Prieto J M, Recio M C, Giner R M, Máñez S, Giner-Larza E M, Ríos J L
Departament de Farmacologia, Facultat de Farmàcia, Universitat de València, Burjassot, Spain.
J Pharm Pharmacol. 2003 Sep;55(9):1275-82. doi: 10.1211/0022357021620.
The enzymes 5-lipoxygenase and elastase are therapeutic targets in dermatological disorders such as psoriasis. Fifteen extracts from traditional Chinese medicinal plants used to treat topical inflammations were screened for their inhibitory effect on lipoxygenase, cyclooxygenase and elastase activity in intact leukocytes and platelets. Astragalus membranaceus, Forsythia suspensa and Poria cocos inhibited 5-lipoxygenase, with IC50 values of 141, 80 and 141 microg mL(-1), respectively. The latter two species, along with Angelica dahurica and Angelica pubescens, also inhibited elastase (IC50 values of 80, 123, 68 and 93 microg mL(-1), respectively), while A. pubescens, Atractylodes macrocephala, Lentinus edodes, Rehmannia glutinosa and Paeonia lactiflora selectively inhibited 12-(S)-HHTrE production, a valid marker of cyclooxygenase activity. The inhibition of phospholipase A(2) activity by P. cocos is discussed. Dehydrotumulosic and pachymic acids, which have been isolated from P. cocos, were shown to inhibit leukotriene B(4) release. The results indicate that both P. cocos and F. suspensa are potentially valuable species in the management of skin pathologies involving chronic inflammation.
5-脂氧合酶和弹性蛋白酶是银屑病等皮肤病的治疗靶点。对15种用于治疗局部炎症的传统中药植物提取物进行了筛选,考察它们对完整白细胞和血小板中脂氧合酶、环氧化酶和弹性蛋白酶活性的抑制作用。黄芪、连翘和茯苓抑制5-脂氧合酶,IC50值分别为141、80和141μg mL(-1)。后两种植物以及白芷和独活也抑制弹性蛋白酶(IC50值分别为80、123、68和93μg mL(-1)),而独活、白术、香菇、生地黄和芍药选择性抑制12-(S)-HHTre生成,这是环氧化酶活性的有效标志物。讨论了茯苓对磷脂酶A(2)活性的抑制作用。从茯苓中分离出的去氢土莫酸和茯苓酸显示出抑制白三烯B(4)释放的作用。结果表明,茯苓和连翘在治疗涉及慢性炎症的皮肤疾病方面都具有潜在的价值。