(lps)-induced

Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist and IL receptor modulator with anti-inflammatory and immunosuppressive properties that induces autophagy and inhibits LPS-induced inflammatory responses in macrophages.

NSC-37445 has anti-tumor activity, such as inhibits growth of bladder tumor cells in a nude mice model , prevents the recurrence and progression of non-muscle-invasive urothelial cell carcinoma. NSC-37445 can significantly reduce the expression of CDK1-inhibitory kinases, Myt1 and Wee1, and cause cyclin B1 protein accumulation leading to CDK1 activation in T24 cells. 3. Flavokawain A (Flavokavain A) may exert anti-inflammatory responses by suppressing LPS-induced expression of pro-inflammatory mediators via blockage of NF-κB-AP-1-JNK p38 MAPK signaling pathways in the murine macrophages.

Dexamethasone acetate (NSC 39471) is the acetate salt form of Dexamethasone, a synthetic adrenal corticosteroid with potent anti-inflammatory properties. In addition to binding to specific nuclear steroid receptors, dexamethasone also interferes with NF-kB activation and apoptotic pathways. This agent lacks the salt-retaining properties of other related adrenal hormones.

Sesamol (1,3-Benzodioxol-5-ol) could decrease lung inflammation and lipopolysaccharide (LPS)-induced lung injury in rats. Sesamol ameliorates inflammatory and oxidative damage by upregulating AMPK activation and Nrf2 signaling and blocking the NF-κB and MAPK signaling pathways and inhibits melanin biosynthesis by down-regulating tyrosinase activity and melanin production via regulation of gene expression of melanogenesis-related proteins through modulation of MITF activity, which promotes phosphorylation of p38 and JNK in melan-a cells.

5,6-Benzoflavone (β-Naphthoflavone) is an exogenous ligand for the aryl hydrocarbon receptor, which disrupts zinc homeostasis in human hepatocellular carcinoma HepG2 cells. 5,6-Benzoflavone (β-Naphthoflavone) possesses anti-inflammatory and antioxidant activities, inhibits LPS-induced inflammation through the AKT Nrf-2 HO-1-NF-kappaB signaling axis, inhibits TNF-α-induced ICAM-1 and VCAM-1 expression, which can be used to study neurodegenerative diseases.

(-)-Epigallocatechin Gallate (EGCG) is a phenolic antioxidant polyphenol flavonoid found in plants such as green and black tea, which inhibits telomerase and DNA methyltransferase, blocks the activation of EGF receptors and HER-2 receptors, inhibits cellular oxidation, and prevents free radical damage to cells.

Geranylgeraniol (FT0626663) is an isoprenoid found in fruits, vegetables, and grains, including rice. Geranylgeraniol (FT0626663) inhibits growth and induces apoptosis of various tumor cells. Geranylgeraniol (FT0626663) protects monocytes against statin-induced cytotoxicity and suppresses the growth of Mycobacterium.

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.

Menthone has anti-inflammary activity,, it can suppress the lipopolysaccharide (LPS)-induced proinflammatory cytokines, interleukin-1beta (IL-1beta) and tumor necrosis factor-alpha (TNF-alpha),as well as nuclear factor kappaB (NF-kB).

Lobeglitazone Sulfate（CKD-501 Sulfate） is a novel thiazolidinedione with anti-inflammatory activity that inhibits LPS-induced NLRP3 inflammasome activation and hepatic inflammation, and can be used in the study of type 2 diabetes mellitus (T2DM).

LCB 03-0110 Dihydrochloride is a potent inhibitor of the c-Src kinase (IC50 = 1.3 nM) and tyrosine kinases in the BTK and SYK family, as well as in the DDR2 family. It inhibits LPS-induced activation of macrophages and TGF-β1-induced activation of fibroblasts in vitro, inhibits activation of macrophages and fibroblasts, and inhibits scarring in wound healing models.

4-methoxylonchocarpin was isolated from the roots of Abrus precatorius as a potent anti-inflammatory compound. 4-methoxylonchocarpin inhibited NF-κB-activated TNF expression by inhibiting the binding of LPS to TLR4 in macrophages and suppressed TNBS-induced colitis in mice.

