-killed E. coli(ii) Neutralizes LPS and decreases serum endotoxin level in mice

Cardioprotective activity [80](i) Inhibits cardiac hypertrophy in mice

Antinociceptive activity [81](i) Produces antinociception during persistent pain in rats

Apoptotic activity [82](i) Induces fibroblast-like synoviocytes apoptosis in rats

Antithrombotic activity [83](i) Inhibits platelet aggregation(i) Inhibits venous thrombosis in mice

Antiviral activity [84](i) Inhibits enterovirus 71 infections

Promelanogenesis activity [85](i) Enhances melanogenesis in human epidermal melanocyte

Antitumoral activity [86](i) Induces the formation of DNA cleavage complex