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奥美拉唑诱导胃黏膜对肽类缓激肽的跨黏膜通透性。

Omeprazole induces gastric transmucosal permeability to the peptide bradykinin.

机构信息

Lankenau Institute for Medical Research, 100 Lancaster Avenue, Wynnewood, PA 19096, USA.

出版信息

World J Gastroenterol. 2010 Mar 7;16(9):1097-103. doi: 10.3748/wjg.v16.i9.1097.

DOI:10.3748/wjg.v16.i9.1097
PMID:20205280
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2835786/
Abstract

AIM

To investigate omeprazole-induced transepithelial gastric leak and its effects on the permeability of the peptides bradykinin and oxytocin.

METHODS

Rat gastric corpus tissue was isolated and mounted in an Ussing chamber apparatus to evaluate the permeability of (3)H-bradykinin, (3)H-oxytocin, and (14)C-EDTA in the presence or absence of omeprazole. Thin-layer chromatography was performed to identify any metabolic breakdown products of the peptides resulting from permeation through the gastric tissue, and thereby calculate the true flux of the peptide.

RESULTS

The flux rate of intact (3)H-bradykinin increased substantially after omeprazole addition (109.5%) compared to the DMSO vehicle control (14%). No corresponding change in flux of intact (3)H-oxytocin was observed under the same conditions (11.9% and 6.4% in the DMSO- and omeprazole-treated conditions, respectively). After exposure to omeprazole, the flux rate of (14)C-EDTA also increased dramatically (122.3%) compared to the DMSO condition (36.3%).

CONCLUSION

The omeprazole-induced gastric leak allows for transmucosal permeability to charged molecules as well as non-electrolytes. This induced leak will allow certain peptides to permeate.

摘要

目的

研究奥美拉唑诱导的跨上皮胃漏及其对肽类缓激肽和催产素通透性的影响。

方法

分离大鼠胃体组织并安装在 Ussing 室装置中,以评估(3)H-缓激肽、(3)H-催产素和(14)C-EDTA 在存在或不存在奥美拉唑时的通透性。进行薄层层析以鉴定肽类物质透过胃组织后产生的任何代谢分解产物,从而计算肽类物质的真实通量。

结果

与 DMSO 溶剂对照(14%)相比,奥美拉唑加入后完整(3)H-缓激肽的通量率显著增加(109.5%)。在相同条件下,完整(3)H-催产素的通量没有相应变化(DMSO 和奥美拉唑处理条件下分别为 11.9%和 6.4%)。暴露于奥美拉唑后,(14)C-EDTA 的通量率也与 DMSO 条件相比显著增加(122.3%)(36.3%)。

结论

奥美拉唑诱导的胃漏允许带电分子以及非电解质经黏膜通透性。这种诱导性渗漏将允许某些肽类物质渗透。

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Drug Discov Today. 2009 Jul;14(13-14):647-60. doi: 10.1016/j.drudis.2009.03.014. Epub 2009 Apr 8.
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Dig Dis Sci. 2009 Jul;54(7):1408-17. doi: 10.1007/s10620-008-0528-z. Epub 2008 Nov 18.
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Esomeprazole induces upper gastrointestinal tract transmucosal permeability increase.埃索美拉唑可导致上消化道黏膜通透性增加。
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