Prostaglandin Receptor

Rutin (Quercetin 3-O-rutinoside), a flavonoid, has a variety of biological activities including antiallergic, anti-inflammatory, antiproliferative, and anticarcinogenic properties.

Evodiamine (d-Evodiamine) is an alkaloid isolated from the fruit of daylily and has a variety of biological activities including anti-inflammatory, anti-obesity and anti-tumor.

p-Hydroxycinnamic acid (NSC-59260) can inhibit platelet activity, with IC50s of 371 μM, 126 μM for thromboxane B2 production and lipopolysaccharide-induced prostaglandin E2 generation, respectively.

2-Acetylbenzoic acid is more potent than 2-propionyloxybenzoic acid in inhibiting platelet function and platelet prostaglandin (PG) synthesis although the potencies of these agents were comparable in inhibiting prostacyclin (PGI2) synthesis.

Embelin (Embelic acid), isolated from the Japanese Ardisia herb, is an inhibitor of the X-linked inhibitor of apoptosis (IC50: 4.1 uM).

Iloprost (Ciloprost) is a stabilized synthetic analog of prostaglandin I2, an inhibitor of platelet aggregation and vasodilation, used in the study of cardiovascular disease.

Epibetulinic acid has anti-inflammatory activity, it exhibits potent inhibitory effects on NO and prostaglandin E(2) production in mouse macrophages (RAW 264.7) stimulated with bacterial endotoxin.

Taraxasterol (Taraxasterin) is compound with anti-inflammatory activity.

Kdo2-Lipid A ammonium (KLA) is a selective and potent TLR4 agonist, a lipopolysaccharide.Kdo2-Lipid A ammonium induces the release of TNF and PGE2.

Platycodin D may stimulate TNF-α synthesis or inhibit degradation of TNF-α mRNA. Platycodin D (10/30 μM) suppresses prostaglandin E2 production in rat peritoneal macrophages stimulated by the protein kinase C activator 12-O-tetradecanoyl phorbol 13-acetate (TPA). Platycodin D and D3 are useful as expectorant agents in the treatment of various airway diseases, they can increase mucin release from rat and hamster tracheal surface epithelial cell culture and also from intact rat trachea upon nebulization.

MRE-269 (ACT-333679) is an orally available and long-acting prostacyclin receptor agonist prodrug. MRE-269(ACT-333679) is used for the treatment of pulmonary arterial hypertension. MRE-269(ACT-333679) is an active metabolite of Selexipag (S253150).

Sphondin has anticonvulsant, anti-inflammatory, and anti-proliferative activities, it possessed an inhibitory effect on IL-1beta-induced increase in the level of COX-2 protein and PGE(2) release in A549 cells.

7-Demethylsuberosin (7-demethylsuberosin) is a coumarin compound isolated from Angelica gigas Nakai,and has anti-inflammatory activity,and exhibited inhibitory effects on PGE2 production with the IC50 values of 9.42 μM.

Tirucallol is an antiinflammatory agent isolated from Euphorbia lactea.Tirucallol exerts a topical anti-inflammatory effect in vivo, via a mechanism of action related to the neutrophil migration.

Euscaphic acid has anti-diabetic, and anti-inflammatory activities, it inhibits LPS-induced inflammatory responses by interference with the clustering of TRAF6 with IRAK1 and TAK1, resulting in blocking the activation of IKK and MAPKs signal transduction

3-O-Acetyl-α-boswellic acid (α-Boswellic acid acetate) exhibits potent anti-inflammatory activity.

Afzelin (Kaempferol-3-O-rhamnoside) exhibits several cellular activities such as DNA-protective, antibacterial, antioxidant, anti-inflammatory, and UV-absorbing properties, potentially protecting human skin from UVB-induced damage through a combination of UV-absorbing and cellular actions. Afzelin mitigates mitochondrial damage, promotes mitochondrial biogenesis, and reduces levels of mitophagy-related proteins, parkin and PTEN-induced putative kinase 1.

α-Viniferin known as 2-arylbenzofuran flavonoids, that are inhibitors of prostaglandin H2 synthetase. α-Viniferin has anti-Alzheimer's disease, anti-tuberculosis, anti-tumor, anti-inflammation, anti-diabetes and other pharmacological activitie

Bavachromene, an isoprenylated chalcone extractable from Fructus in the family Psoraceae, has estrogenic and antimicrobial activities, and concentration-dependent inhibition of Lipopolysaccharide (LPS)-activated NO and PGE2 production in microglia.

Beta-Hydroxyisovalerylshikonin is an inhibitor of protein-tyrosine kinases such as v-Src and EGFR, and has been shown to induce apoptosis in several human tumor cell lines. Beta-Hydroxyisovalerylshikonin significantly decreased viability of HCT116 cells (IC50 values = 30.9 μg/mL).

Continentalic acid from Aralia continentalis exhibits minimum inhibitory concentrations (MICs) of approximately 8-16 µg/mL against S. aureus, including Methicillin-resistant Staphylococcus aureus (MRSA), Methicillin-susceptible Staphylococcus aureus (MSSA), and standard strains.

Friedelin possesses antioxidant, gastroprotective, anti-diarrhoeal, liver protective, anti-inflammatory, analgesic and antipyretic activities.

Liriodendrin regulates lung inflammation, the phosphorylation of the NF-kB (p65) and expression of vascular endothelial growth factor (VEGF). Liriodendrin has anti-inflammatory, antinociceptive, hypoglycemic activities and plays protective role in sepsis-

6,4'-Dihydroxy-7-methoxyflavanone is a biologically active compound isolated from the heartwood of Dalbergia odorifera T. Chen (Leguminosae) with antioxidant, anti-inflammatory and neuroprotective effects. 6,4'-Dihydroxy-7-methoxyflavanone can be used in studies about the treatment of osteoclastogenic bone diseases such osteoporosis, rheumatoid arthritis and periodontal diseases.