Membrane Prostaglandin E Synthase-1: A Novel Therapeutic Target

Samuelsson, Bengt; Morgenstern, Ralf; Jakobsson, Per‐Johan

doi:10.1124/pr.59.3.1

Cited by 479 publications

(492 citation statements)

References 190 publications

(197 reference statements)

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“…Some studies reported that Lactobacillus had high levels of resistance to ampicillin vancomycin and streptomycin [59]. Similar results were confirmed by our study.…”

Section: Discussionsupporting

confidence: 92%

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In vitro and in vivo defensive effect of probiotic LAB against Pseudomonas aeruginosa using Caenorhabditis elegans model

et al. 2018

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This study aimed to investigate in vitro and in vivo the probiotic characteristics of lactic acid bacteria (LAB) isolated from Korean traditional fermented foods. Caenorhabditis elegans (C. elegans) was used for analytical assays of fertility, chemotaxis, life-span, worm-killing and bacterial colonization in the intestinal lumen of the worm. All 35 strains of LAB reduced fertility and slowed development in the worms. The worm-killing assay showed that LAB significantly increased the lifespan (P < 0.05) and reduced the susceptibility to virulent PA14; however, the heat-killed LAB did not. The bacterial colonization assay revealed that LAB proliferated and protected the gut of the worm against infection by Pseudomonas aeruginosa PA14. In addition, specific LAB Pediococcus acidilactici(P. acidilactici DM-9), Pediococcus brevis (L. brevis SDL1411), and Pediococcus pentosaceus (P. pentosaceus SDL1409) strains showed acid resistance (66–91%), resistance to pepsin (64–67%) and viability in simulated intestinal fluid (67–73%) based on in vitro probiotic analyses. Taken together, these results suggest that C. elegans may be a tractable model for screening efficient probiotics.

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“…Some studies reported that Lactobacillus had high levels of resistance to ampicillin vancomycin and streptomycin [59]. Similar results were confirmed by our study.…”

Section: Discussionsupporting

confidence: 92%

“…This defensive mechanism may be due to the probiotic efficiency of the LAB 26 . In addition, some of the previously reported secondary metabolites that enhance the immune modulating activity may also act as defensive factors [59]. …”

Section: Discussionmentioning

confidence: 99%

In vitro and in vivo defensive effect of probiotic LAB against Pseudomonas aeruginosa using Caenorhabditis elegans model

et al. 2018

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“…However, because of the different experimental settings applied for analysis of the interference of garcinol with these targets, direct comparison of garcinol´s potencies is difficult. 5-LO and mPGES-1 are crucial enzymes in the biosynthesis of key mediators in inflammatory processes [16,19], providing a rationale for the anti-inflammatory effects of garcinol. Moreover, 5-LO and mPGES-1 are overexpressed in many tumors, and PGE 2 as well as 5-LO products play important roles in tumorigenesis [16,18,19].…”

Section: Discussionmentioning

confidence: 99%

“…5-LO and mPGES-1 are crucial enzymes in the biosynthesis of key mediators in inflammatory processes [16,19], providing a rationale for the anti-inflammatory effects of garcinol. Moreover, 5-LO and mPGES-1 are overexpressed in many tumors, and PGE 2 as well as 5-LO products play important roles in tumorigenesis [16,18,19]. Together, we conclude that the interference of garcinol with 5-LO and mPGES-1 provides a molecular basis for its documented anti-carcinogenic and antiinflammatory properties.…”

Section: Discussionmentioning

confidence: 99%

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Identification of 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 as functional targets of the anti-inflammatory and anti-carcinogenic garcinol

Koeberle

Northoff

Werz

2009

Biochemical Pharmacology

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To cite this version:Andreas Koeberle, Hinnak Northoff, Oliver Werz. Identification of 5-lipoxygenase and microsomal prostaglandin E synthase-1 as functional targets of the anti-inflammatory and anti-carcinogenic garcinol. Biochemical Pharmacology, Elsevier, 2009, 77 (9) This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. A c c e p t e d M a n u s c r i p t 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 61 62 63 64 Ca 2+ -ionophore (A23187)-induced arachidonic acid release in neutrophils nor COX-2 activity in A549 cells or whole blood, measured as formation of 6-keto PGF 1α , or isolated human recombinant COX-2 were significantly affected by garcinol (≤ 30 µM). Together, the high potency of garcinol to selectively suppress PGE 2 synthesis and 5-lipoxygenase product formation provides a molecular basis for the anti-inflammatory and anti-carcinogenic effects of garcinol and rationalizes its therapeutic use.

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Eicosanoid Pathway Modulators: Prostaglandins, Prostacyclin, and Thromboxane

Mazaleuskaya

Ricciotti

2021

Burger's Medicinal Chemistry and Drug Discovery

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Prostanoids (prostaglandins, prostacyclin, and thromboxane) are bioactive lipids, members of the eicosanoid class of compounds, derived from arachidonic acid (AA). They are involved in controlling homeostatic and pathophysiological processes. Their biosynthesis is the result of the coordinated actions of several enzymes. Cyclooxygenases (COXs) catalyze the committed step in the conversion of AA into prostanoids. There are two COX isozymes: the constitutive COX‐1 and the inducible COX‐2, both of which have different patterns of expression and biological functions. COX‐1 and COX‐2 are the targets of traditional nonsteroidal anti‐inflammatory drugs (tNSAIDs), which are used to relieve pain, fever and inflammation. Despite their clinical efficacy, tNSAIDs cause side effects, particularly in the gastrointestinal (GI) tract. NSAIDs selective for COX‐2 inhibition (coxibs) were purposefully designed to spare GI side effects, but predisposed patients to increased cardiovascular (CV) risks. The GI and CV complications from existing NSAIDs prompted interest in the downstream effectors of the COX enzymes as novel drug targets. This article describes various safety issues with tNSAIDs and coxibs, and discusses the current development of novel classes of drugs targeting the AA pathway, including nitric oxide‐releasing and hydrogen sulfide‐releasing NSAIDs, inhibitors of prostanoid synthases, dual inhibitors, and prostanoid receptor agonists and antagonists.

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Membrane Prostaglandin E Synthase-1: A Novel Therapeutic Target

Cited by 479 publications

References 190 publications

In vitro and in vivo defensive effect of probiotic LAB against Pseudomonas aeruginosa using Caenorhabditis elegans model

In vitro and in vivo defensive effect of probiotic LAB against Pseudomonas aeruginosa using Caenorhabditis elegans model

Identification of 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 as functional targets of the anti-inflammatory and anti-carcinogenic garcinol

Eicosanoid Pathway Modulators: Prostaglandins, Prostacyclin, and Thromboxane

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