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Protective effect of Aframomum melegueta phenolics against CCl₄-induced rat hepatocytes damage; role of apoptosis and pro-inflammatory cytokines inhibition.

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Aframomum melegueta is a commonly used African spice. Through a hepatoprotective bioassay-guided isolation, the chloroform fraction of A.melegueta seeds yielded one new diarylheptanoid named 3-(S)-acetyl-1-(4'-hydroxy-3', 5'-di methoxyphenyl)-7-(3″,4″, 5″-trihydroxyphenyl)heptane (1), and two new

Volatile organic compounds in exhaled breath are independent of systemic inflammatory syndrome caused by intravenous lipopolysaccharide infusion in humans: results from an experiment in healthy volunteers.

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Systemic inflammatory response syndrome (SIRS) is observed during critical illness in most patients. It is defined by a clinical definition. The composition of volatile organic compounds (VOCs) in exhaled breath may change during SIRS and may thus serve as a diagnostic tool. We investigated whether

Anti-inflammatory drugs alter amino acid transport in HTC cells.

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Following the addition of indomethacin to exponentially growing rat hepatoma cell (HTC) cultures, cells accumulated in the G1 phase. Over the course of several hours, specific changes in membrane transport accompanied this inhibition. Indomethacin stimulated the uptake of

Effects of CoA-independent transacylase inhibitors on the production of lipid inflammatory mediators.

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The enzyme CoA-independent transacylase (CoA-IT) has been proposed to mediate the movement of arachidonate between specific phospholipid subclasses, and we have shown that two inhibitors of CoA-IT (SK&F 98625 and SK&F 45905) block this movement. In this report, we use these inhibitors to further

Pharmacological characterization of the muscarinic agonist (3R,4R)-3-(3-hexylsulfanyl-pyrazin-2-yloxy)-1-aza-bicyclo[2.2.1]heptane (WAY-132983) in in vitro and in vivo models of chronic pain.

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Here, we have investigated the in vitro pharmacology of a muscarinic agonist, (3R,4R)-3-(3-hexylsulfanyl-pyrazin-2-yloxy)-1-aza-bicyclo[2.2.1]heptane (WAY-132983), and we demonstrated its activity in several models of pain. WAY-132983 had a similar affinity for the five muscarinic receptors

Chemopreventative effect of an inducible nitric oxide synthase inhibitor, ONO-1714, on inflammation-associated biliary carcinogenesis in hamsters.

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The present study was designed to investigate whether an inducible nitric oxide synthase (iNOS)-specific inhibitor, ONO-1714 [(1S, 5S, 6R, 7R)-7-chloro-3-imino-5-methyl-2-azabicyclo[4.1.0] heptane], could prevent inflammation-associated biliary carcinogenesis in bilioenterostomized hamsters. Syrian

Plant-based hydrocarbon esters from Tragia involucrata possess antimicrobial and anti-inflammatory activities.

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Antimicrobial and anti-inflammatory activities of hydrocarbon esters obtained from Tragia involucrata were evaluated by disk-diffusion (250 µg/ml), and broth-dilution (500-7.8 µg/ml), methods against bacteria. Among the compounds, shellsol showed the most potent activity against Burkholderia

Synthesis and biological activity of various derivatives of a novel class of potent, selective, and orally active prostaglandin D2 receptor antagonists. 2. 6,6-Dimethylbicyclo[3.1.1]heptane derivatives.

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In an earlier paper, we reported that novel prostaglandin D(2) (PGD(2)) receptor antagonists having the bicyclo[2.2.1]heptane ring system as a prostaglandin skeleton were a potent new class of antiallergic agents and suppressed various allergic inflammatory responses such as those observed in

Synthesis and biological activity of various derivatives of a novel class of potent, selective, and orally active prostaglandin D2 receptor antagonists. 1. Bicyclo[2.2.1]heptane derivatives.

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Novel prostaglandin D(2) (PGD(2)) receptor antagonists were synthesized as a potential new class of antiallergic agents having a bicyclo[2.2.1]heptane ring system with sulfonamide groups. Some of them exhibit extremely potent antagonism of the PGD(2) receptor in radioligand binding and cAMP

Antibacterial, anti-inflammatory, and antioxidant effects of Yinzhihuang injection.

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The Yinzhihuang injection, a traditional Chinese medicine, has been the recent target of increasing interest due to its anti-inflammatory properties. The molecular basis by which Yinzhihuang injection could cure Riemerella anatipestifer (RA) serositis in ducks is unclear. This study evaluated the

Formyl peptide receptor modulators: a patent review and potential applications for inflammatory diseases (2012-2015).

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BACKGROUND The activation of leukocytes and the subsequent immune cascade play an essential role in sterile and infectious inflammation. Dysregulation of these immune responses or excess leukocyte activation can induce tissue damage, organ dysfunction and mortality. Formyl peptide receptors (FPRs)

A new diarylheptanoid and a new diarylheptanoid glycoside isolated from the roots of Juglans mandshurica and their anti-inflammatory activities.

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A new diarylheptanoid, (2S,3S,5S)-2,3,5-trihydroxy-1,7-bis(4-hydroxy- 3-methoxyphenyl)heptane (1), and a new diarylheptanoid glycoside, (2S,3S,5S)-2,3-dihydroxy-5-O-β-d-xylopyranosyl-7-(4-hydroxy-3-methoxyphenyl)-1-(4-hydroxyphenyl)heptane (2), together with three known compounds, rhoiptelol C (3),

Physicochemical properties of dexamethasone palmitate, a high fatty acid ester of an anti-inflammatory drug: polymorphism and crystal structure.

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Two polymorphic crystalline forms of dexamethasone palmitate were obtained from acetone (Form A) and n-heptane (Form B), and characterized by X-ray powder patterns and IR spectra. The crystal structure of Form B was further analyzed by the X-ray diffraction method. The molecular conformation of the

In vitro anti-inflammatory activity of larch (Larix decidua L.) sawdust.

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The influence of larch (Larix decidua L.) sawdust extracts on arachidonate metabolism has been evaluated in vitro. Extracts of different polarities were tested for their ability to inhibit prostaglandin formation by COX-1 and COX-2 and LTB(4) formation by 5-LOX. The lipophilic n-heptane extract

The inducible nitric oxide synthase inhibitor ONO-1714 blunts dextran sulfate sodium colitis in mice.

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In mice with acute dextran sulfate sodium colitis, we examined the effect of inducible nitric oxide synthase inhibition by (1S,5S,6R,7R)-7chloro-3-amino-5methyl-2-azabicyclo[4.1.0]heptane hydrochloride (ONO-1714) on colonic biochemistry, injury, and inflammation. Colonic luminal nitrate and nitrite

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