Tordera M, Ferrándiz M L, Alcaraz M J
Departamento de Farmacología, Universidad de Valencia, Facultad de Farmacia, Spain.
Z Naturforsch C J Biosci. 1994 Mar-Apr;49(3-4):235-40. doi: 10.1515/znc-1994-3-412.
We assessed the effects of 24 flavonoid derivatives, reported as anti-inflammatory, on lysosomal enzyme secretion and arachidonic acid release in rat neutrophils. Amentoflavone, quercetagetin-7-O-glucoside, apigenin, fisetin, kaempferol, luteolin and quercetin were the most potent inhibitors of beta-glucuronidase and lysozyme release. The first compound was also able to inhibit basal release. These flavonoids besides chrysin and to a reduced extent, naringenin, significantly inhibited arachidonic acid release from membranes. A correlation between degranulation and arachidonic acid release was found for this series of compounds. Structure-activity relationships and implications for the anti-inflammatory effects of these flavonoids were discussed.
我们评估了24种据报道具有抗炎作用的黄酮类衍生物对大鼠中性粒细胞溶酶体酶分泌和花生四烯酸释放的影响。穗花杉双黄酮、泽兰黄酮-7-O-葡萄糖苷、芹菜素、非瑟酮、山奈酚、木犀草素和槲皮素是β-葡萄糖醛酸酶和溶菌酶释放的最有效抑制剂。第一种化合物还能够抑制基础释放。这些黄酮类化合物除了白杨素以及程度较低的柚皮素外，还能显著抑制膜中花生四烯酸的释放。对于这一系列化合物，发现脱颗粒与花生四烯酸释放之间存在相关性。讨论了这些黄酮类化合物的构效关系及其抗炎作用的意义。
