Activity-Based Photosensitizers with Optimized Triplet State Characteristics Toward Cancer Cell Selective and Image Guided Photodynamic Therapy,ACS Applied Bio Materials

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Activity-Based Photosensitizers with Optimized Triplet State Characteristics Toward Cancer Cell Selective and Image Guided Photodynamic Therapy
ACS Applied Bio Materials ( IF 4.6 ) Pub Date : 2022-05-10 , DOI: 10.1021/acsabm.2c00202
Eda Kilic ₁ , Zubeyir Elmazoglu ₂ , Toghrul Almammadov ₁ , Dilay Kepil ₂ , Thibaud Etienne ₃ , Antoine Marion ₂ , Gorkem Gunbas ₂ , Safacan Kolemen _{1,

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Affiliation

Activity-based theranostic photosensitizers are highly attractive in photodynamic therapy as they offer enhanced therapeutic outcome on cancer cells with an imaging opportunity at the same time. However, photosensitizers (PS) cores that can be easily converted to activity-based photosensitizers (aPSs) are still quite limited in the literature. In this study, we modified the dicyanomethylene-4H-chromene (DCM) core with a heavy iodine atom to get two different PSs (DCM_O-I, I-DCM_O-Cl) that can be further converted to aPS after simple modifications. The effect of iodine positioning on singlet oxygen generation capacity was also evaluated through computational studies. DCM_O-I showed better performance in solution experiments and further proved to be a promising phototheranostic scaffold via cell culture studies. Later, a cysteine (Cys) activatable PS based on the DCM_O-I core (DCM_O-I-Cys) was developed, which induced selective photocytotoxicity along with a fluorescence turn-on response in Cys rich cancer cells.

中文翻译：

具有优化三重态特征的基于活性的光敏剂，用于癌细胞选择性和图像引导光动力治疗

基于活性的治疗诊断光敏剂在光动力疗法中非常有吸引力，因为它们可以增强癌细胞的治疗效果，同时提供成像机会。然而，能够轻松转换为活性光敏剂（aPS）的光敏剂（PS）核心在文献中仍然相当有限。在本研究中，我们用重碘原子修饰二氰亚甲基-4H-色烯（DCM）核心，得到两种不同的PS（DCM _O -I，I-DCM _O -Cl），经过简单修饰后可以进一步转化为aPS 。还通过计算研究评估了碘定位对单线态氧生成能力的影响。 DCM _O -I 在溶液实验中表现出更好的性能，并通过细胞培养研究进一步证明是一种有前途的光治疗支架。后来，开发了一种基于 DCM _O -I 核心 (DCM _O -I-Cys) 的半胱氨酸 (Cys) 可激活 PS，它在富含 Cys 的癌细胞中诱导选择性光细胞毒性以及荧光开启反应。

更新日期：2022-05-10

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