Harris R R, Batt D G, Galbraith W, Ackerman N R
Medical Products Department, E. I. Du Pont de Nemours & Co., Wilmington, DE 19880-0400.
Agents Actions. 1989 Jun;27(3-4):297-9. doi: 10.1007/BF01972803.
Recent work suggests that one of the common biochemical characteristics of skin inflammatory diseases such as psoriasis is altered arachidonic acid metabolism with elevated levels of prostaglandins and leukotrienes. DuP 654, a 2-substituted 1-naphthol, is an exceptionally potent inhibitor of 5-lipoxygenase. DuP 654 was tested in various models of skin inflammation and was found to be potent at inhibiting edema induced by the topical application of arachidonic acid, tetradecanoyl phorbol acetate or the calcium ionophore A23187. DuP 654 was also effective in a murine model of contact sensitivity. DuP 654 was effective at reducing the numbers of infiltrating polymorphonuclear leukocytes in AA and TPA induced edema. These data, taken together, suggest that DuP 654 may be effective in treating human skin diseases.
近期研究表明，诸如牛皮癣等皮肤炎症性疾病的常见生化特征之一是花生四烯酸代谢改变，前列腺素和白三烯水平升高。DuP 654，一种2-取代的1-萘酚，是一种极其有效的5-脂氧合酶抑制剂。在各种皮肤炎症模型中对DuP 654进行了测试，发现它能有效抑制局部应用花生四烯酸、十四烷酰佛波醇乙酸酯或钙离子载体A23187所诱导的水肿。DuP 654在接触性敏感的小鼠模型中也有效。DuP 654能有效减少花生四烯酸和十四烷酰佛波醇乙酸酯诱导的水肿中浸润的多形核白细胞数量。综合这些数据表明，DuP 654可能对治疗人类皮肤疾病有效。
