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索法酮对酪氨酰蛋白磺基转移酶的作用。

Effect of sofalcone on tyrosylprotein sulfotransferase.

作者信息

Kasinathan C, Rizwan M, Slomiany A, Slomiany B L

机构信息

Research Center, New Jersey Dental School, University of Medicine and Dentistry of New Jersey, Newark 07103-2400.

出版信息

Gen Pharmacol. 1994 Sep;25(5):1017-20. doi: 10.1016/0306-3623(94)90112-0.

Abstract
  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.
摘要
  1. 胃黏液糖蛋白积极参与维持黏膜完整性,其合成过程受损往往是胃部病理学的一个显著特征。在本研究中,我们调查了抗溃疡药物索法酮对8周龄雄性大鼠中参与蛋白质和糖蛋白分泌的酪氨酰蛋白磺基转移酶活性的影响。2. 以聚-Glu6、Ala3、Tyr1(EAY)作为硫酸盐受体,3'-磷酸腺苷5'-磷酸硫酸酯(PAPS)作为硫酸盐供体,在pH 6.8、存在0.5% Triton X-100、20 mM MnCl2、50 mM NaF和2 mM 5'-AMP的条件下可获得最佳高尔基体TPST活性。3. 将索法酮引入反应混合物导致TPST活性增强。刺激速率与药物浓度成正比,直至30微克,在该浓度下,TPST活性提高了55%。4. 结果进一步证明了索法酮作为一种有效的黏膜强化剂的价值,并表明该药物可能通过激活酪氨酸硫酸化促进黏蛋白分泌。

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