Effects of Intravenous Administration of FR122047 (a Selective Cyclooxygenase 1 Inhibitor) and FR188582 (a Selective Cyclooxygenase 2 Inhibitor) on Prostaglandin-E2-Induced Aqueous Flare Elevation in Pigmented Rabbits

2004 ◽  
Vol 36 (6) ◽  
pp. 321-326 ◽  
Author(s):  
Tomohiro Abe ◽  
Yoriko Hayasaka ◽  
Xue-Yun Zhang ◽  
Seiji Hayasaka
Keyword(s):  
Intravenous Administration ◽  
Cyclooxygenase 2 ◽  
Prostaglandin E ◽  
Aqueous Flare ◽  
Cyclooxygenase 1 ◽  
Pigmented Rabbits

Effects of Topical Mydriatics and Vasoconstrictors on Prostaglandin-E2-Induced Aqueous Flare Elevation in Pigmented Rabbits

2003 ◽  
Vol 35 (5) ◽  
pp. 256-260 ◽  
Author(s):  
Yoriko Hayasaka ◽  
Seiji Hayasaka ◽  
Xue-Yun Zhang ◽  
Yasunori Nagaki
Keyword(s):  
Prostaglandin E ◽  
Aqueous Flare ◽  
Pigmented Rabbits

Meloxicam Inhibits Prostaglandin E2 Generation via Cyclooxygenase 2 in the Inflammatory Site but Not That via Cyclooxygenase 1 in the Stomach

Pharmacology ◽  
2000 ◽  
Vol 61 (4) ◽  
pp. 244-250 ◽  
Author(s):  
Keiko Ogino ◽  
Ko Hatanaka ◽  
Michiko Kawamura ◽  
Takashi Ohno ◽  
Yoshiteru Harada
Keyword(s):  
Cyclooxygenase 2 ◽  
Prostaglandin E ◽  
Cyclooxygenase 1 ◽  
Inflammatory Site

scholarly journals Amebic Infection in the Human Colon Induces Cyclooxygenase-2

2001 ◽  
Vol 69 (5) ◽  
pp. 3382-3388 ◽  
Author(s):  
William F. Stenson ◽  
Zhi Zhang ◽  
Terrence Riehl ◽  
Samuel L. Stanley
Keyword(s):  
Epithelial Cells ◽  
Severe Combined Immunodeficiency ◽  
Fold Increase ◽  
Neutrophil Infiltration ◽  
Human Colon ◽  
Cyclooxygenase 2 ◽  
Prostaglandin E ◽  
Myeloperoxidase Activity ◽  
Epithelial Permeability ◽  
Cyclooxygenase 1

ABSTRACT We sought to determine if infection of the colon withEntamoeba histolytica induces the expression of cyclooxygenase-2 and, if it does, to determine the contribution of prostaglandins produced through cyclooxygenase-2 to the host response to amebic infection. Human fetal intestinal xenografts were implanted subcutaneously in mice with severe combined immunodeficiency and allowed to grow; the xenografts were then infected with E. histolytica trophozoites. Infection with E. histolytica resulted in the expression of cyclooxygenase-2 in epithelial cells and lamina propria macrophages. Infection with E. histolytica increased prostaglandin E2(PGE2) levels 10-fold in the xenografts and resulted in neutrophil infiltration, as manifested by an 18-fold increase in myeloperoxidase activity. Amebic infection also induced an 18-fold increase in interleukin 8 (IL-8) production and a >100-fold increase in epithelial permeability. Treatment of the host mouse with indomethacin, an inhibitor of cyclooxygenase-1 and cyclooxygenase-2, or with NS-398, a selective inhibitor of cyclooxygenase-2, resulted in (i) decreased PGE2 levels, (ii) a decrease in neutrophil infiltration, (iii) a decrease in IL-8 production, and (iv) a decrease in the enhanced epithelial permeability seen with amebic infection. These results indicate that amebic infection in the colon induces the expression of cyclooxygenase-2 in epithelial cells and macrophages. Moreover, prostaglandins produced through cyclooxygenase-2 participate in the mediation of the neutrophil response to infection and enhance epithelial permeability.

