Effect of sofalcone on tyrosylprotein sulfotransferase.
1. Gastric mucus glycoproteins are actively involved in the maintenance of mucosal integrity and the impairment in their elaboration is often a prominent feature in gastric pathology. In this study, we investigated the effect of an antiulcer drug, sofalcone, on the activity of tyrosylprotein sulfotransferase enzyme involved in the secretion of proteins and glycoproteins in male 8 week old rats. 2. Using poly-Glu6, Ala3, Tyr1 (EAY) as sulfate acceptor, and 3'phosphoadenosine 5'-phosphosulfate (PAPS) as sulfate donor the optimum Golgi TPST activity was obtained at pH 6.8, in presence of 0.5% Triton X-100, 20 mM MnCl2, 50 mM NaF and 2 mM 5'-AMP. 3. Introduction of sofalcone to the reaction mixture led to the enhancement in TPST activity. The rate of stimulation was proportional to the drug concentration up to 30 micrograms, at which concentration, a 55% increase in TPST activity was attained. 4. The results attest further to the value of sofalcone as a potent mucosal strengthening agent, and suggest that the agent may promote mucin secretion via activation of tyrosine sulfation.
Research Center, New Jersey Dental School, University of Medicine and Dentistry of New Jersey, Newark 07103-2400.
C
C
Kasinathan
M
M
Rizwan
A
A
Slomiany
B L
BL
Slomiany
D000818:Animals; D000897:Anti-Ulcer Agents / Q000494:pharmacology*; D002599:Chalcone / Q000031:analogs & derivatives* / Q000494:pharmacology; D047188:Chalcones; D004789:Enzyme Activation / Q000187:drug effects; D005753:Gastric Mucosa / Q000187:drug effects* / Q000201:enzymology; D006863:Hydrogen-Ion Concentration; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D015238:Sulfotransferases / Q000378:metabolism*
D000897:Anti-Ulcer Agents; D047188:Chalcones; C035032:sofalcone; D002599:Chalcone; D015238:Sulfotransferases; C039079:protein-tyrosine sulfotransferase