Abstract
Sucralfate is effective for the treatment of gastric and duodenal ulcers owing to its protective gel-forming ability. However, the mechanism by which sucralfate protects the oesophageal mucosa against reflux oesophagitis has not been clarified. We aimed to investigate the mechanisms of action of sucralfate and sucrose octasulfate (SOS), a component of sucralfate. SOS and sucralfate were administered to oesophagitis-induced rats, and the ulcer lesion size was macroscopically examined and scored. Effective pepsin activity in the gastric juices obtained from the animal model was evaluated by a casein digestion test. Sucralfate and SOS improved the pathology scores in a dose-dependent manner, whereas gastric juice pepsin activity was not impaired by therapeutic doses of SOS. As SOS lacks the ability to form a thick gel layer by polymerisation, we examined the distribution of SOS in the mucosal lumen by imaging mass spectrometry (IMS) to determine whether SOS directly adheres to the mucosal surface. A clear homogeneous thin-layer SOS film (>100 μm thick) was visualized on the oesophageal mucosal surface. Moreover, this SOS film formation was enhanced at ulcer lesion sites. Taken together, SOS appears to protect oesophageal mucosa against reflux oesophagitis via thin-layer formation on the mucosal surface.
Highlights
Sucralfate, a complex salt composed of aluminium hydroxide and sucrose octasulfate (SOS) polymer, is widely used to treat gastrointestinal diseases such as gastric and duodenal ulcers
Macroscopic observations of oesophageal tissues obtained from reflux oesophagitis modelled-rats clearly demonstrated that both compounds improved the gross pathology of reflux oesophagitis (Fig. 3)
We aimed to evaluate the mucosal-protective ability and mechanisms employed by SOS and sucralfate in oesophagitis, using a rat reflux oesophagitis model
Summary
Sucralfate, a complex salt composed of aluminium hydroxide and sucrose octasulfate (SOS) polymer, is widely used to treat gastrointestinal diseases such as gastric and duodenal ulcers. In a series of studies, Orlando and colleagues attempted to determine the protective mechanisms of sucralfate against reflux oesophagitis[13,14,15,16], focusing on the main chemical component of sucralfate, SOS, which lacks the ability to form a gel. Their research showed that SOS administration is effective in models of oesophagitis because SOS is able to suppress H+ ion permeability in biopsied human oesophageal mucosa. It is still unclear whether SOS directly adheres to the mucous surface. The obtained images clearly demonstrate that a thin layer of SOS was tightly attached to the surface of the oesophageal mucosa, especially within ulcer sites, in an oesophagitis model
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