文献：

Novel Near-Infrared Hypocrellin Derivatives for Synergistic Photodynamic and Photothermal Therapy

文献链接：

作者：

Ying Ding, Weimin Liu, Jiasheng Wu, Xiuli Zheng, Jiechao Ge, Haohui Ren, Wenjun Zhang, Chun-Sing Lee, and Pengfei Wang

相关产品：

DSPE-mPEG2000（磷脂-甲氧基聚乙二醇2000）

原文摘要：

Hypocrellin B (HB) derived from naturally produced hypocrellins has attracted considerable attention in photodynamic therapy (PDT) because of its excellent photosensitive properties. However, the weak absorption within a “phototherapy window” (600–900 nm) and poor water solubility of HB have limited its clinical application. In this study, two HB derivatives (i.e., HE and HF) were designed and synthesized for the first time by introducing two different substituent groups into the HB structure. The obtained derivatives showed a broad absorption band covering the near-infrared (NIR) region, NIR emission (peaked at 805 nm), and singlet oxygen quantum yields of 0.27/0.31. HE-PEG-NPs were also prepared using 2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethyleneglycol)-2000] (DSPE-mPEG2000) to achieve excellent dispersion in water and further explored their practical applications. HE-PEG-NPs not only retained their 1O2-generating ability, but also exhibited a photothermal conversion efficiency of 25.9%. In vitro and in vivo therapeutic results revealed that the synergetic effect of HE-PEG-NPs on PDT and photothermal therapy (PTT) could achieve a good performance. Therefore, HE-PEG-NPs could be regarded as a promising phototheranostic agent.

DSPE - mPEG2000 是一种聚乙二醇化的磷脂。其中 “DSPE” 代表 1,2 -二硬脂酰- sn -甘油- 3 -磷酸乙醇胺，它是一种磷脂成分，具有亲水性的头部（磷酸乙醇胺部分）和两条疏水性的脂肪酸链（硬脂酸）。“mPEG2000” 表示甲氧基聚乙二醇，其分子量约为 2000Da，聚乙二醇（PEG）链段通过共价键连接到 DSPE 上。它的结构具有两亲性。DSPE 部分的两条长的脂肪酸链使得该分子在水溶液中有自发形成胶束的倾向，其疏水性的脂肪酸链会聚集在一起以避开水相，而亲水性的 PEG 链段则伸展在水溶液中。这种胶束结构可以用于包裹疏水性的化合物、成像剂等物质，实现对这些物质的增溶和递送。该文献基于DSPE - mPEG2000的相关特性，该文献制备了HE-PEG-NPs纳米材料，流程如下：

图：产品合成路线

合成HD：将低克雷林B和盐酸半胱胺溶解在DMSO中，加入一定量的氨调整溶液pH值，然后在室温下搅拌混合物。用盐酸中和后，用二氯甲烷和水提取混合物溶液。收集所有二氯甲烷溶液得到粗产物，去除二氯甲烷后得到的固体用CH2CL2/乙酸乙酯进行硅胶柱层析，得到纯HD。

将HE或HF的合成：环己胺或环戊胺分别加入含HD的无水THF中，搅拌。蒸发溶剂后，用CH2CL2/乙酸乙酯进行硅胶层析纯化残留产物，分别得到蓝色化合物HE和HF。

纳米共沉淀的方法合成HE-PEG-NPs将含有HE的THF溶液快速加入到含有PVA的DSPE-mPEG2000水溶液中中。通过蒸发进一步去除THF，通过滤膜过滤得到纯化的HE-PEG-NPs。

图：作用机理

结论：

该文献成功制备了基于DSPE-mPEG2000修饰的新材料HE-PEG-NPs，结果表明，它们在体内外均表现出良好的PDT和PTT协同效果。因此，将不同的官能团结合到HB结构中，以获得更多的具有良好效果的HB衍生物是一种很有前途的策略，作为一种荧光成像引导的光动力和光热Treatment 剂。