In recent years, BODIPY derivatives have become one of the research hotspots in the field of bioprobes, but most of them have the problems of poor hydrophilicity, low biocompatibility and no targeting. In this paper, novel ethylenediamine bridging bis-sulfonyl-BODIPY fluorescent probes were successfully designed and synthesized to solve these problems; What’s more, the cytotoxicity analysis, cell imaging, in vivo imaging and apoptosis experiments were carried out. Ethylenediamine bridges and oxygen-rich sulfonyl groups made such probes had certain hydrophilicity, so they could be dissolved in dimethylsulfoxide and methanol. The IC₅₀ value of compound 9 in HCT-116 cells was 93.12 ± 6.33 µM, and in HeLa cells was 89.09 ± 11.84 µM, which indicating that the probe had certain inhibitory effect on cancer cells. The excellent biocompatibility and potential tumor targeting properties of the compound were clearly observed in cell and mice imaging. This study is of great significance for the rational design of novel targeted BODIPY probes with good hydrophilicity and biocompatibility.

近年来，BODIPY衍生物成为生物探针领域的研究热点之一，但大多存在亲水性差、生物相容性低、无靶向性等问题。本文成功设计并合成了新型乙二胺桥连双磺酰基-BODIPY荧光探针来解决这些问题；此外，还进行了细胞毒性分析、细胞成像、体内成像和细胞凋亡实验。乙二胺桥和富氧磺酰基使这种探针具有一定的亲水性，因此可以溶解在二甲亚砜和甲醇中。化合物9的IC ₅₀值在HCT-116细胞中为93.12±6.33μM，在HeLa细胞中为89.09±11.84μM，说明该探针对癌细胞有一定的抑制作用。在细胞和小鼠成像中清楚地观察到该化合物优异的生物相容性和潜在的肿瘤靶向特性。该研究对于合理设计具有良好亲水性和生物相容性的新型靶向BODIPY探针具有重要意义。