Study Centre for Clinical Trials, Dermatology, Gesellschaft für Wissens- und Technologietransfer der Technischen Universität Dresden mbH, Blasewitzer Str. 43, 01307, Dresden, Germany,
Arch Dermatol Res. 2014 Mar;306(2):103-24. doi: 10.1007/s00403-013-1409-7. Epub 2013 Dec 6.
Dapsone (4,4'-diaminodiphenylsulfone) is an aniline derivative belonging to the group of synthetic sulfones. In 1937 against the background of sulfonamide era the microbial activity of dapsone has been discovered. Shortly thereafter, the use of dapsone to treat non-pathogen-caused diseases revealed alternate antiinflammatory mechanisms that initially were elucidated by inflammatory animal models. Thus, dapsone clearly has dual functions of both: antimicrobial/antiprotozoal effects and anti-inflammatory features similarly to non-steroidal anti-inflammatory drugs. The latter capabilities primarily were used in treating chronic inflammatory disorders. Dapsone has been investigated predominantly by in vitro methods aiming to get more insights into the effect of dapsone to inflammatory effector cells, cytokines, and/or mediators, such as cellular toxic oxygen metabolism, myoloperoxidase-/halogenid system, adhesion molecules, chemotaxis, membrane-associated phospholipids, prostaglandins, leukotrienes, interleukin-8, tumor necrosis factor α, lymphocyte functions, and tumor growth. Moreover, attention has been paid to mechanisms by which dapsone mediates effects in more complex settings like impact of lifespan, stroke, glioblastoma, or as anticonvulsive agent. Additionally, there are some dermatological investigations in human being using dapsone and its metabolites (e.g., leukotriene B4-induced chemotaxis, ultraviolet-induced erythema). It could be established that dapsone metabolites by their own have anti-inflammatory properties. Pharmacology and mechanisms of action are determining factors for clinical use of dapsone chiefly in neutrophilic and/or eosinophilic dermatoses and in chronic disorders outside the field of dermatology. The steroid-sparing effect of dapsone is useful for numerous clinical entities. Future avenues of investigations will provide more information on this fascinating and essential agent.
氨苯砜（4,4'-二氨基二苯砜）是一种苯胺衍生物，属于合成砜类。1937 年，在磺胺类药物时代的背景下，发现了氨苯砜的微生物活性。此后不久，人们发现氨苯砜可用于治疗非病原体引起的疾病，并揭示了最初通过炎症动物模型阐明的替代抗炎机制。因此，氨苯砜具有双重作用：抗菌/抗原生动物作用和抗炎作用，类似于非甾体抗炎药。后一种作用主要用于治疗慢性炎症性疾病。人们主要通过体外方法研究氨苯砜，旨在更深入地了解氨苯砜对炎症效应细胞、细胞因子和/或介质的作用，如细胞毒性氧代谢、髓过氧化物酶/卤化物系统、粘附分子、趋化性、膜相关磷脂、前列腺素、白三烯、白细胞介素-8、肿瘤坏死因子α、淋巴细胞功能和肿瘤生长。此外，人们还关注了氨苯砜在更复杂环境中发挥作用的机制，如寿命、中风、胶质母细胞瘤或作为抗惊厥剂的影响。此外，还有一些关于人类使用氨苯砜及其代谢物（如白三烯 B4 诱导的趋化性、紫外线诱导的红斑）的皮肤科研究。已经确定，氨苯砜代谢物本身具有抗炎特性。药理学和作用机制是决定氨苯砜主要在中性粒细胞和/或嗜酸性粒细胞皮肤病以及皮肤科以外的慢性疾病中的临床应用的因素。氨苯砜的类固醇节约作用对许多临床实体都很有用。未来的研究方向将为这种引人入胜且必不可少的药物提供更多信息。
