Anti-inflammatory agent 6

Anti-inflammatory agent 6 exhibits anti-inflammatory potential by blocking the phosphorylation of Iκb kinase α/β (IKKα/β), IκBα and nuclear factor kB p65 (NF-κb p65), which are key controllers of inflammation.

Anti-inflammatory agent 64 (compound 4b) demonstrates antioxidant and anti-inflammatory properties, effectively inhibiting IL-6 and TNF-α secretion and reducing paw edema [1] in both in vitro and in vivo studies.

Anti-inflammatory agent 66 (compound 8) is a pterostilbene derivative with anti-inflammatory properties. It inhibits pro-inflammatory cytokines by blocking the LPS-induced NF-κB/MAPK signaling pathway and effectively alleviates DSS-induced acute colitis in mice.

Anti-inflammatory agent 67 (compound 7a) is a dual inhibitor targeting Carbonic Anhydrase and COX-2, and is a sulfonamide derivative of Polmacoxib. It exhibits anti-inflammatory and analgesic properties. The IC50 values for COX-1 and COX-2 are 10.4 μM and 50 nM, respectively. The Ki values for binding to various Carbonic Anhydrase isoforms are 48.3 nM (CA I), 42.2 nM (CA II), 52.3 nM (CA IX), and 13.3 nM (CA XII).

Anti-inflammatory agent 68 (compound 7b) is a dual inhibitor that targets Carbonic Anhydrase and COX-2, and is a sulfonamide derivative of Polmacoxib, exhibiting anti-inflammatory and analgesic properties. The IC50 values of Anti-inflammatory agent 68 for COX-1 and COX-2 are 12.6 μM and 60 nM, respectively. It binds to different Carbonic Anhydrase isoforms with Ki values of 52.6 nM (CA I), 79.1 nM (CA II), 58.1 nM (CA IX), and 17.2 nM (CA XII).

Anti-inflammatory agent 65 (compound 29), a Hederagonic acid derivative, exhibits potent activity by inhibiting nitric oxide (NO) release, nuclear translocation of IRF3 and p65, and disrupting the STING/IRF3/NF-κB signaling pathway, thus attenuating the inflammatory response [1].

Anti-inflammatory agent 63 exhibits potent inhibitory activity (EC50 = 5.33±0.57 μM) against lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW264.7 cells [1].

Anti-inflammatory agent 62 mitigates acetaminophen-induced hepatotoxicity in HepG2 cells by modulating inflammatory and oxidative stress pathways [1].

Compound 5b (Anti-inflammatory agent 61) is a potent anti-inflammatory agent that diminishes TNF-α expression in LPS-induced inflammation within RAW 264.7 cells and mitigates APAP-induced inflammation in HepG2 cells [1].

Anti-inflammatory agent 60 (compound 21) inhibits nitric oxide production, presenting an IC50 of 12.95 μM, and reduces iNOS, phosphorylated p65, and β-catenin expression in a concentration-dependent manner [1].

4-Hydroxy-6-methylcoumarin (4-HMC) is a naturally occurring phenolic compound, a derivative of coumarin, found in a variety of plants, fungi, and bacteria. It has anti-inflammatory and anti-tumor activity.4-HMC is used as a flavoring agent, preservative and antioxidant in the food industry.

Anti-inflammatory agent 42 has anti-inflammatory activity and inhibits the expression of TNF-α and IL-6 in LPS-stimulated macrophages.

Triamcinolone (Aristocort) is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. Upon cell entry, triamcinolone binds to and activates the glucocorticoid receptor, which leads to translocation of the ligand-receptor complex to the nucleus and induces expression of glucocorticoid-responsive genes such as lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both mediators of inflammation. In addition, pro-inflammatory cytokine production, including interleukin (IL)-1and IL-6, and the activation of cytotoxic T-lymphocytes is also inhibited. T-cells are prevented from making IL-2 and proliferating. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis through increasing Ikappa-B expression and curtailing activation of nuclear factor (NF)kappa-B.

