Lignan and phenylpropanoid glycosides from Phillyrea latifolia and their in vitro anti-inflammatory activity
Lignan and phenylpropanoid glycosides from Phillyrea latifolia and their in vitro anti-inflammatory activity
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DOI：
10.1055/s-2001-12004
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发表时间：
2001-04-01
期刊：
影响因子：
2.7
通讯作者：
Benito, PB
中科院分区：
文献类型：
--
作者：
Lanza, AMD;Martínez, MJA;Benito, PB
测试了从Phillyrea latifolia L.（木犀科）叶子中分离出的三种苯丙素苷（红景天苷、紫丁香苷和松柏苷）和一种木脂素（连翘苷）与钙刺激的小鼠腹腔巨噬细胞和人血小板中花生四烯酸代谢的环氧化酶和5-脂氧化酶途径的相互作用，以及它们对细胞活力的影响。这些化合物能够对花生四烯酸级联酶发挥抑制作用。连翘苷、红景天苷和丁香苷对环加氧酶途径发挥优先作用，抑制环加氧酶代谢物前列腺素 E-2 的释放（IC50 值分别为 45.6 μM、72.1 μM 和 35.5 μM），并在较小程度上降低血栓素 B-2 水平（IC50 值分别为 168 μM、154 μM 和 29.3）相比之下，松柏素可以被归类为“双重抑制剂”，因为它可以减少环加氧酶（前列腺素 E-2 的 IC50 值为 75.2 muM，血栓素 B-2 的 IC50 值为 619 muM）和 5-脂氧合酶代谢物的产生，但对白三烯 C-4 的影响更大（IC50 值为 63.6 muM）。讨论了三种苯丙苷的构效关系。因此，与药草中发现的其他一些化合物一样，我们的分子具有一系列潜在有益的抗类二十烷酸特性，这些特性可能与其他成分一起有助于其来源植物所声称的治疗特性。
Three phenylpropanoid glycosides (salidroside, syringin and coniferin) and one lignan (phillyrin) isolated from the leaves of Phillyrea latifolia L. (Oleaceae) were tested for interactions with the cyclo-oxygenase and 5-lipoxygenase pathways of arachidonate metabolism in calcium-stimulated mouse peritoneal macrophages and human platelets, and for their effects on cell viability. These compounds are capable of exerting inhibitory actions on enzymes of the arachidonate cascade. Phillyrin, salidroside and syringin exert a preferential effect on the cyclooxygenase pathway, inhibiting release of the cyclo-oxygenase metabolites prostaglandin E-2 (IC50 values 45.6 muM, 72.1 muM and 35.5 muM, respectively) and to a lesser extent reducing thromboxane B-2 levels (IC50 values 168 muM. 154 muM and 29.3 muM. respectively), In contrast, coniferin can be classified as a "dual inhibitor", since it produces reduction in generation of both cyclo-oxygenase (IC50 values 75.2 muM for prostaglandin E-2 and 619 muM for thromboxane B-2) and 5-lipoxygenase metabolites, but the effects are greater against leukotriene C-4 (IC50 Value 63.6 muM). Structure-activity relationships of the three phenylpropanoid glycosides are discussed. Thus, like some other compounds found in medicinal herbs, our molecules possess an array of potentially beneficial anti-eicosanoid properties which may, alongside other constituents, contribute to the claimed therapeutic properties of the plant from which they are derived.