Gentianaceae

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.

Roburic acid acts as an anti-inflammatory, anti-tumor and osteoclastogenesis inhibitor, with a K_i of 7.066 μM against human TNF, an IC₅₀ of 9 μM against human COX-2, and an IC₅₀ of 5 μM against ovine COX-1. Roburic acid reduces the production of inflammatory mediators such as NO and IL-6 in macrophages by inhibiting the NF-κB and MAPK (p38/JNK) pathways. By competitively inhibiting the TNF-TNF-R1 interaction, Roburic acid blocks the downstream NF-κB signaling pathway, thereby inducing cell cycle arrest and apoptosis in cancer cells. Roburic acid specifically inhibits osteoclastogenesis and bone resorption by suppressing the RANKL/TRAF6/NF-κB/NFATc1 axis. Roburic acid can be used in research related to osteolytic diseases such as osteoporosis, colorectal cancer and inflammatory diseases.

Amarogentin is a secoiridoid glycoside that is mainly extracted from Swertia and Gentiana roots. Amarogentin exhibits many biological effects, including anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin exerts hepatoprotective and immunomodulatory effects. Amarogentin promotes apoptosis, arrests G2/M cell cycle and downregulates of PI3K/Akt/mTOR signalling pathways. Amarogentin exerts beneficial vasculo-metabolic effect by activating AMPK.

β-Gentiobiose (Gentiobiose) is a natural oligosaccharide. β-Gentiobiose can promote ripening of tomato fruit.

Isoscoparin is a flavonoid that could be isolated from EtOAc extract of Gentiana algida Pall. Isoscoparin possesses antioxidant activity.

Diffutin is a glucosyloxyflavan found in the roots of Hoppea dichotoma and Canscora diffusa. Diffutin produces adaptogenic, anti-stress, anti-anxiety effects. Diffutin can be used for the research of stress/anxiety.

Swertiachoside B (compound 4) is a tetrahydroxanthone glycoside (3-nortetrahydroswertiamarin) that occurs throughout the whole plant of Swertia chirayita.

Protocatechuic acid-2-glucoside (compound 6) is a phenolic acid glycoside. Protocatechuic acid-2-glucoside can be found in the rhizome and radix of Millettia speciosa Champ.

Isogentisin is a cell protector. Isogentisin can shield human umbilical vein endothelial cells (HUVEC) from cell death caused by H₂0₂ and UV exposure. Isogentisin can also prevent endothelial damage triggered by smoking by activating cell repair functions to promote cell survival.

1,3,5,8-Tetrahydroxyxanthone (Desmethylbellidifolin) is a natural xanthone extracted from Swertia chirata. 1,3,5,8-Tetrahydroxyxanthone has antispasmodic effect and anti-inflammatory activity.

Gentianine, an active metabolite of Swertiamarin, has anti-diabetic effect and anti-inflammatory property.

Bellidifolin is an orally active compound with antiproliferative, anti-inflammatory and antioxidant properties. Bellidifolin modulates key signaling pathways including STAT3, PI3K-Akt, mTOR and BRD4, and inhibits the viral protein R (Vpr). Bellidifolin induces cell cycle arrest and apoptosis, exerts significant antifibrotic effects, and protects the heart, liver and nervous system. Bellidifolin is applicable to the research of various diseases such as lung cancer, non-alcoholic fatty liver disease, myocardial hypertrophy and ischemic cranial nerve injury.

6'-O-beta-D-Glucosylgentiopicroside is a secoiridoid isolated from the roots of G. straminea. 6'-O-beta-D-Glucosylgentiopicroside strongly suppresses N-formyl-methionyl-leucyl-phenylalanine (fMLP)-induced superoxide generation.

Amaroswerin is a bioactive secoiridoid glucoside from Swertia mussotii. Amaroswerin has anti-inflammatory, antidiabetic, antiviral, anticholinergic and immunomodulatory activities. Amaroswerin inhibits NO release with an IC₅₀ value of 5.42 μg/mL in RAW264.7 cells.

Norswertianolin acts as a CSE activator and is isolated from G. acuta. Norswertianolin may be a potential agent for cardiovascular diseases.

Norswertianin, a xanthone compound, serves as a powerful anti-glioma compound. Norswertianin induces GBM cells differentiation through oxidative stress and Akt/mTOR dependent autophagy.

Swertianolin is a xanthone glycoside. Swertianolin can be isolated from plants of the Gentianaceae family (e.g., Gentiana campestris and Swertia punicea). Swertianolin inhibits p38 phosphorylation and NF-κB activation, and reduces NO and ROS production. Swertianolin exhibits anti-Helicobacter pylori activity with an IC₅₀ of 6.1 μM and a minimum bactericidal concentration of 91.7 μM. Swertianolin modulates immune function in sepsis. Swertianolin is useful in the research of diseases such as Alzheimer's disease, hepatitis B, Helicobacter pylori infection, and sepsis.

Tetrahydro bellidifolin (Compound 1a) is the aglycone obtained from the hydrolysis of Tetrahydroswertianolin (HY-N18018) by β-glucosidase. Tetrahydro bellidifolin exhibits significant hepatoprotective activity and reduce serum ALT levels. Tetrahydro bellidifolin can be used for the research of liver injury.

1-Hydroxy-3,5-dimethoxyxanthone is a xanthone and Antibacterial agent. 1-Hydroxy-3,5-dimethoxyxanthone can be isolated from Lomatogonium rotatum. 1-Hydroxy-3,5-dimethoxyxanthone inhibits the growth of Pseudomonas aeruginosa ATCC27853 and Escherichia coli ATCC25923 with an MIC of 640 μg/mL. 1-Hydroxy-3,5-dimethoxyxanthone exhibits anticancer activity against cervical cancer, breast cancer, melanoma, liver cancer, and gastric cancer.

Tetrahydroswertianolin (Compound 1) is a tetrahydroxyxanthone glycoside that can be isolated from the whole plant of Swertia japonica Makino. Tetrahydroswertianolin reduces the elevated blood ALT levels in mice with immune-induced liver injury and exhibits protective activity against liver injury. Tetrahydroswertianolin can be used in studies related to anthelmintic, antipyretic and immune-induced liver injury.