INHIBITION OF HELICOBACTER-PYLORI GLYCOSULFATASE ACTIVITY TOWARDS HUMAN GASTRIC SULFOMUCIN BY A GASTROPROTECTIVE AGENT, SULGLYCOTIDE

被引:8
作者
MURTY, VLN [1 ]
PIOTROWSKI, J [1 ]
CZAJKOWSKI, A [1 ]
SLOMIANY, A [1 ]
SLOMIANY, BL [1 ]
机构
[1] UNIV MED & DENT NEW JERSEY, RES CTR, NEWARK, NJ 07103 USA
来源
GENERAL PHARMACOLOGY-THE VASCULAR SYSTEM | 1993年 / 24卷 / 06期
关键词
D O I
10.1016/0306-3623(93)90436-2
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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 mug/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.
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页码:1463 / 1466
页数:4
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