von Zabern I, Nolte R, Przyklenk H, Vogt W
Int Arch Allergy Appl Immunol. 1985;76(3):205-13. doi: 10.1159/000233693.
Incubation of normal human serum with different sulfonamides led to a dose-dependent inactivation of total hemolytic complement activity. A decrease of the activities of C1, C2, C3, C5 and one or several of the components C6-9 was observed after treatment of normal human serum with the sulfonamide sulfisomidine. Inactivation of complement components by sulfonamides seems to result from direct interaction with the drug as well as, to a minor extent, from activation of the alternative pathway. At relatively high concentrations, sulfonamides caused a conformational change in C3 and C4. The observed structural change is equivalent to that induced by cleavage of the internal thiolester bond in these molecules. The generation of such structurally altered C3 (C3b-like C3) as well as an antagonizing effect of sulfonamides towards the action of the regulatory protein factor I might be responsible for alternative pathway activation. The physiological relevance in vivo of the observed effects of sulfonamides remains to be assessed.
将正常人血清与不同的磺胺类药物一起温育，导致总溶血补体活性呈剂量依赖性失活。用磺胺类药物磺胺异嘧啶处理正常人血清后，观察到C1、C2、C3、C5以及C6 - 9中的一种或几种成分的活性降低。磺胺类药物对补体成分的失活似乎是由于与药物的直接相互作用，以及在较小程度上由于替代途径的激活。在相对高的浓度下，磺胺类药物引起C3和C4的构象变化。观察到的结构变化等同于这些分子中内部硫酯键断裂所诱导的变化。这种结构改变的C3（类似C3b的C3）的产生以及磺胺类药物对调节蛋白I因子作用的拮抗作用可能是替代途径激活的原因。磺胺类药物所观察到的效应在体内的生理相关性仍有待评估。
