pro-inflammatory cytokines

(±)-Lisofylline is an enantiomer-specific, alkyl-substituted methylxanthine, which has specific and potent activity in down-regulating leukocyte activation. (±)-Lisofylline is an anti-inflammatory agent.

7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone) exhibits anti-inflammatory, antibacterial, and antifungal activities, along with moderate antitrypanosomal activity, having an MIC value of 19.0 µg/mL.

Dovramilast (CC-11050) is an orally active phosphodiesterase 4 (PDE4) inhibitor that reduces the production of pro-inflammatory mediators and cytokines. Dovramilast is used in the study of Mycobacterium tuberculosis infections and lupus erythematosus.

3-Hydroxykynurenamine, also known as 3-Hydroxy-L-kynurenamine or 3-HKA, is a biogenic amine produced via an alternative pathway of tryptophan metabolism. In vitro, 3-HKA has an anti-inflammatory profile by inhibiting the IFN-γ mediated STAT1/NF-κΒ pathway in both mouse and human dendritic cells (DCs) with a consequent decrease in the release of pro-inflammatory chemokines and cytokines, most notably TNF, IL-6, and IL12p70. 3-HKA has protective effects in an experimental mouse model of psoriasis by decreasing skin thickness, erythema, scaling and fissuring, reducing TNF, IL-1β, IFN-γ, and IL-17 production, and inhibiting generation of effector CD8+ T cells. Similarly, in a mouse model of nephrotoxic nephritis, besides reducing inflammatory cytokines, 3-HKA improves proteinuria and serum urea nitrogen, overall ameliorating immune-mediated glomerulonephritis and renal dysfunction.This compound is unstable in powder form and other related salt forms are recommended.

Lidocaine (Alphacaine) is an amide local anesthetic with anti-inflammatory properties in vitro and in vivo. It has this functions perhaps due to an attenuation of intracellular adhesion molecule-1 (ICAM-1), pro-inflammatory cytokines, and reduction of neutrophils influx.

Betamethasone disodium phosphate (Betamethasone 21-phosphate disodium salt) is a corticosteroid with anti-inflammatory properties that promotes the polarization of M1 to M2 macrophages by reducing the secretion of pro-inflammatory cytokines, and is utilized in research on keloids and rheumatoid arthritis.

Acetyl-L-carnitine hydrochloride (Acetyl L-carnitine hydrochloride) is a nutritional supplement composed of the hydrochloride salt form of the acetylated form of the endogenously produced L-carnitine, with potential neuroprotective, cognitive-enhancing, anti-depressive and immunomodulating activities. It may also relieve peripheral neuropathy induced by chemotherapy, diabetes or other diseases. In addition, acetyl-L-carnitine may modulate the immune response by increasing T-lymphocytes maturation and may downregulate pro-inflammatory cytokines in response to viruses, such as SARS-CoV-2. It may also disrupt the ACE2 signaling pathway and inhibit the production of reactive oxygen species (ROS).

1. Linalool (Linalol), a natural compound of the essential oils, has been shown to have antinociceptive, antimicrobial, and anti-inflammatory properties. 2. Linalool was protected against LPS/GalN-induced liver injury through induction of antioxidant defense via Nrf2 activating and reduction inflammatory response via NF-κB inhibition. 3. Linalool biosynthesis and accumulation might be involved in plant defense against bacterial and fungal pathogens and be associated with field resistance to citrus canker. 4. Linalool significantly increased the expression of antioxidant enzymes regulated by Nrf-2 and diminished lung tissue levels of several pro-inflammatory cytokines, including tumor necrosis factor α (TNF-α) and interleukin (IL)-6.

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.

ABzOH is a benzoic acid derivative, similar in structure to non-steroidal anti-inflammatory drugs such as aspirin, with anti-inflammatory, anti-tumor and anti-proliferative effects. ABzOH can not only inhibit the expression of tumor necrosis factor-α (TNF-a), interleukin-1β (IL-1β), interleukin-6 (IL-6) and other pro-inflammatory cytokines, but also inhibit breast cancer, lung cancer and pancreatic cancer.

CB2R/FAAH modulator-1, a cannabinoid type 2 receptor (CB2R) agonist, is also a fatty acid amide hydrolase (FAAH) inhibitor (IC50=4 μM) that reduces the production of pro-inflammatory and anti-inflammatory cytokines and is commonly used in inflammation studies. The Kis for CB2R and CB1R are 14.8 nM and 241.3 nM, respectively.

