125i-il-8-cxcr2

9(Z),11(E)-Conjugated linoleic acid is an isomer of linoleic acid that has been found in beef and milk fat.1It binds to peroxisome proliferator-activated receptor α (PPARα; IC50= 140 nM) and activates the receptor in a reporter assay using COS-1 cells expressing mouse PPARα when used at a concentration of 100 μM.29(Z),11(E)-Conjugated linoleic acid inhibits TNF-α-inducedGLUT4expression and increases insulin-stimulated glucose transport in 3T3-L1 adipocytes.3Dietary administration of 9(Z)11(E)-conjugated linoleic acid reduces serum fasting glucose, insulin, and triglyceride levels and decreases white adipose tissue macrophage infiltration inob/obmice. It also increases body weight gain and body fat in weanling mice.4[Matreya, LLC. Catalog No. 1278] 1.Shultz, T.D., Chew, B.P., Seaman, W.R., et al.Inhibitory effect of conjugated dienoic derivatives of linoleic acid and β-carotene on the in vitro growth of human cancer cellsCancer Lett.63(2)125-133(1992) 2.Moya-Camarena, S.Y., Heuvel, J.P.V., Blanchard, S.G., et al.Conjugated linoleic acid is a potent naturally occurring ligand and activator of PPARαJ. Lipid Res.40(8)1426-1433(1999) 3.Moloney, F., Toomey, S., Noone, E., et al.Antidiabetic effects of cis-9, trans-11-conjugated linoleic acid may be mediated via anti-inflammatory effects in white adipose tissueDiabetes56(3)574-582(2007) 4.Pariza, M.W., Park, Y., and Cook, M.E.The biologically active isomers of conjugated linoleic acidProg. Lipid Res.40(4)283-298(2001)

7,10-dihydroxy-8(E)-Octadecenoic acid is a hydroxy fatty acid and metabolite of oleic acid that is produced byP. aeruginosafrom vegetable oils.1It is active against the food-borne pathogenic bacteriaS. aureus,S. typhimurium,L. monocytogenes,B. subtilis, andE. coli(MIC50s = 31.3, 125, 125, 62.5, and 250 μg/ml, respectively), as well as the plant pathogenic bacteriaErwinia,R. solanacearum,C. glutamicum, andP. syringae(MIC90s = 125, 125, 250, and 500 μg/ml, respectively).2,1 1.Sohn, H.-R., Bae, J.-H., Hou, C.T., et al.Antibacterial activity of a 7,10-dihydroxy-8(E)-octadecenoic acid against plant pathogenic bacteriaEnzyme Microb. Technol.53(3)152-153(2013) 2.Chen, K.Y., Kim, I.H., Hou, C.T., et al.Monoacylglycerol of 7,10-dihydroxy-8(E)-octadecenoic acid enhances antibacterial activities against food-borne bacteriaJ. Agric. Food Chem.67(29)8191-8196(2019)

Sordarin is an inhibitor of fungal protein synthesis originally isolated from S. araneosa.[1] It binds to elongation factor 2 (EF-2) in the presence of ribosomes and inhibits the uncoupled GTPase activity of equimolar mixtures of EF-2 and ribosomes from C. albicans (IC50 = 0.1 μM). Sordarin inhibits protein synthesis in cell-free lysates of C. albicans, C. glabrata, and C. neoformans (IC50s = 0.01, 0.2, and 0.06 μg/ml, respectively) but not in rabbit reticulocytes (IC50 = >100 μg/ml).[1] [2] It inhibits the growth of C. albicans (MIC = 8 μg/ml) but not C. glabrata or C. neoformans (MICs = >125 μg/ml).

Galbinic acid is a depsidone lichen metabolite that has been found in U. undulata.1,2 It is active against the Gram-positive bacteria B. cereus, B. subtilis, and S. aureus, but not S. epidermidis (MICs = 62.5, 62.5, 250, and >250 μg/ml, respectively), as well as the Gram-negative bacterium E. coli, but not S. sonnei (MICs = 125 and >250 μg/ml, respectively).3 |1. Salgado, F., Albornoz, L., Cortéz, C., et al. Secondary metabolite profiling of species of the genus Usnea by UHPLC-ESI-OT-MS-MS. Molecules 23(1), E54 (2017).|2. Elix, J.A., and Engkaninan, U. The structure of galbinic acid. A depsidone from the lichen Usnea undulata. Aust. J. Chem. 28(8), 1793-1797 (1975).|3. Sultana, N., and Afolayan, A.J. A new depsidone and antibacterial activities of compounds from Usnea undulata Stirton. J. Asian Nat. Prod. Res. 13(12), 1158-1164 (2011).

Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.IC50 value:Target: 5-HT1A/1B agonist; 5-HT2C antagonistin vitro: The binding of [3H]eltoprazine to whole tissue sections was saturable and revealed an apparent dissociation constant (Kd) of 11 nM. Specific [3H]eltoprazine binding was completely displaced by 5-HT; conversely, unlabelled eltoprazine reduced [3H]5-HT binding to the levels of non-specific binding [1]. Eltoprazine evoked membrane changes that were similar to but much weaker than those induced by 5HT. Both the 5HT- and eltoprazine-evoked membrane hyperpolarizations were largely suppressed in the presence of spiperone [2].in vivo: eltoprazine is extremely effective in suppressing dyskinesia in experimental models, although this effect was accompanied by a partial worsening of the therapeutic effect of l-dopa. Interestingly, eltoprazine was found to (synergistically) potentiate the antidyskinetic effect of amantadine. The current data indicated that eltoprazine is highly effective in counteracting dyskinesia in preclinical models [3]. Rats were chronically treated with mianserin (10 mg/kg i.p.) or eltoprazine (1 mg/kg i.p.) and were tested in the elevated plus-maze test for anxiety. Mianserin and eltoprazine displayed opposite effects in the elevated plus-maze: mianserin induced anxiolytic-like effects, while eltoprazine showed anxiogenic-like ones [4]. [1]. Sijbesma H, et al. Eltoprazine, a drug which reduces aggressive behaviour, binds selectively to 5-HT1 receptor sites in the rat brain: an autoradiographic study. Eur J Pharmacol. 1990 Feb 20;177(1-2):55-66. [2]. Joels M, et al. Eltoprazine suppresses hyperpolarizing responses to serotonin in rat hippocampus. J Pharmacol Exp Ther. 1990 Apr;253(1):284-9. [3]. Bezard E, et al. Study of the antidyskinetic effect of eltoprazine in animal models of levodopa-induced dyskinesia. Mov Disord. 2013 Jul;28(8):1088-96. [4]. Rocha B, et al. Chronic mianserin or eltoprazine treatment in rats: effects on the elevated plus-maze test and on limbic 5-HT2C receptor levels. Eur J Pharmacol. 1994 Sep 1;262(1-2):125-31.