豚鼠肺中前列腺素的失活及其抑制作用。
Prostaglandin inactivation in guinea-pig lung and its inhibition.
作者信息
Crutchley D J, Piper P J
出版信息
Br J Pharmacol. 1974 Oct;52(2):197-203. doi: 10.1111/j.1476-5381.1974.tb09700.x.
1 Several compounds were tested for their ability to inhibit prostaglandin metabolism in guinea-pig lungs.2 In isolated perfused lungs polyphoretin phosphate (PPP) inhibited prostaglandin metabolism being active at concentrations greater than 100 ng/ml and having an ID(50) of 2.15 mug/ml against prostaglandin E(2) metabolism and 1.55 mug/ml against prostaglandin F(2alpha) metabolism.3 At these doses no antagonism of the actions of prostaglandins was seen.4 Diphloretin phosphate (DPP) was more active on a weight for weight basis and inhibition of inactivation of prostaglandins was seen at concentrations greater than 10 ng/ml, the ID(50) being 0.54 mug/ml against both prostaglandins E(2) and F(2alpha).5 At concentrations greater than 5 mug/ml DPP antagonized the actions of prostaglandin F(2alpha).6 The sulphydryl-binders N-ethyl maleimide (NEM) and sodium p-chloromercuriphenyl sulphonate (PCMS) also inhibited prostaglandin inactivation by guinea-pig isolated lungs.7 All four compounds inhibited prostaglandin metabolism by a crude enzyme preparation from guinea-pig lungs.
测试了几种化合物抑制豚鼠肺中前列腺素代谢的能力。
在离体灌注肺中，聚磷酸根皮苷（PPP）抑制前列腺素代谢，其在浓度大于100 ng/ml时具有活性，对前列腺素E₂代谢的半数抑制浓度（ID₅₀）为2.15 μg/ml，对前列腺素F₂α代谢的ID₅₀为1.55 μg/ml。
在这些剂量下，未观察到对前列腺素作用的拮抗作用。
磷酸二根皮苷（DPP）按重量计算更具活性，在浓度大于10 ng/ml时可见对前列腺素失活的抑制作用，对前列腺素E₂和F₂α的ID₅₀均为0.54 μg/ml。
在浓度大于5 μg/ml时，DPP拮抗前列腺素F₂α的作用。
巯基结合剂N-乙基马来酰胺（NEM）和对氯汞苯磺酸钠（PCMS）也抑制豚鼠离体肺中前列腺素的失活。
所有这四种化合物均通过豚鼠肺的粗酶制剂抑制前列腺素代谢。
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