VASODILATORY EFFECTS OF FLAVONOIDS IN RAT AORTIC SMOOTH-MUSCLE - STRUCTURE-ACTIVITY-RELATIONSHIPS
VASODILATORY EFFECTS OF FLAVONOIDS IN RAT AORTIC SMOOTH-MUSCLE - STRUCTURE-ACTIVITY-RELATIONSHIPS
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DOI：
10.1016/0306-3623(93)90159-u
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发表时间：
1993-07-01
期刊：
影响因子：
--
通讯作者：
ZARZUELO, A
中科院分区：
文献类型：
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作者：
DUARTE, J;VIZCAINO, FP;ZARZUELO, A
1.黄酮类化合物对去甲肾上腺素、KCl或佛波醇12-肉豆蔻酸、13-乙酸酯引起的大鼠主动脉收缩有松弛作用，其作用强弱顺序为：黄酮醇类(槲皮素、山奈酚、五甲基槲皮素)>黄酮类(木犀草素、芹菜素)>黄烷醇类((+)-儿茶素、(-)-表儿茶素)。与报告的抑制蛋白激酶 C.2 的效力顺序相关。异丙肾上腺素略微增强山奈酚和木犀草素的松弛作用，硝普钠略微增强五甲基槲皮素、山奈酚和芹菜素的松弛作用。3．结论是，黄酮类化合物的主要舒血管机制似乎是抑制蛋白激酶C。抑制环核苷酸磷酸二酯酶或减少Ca2+摄取也可能有助于其舒血管作用。
1. Flavonoids relaxed the contractions induced by noradrenaline, KCl or phorbol 12-myristate,13-acetate in rat aortic strips, the order of potency being: flavonols (quercetin, kaempferol, pentamethylquercetin) > flavones(luteolin, apigenin) > flavanols((+)-catechin, (-)-epicatechin) which correlates with the reported order of potency to inhibit protein kinase C.2. The relaxant effects of kaempferol and luteolin were slightly potentiated by isoprenaline and those of pentamethylquercetin, kaempferol and apigenin by sodium nitroprusside.3. It is concluded that the main vasodilatory mechanism of flavonoids seems to be the inhibition of protein kinase C. Inhibition of cyclic nucleotide phosphodiesterases or decreased Ca2+ uptake may also contribute to their vasodilatory effects.