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Abstract
Butyrolactone I (BTL-I) is a butanolide isolated from the deep-sea-derived fungus, Aspergillus sp. It provides a potential new target for the prevention and treatment of food allergies. This study aimed to investigate the metabolic and pharmacokinetic profile of BTL-I in rats. The metabolic profiles were obtained by UHPLC–Q-TOF-MS. As a result, eleven metabolites were structurally identified, and the proposed metabolic pathways of BTL-I were characterized. The main metabolites were the oxidative and glucuronidative metabolites. In addition, a sensitive UHPLC–MS/MS method was established for the quantitation of BTL-I in rat plasma (LOQ = 2 ng/mL). The method was fully validated and successfully applied to the pharmacokinetic study of BTL-I in rats after oral administration or intravenous administration. The oral bioavailability was calculated as 6.29%, and the maximum plasma concentrations were 9.85 ± 1.54 ng/mL and 17.97 ± 1.36 ng/mL for intravenous and intragastric dosing groups, respectively.
Highlights
Food allergies are an immune-mediated adverse reaction to food [1,2]
Butyrolactone I (BTL-I) was quickly eliminated from the plasma, with a T1/2 value of 1.36 ±
BTL-I was quickly eliminated from the plasma, with a T1/2 value of 1.23 ± 0.22 h
Summary
Food allergies are an immune-mediated adverse reaction to food [1,2]. Food allergies to cow’s milk and eggs have become prevalent among young children over the past 20 years [3,4]. Providing improved therapeutic options has become an important avenue in food allergy research. The exploitation of small-molecule inhibitors is one important research direction for anti-food allergy studies, due to their diverse chemical structures [6]. There is certain evidence from human and animal studies that basophils and mast cells are key effector cells that contribute to allergic reactions to foods [7]. It has been reported that several compounds from marine microorganisms could partially inhibit degranulation in IgE-mediated mast cell responses [8,9]
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