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Overview
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Background
γ-Linolenic Acid methyl ester is a weak leukotriene B4 (LTB4) receptor antagonist.LTB 4, a potent neutrophil chemoattractant, is present at high concentrations in psoriatic lesions, bronchoalveolar lavage in asthmatics and rectal dialysates in patients with inflammatory bowel disease. In vitro: γ-Linolenic acid methyl ester is an esterified version of the free acid which is less water soluble but more amenable for the formulation of GLA-containing diets and dietary supplements. GLA was identified as an ω-6 fatty acid which could be elongated to arachidonic acid for endogenous eicosanoid synthesis. GLA was found to be a weak leukotriene B4 (LTB4) receptor antagonist, which was able to inhibit [3H]-LTB4 binding to porcine neutrophil membranes with a Ki of 1 μM [1].In vivo: In an in-vivo model of LTB4-induced bronchoconstriction, ricinelaidic acid andγ-Linolenic acid methyl ester at a 1 mg/kg i.v. dose could result in 46% and 53% inhibition, respectively, indicating that essential fatty acids are LTB4 receptor antagonists, which may account in part for their reported anti-inflammatory activities [1]. Clinical trial: So far, no clinical study has been conducted.
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Overview