福州大学黄剑东团队报道了聚集增强酞菁-青蒿琥酯偶联物的声动力学活性。相关研究成果发表在2021年11月11日出版的国际知名学术期刊《德国应用化学》。

由于缺乏有效的声致敏剂，声动力疗法（SDT）的临床前景尚未完全实现。

该文中，研究人员设计了酞菁-青蒿琥酯缀合物（例如ZnPcT4A），其产生的活性氧物种（ROS）比已知的声敏化剂原卟啉IX高约10倍。同时，首次观察到了聚集增强声动力学活性（AESA）。ZnPcT4A在水溶液中以聚集形式产生的声动力活性氧比以解聚形式产生的声动力活性氧高约60倍。这可以归因于纳米结构的超声空化增强。AESA效应的水平取决于声致敏剂分子的聚集能力及其聚集体的粒径。此外，生物学研究表明ZnPcT4A具有很高的抗癌活性和生物安全性。

该研究为开发高效的有机声致敏剂开辟了一条新的途径。

附：英文原文

Title: Aggregation-Enhanced Sonodynamic Activity of Phthalocyanine-Artesunate Conjugates

Author: Peng-Hui Zhao, Yu-Lin Wu, Xue-Yan Li, Lin-Lin Feng, Ling Zhang, Bi-Yuan Zheng, Mei-Rong Ke, Jian-Dong Huang

Issue&Volume: 2021-11-11

Abstract: The clinic prospect of sonodynamic therapy (SDT) has not been fully realized due to the scarcity of efficient sonosensitizers. Herein, we designed phthalocyanine-artesunate conjugates (e.g. ZnPcT  4  A), which could generate up to ca. 10-fold more reactive oxygen species (ROS) than the known sonosensitizer protoporphyrin IX. Meanwhile, an interesting and significant finding of aggregation-enhanced sonodynamic activity (AESA) was observed for the first time. ZnPcT  4  A showed about 60-fold higher sonodynamic ROS generation in aggregation form than disaggregation form in aqueous solutions. That could be attributed to the boosted ultrasonic cavitation of nanostructures. The levels of AESA effect depended on the aggregation ability of sonosensitizer molecules and the particle sizes of their aggregates. Moreover, biological studies demonstrated that ZnPcT  4  A had high anticancer activities and biosafety. This study thus opens up a new avenue the development of efficient organic sonosensitizers.

DOI: 10.1002/anie.202113506

Source: https://onlinelibrary.wiley.com/doi/10.1002/anie.202113506