Ebrotidine effect on the proteolytic and lipolytic activities of Helicobacter pylori.
1. The effect of ebrotidine, a new antiulcer agent, on the activity of mucus degrading of protease and lipase enzymes elaborated by Helicobacter pylori was investigated. 2. In the absence of ebrotidine, the H. pylori protease caused extensive degradation of gastric mucus protein, while free fatty acids, glycerol mono-oleate and lysophosphatidylcholine were produced by the action of H. pylori lipase and phospholipase A enzymes. 3. Introduction of ebrotidine to the incubation system led to the reduction in the rate of mucus protein and lipid degradation. The rate of proteolysis inhibition was proportional to ebrotidine concentration up to 35 micrograms/ml at which point, a 57% reduction in mucus degradation was obtained, while the maximum inhibition of phospholipase A (96%) and lipase (93%) activities occurred at ebrotidine concentration of 60 micrograms/ml. 4. The results indicate that ebrotidine is capable of counteracting the mucolytic activity of H. pylori towards protein and lipid constituents of gastric mucus layer.
Slomiany
B L
BL
New Jersey Dental School, University of Medicine and Dentistry of New Jersey, Newark 07103-2400.
Piotrowski
J
J
Mojtahed
H
H
Slomiany
A
A
D000897:Anti-Ulcer Agents / Q000494:pharmacology*; D001557:Benzenesulfonates / Q000494:pharmacology*; D010450:Endopeptidases / Q000378:metabolism; D005753:Gastric Mucosa / Q000187:drug effects / Q000201:enzymology; D016480:Helicobacter pylori / Q000187:drug effects* / Q000201:enzymology / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D008049:Lipase / Q000037:antagonists & inhibitors / Q000378:metabolism; D008066:Lipolysis / Q000187:drug effects*; D008297:Male; D010740:Phospholipases / Q000037:antagonists & inhibitors / Q000378:metabolism; D011480:Protease Inhibitors / Q000494:pharmacology*; D013844:Thiazoles / Q000494:pharmacology*
D000897:Anti-Ulcer Agents; D001557:Benzenesulfonates; D011480:Protease Inhibitors; D013844:Thiazoles; D010740:Phospholipases; D008049:Lipase; D010450:Endopeptidases; C075156:ebrotidine