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人胃黏膜中前列腺素的合成及其药物修饰

On the synthesis of prostaglandins by human gastric mucosa and its modification by drugs.

作者信息

Peskar B M

出版信息

Biochim Biophys Acta. 1977 May 25;487(2):307-14. doi: 10.1016/0005-2760(77)90007-8.

Abstract
  1. Specific radioimmunoassays for the prostaglandins E2, A2 and F2alpha were used to study the synthesis of prostaglandins by gastroscopically obtained small biopsy specimens of human gastric corpus mucosa. 2. Both prostaglandin E2 and prostaglandin F2alpha were found to be synthesized from arachidonic acid by themicrosomal fraction of human gastric mucosa. The synthesis of prostaglandin E2 exceeded that of prostagladin F2alpha by a factor of about 10. 3. Synthesis of prostaglandin A2 or prostaglandin B2 was not observed under the same incubation conditions. 4. Indometacin effectively inhibited synthesis of both prostaglandin E2 (ID50 4.2 microng/ml) and prostaglandin F2alpha (ID50 1.8 microng/ml) by human gastric mucosa, while paracetamol even in a concentration of 310 microng/ml did not influence prostaglandin synthesis. The anti-ulcer agent carbenoxolone, which has been shown to inhibit prostaglandin inactivation, at the same concentration only slightly inhibited (about 20%) prostaglandin synthesis. 5. The results support the hypothesis that the gastro-intestinal effects or side effects of several drugs are mediated by an influence on the enzymes of prostaglandin synthesis or inactivation.
摘要
  1. 采用前列腺素E2、A2和F2α的特异性放射免疫分析法,研究通过胃镜获取的人胃体黏膜小活检标本中前列腺素的合成情况。2. 发现人胃黏膜微粒体部分可从花生四烯酸合成前列腺素E2和前列腺素F2α。前列腺素E2的合成量比前列腺素F2α高出约10倍。3. 在相同孵育条件下未观察到前列腺素A2或前列腺素B2的合成。4. 吲哚美辛可有效抑制人胃黏膜前列腺素E2(半数抑制浓度4.2微克/毫升)和前列腺素F2α(半数抑制浓度1.8微克/毫升)的合成,而对乙酰氨基酚即使浓度达310微克/毫升也不影响前列腺素合成。已证明具有抑制前列腺素失活作用的抗溃疡药物甘珀酸,在相同浓度下仅轻微抑制(约20%)前列腺素合成。5. 这些结果支持以下假说:几种药物的胃肠道效应或副作用是通过对前列腺素合成或失活酶的影响介导的。

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