Mrowietz U, Falsafi M, Schröder J M, Christophers E
Department of Dermatology, University of Kiel, Germany.
Br J Dermatol. 1992 Oct;127(4):382-6. doi: 10.1111/j.1365-2133.1992.tb00458.x.
Anthralin is a well-established and widely used compound for topical treatment of psoriasis. In recent years attention has been focused on the anti-inflammatory properties of anthralin, with particular reference to psoriasis. In this study the effect of anthralin on human monocyte chemotaxis, superoxide-anion generation, and enzyme degranulation, were investigated. For comparison, the effect of the clinically inactive anthralin derivative danthrone and the solvent (acetone) were also studied. The results show that anthralin potently inhibits stimulated human monocyte superoxide-anion generation and enzyme degranulation, with a half-maximal inhibitory concentration (IC50) of as low as 0.02 micrograms/ml. Chemotactic migration of monocytes, however, was only affected when very high doses of anthralin (10 micrograms/ml) were used for pretreatment of the cells. Danthrone, up to a concentration of 10 micrograms/ml, or acetone alone (0.1%, v/v), did not inhibit the monocyte functions tested. Our results indicate that anthralin at pharmacological concentrations is a potent and selective inhibitor of human monocyte pro-inflammatory activities, by inhibiting respiratory burst activity (e.g. superoxide-anion generation) and enzyme degranulation, without affecting chemotactic migration.
蒽林是一种成熟且广泛用于银屑病局部治疗的化合物。近年来，人们的注意力集中在蒽林的抗炎特性上，尤其是与银屑病相关的特性。在本研究中，研究了蒽林对人单核细胞趋化性、超氧阴离子生成和酶脱颗粒的影响。为作比较，还研究了临床无活性的蒽林衍生物丹蒽醌和溶剂（丙酮）的作用。结果表明，蒽林能有效抑制刺激后的人单核细胞超氧阴离子生成和酶脱颗粒，其半数最大抑制浓度（IC50）低至0.02微克/毫升。然而，只有当用非常高剂量的蒽林（10微克/毫升）对细胞进行预处理时，单核细胞的趋化迁移才会受到影响。浓度高达10微克/毫升的丹蒽醌或单独的丙酮（0.1%，v/v）均未抑制所测试的单核细胞功能。我们的结果表明，在药理浓度下，蒽林通过抑制呼吸爆发活性（如超氧阴离子生成）和酶脱颗粒，而不影响趋化迁移，是一种有效的人单核细胞促炎活性选择性抑制剂。
