macrophage

Muscone (3-Methylcyclopentadecanone) is an organic compound that is the primary contributor to the odor of musk.

Madecassic acid (L-fucopyranose) is extracted from the whole herb of Centella asiatica.

Bestatin (Ubenimex) competitively inhibits many aminopeptidases, including B, N and leucine aminopeptidases. Ubenimex is a microbial metabolite and dipeptide with potential immunomodulatory and antitumor activities. Aminopeptidases has been implicated in the process of cell adhesion and invasion of tumor cells. Therefore, inhibiting aminopeptidases may partially attribute to the antitumor effect of ubenimex. This agent also activates T lymphocyte, macrophage, and bone marrow stem cell as well as stimulates the release of interleukin-1 and -2, thus further enhances its antitumor activity.

L-Methionine sulfoxide (H-Met(O)-OH) is a metabolite of Methionine that modulates oxidative stress and purinergic signaling parameters, while inducing M1 classical macrophage polarization.

Itaconic acid is a precursor for the synthesis of polymers, chemicals, and fuels, and has anti-inflammatory activity.Itaconic acid can be synthesized by fungi. It is also a macrophage-specific metabolite. It mediates crosstalk between macrophage metabolism and peritoneal tumors.

Bisdemethoxycurcumin (Curcumin III) is a natural demethoxy derivative of curcumin. It is a potent activator of macrophage phagocytosis, interacting with 1α, 25-dihydroxy vitamin D3 to stimulate amyloid-β clearance by macrophages (optimal stimulation at 100 nM BDMC) [1]. More stable than curcumin in physiological media, BDMC suppresses proliferation of cancer cells [2]. It down-regulates the transcriptional coactivator p300, suppressing the Wnt β-catenin pathway, and inhibits LPS induction of iNOS expression [3].

Cimifugin (Cimitin) inhibits NO production induced by lipopolysaccharide in macrophage cell line RAW 264.7 and for 1, 1-diphenyl-2-picrylhydrazyl free-radical scavenging activity in cell-free bioassay system.

Carbenoxolone (Biogastrone) is an inhibitor of 11β-HSD and gap junction connexin channels. Carbenoxolone inhibits macrophage migration into atria and prevents the development of fatty liver disease.

Resolvin D1 (RvD1) is an endogenous pro-inflammatory mediator that blocks pro-inflammatory neutrophil migration by regulating actin polymerization, reduces TNF-α-mediated inflammation in macrophages, and enhances macrophage phagocytosis of apoptotic cells.

Myriocin (Thermozymocidin), a metabolite derived from Myriococcum albomyces, is a serine-palmitoyltransferase (SPT) inhibitor with potential antitumour, anticancer, and antiparasitic activities.Myriocin inhibits tumour growth by regulating macrophage polarisation and function through the PI3K Akt mTOR pathway.Myriocin inhibits HCV infection and can be used in the study of neurological diseases. Myriocin inhibits HCV infection and can be used to study neuropathy and fungal infections.

3-Phosphoglyceric acid is a metabolic intermediate in glycolysis and the Calvin cycle, and it is also involved in alveolar macrophage epigenetic regulation.

Desmosterol (24-Dehydrocholesterol) is a cholesterol biosynthesis intermediate that inhibits macrophage inflammatory vesicle activation and prevents vascular inflammation and atherosclerosis.

D-Trimannuronic acid is an alginate oligomer that originates from seaweed. It can induce TNF-α secretion by mouse macrophage cell lines, making it valuable in pain and vascular dementia research [1][2][3].

Lipoxin A4 (LXA4) is a lipoxygenase-derived arachidonate-like mediator with anti-inflammatory properties.Lipoxin A4 attenuates MSU crystal-induced NLRP3 inflammasome activation through inhibition of Nrf2, and regulates M1 M2 macrophage polarization through the FPR2-IRF pathway.Lipoxin inhibits oxidative stress and inflammation.

Beauveriolide I is a cyclodepsipeptide that has been found inBeauveriaand an inhibitor of lipid droplet formation.1It inhibits lipid droplet formation when used at concentrations of 3 and 10 μM, as well as inhibits cholesterol synthesis (IC50= 0.78 μM), in primary mouse peritoneal macrophages.1,2Beauveriolide I also inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity in mouse macrophage membranes (IC50= 6 μM).2 1.Namatame, I., Tomoda, H., Si, S., et al.Beauveriolides, specific inhibitors of lipid droplet formation in mouse macrophages, produced by Beauveria sp. FO-6979J. Antibiot. (Tokyo)52(1)1-6(1999) 2.Namatame, I., Tomoda, H., Ishibashi, S., et al.Antiatherogenic activity of fungal beauveriolides, inhibitors of lipid droplet accumulation in macrophagesProc. Nat. Acad. Sci. USA101(3)737-742(2004)

