钯-四苯基卟啉对培养肿瘤细胞的光敏特性。

Anti-cancer drug design Pub Date : 2000-04-01
M Cañete, A Ortiz, A Juarranz, A Villanueva, S Nonell, J I Borrell, J Teixidó, J C Stockert
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引用次数: 0

摘要

在本研究中,我们描述了钯(II)-四苯基卟啉(PdTPP(0))诱导的HeLa细胞的光杀伤特性及其对有丝分裂指数(MI)的影响。四苯基卟啉(TPP(0))和PdCl2在二甲基甲酰胺中回流合成,蒸发,色谱纯化。将不同浓度的PdTPPo掺入双棕榈酰磷脂酰胆碱脂质体处理细胞,以21 mW/cm2的红光照射(λ > 600 nm)。在我们的实验条件下,没有发现药物的暗毒性。致死(LD(100))处理后,细胞在质膜上立即出现气泡,3-24 h后出现均匀的核凝聚和细胞质损失。在亚致死LD(25)和LD(40)治疗后6-8小时,心肌梗死增加,并且纺锤体微管改变的异常中期比例很高。在LD(75)处理8 h后观察到染色质凝结和断裂。这些结果表明,与TPP(0)相比,新的增敏剂PdTPPo具有更有效的光杀伤性能,在癌症的光动力治疗中具有重要价值。
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Photosensitizing properties of palladium-tetraphenylporphycene on cultured tumour cells.

In this study we describe photokilling properties and effects on the mitotic index (MI) of cultured HeLa cells induced by palladium(II)-tetraphenylporphycene (PdTPP(0)). The drug was synthesized by refluxing tetraphenylporphycene (TPP(0)) and PdCl2 in dimethylformamide, followed by evaporation and purification by chromatography. Cells were treated with different concentrations of PdTPPo incorporated into dipalmitoylphosphatidylcholine liposomes, and red light irradiation (lambda > 600 nm) was performed at 21 mW/cm2. No dark toxicity was found when the drug was applied under our experimental conditions. Using lethal (LD(100)) treatments, cells showed the immediate occurrence of bubbles on the plasma membrane, whereas homogeneous nuclear condensation and loss of cytoplasm appeared 3-24 h later. An increased MI was found 6-8 h after sublethal LD(25) and LD(40) treatments as well as a high proportion of abnormal metaphases with altered spindle microtubules. Chromatin condensation and fragmentation were observed 8 h after LD(75) treatments. These results show that in comparison with TPP(0), the new sensitizer PdTPPo has more efficient photokilling properties which could be very valuable for the photodynamic therapy of cancer.

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