2',3'-cGAMP is an endogenous cyclic dinucleotide (CDN) produced by cGAS (cGAMP synthase) in response to double-stranded DNA in the cytoplasm. It acts as a STING activator and ligand, inducing interferons (IFNs) via the TBK1/IRF3 pathway and pro-inflammatory factors via the NF-κB pathway.

ADU-S100 (MIW815) is a cyclic dinucleotide (CDN) class STING agonist that significantly induces the production of IFN-β and pro-inflammatory cytokines TNF-α, IL-6, and MCP-1, induces TBK1 and IRF3 phosphorylation, and exhibits antitumour activity.

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.

Cucurbitacin E-2-O-glucoside (2-β-glucopyranoside) is a triterpene compound derived from the roots of Citrullus colocynthis that inhibits pro-inflammatory cytokines.

AICAR phosphate (Acadesine phosphate) is an AMPK activator and inhibitor of autophagy, YAP, and mitophagy. It serves as an adenosine analog, regulating glucose and lipid metabolism, and inhibiting the production of pro-inflammatory cytokines and iNOS.

L-798106 (CM9) is a selective and potent prostaglandin-like EP3 receptor antagonist that inhibits EP4, EP1, and EP2 receptors, suppresses levels of pro-inflammatory cytokines in atherosclerosis, and attenuates PGE2-induced cough.

Eucalyptol, a natural monoterpenoid and cyclic ether found in eucalyptus species, effectively controls excessive airway mucus secretion and asthma by inhibiting pro-inflammatory cytokines. It serves as an efficacious treatment for non-purulent sinusitis, reducing inflammation and pain when applied topically, and demonstrating leukemic cell-killing capabilities in vitro.

PG-PS, a composite of streptococcal cell wall peptidoglycans and polysaccharides, exhibits pro-inflammatory and arthritis-inducing properties. This compound is instrumental in creating arthritis models due to its ability to induce inflammation and joint damage. Additionally, PG-PS increases the expression of pro-inflammatory cytokines (TNF-α and IL-1β) and disrupts cellular redox balance.

4 -C18 EGCG is an effective inhibitor of α-amylase and α-glucosidase, with IC50 values of 3.74 μM and 0.81 μM respectively. It inhibits carbohydrate-hydrolyzing enzymes, reducing oxidative stress and inflammation, and demonstrates anti-diabetic activity. Additionally, 4 -C18 EGCG downregulates pro-inflammatory cytokines and exhibits cytotoxicity at 50 μM in primary human peripheral blood mononuclear cells (PBMC), and non-cancerous cell lines 3T3-L1 and HEK 293.

DiABZI-4 is an orally active STING agonist that exhibits broad-spectrum antiviral activity. It functions by activating STING to induce the production of pro-inflammatory cytokines and activation of lymphocytes. This action inhibits the replication of Influenza A virus (IAV), SARS-CoV-2, and Human Rhinovirus (HRV), with an EC50 range of 11.8-199 nM.

Compound 11, a selective PPARδ agonist, demonstrates an EC50 of 20 nM, indicating its high affinity for PPARδ receptors. This compound efficiently reduces levels of nitric oxide (NO), as well as the pro-inflammatory cytokines TNFα and IL-6 in LPS-stimulated RAW264.7 cells via the NF-κB pathway, showcasing its anti-inflammatory properties. Additionally, Compound 11 exhibits remarkable stability in human liver microsomes and plasma. It significantly ameliorates foot edema induced by Carrageenan, displaying favorable pharmacokinetic properties with a bioavailability of approximately 100%.

NOD1 2-IN-1 (Compound 18) is a potent RIPK2 inhibitor, demonstrating an IC50 value of 1.4 nM in the ADP-Glo assay. It blocks the production of pro-inflammatory cytokines by inhibiting the NOD1 NOD2 pathway (IC50 values are 18 nM and 170 nM for NOD1 and NOD2, respectively), thereby reducing inflammatory responses. This compound is utilized in research related to colitis.

NOD1 2-IN-1 (Compound 2) is a potent inhibitor of RIPK2 with an IC50 value of 0.65 nM as determined by the ADP-Glo assay. It selectively inhibits the NOD1 pathway, with an IC50 of 33 nM, effectively blocking the production of pro-inflammatory cytokines and thereby reducing inflammatory responses. This compound has potential applications in the research of colitis.