scholarly journals Fish Oil in the Treatment of Ulcerative Colitis

1990 ◽  
Vol 4 (7) ◽  
pp. 420-423 ◽  
Author(s):  
C Ó'Moráin ◽  
A Tobin ◽  
T McColl ◽  
Y Suzuki
Keyword(s):  
Ulcerative Colitis ◽  
Arachidonic Acid ◽  
Mechanism Of Action ◽  
Mode Of Action ◽  
Rectal Mucosa ◽  
Leukotriene B4 ◽  
Biologically Active ◽  
Active Ulcerative Colitis ◽  
Pilot Studies ◽  
Lysosomal Membrane Stability

Patients with active ulcerative colitis have increased levels of leukotriene B4 in their rectal mucosa. Eicosapentaenoic acid (EPA) competitively inhibits the cyclo-oxgenase pathway and reduces the formation of cyclo-oxygenase pathway products. EPA is a good substrate for lipoxygenase enzymes and is efficiently converted to leukotriene 85, which is less biologically active. The conversion of EPA to leukotriene B5 is as efficient as that of arachidonic acid to teukotriene B4. Two pilot studies showed benefit of EPA in the treatment of ulcerative colitis. Two of three controlled studies suggest that EPA is more effective than placebo in the treatment of active chronic ulcerative colitis. The mechanism of action is probably reduction of leukotriene B4, but EPA could increase cell and lysosomal membrane stability, or it may exert its effect by reducing interleukin-l. More controlled studies and detailed investigation into the mode of action of EPA are required.

A Comparison Between the Inflammatory Mediators Produced by the Blue-Tongue Lizard (Tiliqua-Scincoides) and Human White Blood-Cells

1988 ◽  
Vol 36 (2) ◽  
pp. 209 ◽  
Author(s):  
SR Mccoll ◽  
CB Daniels
Keyword(s):  
Arachidonic Acid ◽  
Free Radicals ◽  
Blood Cells ◽  
White Blood Cells ◽  
Leukotriene B4 ◽  
Biologically Active ◽  
Hydroxyeicosatetraenoic Acid ◽  
Oxygen Derived Free Radicals ◽  
Derivatives Of ◽  
Human White Blood Cells

Human white blood cells, particularly neutrophils and macrophages produce several biologically active molecules including oxygen-derived free radicals and some metabolites of arachidonic acid which are involved in mechanisms of host defence. White blood cells of the blue-tongue lizard Tiliqua scincoides produce certain derivatives of arachidonic acid which include prostaglandins, thromboxane and 12- and 15-hydroxyeicosatetraenoic acid. The ability to produce these compounds indicates that these animals possess the enzymes cyclooxygenase, 12- and 15-lipoxygenase, T. scincoides white blood cells did not produce leukotriene B4 or 5-hydroxyeicosatetraenoic acid indicating that, unlike human white blood cells, they do not possess a 5-lipoxygenase enxyme. T. scincoides cells are also capable of producing the oxygen-derived free radical superoxide enzyme.

scholarly journals Increased arachidonic acid composition of phospholipids in colonic mucosa from patients with active ulcerative colitis.

Gut ◽  
1987 ◽  
Vol 28 (8) ◽  
pp. 1002-1007 ◽  
Author(s):  
T Nishida ◽  
H Miwa ◽  
A Shigematsu ◽  
M Yamamoto ◽  
M Iida ◽  
...  
Keyword(s):  
Ulcerative Colitis ◽  
Arachidonic Acid ◽  
Acid Composition ◽  
Colonic Mucosa ◽  
Active Ulcerative Colitis

Verapanzil inhibits in-vitro leucotriene B4 release by rectal mucosa in active ulcerative colitis

2007 ◽  
Vol 6 (2) ◽  
pp. 163-168 ◽  
Author(s):  
D. J. GERTNER ◽  
D. S. RAMPTON ◽  
T. R. J. STEVENS ◽  
J. E. LENNARD-JONES
Keyword(s):  
Ulcerative Colitis ◽  
Rectal Mucosa ◽  
Active Ulcerative Colitis

Phase II study of safety, efficacy and pharmacokinetics of BXT-51072 in patients with mild-moderately active ulcerative colitis

2001 ◽  
Vol 120 (5) ◽  
pp. A280-A280
Author(s):  
S HANAUER ◽  
P MINER ◽  
A KESHAVARZIAN ◽  
E MORRIS ◽  
B SALZBERG ◽  
...  
Keyword(s):  
Ulcerative Colitis ◽  
Phase Ii ◽  
Phase Ii Study ◽  
Active Ulcerative Colitis

Diacylfuroxans Are Masked Nitrile Oxides That Inhibit GPX4 Covalently

2019 ◽  
Author(s):  
John Eaton ◽  
Richard A. Ruberto ◽  
Anneke Kramm ◽  
Vasanthi S. Viswanathan ◽  
Stuart Schreiber
Keyword(s):  
Molecular Mechanism ◽  
Mechanism Of Action ◽  
Therapeutic Target ◽  
Biologically Active ◽  
Drug Resistant ◽  
Nitrile Oxides ◽  
Molecular Mechanism Of Action

<div><div><div><p>GPX4 represents a promising yet difficult-to-drug therapeutic target for the treatment of, among others, drug-resistant cancers. While most GPX4 inhibitors rely on a chloroacetamide moiety to modify covalently the protein’s catalytic selenocysteine residue, the discovery and mechanistic elucidation of structurally diverse GPX4-inhibiting molecules has uncovered novel electrophilic warheads that bind and inhibit GPX4. Here we report our discovery that diacylfuroxans can act as masked nitrile oxides that inhibit GPX4 covalently. These observations illuminate a novel molecular mechanism of action for biologically active furoxans and also suggest that nitrile oxides may be uniquely suited to targeting GPX4.</p></div></div></div>

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