Effects of Oral Administration of Gardeniae fructus Extract and Intravenous Injection of Crocetin on Lipopolysaccharide- and Prostaglandin E2-induced Elevation of Aqueous Flare in Pigmented Rabbits

2003 ◽  
Vol 31 (05) ◽  
pp. 729-738 ◽  
Author(s):  
Yasunori Nagaki ◽  
Seiji Hayasaka ◽  
Tomohiro Abe ◽  
Xue-Yun Zhang ◽  
Yoriko Hayasaka ◽  
...  
Keyword(s):  
Oral Administration ◽  
Intravenous Injection ◽  
Area Under The Curve ◽  
Prostaglandin E ◽  
Dependent Manner ◽  
Aqueous Flare ◽  
Laser Flare ◽  
Coptidis Rhizoma ◽  
Phellodendri Cortex ◽  
Pigmented Rabbits

The purpose of this study was to evaluate the effects of extracts of Coptidis rhizoma, Phellodendri cortex and Gardeniae fructus, which are medicinal herbs in Orengedoku-to (Huanglin-Jie-Du-Tang in Chinese), and crocetin (a major component of Gardeniae fructus) on experimental elevation of aqueous flare in pigmented rabbits. To produce aqueous flare elevation, 0.5 μg/kg lipopolysaccharide (LPS) was injected into the ear vein, or prostaglandin E2 (PGE2) 25 μg/ml, was applied to the cornea by means of a glass cylinder. Animals were pretreated by oral administration of 150 g/day of food containing 0.15% (w/w) extract powder of Coptidis rhizoma, 0.10% (w/w) extract powder of Phellodendri cortex or 0.15% (w/w) extract powder of Gardeniae fructus for 4 days, or by intravenous injection of crocetin, 0.3, 3, 30 or 300 μg/kg, 30 minutes before aqueous flare elevation. Aqueous flare was measured with a laser flare-cell meter. Aqueous flare intensity was expressed as the area under the curve (AUC) in arbitrary units. The AUC of LPS- and PGE2-induced aqueous flare elevation was 4685 and 1386 arbitrary units, respectively. Pretreatment by oral administration of 0.15% (w/w) extract of Coptidis rhizoma or 0.10% (w/w) extract of Phellodendri cortex did not inhibit LPS-induced aqueous flare elevation. Pretreatment by oral administration of 0.15% extract of Gardeniae fructus suppressed LPS-induced aqueous flare elevation (AUC: 1411 arbitrary units). Pretreatment by intravenous injection of 3, 30 or 300 μg/kg of crocetin-inhibited LPS-induced aqueous flare elevation in a dose-dependent manner. Pretreatment with 3 or 30 μg/kg of crocetin did not inhibit PGE2-induced aqueous flare elevation, but 300 μg/kg of crocetin inhibited PGE2-induced aqueous flare elevation (AUC: 918 arbitrary units).

scholarly journals gem-Difluorobisarylic derivatives: design, synthesis and anti-inflammatory effect

BMC Chemistry ◽  
2019 ◽  
Vol 13 (1) ◽  
Author(s):  
Abeer J. Ayoub ◽  
Layal Hariss ◽  
Nehme El-Hachem ◽  
Ghewa A. El-Achkar ◽  
Sandra E. Ghayad ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Nitric Oxide Synthase ◽  
Protein Expression ◽  
Interleukin 6 ◽  
Cyclooxygenase 2 ◽  
Prostaglandin E ◽  
Diaryl Ethers ◽  
Cyclooxygenase 1 ◽  
Anti Inflammatory ◽  
Oxide Synthase

Abstract Introduction New fluorinated diaryl ethers and bisarylic ketones were designed and evaluated for their anti-inflammatory effects in primary macrophages. Methods The synthesis of the designed molecules started from easily accessible and versatile gem-difluoro propargylic derivatives. The desired aromatic systems were obtained using Diels–Alder/aromatization sequences and this was followed by Pd-catalyzed coupling reactions and, when required, final functionalization steps. Both direct inhibitory effects on cyclooxygenase-1 or -2 activities, protein expression of cyclooxygenase-2 and nitric oxide synthase-II and the production of prostaglandin E2, the pro-inflammatory nitric oxide and interleukin-6 were evaluated in primary murine bone marrow-derived macrophages in response to lipopolysaccharide. Docking of the designed molecules in cyclooxygenase-1 or -2 was performed. Results Only fluorinated compounds exerted anti-inflammatory activities by lowering the secretion of interleukin-6, nitric oxide, and prostaglandin E2, and decreasing the protein expression of inducible nitric oxide synthase and cyclooxygenase-2 in mouse primary macrophages exposed to lipopolysaccharide, as well as cyclooxygenase activity for some inhibitors with different efficiencies depending on the R-groups. Docking observation suggested an inhibitory role of cyclooxygenase-1 or -2 for compounds A3, A4 and A5 in addition to their capacity to inhibit nitrite, interleukin-6, and nitric oxide synthase-II and cyclooxygenase-2 expression. Conclusion The new fluorinated diaryl ethers and bisarylic ketones have anti-inflammatory effects in macrophages. These fluorinated compounds have improved potential anti-inflammatory properties due to the fluorine residues in the bioactive molecules.