MSC 2032964A is a potent selective ASK1 inhibitor (IC50 = 93 nM) that is oral bioavailable and brain permeable. It inhibited neuroinflammation in mouse EAE models and blocked LPS-induced phosphorylation of ASK1 and p38 in cultured mouse astrocytes.

Adenosine N1-oxide (1-Oxoadenosine), which is found in royal jelly, inhibited the secretion of inflammatory mediators by activated macrophages and reduced lethality in lipopolysaccharide (LPS)-induced endotoxin shock.

Anhydronotoptol (4-{[(2E,5E)-3,7-dimethylocta-2,5,7-trien-1-yl]oxy}-7H-furo[3,2-g]chromen-7-one), a natural compound extracted from the umbelliferae plant Qiangwu, is a potent inhibitor of nitric oxide production, inhibiting LPS-induced NO production in RAW 264.7 cells with an IC50 value of 36.6 μM.

The impact of spleen tyrosine kinase (Syk) signaling might be prominent in lupus because (i) Syk is a shared downstream signaling molecule among circulating immune complex, LPS, and (1→3)-β-D-glucan (BG), and (ii) all of these factors are detectable in the serum of Fc gamma receptor IIb-deficient (FcgRIIb-/-) mice with sepsis. Syk inhibition downregulated several inflammatory pathways in FcgRIIb-/- macrophages activated with BG + LPS suggesting the potential anti-inflammatory impact of Syk inhibitors in lupus. Indeed, administration of a Syk inhibitor prior to cecal ligation and puncture (CLP) sepsis in FcgRIIb-/- mice reduced baseline lupus-induced proinflammatory cytokines and attenuated sepsis severity as evaluated by mortality, organ injury, serum LPS, and post-sepsis serum cytokines.

Loganic acid 6′-O-β-D-glucoside (8-Epi-Loganic acid-6'-O-β-D-glucoside) is a natural product derived from Cistanche deserticola that inhibits LPS-induced NO and TNF-α production.

ARRY-797 (ARRY-371797) is a potent and selective p38α inhibitor and inhibits LPS-Induced IL-6.

Maresin 1 is a small molecule compound biosynthesized by macrophages (MΦ) with significant anti-inflammatory activity that attenuates LPS-induced lung injury in mice by inhibiting neutrophil adhesion and decreasing the levels of pro-inflammatory cytokines, and stimulates intracellular Ca2+ production and secretion.

Emprumapimod (PF-07265803) is an orally active and specific inhibitor of mitogen-activated protein kinase p38α MAPK, inhibits LPS-induced production of IL-6, and can be used to study dilated cardiomyopathy induced by the LMNA gene.

DO-264 is an inhibitor of autohydrolase structural domain 12 (ABHD12) (IC50: 11 nM) and an inhibitor of cellular LysoPS degradation that enhances LPS-induced phagocytosis.

NLRP3-IN-NBC6 is a potent, selective NLRP3 inflammasome inhibitor with an IC50 of 574 nM. It acts independently of Ca 2+ and inhibits Nigericin-induced inflammasome activation in THP-1 cells, as well as Imiquimod-induced IL-1β release from LPS-primed bone marrow-derived macrophages (BMDMs) [1].

MKK7-COV-9 is a selective and potent covalent inhibitor of MKK7 with inhibitory effects on MKK7-induced protein-protein interactions.MKK7-COV-9 interrupts the activation of primary B-cells in response to LPS.MKK7-COV-9 shows low cytotoxicity at high concentrations.

Alliin ((S)-3-(Allylsulphinyl)-L-alanine) is a garlic organosulfur compound that possesses various pharmacological properties.alliin protected against LPS-induced ALI by activating PPARγ, which subsequently inhibited LPS-induced NF-κB activation and inflammatory response. Alliin might be used as an anti-inflammatory agent in the treatment of ALI.

