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大鼠口服d-法戈明后的命运

Fate of d-Fagomine after Oral Administration to Rats.

作者信息

Amézqueta Susana, Ramos-Romero Sara, Martínez-Guimet Carolina, Moreno Albert, Hereu Mercè, Torres Josep Lluís

机构信息

Departament d'Enginyeria Química i Química Analítica and Institut de Biomedicina (IBUB), Universitat de Barcelona , Martí i Franquès 1-11, 08028 Barcelona, Spain.

Institute of Advanced Chemistry of Catalonia (IQAC), Spanish National Research Council (CSIC) , Jordi Girona 18-26, 08034 Barcelona, Spain.

出版信息

J Agric Food Chem. 2017 Jun 7;65(22):4414-4420. doi: 10.1021/acs.jafc.7b01026. Epub 2017 May 22.

Abstract

d-Fagomine is an iminosugar found in buckwheat that is capable of inhibiting the adhesion of potentially pathogenic bacteria to epithelial mucosa and reducing the postprandial blood glucose concentration. This paper evaluates the excretion and metabolism of orally administered d-fagomine in rats and compares outcomes with the fate of 1-deoxynojirimycin. d-Fagomine and 1-deoxynojirimycin show similar absorption and excretion kinetics. d-Fagomine is partly absorbed (41-84%, dose of 2 mg/kg of body weight) and excreted in urine within 8 h, while the non-absorbed fraction is cleared in feces within 24 h. d-Fagomine is partially methylated (about 10% in urine and 3% in feces). The concentration of d-fagomine in urine from 1 to 6 h after administration is higher than 10 mg/L, the concentration that inhibits adhesion of Escherichia coli. Orally administered d-fagomine is partially absorbed and then rapidly excreted in urine, where it reaches a concentration that may be protective against urinary tract infections.

摘要

d-法戈明是一种存在于荞麦中的亚氨基糖,它能够抑制潜在病原菌与上皮黏膜的黏附,并降低餐后血糖浓度。本文评估了大鼠口服d-法戈明后的排泄和代谢情况,并将结果与1-脱氧野尻霉素的情况进行比较。d-法戈明和1-脱氧野尻霉素表现出相似的吸收和排泄动力学。d-法戈明部分被吸收(体重2mg/kg剂量时为41%-84%),并在8小时内随尿液排出,而未被吸收的部分在24小时内随粪便排出。d-法戈明部分被甲基化(尿液中约10%,粪便中3%)。给药后1至6小时尿液中d-法戈明的浓度高于10mg/L,该浓度可抑制大肠杆菌的黏附。口服的d-法戈明部分被吸收,然后迅速随尿液排出,在尿液中达到的浓度可能对预防尿路感染有保护作用。

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