Microtubule destabilizing agent-2 (Compound 21) is an orally active and selective anticancer compound targeting microtubule proteins. It disrupts microtubule stability, inhibiting microtubule polymerization. This agent causes human tumor cells to arrest in the G0/G1 phase and induces apoptosis (Apoptosis) through activation of the Caspase cascade pathway. Additionally, it exhibits anti-inflammatory properties, inhibiting the production of TNF-α and IL-6 in vitro. Microtubule destabilizing agent-2 also suppresses tumor growth in xenograft mice.

MAPK-IN-4 (Compound c1) is an orally active anti-inflammatory agent that inhibits the expression and release of pro-inflammatory cytokines IL-6 and TNF-α induced by LPS. It interacts with IRAK4 to exert its anti-inflammatory effects by inhibiting the MAPK pathway.

Anti-inflammatory agent 100 (Compound (+)-4S-23) is an anti-inflammatory compound. It inhibits the MAPK and NF-κB signaling pathways by preventing the phosphorylation of IκB-α and blocking the nuclear translocation of phosphorylated p65. Anti-inflammatory agent 100 also reduces the production of NO (IC50: 0.5 μM) and the secretion of TNF-α, IL-6, and IL-1β.

iNOs-IN-6 is an anti-inflammatory agent known for inhibiting the expression of NF-κB, iNOS, and MAPK with an IC50 ranging from 0.2 to 0.62 μM. Additionally, it decreases the levels of pro-inflammatory mediators, such as IL-6, TNF-α, and IL-1β, with an IC50 ranging from 0.4 to 0.69 μM.

Anti-inflammatory agent 102 (Compound 11a) is an orally effective anti-inflammatory compound. It exerts its effects by inhibiting the activation of the ASK1/p38 MAPKs/NF-κB signaling pathway. This agent displays significant anti-inflammatory activity by suppressing the release of NO, ROS, and inflammatory cytokines such as IL-6, TNF-α, and IL-1β. Anti-inflammatory agent 102 is applicable in research concerning inflammatory diseases, including ulcerative colitis (UC).

Anti-inflammatory agent 74 (B5) is known for its ability to inhibit NO, IL-6, and TNF-α, with IC50 values of 10.88 μM and 4.93 μM for NO and IL-6, respectively. It alleviates acute lung injury (ALI) by modulating inflammatory mediators and inhibiting the MAPK and NF-κB signaling pathways.

MPO-IN-6 (compound ADC) is an electrophilic agent with excellent antioxidant and anti-inflammatory properties. It acts as an inhibitor of myeloperoxidase (MPO), dipeptidyl peptidase-4 (DPP-4), and α-glucosidase (α-GD), with IC50 values of 10 μM, 31.02 μM, and 46.05 μM, respectively. MPO-IN-6 may serve as a potential cardiovascular protective agent.

Anti-inflammatory agent 77 (C12) is a β-cyclopentenedione-derived monocarbonyl curcumin analog and acts as an inhibitor of interleukin-6 (IL-6). It is applicable in research related to wound healing.

Anti-inflammatory agent 76 (Compd 8b) is an anti-inflammatory compound with notable inhibition activities on NO, IL-1β, and IL-6.

Anti-inflammatory agent 88 (compound 6) is a carbazole derivative found in marine Streptomyces with anti-inflammatory properties. It exerts its effects by inhibiting pro-inflammatory factors and enhancing the expression of anti-inflammatory factors within the Myd88/Nf-κB pathway. This compound holds potential for the development of anti-inflammatory drugs.

Picroside I (6'-Cinnamoylcatalpol), a hepatoprotective agent, is reported to be antimicrobial and used against hepatitis B. It has antioxidant, and anti-inflammatory activities, it may be the valuable anti-invasive drug candidates for cancer therapy by suppressing Collagenases and Gelatinases. Picroside I can enhance basic fibroblast growth factor(bFGF)-, staurosporine- or dbc-mitogen-activated protein (MAP)-induced neurite outgrowth from PC12D cells.