大连理工大学郑楠团队报道了多组分聚合聚（bodipy -磺酰胺），作为声动力和气体联合治疗中独特的SO₂生成器。相关研究成果于2025年1月7日发表于国际一流学术期刊《德国应用化学》。

该文中，研究人员开发了一种涉及联吡咯、磺酰叠氮化物和二炔的多组分聚合（MCP）方法，以高产率和分子量制备聚（联吡咯磺酰亚胺）库，并对其进行进一步改性以形成独特的二氧化硫（SO₂）生成器。聚吡咯作为碳基亲核试剂，在MCP过程中进行铜催化的C-C偶联。研究通过将二吡咯单元转化为二吡咯甲烷硼（BODIPY），并将磺酰亚胺部分转化为磺酰胺进行MCP后修饰，获得了聚（BODIPY-磺酰胺）s（PBSAs）作为强效抗癌治疗剂。

该研究揭示了PBSAs在超声波（US）照射下的分解和SO₂释放能力。此外，这些聚合物中的一种具有活性氧物质-可分离的硫缩酮连接体，用三甘醇链修饰以得到PBSA-EG，其被进一步研究用于体外和体内US-诱导的抗癌治疗。将PBSA-EG纳米颗粒尾膜给药至荷瘤小鼠体内，然后进行US照射，观察到显著的肿瘤抑制作用。

研究表明，创新和有效的MCP方法可以构建含有BODIPY-磺酰胺部分的聚合物，这显示出其作为安全和有效材料的巨大潜力，用于癌症的气体和声动力联合治疗。

附：英文原文

Title: Multicomponent Polymerization toward Poly(BODIPY-sulfonamide)s as Unique SO2 Generators for Sonodynamic and Gas Combination Therapy

Author: Shuxin Liu, Juan Li, Aiguo Wang, Dennis K.P. Ng, Nan Zheng

Issue&Volume: 2025-01-07

Abstract: In this work, a multicomponent polymerization (MCP) approach involving bipyrroles, sulfonyl azides, and diynes was developed to afford a library of poly(bipyrrole-sulfonylimide)s (PPSIs) in high yields and molecular weights, which were further modified to form unique sulfur dioxide (SO2) generators. Bipyrroles served as carbon-based nucleophiles to undergo Cu-catalyzed C-C coupling during the MCP. Upon post-MCP modification by transforming the bipyrrole unit to boron dipyrromethene (BODIPY) and the sulfonylimide moiety to sulfonamide, poly(BODIPY-sulfonamide)s (PBSAs) were obtained as potent anticancer therapeutic agents. This study disclosed the decomposition and SO2-releasing ability of PBSAs under ultrasound (US) irradiation. Furthermore, one of these polymers having a reactive oxygen species-cleavable thioketal linker was modified with triethylene glycol chains to give PBSA-EG, which was further studied for in vitro and in vivo US-induced anti-cancer therapy. Upon tail veil administration of PBSA-EG nanoparticles into tumor-bearing mice followed by US irradiation, remarkable tumor suppression was observed. This study demonstrates that the innovative and efficient MCP method can construct polymers bearing the BODIPY-sulfonamide moieties, which show a great potential as safe and potent materials for combined gas and sonodynamic therapy against cancer.

DOI: 10.1002/anie.202422362

Source: https://onlinelibrary.wiley.com/doi/10.1002/anie.202422362