anti-inflammatory effect

Flunixin meglumine (Banamine) is an effective inhibitor of the enzyme cyclooxygenase with anti-inflammatory and antipyretic activity.

GW9662 (TIMTEC-BB SBB006523) is a PPARγ antagonist (IC50=3.3 nM) with selectivity. GW9662 can be used to study the pathogenesis of metabolic diseases, such as obesity and diabetes, by inhibiting the activity of PPARγ. GW9662 can be used to study the pathogenesis of inflammatory diseases, such as atherosclerosis and rheumatoid arthritis. GW9662 has anti-tumor effect.

Gallic acid (Benzoic acid) is found in almost all plants. Plants known for their high gallic acid content include gallnuts,grapes,tea,hops and oak bark.

Desonide (Prednacinolone) is a synthetic glucocorticosteroid for topical use, with anti-inflammatory activity. Desonide binds to glucocorticoid receptors in the cytoplasm, and the ligand-receptor complex is translocated as a homodimer into the nucleus, where transcription activation via glucocorticoid response elements within glucocorticoid-responsive genes occur. This agent induces transcription of genes coding for anti-inflammatory proteins, including lipocortin-1, interleukin-10, interleukin-1 receptor antagonist and neutral endopeptidase. Increased synthesis of lipocortin-1 has an inhibitory effect on phospholipase A2, which in turn inhibits the release of arachidonic acid, thereby controlling the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.

Bornyl acetate (Isobornyl acetate) has an anti-inflammatory effect. It is the volatile ingredient in some Chinese traditional herbs and numerous conifer oils.

Methyl 3,4-dihydroxybenzoate (Protocatechuic acid methyl ester), a key metabolite of antioxidant polyphenols in green tea, exhibits significant antioxidant and anti-inflammatory properties.

Clobetasol propionate (CGP9555) exerts its effect by binding to cytoplasmic glucocorticoid receptors and subsequently activates glucocorticoid receptor-mediated gene expression. This results in the synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators. Clobetasol Propionate is the propionate salt form of clobetasol, a topical synthetic corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictive properties. Specifically, clobetasol propionate appears to induce phospholipase A2 inhibitory proteins, thereby controlling the release of the inflammatory precursor arachidonic acid from membrane phospholipids by phospholipase A2.

Allicin exerts antioxidant, bactericidal, anti-cancer, anti-inflammatory activities, it exerts an inhibitory immunomodulatory effect on intestinal epithelial cells. Allicin could significantly inhibit vascular smooth muscle cells' proliferation and migration induced by insulin, which may be related to the inhibition of the activation of ERK signal path. Allicin is beneficial in reducing blood cholesterol, triglycerides levels and systolic blood pressure in hypercholesterolemic rats, it may beneficially affect two risk factors for atherosclerosis-hyperlipidemia and hypertension.

Glabridin (KB-289522) may serve as an anti-inflammatory agent in diabetes-related vascular dysfunction, through regulating the synthesis and activity of iNOS under high-glucose levels; may possess a therapeutic effect on metabolic disorders( such as diabetes and hyperglycemia), by modulating glucose metabolism through AMPK in skeletal muscle cells. Glabridin may have potential as a chemopreventive agent against liver Y metastasis, by inhibiting the invasion of human HCC cells.

Gallic Acid Monohydrate (3,4,5-Trihydroxybenzoic acid Monohydrate) is a hydrate of Gallic Acid, a natural polyhydroxyphenol, which inhibits the free radical scavenging effect of COX-2, and possesses a variety of physiological activities such as antioxidant, anti-inflammatory, anti-tumor, and antibacterial.

Nerolidol acetate is a natural sesquiterpene with anti-cancer, anti-inflammatory, antibacterial and anti-insect activities. Nerolidol acetate can inhibit parasite activity and inhibit schistosomiasis, nematodes, malaria, etc. Nerolidol acetate protects cells from oxidative damage to lipids, proteins and DNA, and has a protective effect on mouse hippocampal nerve cells.

Ralimetinib is a selective inhibitor that blocks phosphorylation of MK2 at Thr334, without affecting the phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc. Ralimetinib functions as an ATP-competitive inhibitor of p38 MAPK α/β, demonstrating IC50 values of 5.3 and 3.2 nM, respectively, and is under investigation as an anti-inflammatory and anticancer therapeutic.

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).

Medrysone (6α-Methyl-11β-hydroxyprogesterone) is a topical, synthetic glucocorticoid with metabolic, anti-inflammatory and anti-allergic properties. Medrysone exerts its effect by interacting with specific intracellular glucocorticoid receptors and subsequently binds to DNA to modify gene expression. This results in an induction of the synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators. Consequently, an overall reduction in chronic inflammation and autoimmune reactions is accomplished.

Ankaflavin is isolated from Monascus-Fermented red rice and is a PPARγ agonist with anti-inflammatory activity. It shows the selective cytotoxic effect and induces cell death on cancer cells.

Asatone, an active component isolated from Radix et Rhizoma Asari, has an anti-inflammatory effect via activation of NF-κB and downregulation of p-MAPK (ERK, JNK, and p38) pathways.

Asparagusic acid is unique to asparagus. It is responsible for the odorous urine excreted after eating asparagus. Its derivatives ihydroasparagusic acid have an anti-inflammatory effect.

Beclomethasone 17-propionate is a glucocorticoid that is the active metabolite of Beclomethasone dipropionate (BDP). As a glucocorticoid receptor (GR) agonist, 17-BMP has a 13-fold higher affinity than BDP and inhibits the production of pro-inflammatory cytokines, such as CXCL8, TNF-α, and IL-6, thus exerting an anti-inflammatory effect, and it is mainly used in the treatment of asthma and allergic rhinitis.

hDHODH-IN-1 is a human dihydroorotate dehydrogenase (hDHODH) inhibitor exhibiting anti-inflammatory properties.

J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect. J-113863 is a potent and selective CCR1 (CD18) antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively.

Pyrrolifene is an agent with anti-inflammatory effect.

SB-657510 is a urotensin II (UII) receptor (UT) antagonist. The Ki values of UT for human, monkey, cat, rat and mouse were 61, 17, 30, 65 and 56 nM, respectively. SB-657510 plays an anti-inflammatory role by inhibiting UII-induced inflammatory mediators, such as adhesion molecules, in human vascular endothelial cells and upregulation of cytokines and tissue factors. SB 657510 has a therapeutic effect on diabetes-related atherosclerotic disease in diabetic mouse models.

α-Amyrin acetate is a natural product( triterpeno), with anti-inflammatory activity, antispasmodic profile and the relaxant effect.

2-(Phosphonooxy)benzoic acid (Fosfosal), used as the anti-inflammatory agent, has the anti-bacterial effect.