Department of Pharmaceutical Science & Technology, College of Chemistry and Biology, DongHua University, Shanghai, 201620, China.
Shanghai Xianhui Pharmaceutical Co., Ltd, Shanghai, 200433, China.
Sci Rep. 2021 May 11;11(1):10013. doi: 10.1038/s41598-021-89081-y.
Carbon based polymer dots have piqued attention of researchers because of excellent biocompatibility, and good solubility. Most of the p-dots are able to generate ROS which is effective for photodynamic therapy for the treatment of cancer while some photosensitizers such as porphyrins possess some drawbacks such as hydrophobicity, and dark toxicity. Therefore in this study we conjugated red emission carbon based polymer with pyropheophorbide-α through amide condensation and π-π stacking. One pot synthesis of the conjugate was successfully achieved. Their photophysiological properties were studied and structures were characterized by FT-IR, TEM and HNMR. pH- sensitivity of the conjugates was confirmed using fluorescence and UV-vis spectroscopy. Photo toxicity and dark toxicity of the prepared conjugates were evaluated in human esophageal cancer cell line (Eca-109). Hemocompatibility of the synthesized conjugates was evaluated and proved that the conjugates are safe to use for the treatment of tumor. Our results showed the PS doped p-dots had less dark toxicity and increased light toxicity as well as ROS generation was high as compared to precursor drug. Therefore, incorporation of p-dots to porphyrin improved biocompatibility and enhanced the photodynamic effect.
碳基聚合物点由于其优异的生物相容性和良好的溶解性而引起了研究人员的关注。大多数 p-点能够产生 ROS,这对于癌症的光动力治疗非常有效,而一些光敏剂,如卟啉,具有一些缺点,如疏水性和暗毒性。因此,在这项研究中,我们通过酰胺缩合和 π-π 堆积将红色发射的碳基聚合物与原卟啉-α 连接起来。成功地实现了一锅法合成。通过傅里叶变换红外光谱(FT-IR)、透射电子显微镜(TEM)和 HNMR 对其光物理性质进行了研究,并对其结构进行了表征。通过荧光和紫外-可见光谱证实了该配合物的 pH 敏感性。在人食管癌细胞系(Eca-109)中评价了制备的配合物的光毒性和暗毒性。评估了合成配合物的血液相容性,并证明该配合物可安全用于肿瘤治疗。我们的结果表明,与前药相比,掺杂 PS 的 p-点具有较低的暗毒性和增加的光毒性,并且 ROS 的产生也较高。因此,将 p-点掺入卟啉可以提高生物相容性并增强光动力效应。