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首页> 外文期刊>Life sciences >Effects of naturally occurring dihydroflavonols from Inula viscosa on inflammation and enzymes involved in the arachidonic acid metabolism
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Effects of naturally occurring dihydroflavonols from Inula viscosa on inflammation and enzymes involved in the arachidonic acid metabolism

机译：天然来自Inula viscosa的二氢黄酮醇对花生四烯酸代谢中炎症和酶的影响

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The anti-inflammatory properties of three flavanones isolated from Inula viscosa, sakuranetin, 7-O-methylaromadendrin, and 3-acetyl-7-O-methylaromadendrin, have been tested both in vitro and in vivo. Acute inflammation in vivo was induced by means of topical application of 12-O-tetradecanoylphorbol 13-acetate (TPA) to mouse ears or by subcutaneous injection of phospholipase A(2) (PLA(2)) into mouse paws. The test compounds were evaluated in vitro for their effect on both the metabolism of arachidonic acid and on the release and/or activity of enzymes involved in the inflammatory response such as elastase, myeloperoxidase (MPO), and protein kinase C (PKC). The most active compounds in vivo against PLA(2)-induced paw oedema were 7-O-methylaromadendrin (ED50 = 8 mg/kg) and sakuranetin (ED50 = 18 mg/kg). In contrast, the most potent compound against TPA-induced ear oedema was 3-acetyl-7-O-methylaromadendrin (ED50=185 mu g/ear), followed by sakuranetin (ED50=205 mu g/ear). In vitro, the latter compound was the most potent inhibitor of leukotriene (LT) B-4 production by peritoneal rat neutrophils (IC50=9 mu M) and it was also the only compound that directly inhibited the activity of 5-lipoxygenase (5-LOX). 3-Acetyl-7-O-methylaromadendrin also inhibited LTB4 production (IC50= 15 mu M), but had no effect on 5-LOX activity. The only flavanone that inhibited the secretory PLA, activity in vitro was 7-O-methylaromadendrin. This finding may partly explain the anti-inflammatory effect observed in vivo, although other mechanisms such as the inhibition of histamine release by mast cells may also be implicated. Sakuranetin at 100 mu M was found to inhibit elastase release, although this result is partly due to direct inhibition of the enzyme itself At the same concentration, 7-O-methylaromadendrin only affected the enzyme release. Finally, none of the flavanones exhibited any effect on MPO or PKC activities. Taken together, these findings indicate that sakuranetin may be a selective inhibitor of 5-LOX. (c) 2007 Elsevier Inc. All rights reserved.
机译：已经从体内和体外测试了从Inula viscosa，sakuranetin，7-O-甲基香豆精和3-乙酰基-7-O-甲基香豆精中分离出的三种黄烷酮的抗炎特性。通过在小鼠耳朵上局部应用12-O-十四烷酰佛波醇13-乙酸盐（TPA）或通过向小鼠爪中皮下注射磷脂酶A（2）（PLA（2））诱导体内急性炎症。体外评估了测试化合物对花生四烯酸代谢以及与炎症反应有关的酶（如弹性蛋白酶，髓过氧化物酶（MPO）和蛋白激酶C（PKC））的释放和/或活性的影响。体内针对PLA（2）引起的爪水肿的活性最高的化合物是7-O-甲基芳樟脑（ED50 = 8 mg / kg）和sakuranetin（ED50 = 18 mg / kg）。相反，对抗TPA引起的耳部水肿的最有效的化合物是3-乙酰基-7-O-甲基芳基马德林（ED50 = 185微克/耳），其次是樱红素（ED50 = 205微克/耳）。在体外，后一种化合物是腹膜大鼠中性粒细胞（IC50 = 9μM）产生白三烯（LT）B-4的最有效抑制剂，它也是唯一直接抑制5-脂氧合酶（5-熏鲑鱼）。 3-乙酰基-7-O-甲基芳樟脑素也抑制LTB4的产生（IC50 = 15μM），但对5-LOX活性没有影响。在体外，唯一抑制分泌型PLA的黄烷酮活性是7-O-甲基香豆精。该发现可能部分解释了体内观察到的抗炎作用，尽管也可能涉及其他机制，例如肥大细胞抑制组胺释放。发现Sakuranetin在100μM时可抑制弹性蛋白酶的释放，尽管此结果部分是由于对酶本身的直接抑制。在相同的浓度下，7-O-甲基芳族马登精仅影响酶的释放。最后，黄烷酮对MPO或PKC活性均无影响。综上所述，这些发现表明sakuranetin可能是5-LOX的选择性抑制剂。 （c）2007 Elsevier Inc.保留所有权利。

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