Beauveriolide III is a cyclodepsipeptide that has been found inBeauveriaand an inhibitor of lipid droplet formation.1It inhibits lipid droplet formation when used at concentrations of 3 and 10 μM, as well as inhibits cholesterol synthesis (IC50= 0.41 μM), in primary mouse peritoneal macrophages.1,2Beauveriolide III also inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity in mouse macrophage membranes (IC50= 5.5 μM).2Beauveriolide III (25 and 50 mg/kg) reduces the size of aortic atherosclerotic lesions inLdlr-/-andApoE-/-mouse models of atherosclerosis. 1.Namatame, I., Tomoda, H., Si, S., et al.Beauveriolides, specific inhibitors of lipid droplet formation in mouse macrophages, produced by Beauveria sp. FO-6979J. Antibiot. (Tokyo)52(1)1-6(1999) 2.Namatame, I., Tomoda, H., Ishibashi, S., et al.Antiatherogenic activity of fungal beauveriolides, inhibitors of lipid droplet accumulation in macrophagesProc. Nat. Acad. Sci. USA101(3)737-742(2004)

Fuscin is a quinonoid fungal metabolite originally isolated from O. fuscum that has diverse biological activities. It inhibits binding of the ADP/ATP translocase inhibitor atractyloside to rat liver mitochondria in an ADP-dependent manner when used at a concentration of 50 μM in a radioligand binding assay. Fuscin (20 μM) reduces the glutathione content of rat liver mitochondria to 28% of controls and inhibits NADH oxidation in sonicated pigeon heart mitochondria preparations in a concentration-dependent manner. It competes with macrophage inflammatory protein 1α (MIP-1α) for binding to CCR5 chemokine receptors in vitro with an IC50 value of 21 μM.

Antibiotic PF 1052 is a fungal metabolite originally isolated from Phoma.1,2 It is active against S. aureus, S. parvulus, and C. perfringens (MICs = 3.13, 0.78, and 0.39 μg/ml, respectively), among others.1 It inhibits neutrophil migration in a wound assay using zebrafish larvae expressing GFP-labeled neutrophils, reducing pseudopodia formation and inducing rounding of neutrophils.2 Antibiotic PF 1052 is selective for neutrophil migration over macrophage migration in zebrafish larvae. It also inhibits the migration of murine neutrophils when used at concentrations of 10 and 20 μM.References Antibiotic PF 1052 is a fungal metabolite originally isolated from Phoma.1,2 It is active against S. aureus, S. parvulus, and C. perfringens (MICs = 3.13, 0.78, and 0.39 μg/ml, respectively), among others.1 It inhibits neutrophil migration in a wound assay using zebrafish larvae expressing GFP-labeled neutrophils, reducing pseudopodia formation and inducing rounding of neutrophils.2 Antibiotic PF 1052 is selective for neutrophil migration over macrophage migration in zebrafish larvae. It also inhibits the migration of murine neutrophils when used at concentrations of 10 and 20 μM. References

1. Norisoboldine ((+)-Laurelliptine) might be a potential therapeutic agent for rheumatoid arthritis, and it functions through protecting joint destruction as well as regulating the abnormal immune responses. 2. Norisoboldine inhibits the macrophage activation and the resultant production of pro-inflammatory cytokines via down-regulating the activation of MAPKs signaling pathways rather than NF-κB.

2,4,5-Trimethoxybenzoic acid, identified in purple perilla extracts, inhibits M1 macrophage phenotype-mediated inflammation in diabetes [1].

Cochlioquinone A is an inhibitor of diacylglycerol kinase (DGK) and diacylglycerol acyltransferase (DGAT). It has been shown to reduce the concentration of phosphatidic acid in T cell lymphoma and has also been shown to compete with macrophage inflammatory protein-1α for binding to human CCR5 chemokine receptors.

Itaconic acid is a precursor for the synthesis of polymers, chemicals, and fuels, and has anti-inflammatory activity.Itaconic acid can be synthesized by fungi. It is also a macrophage-specific metabolite. It mediates crosstalk between macrophage metabolism and peritoneal tumors.

Hyperectumine demonstrates moderate anti-inflammatory efficacy by inhibiting the activity of inflammatory mediators induced by LPS in RAW 264.7 macrophage cells.

D-Glucosyl-β-1,1′-N-palmitoylsphingosine (C16 Glucosyl(β) Ceramide (d18:1 16:0)) is an endogenous ligand for the Macrophage-Inducible C-type Lectin (Mincle) with immunostimulatory properties [1].