Effect of Topical Iganidipine on Experimental Elevation of Aqueous Flare Induced by Prostaglandin E2 and EP Agonists in Pigmented Rabbits

2002 ◽  
Vol 34 (4) ◽  
pp. 195-199 ◽  
Author(s):  
Shuichiro Yanagisawa ◽  
Seiji Hayasaka ◽  
Xue-Yun Zhang ◽  
Yoriko Hayasaka ◽  
Yasunori Nagaki
Keyword(s):  
Prostaglandin E ◽  
Aqueous Flare ◽  
Pigmented Rabbits

Effect of Topical Betaxolol on the Acute Rise of Aqueous Flare Induced by Highly Selective Agonists for Prostaglandin E2 Receptor Subtypes in Pigmented Rabbits

2002 ◽  
Vol 34 (1) ◽  
pp. 48-50 ◽  
Author(s):  
Shuichiro Yanagisawa ◽  
Seiji Hayasaka ◽  
Xue-Yun Zhang ◽  
Yoriko Hayasaka ◽  
Yasunori Nagaki ◽  
...  
Keyword(s):  
Prostaglandin E ◽  
Receptor Subtypes ◽  
Aqueous Flare ◽  
Selective Agonists ◽  
Pigmented Rabbits

scholarly journals Relative contribution of cyclooxygenases, epoxyeicosatrienoic acids, and pH to the cerebral blood flow response to vibrissal stimulation

2012 ◽  
Vol 302 (5) ◽  
pp. H1075-H1085 ◽  
Author(s):  
Xiaoguang Liu ◽  
Chunyuan Li ◽  
John R. Falck ◽  
David R. Harder ◽  
Raymond C. Koehler
Keyword(s):  
Blood Flow ◽  
Cerebral Blood Flow ◽  
Metabotropic Glutamate Receptors ◽  
Cyclooxygenase 2 ◽  
Model Systems ◽  
Epoxyeicosatrienoic Acids ◽  
Prostaglandin E ◽  
Cyclooxygenase 1 ◽  
Group I ◽  
Whisker Stimulation

The increase in cerebral blood flow (CBF) during neuronal activation can be only partially attenuated by individual inhibitors of epoxyeicosatrienoic acids (EETs), cyclooxgenase-2, group I metabotropic glutamate receptors (mGluR), neuronal nitric oxide synthase (nNOS), N-methyl-D-aspartate receptors, or adenosine receptors. Some studies that used a high concentration (500 μM) of the cyclooxygenase-1 inhibitor SC-560 have implicated cyclooxygenase-1 in gliovascular coupling in certain model systems in the mouse. Here, we found that increasing the concentration of SC-560 from 25 μM to 500 μM over whisker barrel cortex in anesthetized rats attenuated the CBF response to whisker stimulation. However, exogenous prostaglandin E2 restored the response in the presence of 500 μM SC-560 but not in the presence of a cyclooxygenase-2 inhibitor, thereby suggesting a limited permissive role for cyclooxygenase-1. Furthermore, inhibition of the CBF response to whisker stimulation by an EET antagonist persisted in the presence of SC-560 or a cyclooxygenase-2 inhibitor, thereby indicating that the EET-dependent component of vasodilation did not require cyclooxygenase-1 or -2 activity. With combined inhibition of cyclooxygenase-1 and -2, mGluR, nNOS, EETs, N-methyl-D-aspartate receptors, and adenosine 2B receptors, the CBF response was reduced by 60%. We postulated that the inability to completely block the CBF response was due to tissue acidosis resulting from impaired clearance of metabolically produced CO2. We tested this idea by increasing the concentration of superfused bicarbonate from 25 to 60 mM and found a markedly reduced CBF response to hypercapnia. However, increasing bicarbonate had no effect on the initial or steady-state CBF response to whisker stimulation with or without combined inhibition. We conclude that the residual response after inhibition of several known vasodilatory mechanisms is not due to acidosis arising from impaired CO2 clearance when the CBF response is reduced. An unidentified mechanism apparently is responsible for the rapid, residual cortical vasodilation during vibrissal stimulation.

Effects of Isopropyl Unoprostone, Latanoprost, and Prostaglandin E2 on Acute Rise of Aqueous Flare in Pigmented Rabbits

2002 ◽  
Vol 34 (2) ◽  
pp. 90-93 ◽  
Author(s):  
Xue-Yun Zhang ◽  
Seiji Hayasaka ◽  
Yoriko Hayasaka ◽  
Shuichiro Yanagisawa ◽  
Yasunori Nagaki
Keyword(s):  
Prostaglandin E ◽  
Aqueous Flare ◽  
Pigmented Rabbits
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