A series of HepDirect pH responsive fluorescence probes of glycosyl-rhodamine are synthesized. The recognition trend of glucoside < lactoside < galactoside illuminates that the galactose is a targeting group toward HepG2 cells and its recognition is affected by the bulk of targeting group. The HepG2 cells binding trend of RDGal1< RDGal2< RDGal3 supports the cluster effect of galactose. RDGal3 with the optimum targeting potential is verified to selectively recognize HepG2 cells via a galactose dependent ASGPR binding mechanism. These nontoxic probes could be controllably activated by the acidic microenvironment of cancer cells, which is very significant to achieve diagnosis of hepatocellular carcinoma and provide a novel HepDirect carrier for precision treatment of hepatocarcinoma.

合成了一系列糖基罗丹明的HepDirect pH响应荧光探针。葡萄糖苷<乳糖苷<半乳糖苷的识别趋势表明，半乳糖是针对HepG2细胞的靶向组，其识别受靶向组的影响。RDGal1 <RDGal2 <RDGal3的HepG2细胞结合趋势支持半乳糖的簇效应。已验证具有最佳靶向潜力的RDGal3可通过半乳糖依赖性ASGPR结合机制选择性识别HepG2细胞。这些无毒探针可以被癌细胞的酸性微环境可控地激活，这对于实现肝细胞癌的诊断和为精确治疗肝癌提供了新的HepDirect载体具有非常重要的意义。