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依溴替丁对幽门螺杆菌蛋白水解和脂肪分解活性的影响。

Ebrotidine effect on the proteolytic and lipolytic activities of Helicobacter pylori.

作者信息

Slomiany B L, Piotrowski J, Mojtahed H, Slomiany A

机构信息

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

出版信息

Gen Pharmacol. 1992 Mar;23(2):203-6. doi: 10.1016/0306-3623(92)90010-h.

Abstract
  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.
摘要
  1. 研究了新型抗溃疡药物依溴替丁对幽门螺杆菌产生的蛋白酶和脂肪酶黏液降解活性的影响。2. 在没有依溴替丁的情况下,幽门螺杆菌蛋白酶会导致胃黏液蛋白大量降解,而幽门螺杆菌脂肪酶和磷脂酶A的作用会产生游离脂肪酸、单油酸甘油酯和溶血磷脂酰胆碱。3. 将依溴替丁引入孵育系统会导致黏液蛋白和脂质降解速率降低。蛋白水解抑制率与依溴替丁浓度成正比,直至35微克/毫升,此时黏液降解减少了57%,而在依溴替丁浓度为60微克/毫升时,磷脂酶A(96%)和脂肪酶(93%)的活性受到最大抑制。4. 结果表明,依溴替丁能够对抗幽门螺杆菌对胃黏液层蛋白质和脂质成分的黏液溶解活性。

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