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 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.

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.

1, 2, 3, 4, 6-Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) and gallic acid from Pistacia lentiscus have antimutagenic and antioxidant activities. 2. 1, 2, 3, 4, 6-Penta-O-galloyl-beta-D-glucose (PGG) possesses potent anti-proliferative and anti-invasive effects, it also has inhibition of inducible nitric oxide synthase and cyclooxygenase-2 activity. 3. PGG may serve as a model for the development of new types of anti-diabetic and anti-metabolic syndrome therapeutics. 4. 1, 2, 3, 4, 6-Penta- O -galloyl-β- d -glucose has vasodilatory and anti-inflammatory effects, it dilates vascular smooth muscle and suppresses the vascular inflammatory process via endothelium-dependent nitric oxide (NO) cGMP signaling. 5. 1, 2, 3, 4, 6-Penta-O-galloyl-beta-D-glucose can decrease the level of extracellular hepatitis B virus (HBV) (IC5, 1. microg ml) in a dose-dependent manner, it also can reduce the HBsAg level by 25% at a concentration of 4 microg ml; the gallate structure of PGG may play a critical role in the inhibition of anti-HBV activity, suggests that PGG could be a candidate for developing an anti-HBV agent. 6. 1, 2, 3, 4, 6-Penta-O-galloyl-β-D-glucose has anti-parasitic activity, displays an EC5 value of 67 μM, at least 6.6-fold more effective than the standard drug benznidazole against trypomastigote forms of T. cruzi.

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.

Olsalazine-13C6is intended for use as an internal standard for the quantification of olsalazine by GC- or LC-MS. Olsalazine is an orally bioavailable prodrug form of the anti-inflammatory agent 5-aminosalicylic acid that is cleaved by bacterial azo reductases in the gut to generate active 5-ASA.1In vitro, olsalazine increases ion transport in isolated rabbit distal ileum when applied to the luminal side (ED50= 0.3 mM) and stimulates fluid transport in rat jejunum when used at a concentration of 5 mM.2,3Olsalazine (150 mg/kg for 8 days) improves stool consistency and decreases occult and gross bleeding as well as myeloperoxidase (MPO) activity and leukotriene B4levels in colon tissue in a mouse model of acute colitis induced by dextran sulfate .4Olsalazine also inhibits bovine xanthine oxidasein vitro(IC50= 3.4 mg/L) and lowers serum uric acid levels in a mouse model of hyperuricemia induced by oxonic acid when administered at a dose of 20 mg/kg.5Formulations containing olsalazine have been used in the treatment of inflammatory bowel disease (IBD) and ulcerative colitis. 1.Nugent, S.G., Kumar, D., Rampton, D.S., et al.Intestinal luminal pH in inflammatory bowel disease: Possible determinants and implications for therapy with aminosalicylates and other drugsGut48(4)571-577(2001) 2.Pamukcu, R., Hanauer, S.B., and Chang, E.B.Effect of disodium azodisalicylate on electrolyte transport in rabbit ileum and colon in vitro. Comparison with sulfasalazine and 5-aminosalicylic acidGastroenterology95(4)975-981(1988) 3.Mohsen, A.Q.M., Mulvey, D., Priddle, J.D., et al.Effects of olsalazine in the jejunum of the ratGut28(3)346-352(1987) 4.Murthy, S., Murthy, N.S., Coppola, D., et al.The efficacy of BAY y 1015 in dextran sulfate model of mouse colitisInflamm. Res.46(6)224-233(1997) 5.Niu, Y., Li, H., Gao, L., et al.Old drug, new indication: Olsalazine sodium reduced serum uric acid levels in mice via inhibiting xanthine oxidoreductase activityJ. Pharmacol. Sci.135(3)114-120(2017)

1. (+)-(3R,8S)-Falcarindiol is a potential new anticancer agent that exerts its activity through inducing ER stress and apoptosis. 2. Falcarindiol induces immunosuppressive effects in vitro and in vivo and might be a novel therapy for autoimmune or allergic diseases. 3. Falcarindiol has protective effect against CCl(4) toxicity , in part, be explained by anti-lipid peroxidation activity associated with the induction of the GSTs including GSTA4.

NF-κB-IN-6 (Compound 3d) is an anti-inflammatory agent that suppresses the NF-κB signaling pathway, thereby reducing iNOS and COX-2 protein expression. It inhibits NO production in LPS-induced RAW264.7 cells with an IC50 of 23.1 μM[1].

Anti-inflammatory agent 17 an orally active anti-inflammatory agent, demonstrates potent efficacy in inhibiting the release of IL-6 and TNF-α without causing cytotoxicity in in vitro experiments. Furthermore, in vivo studies confirm its anti-inflammatory activity. Given its attributes, Compound 17 holds promise for investigating Acute lung injury (ALI) [1].

Anti-Aβ agent 1A is a potent anti-amyloid-β agent. Anti-Aβ agent 1A significantly inhibits LPS-induced IL-1β, IL-6 and TNF-α levels and reduces H2O2-induced apoptosis in SH-SY5Y cells using the mitochondrial pathway, exhibiting antioxidant, anti-inflammatory, anti-Aβ toxicity and neuroprotective activities. Anti-Aβ agent 1A can be used to study Alzheimer's disease.

Anti-inflammatory agent 36 is an anti-inflammatory agent that exhibited dose-dependent inhibition of LPS-induced release of TNF-a and IL-6 in active RAW 264.7 mouse macrophages (IC50 = 3.69 μM and 3.68 μM, respectively).

1. Neobavaisoflavone is isolated as a DNA polymerase inhibitor. 2. Neobavaisoflavone might be a potential anabolic agent to treat bone loss-associated diseases. 3. Neobavaisoflavone has anti-inflammatory activity, can significantly inhibit the production

6-trans-12-epi-Leukotriene B4, a metabolite of arachidonic acid, acts as a potent anti-inflammatory agent.

Antimicrobial Agent-6, exhibiting a minimum inhibitory concentration (MIC) range of 4-8 μg mL, is effective against both gram-positive and gram-negative bacteria. Additionally, it demonstrates anti-inflammatory properties.

Anti-inflammatory agent 50 (compound a1), a derivative of Fusidic acid, exerts its effects through inhibition of inflammatory mediators including NO, IL-6, and TNF-α. It mitigates acute lung injury by modulating these mediators and suppressing the MAPK, NF-κB, and NLRP3 inflammasome signaling pathways [1].

Anti-inflammatory agent 54 (compound 9c), a Coixol derivative, exhibits anti-inflammatory properties by inhibiting the NF-κB pathway and reducing the expression of pro-inflammatory cytokines such as iNOS, TNF-α, IL-6, and IL-1β. It effectively suppresses LPS-induced nitric oxide (NO) production in RAW264.7 macrophages with an IC50 of 2.4 μM and demonstrates in vivo efficacy in a mouse auricular edema model [1].