Tonew E, Kittler L, Hesse G, Schade W
Zentralbl Bakteriol Orig A. 1979 Sep;244(4):417-26.
Eleven pyrimido-pyrimidine derivatives, seven with significant antiviral activity against Mengovirus, five against Coxsackie B1 virus and four antiviral negative compounds were tested for their photosensitizing ability. All seven compounds with antiviral activity in vitro showed an enhanced antiviral action against Mengovirus under irradiation with visible light, a fact that may be caused by photodynamic processes. It was tried to correlate the oxidation potentials of sensitizers with their photodynamic activity. By means of mass-spectrometric investigations, molecular fragmentation was examined following thin layer chromatography (TCL) before and after irradiation. Furthermore, binding affinity to biopolymers (BSA and RNA) was investigated to reveal conformity in differences of antiviral activity. The main results are the following: 1. Generally, strong antiviral activity can be correlated with strong binding affinity. 2. No significant correlation could be detected between oxidation potentials of antiviral compounds and their enhanced antiviral activity under irradiation conditions, although in some cases sensitizer with higher oxidation potentials are more effective than those with lower ones. 3. The lower the photostability of the compounds the higher was the light-induced antiviral activity. 4. No alteration of the molecular ion peak and fragmentation pattern before and after irradiation was indicated by means of mass-spectrometry and TLC using fairly comparable conditions.
测试了11种嘧啶并嘧啶衍生物、7种对门戈病毒具有显著抗病毒活性的化合物、5种对柯萨奇B1病毒具有抗病毒活性的化合物以及4种抗病毒阴性化合物的光敏能力。所有7种具有体外抗病毒活性的化合物在可见光照射下对门戈病毒均表现出增强的抗病毒作用，这一事实可能是由光动力过程引起的。试图将敏化剂的氧化电位与其光动力活性相关联。通过质谱研究，在薄层色谱（TCL）照射前后检查分子碎片。此外，还研究了与生物聚合物（牛血清白蛋白和RNA）的结合亲和力，以揭示抗病毒活性差异的一致性。主要结果如下：1.一般来说，强抗病毒活性与强结合亲和力相关。2.在照射条件下，抗病毒化合物的氧化电位与其增强的抗病毒活性之间未检测到显著相关性，尽管在某些情况下，氧化电位较高的敏化剂比氧化电位较低的敏化剂更有效。3.化合物的光稳定性越低，光诱导的抗病毒活性越高。4.在相当可比的条件下，通过质谱和薄层色谱法未表明照射前后分子离子峰和碎片模式有变化。
