Iridoids

Genipin ((+)-Genipin) is a natural crosslinking reagent derived from Gardenia jasminoides Ellis fruits. Genipin inhibits UCP2 (uncoupling protein 2) in cells. Genipin has a variety of bioactivities, including modulation on proteins, antitumor, anti-inflammation, immunosuppression, antithrombosis, and protection of hippocampal neurons. Genipin also can be used for type 2 diabetes research.

Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity. Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase.

Geniposide is an iridoid glucoside extracted from Gardenia jasminoidesEllis fruits; exhibits a varity of biological activities such as anti-diabetic, antioxidative, antiproliferative and neuroprotective activities.

Aucubin is an iridoid glycoside component that acn be found in E. ulmoides. Aucubin can cross the blood-brain barrier (BBB) and has anti-anxiety, antidepressive and anti-neuroinflammatory effects. Aucubin has many biological activities, such as antioxidant, anti-aging, anti-inflammatory, antimicrobial, anti-fibrotic, anti-cancer, hepatoprotective, neuroprotective and osteoprotective effects.

Catalpol (Catalpinoside), an iridoid glycoside found in Rehmannia glutinosa. Catalpol has neuroprotective, hypoglycemic, anti-inflammatory, anti-cancer, anti-spasmodic, anti-oxidant effects and anti-HBV effects.

(±)-rel-Neomenthol is an alcohol component and isomer of (+)-Neomenthol (HY-135286A). (±)-rel-Neomenthol is derived from the essential oils of Mentha arvensis var. piperascens and the Mentha arvensis × Mentha crispa F1 hybrid.

6''-O-trans-Sinapoylgenipin gentiobioside is an iridoid glycoside that can be found in Zhuyeqing Liquor.

Gentiopicroside, a naturally occurring iridoid glycoside, inhibits P450 activity, with an IC₅₀ and a K_i of 61 μM and 22.8 μM for CYP2A6; Gentiopicroside has anti-inflammatoryand antioxidative effects.

Geniposidic acid is an orally active FXR modulator and SIRT6 activator. Geniposidic acid binds to the Ser332 and His447 sites on the FXR ligand-binding domain, thereby driving nuclear translocation, coactivator recruitment, and transcription of downstream bile acid and cholesterol metabolism-related genes. Geniposidic acid improves metabolic dysfunction-related fatty liver disease by activating the SIRT6 signaling pathway. Geniposidic acid inhibits inflammation and modulates gut microbiota to alleviate colitis. Geniposidic acid can be used in research on drug-induced liver injury, inflammatory bowel disease, metabolic dysfunction-related fatty liver disease, and metabolic dysfunction-related steatohepatitis.

Valepotriate can be isolated from Valeriana jatamansi Jones, has anti-epileptic and anti-cancer activities.

Acevaltrate inhibits the Na⁺/K⁺-ATPase activity in the rat kidney and brain hemispheres with IC₅₀s of 22.8 μM and 42.3 μM, respectively.

Picroside II is an antioxidant with oral activity that can reduce the production of ROS and protect the blood-brain barrier (BBB) after CI/R injury, offering neuroprotective effects. Picroside II has antioxidant, immune-regulating, antiviral properties, and inhibits apoptosis. Picroside II alleviates the inflammatory response in sepsis by suppressing the activation of the NLRP3 inflammasome and NF-κB pathways.

Morroniside has neuroprotective effect by inhibiting neuron apoptosis and MMP2/9 expression.

Loganin is a type of iridoid glycoside compound that possesses anti-inflammatory, antioxidant, and antitumor properties, and offers protective effects against acute lung injury and pulmonary fibrosis. Loganin exerts its protective effects against LPS (HY-D1056)-mediated inflammation and oxidative stress by upregulating the Nrf2/HO-1 signaling pathway, and it reduces neuroinflammation caused by spinal cord injury (SCI).

4aα,7α,7aα-Nepetalactone exhibits antibacterial activity, and inhibits Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Salmonella typhi and Enterococcus faecalis.

Harpagoside can be obtained by Harpagophytum procumbens, which has anti-inflammatory, anti-cancer, protective activity, and efficacy. Harpagoside has an inhibitory effect on COX-1 and COX-2 active, and suppresses NO production. Harpagoside inhibits HepG2 cell lipid polysaccharide, which is a protein that is expressed horizontally and selectively, and has anti-inflammatory and latent pain effects. Harpagoside has the ability to protect the body, and has a degenerative effect on the β-oxidation (Aβ).

Rehmannioside D is an orally active Sirt7 modulator. Rehmannioside D upregulates Sirt7 expression, inhibits the level of acetylated p53, and blocks the activation of the p53 signaling pathway. Rehmannioside D alleviates liver injury, inflammatory response, collagen deposition and hepatocyte apoptosis. Rehmannioside D is applicable to research related to liver fibrosis.

Monotropein is an iridoid glycoside that can be isolated from the roots of Morinda officinalis. Monotropein inhibits the expression of inflammatory mediators in dextran sulfate sodium (DSS)-induced colitis mouse model. Monotropein exerts protective effects against IL-1β-induced apoptosis and catabolic responses on osteoarthritis chondrocytes. Monotropein has cartilage protective activity. Monotropein can alleviate Cisplatin (HY-17394)-induced acute kidney injury by inhibiting oxidative damage, inflammation and apoptosis through activation of Nrf2/HO-1 pathway and inhibition of NF-κB signaling. Monotropein can be studied in research for osteoarthritis, acute kidney injury and acute lung injury.

Loganic acid is an iridoid isolated from cornelian cherry fruits. Loganic acid inhibits NF-κB signaling pathway, activates Nrf2 signaling pathway, exhibits anti-inflammatory activity. Loganic acid can modulate diet-induced atherosclerosis and redox status. Loganic acid has strong free radical scavenging activity and remarkable cyto-protective effect against heavy metal mediated toxicity. Loganic acid is orally active.