Polygalasaponin F has anti-neuroinflammatory activity, can inhibit the release of inflammatory cytokines TNF-α and NO induced by lipopolysaccharides (LPS) and reduce the expression of inducible nitric oxide synthases. Polygalasaponin F can significantly i

1. β-Anhydroicaritin exhibits immunosuppressive effect on the mouse macrophages stimulated by LPS. 2. β-Anhydroicaritin phytosomes can inhibit enhanced bone turnover induced by ovariectomy, improve BMD the biomechanical properties of vertebrae, without any stimulation on uterus. 3. β-Anhydroicaritin possesses significant protective effects on the zymosan-induced peritonitis mice, which might be associated with the regulation of Ca(2+); influx in macrophages and iNOS expression.

1. Linarin (Acacetin-7-O-rutinoside) (acacetin-7-O-β-d-rutinoside) shows selective dose dependent inhibitory effect on acetylcholinesterase. 2. Linarin alleviates GalN LPS-induced liver injury by suppressing TNF-α-mediated apoptotic pathways. 3. Linarin prevents A beta-induced neurotoxicity through the activation of PI3K Akt, which subsequently inhibits GSK-3b and up-regulates Bcl-2. 4. The piperine significantly enhanced the oral absorption of Linarin in rats by inhibiting P-glycoprotein mediated cellular efflux during the intestinal absorption and likely simultaneously by inhibiting the metabolism of Linarin.

SKF-86002 is an effective inhibitor of p38 MAP kinase (IC50: 0.5-1 uM); inhibits LPS-induced IL-1 and TNF-α production in human monocytes (IC50: 1 μM).

Polygalacin D shows anti- proliferation, anti-inflammary, and hepatoprotective activities, it can inhibit the expression of lipopolysaccharide (LPS)-induced iNOS and COX-2 protein and mRNA without an appreciable cytotoxic effect on RAW 264.7 macrophages, and can suppress induction by LPS of pro-inflammatory cytokines such as prostaglandin E2 (PGE2).

1. Flavokawain B (Flavokavain B) has potent anti-inflammatory activity, can significantly inhibit production of NO and PGE2 in LPS-induced RAW 264.7 cells. 2. Flavokawain B, the hepatotoxic constituent from kava root, induces GSH-sensitive oxidative stress through modulation of IKK NF-κB and MAPK signaling pathways. 3. Flavokawain B induces apoptosis, has the potential usefulness of FKB for prevention and treatment of hormone-refractory prostate cancer in an adjuvant setting. 4. Flavokawain B acts through ROS generation and GADD153 up-regulation to regulate the expression of Bcl-2 family members, thereby inducing mitochondrial dysfunction and apoptosis in HCT116 cells.

1. Peimisine (Ebeiensine) can affect M-receptor, excit β-receptor, restrain the release of internal calcium, and promote to releaseing nitrogen monoxidum in order to relax tracheal smooth muscle and relieve asthma. 2. Peimisine can attenuate lung tissue injury( ALI), LDH and MDA amount in ALI mice in a dose dependent manner, it also lower the total protein, total white blood cells, lymphocyte and neutrophilic leukocyte in bronchoalveolar lavage fluid( BALF); suggests that peimisine can play a protective role against LPS-induced acute lung injury. 3. Peimisine has the protective effect on the experimental hepatic fibrosis formation, the possible mechanisms are associated with inhibiting fibrogenesis and fibrosis accumulation, and decreasing lipid peroxidation. 4. Peimisine can inhibit angiotensin I converting enzyme activity in a dose-dependent manner, displaying 5 % inhibitory concentration values of 526.5 microM, thus, it may have antihypertensive action.

BW-A 78U, a PDE4 inhibitor (IC50: 3 μM), does not inhibit lipopolysaccharide (LPS)-induced TNF-α release.

(E Z)-BCI (NSC-150117), a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory properties, reduces LPS-induced inflammatory mediators and ROS production in macrophage cells by activating the Nrf2 signaling axis and inhibiting the NF-κB pathway.

Kaurenoic acid (kaurenoate) has anti-inflammatory potential in acetic acid-induced colitis, decreases in MDA level. Kaurenoic acid exerts a uterine relaxant effect acting principally through calcium blockade and in part, by the opening of ATP-sensitive potassium channels. Kaurenoic acid exhibits an analgesic effect in a consistent manner and that its mechanisms involve the inhibition of cytokine production and activation of the NO-cyclic GMP-protein kinase G-ATP-sensitive potassium channel signaling pathway. Kaurenoic acid derivatives have an antimicrobial activity of substituted on carbon-15 at concentrations greater than or equal to 250 μg ml. Kaurenoic acid has inhibitory effects on the LPS-induced inflammatory response in RAW264.7 macrophages.

