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首页> 外文期刊>ChemPlusChem >beta-Ionic Conjugated Chlorin-Type Photosensitizers Based on Porpholactone: Synthesis, Photophysical Properties, and Photodynamic Activity
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beta-Ionic Conjugated Chlorin-Type Photosensitizers Based on Porpholactone: Synthesis, Photophysical Properties, and Photodynamic Activity

机译：基于卟啉酮的β-离子共轭氯型光敏剂：合成，光药性和光动力活动

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Porpholactones and their derivatives have attracted increasing attention for their promising application as photosensitizers. Reduction of the beta-lactone moiety in porpholactone to beta-hemiacetal, named porpholactol, allows the synthesis of chlorin-type photosensitizers with enhanced near-infrared absorption as well as beta functionalization of water-soluble conjugates. By employing beta-hydrophilic conjugates terminated by different ionic groups, such as neutral (ZnL1), anionic (ZnL2), zwitterionic (ZnL3), and cationic (ZnL4-6) groups, a series of photosensitizers (ZnL1-6) were synthesized and characterized, and their photophysical properties were studied, including magnetic circular dichroism measurement. The terminal ionic groups on beta conjugates influence significantly the cellular uptake of ZnL1-6 in the order ZnL4-6 (positive charge) > ZnL1-3 (negative charge or neutral). Importantly, the photocytotoxicity of ZnL1-6 against cancer cells showed IC50 values down to the sub-micromolar range and exhibited the same trend as their cellular uptake, clearly revealing the relationship of beta-ionic conjugates, cellular uptake, and intracellular photodynamic therapy (PDT) activity. Furthermore, using ZnL4 as an example, mechanistic studies, such as cell imaging experiments and Western blot analysis for the PDT process, indicate that ZnL4 exerts photodynamic activity through apoptosis, which is highly associated with lysosome disruption, mitochondria depolarization, and nuclei condensation.
机译：卟啉甲酰胺及其衍生物引起了越来越多的关注，因为他们希望的应用程序作为光敏剂。将β-内甲酮部分的β-内酯部分减少到β-半血缩醛，命名卟啉醇，允许合成具有增强的近红外吸收和水溶性缀合物的β官能化的氯型光敏剂。通过使用由不同离子基团终止的β-亲水缀合物，例如中性（ZnL1），阴离子（ZnL2），两性离子（ZnL3）和阳离子（ZnL4-6）基团，合成一系列光敏剂（ZnL1-6）和研究了其表征，并研究了它们的光物理性质，包括磁性圆形二色性测量。 β缀合物的末端离子基团在ZnL4-6（正电荷）> ZnL1-3（负电荷或中性）中显着影响ZnL1-6的细胞摄取。重要的是，ZnL1-6对癌细胞的光致毒性显示IC50值下降到亚微摩尔范围，并表现出与其细胞摄取相同的趋势，清楚地揭示了β离子缀合物，细胞摄取和细胞内光动力治疗的关系（PDT ） 活动。此外，使用ZnL4作为示例，机械研究，例如用于PDT工艺的细胞成像实验和蛋白质印迹分析，表明ZnL4通过凋亡施加光动力活性，这与溶酶体破碎，线粒体去极化和核缩合高度相关。

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