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黄酮类化合物的体内抗聚集作用及其对体外脂氧合酶和环氧化酶的影响。

Antiaggregatory effects of flavonoids in vivo and their influence on lipoxygenase and cyclooxygenase in vitro.

作者信息

Swies J, Robak J, Dabrowski L, Duniec Z, Michalska Z, Gryglewski R J

出版信息

Pol J Pharmacol Pharm. 1984 Sep-Oct;36(5):455-63.

PMID:6442773
Abstract

Quercetin, rutin and troxerutin were found to inhibit platelet aggregation on collagen strip superfused with blood of anesthetized cats. Quercetin was the most potent acting at the dose of 1 micrograms/kg. Its effect was shortlasting. Troxerutin was a weak inhibitor of platelet aggregation and its effect was delayed. Quercetin inhibited in 50% 15-lipoxygenase and 12-lipoxygenase in vitro at the concentration of 1.3 microm and 13 microM respectively. It stimulated cyclooxygenase when 100 microM of arachidonic acid was applied. Quercetin inhibited cyclooxygenase in the presence of 1.6 microM of substrate. Rutin was a weaker inhibitor of lipoxygenase. Troxerutin was inactive in all experiments in vitro. It is concluded that unusually strong effect of quercetin in vivo can be explained neither by its influence on cyclooxygenase nor on lipoxygenase because the effects in vitro were observed in much higher concentrations.

摘要

槲皮素、芦丁和曲克芦丁被发现可抑制在麻醉猫血液灌注的胶原条上的血小板聚集。槲皮素在1微克/千克的剂量下作用最强。其作用持续时间短。曲克芦丁是血小板聚集的弱抑制剂,其作用延迟。槲皮素在体外分别以1.3微摩尔和13微摩尔的浓度抑制50%的15-脂氧合酶和12-脂氧合酶。当应用100微摩尔花生四烯酸时,它刺激环氧化酶。在存在1.6微摩尔底物的情况下,槲皮素抑制环氧化酶。芦丁是脂氧合酶的较弱抑制剂。曲克芦丁在所有体外实验中均无活性。得出的结论是,槲皮素在体内异常强大的作用既不能通过其对环氧化酶的影响也不能通过其对脂氧合酶的影响来解释,因为体外实验中的作用是在高得多的浓度下观察到的。

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