Gentianaceae

1. Swertianolin (Bellidifolin-8-O-Glucoside), mangiferin, rhodenthoside A-C, isoorientin, isovitexin, and amarogentin would serve as potential chemotaxonomic markers to differentiate Gentianaceae species. 2. Swertianolin and swertiamarin show significant hepatoprotective effect in the liver damage model induced by alpha-naphthylisot hiocyanate. 3. Swertianolin shows anti-acetylcholinesterase activity effects. 4. Swertianolin shows that it can scavenge superoxide and hydroxyl radicals with the studying method of the autoxidation of Pyrogallol and afenton.

Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud. Jolkinolide B induces apoptosis in cancer cells. Jolkinolide B can be used for studies on preventing and treating osteolysis.

1. 6'-O-beta-D-Glucosylgentiopicroside (6'-O-Glucosylgentiopicroside) may have antifungal activity.

1. Sweroside possesses strong hepatoprotective effect. 2. Sweroside is a promising osteoporosis therapeutic natural product, has anti-osteoporotic effect on the human MG-63 cells and rat osteoblasts.

1. Loganic acid (Loganate) and geniposide exhibit both sides effect on superoxide generation.

Swertisin, a novel herbal biomolecule, shows a strong antihyperglycemic action. Swertisin is an adenosine A1 receptor antagonist, is known to have antidiabetic, anti-inflammatory and antioxidant effects.

Orientin-2''-O-p-trans-coumarate, isolated from *Trigonella foenum-graecum*, exhibits antioxidant activity and promotes cell proliferation.

Gentisin is a novel inhibitor of vascular smooth muscle cells (VSMC) proliferation with an IC50 value of 7.84 μM. Gentisin has mutagenic activity.

Swertiamarin (Swertiamaroside) is a common secoiridoid found among the members of Gentianaceae with anti-inflammatory, anticancer, hypoglycemic and hypolipidemic activities.

Amarogentin is mainly extracted from Swertia and Gentiana roots. It plays cemopreventive/therapeutic role during liver carcinogenesis through modulation of cell cycle and apoptosis

Chamaechromone is a natural product isolated from the roots of Stellera chamaejasme L.. Chamaechromone has anti-HBV and insecticidal activity.

Gentiopicroside (Gentiopicrin), a naturally occurring iridoid glycoside, extracted from Gentiana manshurica Kitag, inhibits P450 activity, with an IC50 and a Ki of 61 μM and 22.8 μM for CYP2A6; has antianti-inflammatoryand antioxidative effects.

1. Picfeltarraenin IA (Picfeltarraenin A), IB, IV, X, XI are stronger AChE inhibitions than the known AChE inhibitor Tacrine.

Gentiakochianin (Swertianine), an anthrone from Gentianaceae, has vasodilatory activity, induces glioma cell cycle arrest in the G(2)/M phase and inhibits proliferation, significantly reduces oxLDL-induced cell damage in EA.hy926 cells, inhibits ROS levels and up-regulated the activity of Akt/CREB/eNOS signaling pathway inhibited by oxLDL.

Vitexin 2''-O-p-coumarate (Vitexin2''-O-p-coumarate) is found in fenugreek seeds and promotes 2BS cell proliferation induced by H2O2.

1,3,5,8-Tetrahydroxyxanthone (Desmethylbellidifolin) is a natural xanthone extracted from Gentianella acuta, exhibiting antispasmodic and anti-inflammatory activities. Dimethylbellidifolin shows mutagenicity in Salmonella typhimurium TA100, TA98, TA97, and TA2637 by the preincubation method and significantly inhibits the growth of Staphylococcus aureus at a dose of 200 µg/disk.

Swertiajaponin possesses antimicrobial activity.

Neochamaejasmine B displays nematicidal activity against both Bursaphelenchus xylophilus and Bursaphelenchus mucronatus.

Gentianose is a carbohydrate reserve derived from perennial yellow gentian storage roots.

Roburic acid and phenethyl-trans-ferulate inhibit COX-1 and COX-2.

2,5-Dihydroxybenzoic acid (Gentisic acid) is an active metabolite of salicylic acid degradation with a broad spectrum of biological activity, such as anti-inflammatory, antirheumatic and antioxidant properties.

1. Methyl eugenol (4-allylveratrole) is a natural constituent of the essential oils of a number of plants widely used in foodstuffs as flavouring agents, in view of the carcinogenic potential of ME, the need to check its presence in food products with effective analytical methods. 2. Methyleugenol has insecticidal properties. 3. Methyleugenol can inhibit the production of nitric oxide and decreased the protein expression of inducible nitric oxide synthase, it down-regulates the production of pro-inflammatory cytokines in the ischemic brain as well as in immunostimulated mixed glial cells; indicates that methyleugenol could be useful for the treatment of ischemia/inflammation-related diseases. 4. Methyleugenol has cytotoxicity and genotoxicity. 5. Intravenous (i.v.) treatment with methyleugenol (ME) in either anesthetized or conscious rats elicits hypotension, an effect that seems related to an active vascular relaxation rather than withdrawal of sympathetic tone. 6. Methyleugenol has antinociceptive effect on the second phase of formalin-induced pain, may be due to the inhibition of N-methyl-d-aspartic acid (NMDA) receptor-mediated hyperalgesia via GABA(A) receptors. 7. Methyleugenol has elaxant and antispasmodic actions on guinea-pig isolated ileum.

Bellidifolin (Bellidifoline) has anti-oxidation, hepatoprotective, anti-inflammatory and antitumor actions, it may contribute to the protective effects associated with nerve injury initiated by hypoxia by mechanisms related to inhibition of cell apoptosis independent of the ERK pathway. Bellidifolin shows interesting inhibitory activity of monoamine oxidases (MAO) A, it could be useful for treating type-2 diabetes, likely via the improvement of insulin resistance (IR). Bellidifolin also shows an antifungal effect (MIC values of 50 microg/mL).

1. Picfeltarraenin IB and Picfeltarraenin IA displayes no cytotoxic activity in vitro human tumor cell line panel.