Esculentoside A can suppress inflammatory responses in LPS-induced ALI through inhibition of the NF-κB and mitogen-activated protein kinase signaling pathways. Esculentoside A may be useful for the treatment of autoimmune disease through modulation on T c

Trilobatin (P-Phlorizin) has anti-oxidant effect, can increase superoxide dismutase (SOD) activity.Trilobatin has anti-inflammatory effect, it potentially inhibits the lipopolysaccharide (LPS)-induced inflammatory response by suppressing the NF-κB signaling pathway.Trilobatin shows a strong inhibitory activity against α-glucosidase and a moderate inhibitory activity against α-amylase for management of postprandial hyperglycemia with less side effect.

AG 556 is a selective inhibitor of EGFR and blocks LPS-induced TNF-α production.

Glaucine has antitussive, antioxidative potential and antiviral activities, it may be an anti-arthritic agent, it can enhance LPS and zymosan-induced IL-10 production. Glaucine can inhibit the migration and invasion of human breast cancer cells by MMP-9 i

1. Isofraxidin (Phytodolor) protects leukemia cells from radiation-induced apoptosis via ROS mitochondria pathway in a p53-independent manner. 2. Isofraxidin has a protective effect against LPS-induced ALI, and the protective effect of Isofraxidin seems to result from the inhibition of COX-2 protein expression in the lung, which regulates the production of PGE2. 3. Isofraxidin possesses significant analgesic and anti-inflammatory activities that may be mediated through the regulation of pro-inflammatory cytokines, TNF-α and the phosphorylation of p38 and ERK1 2.

TLR4 inhibitor. Inhibits LPS-induced NF-κB activation in HEK293 cells (IC50 = 2.4 μg mL). Also inhibits LPS-induced cytokine production and procoagulant effects in PBMCs and HUVECs. Prolongs survival in a mouse septic shock model.

Kauran-16,17-diol, a natural diterpenoid product, exhibits anti-tumoral and apoptosis-inducing activities by inhibiting NO production in LPS-induced RAW 264.7 cells with an IC50 value of 17 μM.

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).

Phaeocaulisin E (Compound 5), a guaiane-type sesquiterpene, inhibits LPS-induced NO production in RAW 264.7 macrophages, exhibiting an IC50 value of 10.3 µM [1].

(4S)-10-Nor-calamenen-10-one (Compound 15), an eudesmane sesquiterpene from Alpinia oxyphylla [1], enhances LPS-induced nitric oxide (NO) production in microglial cells.

Human serum albumin (HSA), the most abundant protein in plasma, significantly contributes to plasma oncotic pressure and exhibits antioxidant, anticoagulant, anti-inflammatory, and anti-platelet aggregation activities, as well as colloid osmotic action. It can block the inhibitory effect of GML on human T cells, providing a protective function, and is associated with cardiovascular diseases. HSA partially prevents LPS-induced oxidative stress and the upregulation of NF-κB, NF-κB, and peroxynitrite (ONOO −) in the vascular wall, helping to reduce blood pressure [1] [2] [3].

PDE4-IN-9 (Compound 5j) is a potent PDE4 inhibitor with an IC50 value of 1.4 μM against PDE4 in vitro enzyme assays, which is lower than the 2.0 μM of parent rolipram, and demonstrates good in vivo activity in LPS-induced animal models of asthma COPD and sepsis [1].

COX-2-IN-32 (Compound 2f) is a dual inhibitor of iNOS and COX-2 that downregulates NF-κB expression and demonstrates anti-inflammatory properties by impeding NO production in LPS-induced RAW264.7 macrophages with an IC50 value of 11.2 μM [1].

Sarglaroids F (compound 6), an anti-inflammatory agent extracted from the roots of Grass Coral, suppresses LPS/ATP-induced IL-1β secretion by modulating K+ efflux and diminishing Caspase-1(P20) concentrations. Additionally, Sarglaroids F exhibits no cytotoxic effects on RAW264.7 cells [1].