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半胱氨酸蛋白酶木瓜蛋白酶对胃动力的区域特异性影响。

Region-specific effects of the cysteine protease papain on gastric motility.

机构信息

Chair of Human Biology, Technical University of Munich, Freising, Germany.

出版信息

Neurogastroenterol Motil. 2021 Jul;33(7):e14105. doi: 10.1111/nmo.14105. Epub 2021 Mar 12.

Abstract

BACKGROUND

Papaya is a traditional remedy for gastrointestinal complaints in the folk medicine. On this basis, papain, a cysteine protease of the fruit, is sold as a nutritional supplement, although scientific data on its effects in the gastrointestinal tract are lacking. We aimed to explore the effect of papain on gastric motility in vitro.

METHODS

Guinea pig antrum and corpus strips were mounted in organ bath.

KEY RESULTS

Papain reversibly increased the amplitude of ongoing phasic contractions in both circular and longitudinal antrum strips without having an effect on the frequency or on the muscle tone. All three tested doses of papain (end cc.: 12.5 mg L , 50 mg L , 100 mg L ) were similarly effective. Contrarily, in the corpus circular and longitudinal muscle strips, papain caused a dose-dependent relaxation, which was preceded by a transient contraction in most tissues. The effect was resistant to tetrodotoxin (1 µM), but diminished by the cysteine protease inhibitor E64 (4.5 µM) in both regions. In the corpus, L-NAME (100 µM) and the protease-activated receptor (PAR)-1 antagonist SCH79797 (5 µM) or the PAR-2 antagonist GB 83 (3 µM) did not change the effect of papain significantly. This demonstrates that the effects of papain are not neurally mediated and nitrergic pathways are not involved in the mechanism. The effects are linked to the enzymatic activity, but not executed via PAR-1 or 2.

CONCLUSIONS AND INFERENCES

Papain alters gastric motility in a region-specific manner, which could at least partly explain its claimed beneficial effects in functional gastrointestinal disorders.

摘要

背景

木瓜在民间医学中是一种治疗胃肠道疾病的传统药物。在此基础上,木瓜中的一种半胱氨酸蛋白酶——木瓜蛋白酶,作为一种营养补充剂被销售,尽管其在胃肠道中的作用缺乏科学数据。我们旨在探索木瓜蛋白酶对体外胃动力的影响。

方法

将豚鼠胃窦和胃体条带安装在器官浴中。

主要结果

木瓜蛋白酶可逆地增加了胃窦环行和纵行肌条带中持续相位收缩的幅度,而对频率或肌肉张力没有影响。三种测试剂量的木瓜蛋白酶(终浓度:12.5mg/L、50mg/L、100mg/L)同样有效。相反,在胃体环行和纵行肌条带中,木瓜蛋白酶引起剂量依赖性的松弛,在大多数组织中,松弛前先出现短暂的收缩。这种作用对河豚毒素(1µM)有抗性,但在两个区域中,半胱氨酸蛋白酶抑制剂 E64(4.5µM)会减弱这种作用。在胃体中,L-NAME(100µM)和蛋白酶激活受体(PAR)-1拮抗剂 SCH79797(5µM)或 PAR-2 拮抗剂 GB 83(3µM)对木瓜蛋白酶的作用没有明显改变。这表明木瓜蛋白酶的作用不是通过神经介导的,也不涉及氮能通路。这种作用与酶的活性有关,但不是通过 PAR-1 或 PAR-2 执行的。

结论和推论

木瓜蛋白酶以区域特异性的方式改变胃动力,这至少可以部分解释其在功能性胃肠疾病中声称的有益作用。

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