Inhibition of Helicobacter pylori glycosulfatase activity towards human gastric sulfomucin by a gastroprotective agent, sulglycotide.
1. A glycosulfatase activity towards human gastric sulfomucin was identified in the extracellular material elaborated by Helicobacter pylori, a pathogen implicated in the etiology of gastric disease. 2. The purified enzyme displayed an apparent molecular weight of 30 kDa, and exhibited maximum activity at pH 5.7 in the presence of 0.3% Triton X-100 and 100 mM CaCl2. 3. The H. pylori glycosulfatase activity towards human gastric sulfomucin was inhibited by a gastroprotective agent, sulglycotide. The inhibitory effect was proportional to the concentration of sulglycotide up to 20 micrograms/ml, at which a 98% decrease in mucin desulfation occurred. However, the drug lost the inhibitory effect following its chemical desulfation. 4. The results demonstrate that sulglycotide is a potent inhibitor of H. pylori glycosulfatase and, hence, may be of value in the treatment of gastric disease associated with this bacterial infection.
Murty
V L
VL
Research Center, University of Medicine and Dentistry of New Jersey, Newark 07103-2400.
Piotrowski
J
J
Czajkowski
A
A
Slomiany
A
A
Slomiany
B L
BL
D000897:Anti-Ulcer Agents / Q000494:pharmacology*; D005753:Gastric Mucosa / Q000378:metabolism; D016480:Helicobacter pylori / Q000201:enzymology*; D006801:Humans; D009077:Mucins / Q000378:metabolism*; D011506:Proteins / Q000378:metabolism; D012795:Sialoglycoproteins / Q000494:pharmacology*; D013429:Sulfatases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013462:Sulfur Radioisotopes
D000897:Anti-Ulcer Agents; D009077:Mucins; D011506:Proteins; D012795:Sialoglycoproteins; D013462:Sulfur Radioisotopes; C012564:sulfomucin; C009354:sulglicotide; D013429:Sulfatases; C022758:glycosulphatase