Effects of sophoraflavanone G, a prenylated flavonoid from Sophora flavescens, on cyclooxygenase-2 and in vivo inflammatory response
Effects of sophoraflavanone G, a prenylated flavonoid from Sophora flavescens, on cyclooxygenase-2 and in vivo inflammatory response
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DOI：
10.1007/bf02976635
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发表时间：
2002-06-01
影响因子：
6.7
通讯作者：
Kim, HP
中科院分区：
文献类型：
--
作者：
Kim, DW;Chi, YS;Kim, HP
此前已有研究发现，几种含有C-8薰衣草基片段的烯酰化类黄酮具有抑制环氧合酶-1 （COX-1）和5-脂氧合酶（5-LOX）的活性，其中槐黄酮G是19种烯酰化类黄酮中对这些类二十烷生成酶最有效的抑制剂。本实验研究了槐黄酮G对RAW 264.7细胞COX-2诱导及体内炎症反应的影响。在1-50 uM下，槐黄酮G通过下调COX-2抑制脂多糖（LPS）处理的RAW细胞中前列腺素E-2 （PGE(2)）的产生。在10-25 μ m条件下，其他烯丙化黄酮类化合物，包括苦楝酮和桑根酮D也能下调COX-2的诱导，而苦楝酮和棘皮异黄酮则没有。此外，通过口服（2 ~ 250 mg/kg）或外用（10 ~ 250 ug/ kg）给药，槐黄酮G对巴豆油诱导的小鼠耳部水肿和大鼠角叉菜胶足部水肿具有体内抗炎活性。尽管抑制作用远不如参比药物强的松龙，但该化合物在局部应用时显示出更高的抗炎活性，这表明它可能用于几种类二十烷酸相关的皮肤炎症，如特应性皮炎。
Previously, several prenylated flavonoids having a C-8 lavandulyl moiety were found to inhibit cyclooxygenase-1 (COX-1) as well as 5-lipoxygenase (5-LOX), and sophoraflavanone G was the most potent inhibitor against these eicosanoid generating enzymes among 19 prenylated flavonoids tested. In this investigation, effects of sophoraflavanone G on COX-2 induction from RAW 264.7 cells and in vivo inflammatory response were studied. Sophoraflavanone G inhibited prostaglandin E-2 (PGE(2)) production from lipopolysaccharide (LPS)-treated RAW cells by COX-2 down-regulation at 1-50 uM. Other prenylated flavonoids including kuraridin and sanggenon D also down-regulated COX-2 induction at 10-25 uM, while kurarinone and echinoisoflavanone did not. In addition, sophoraflavanone G showed in vivo anti-inflammatory activity against mouse croton oil-induced ear edema and rat carrageenan paw edema via oral (2-250 mg/kg) or topical administration (10-250 ug/ear). Although the potencies of inhibition were far less than that of a reference drug, prednisolone, this compound showed higher anti-inflammatory activity when applied topically, suggesting a potential use for several eicosanoid-related skin inflammation such as atopic dermatitis.