Abstract：
Multidrug-resistant (MDR) bacteria pose serious threats to public health due to the lack of effective and biocompatible drugs to kill MDR bacteria. Photodynamic antibacterial therapy has been widely studied due to its low induction of resistance. However, photosensitizers that can efficiently generate reactive oxygen species (ROS) through both type I and type II mechanisms and that have the capability of multiple modes of action are rarely reported. Addressing this issue, we developed a near-infrared-emitting triphenylamine indole iodoethane (TTII) and its silver(I) self-assembled (TTIIS) aggregation-induced emission (AIE) photosensitizer for multimode bacterial infection therapy. TTII can efficiently produce both Type I ROS •OH and Type II ROS 1O2. Interestingly, the Ag(I)-π interaction contributed in TTIIS efficiency promotion of the generation of 1O2. Moreover, by releasing Ag+, TTIIS enabled photodynamic-Ag(I) dual-mode sterilization. As a result, TTIIS achieved an effective enhancement of antibacterial activity, with a 1-2-fold boost against multidrug-resistant Escherichia coli (MDR E. coli). Both TTII and TTIIS at a concentration as low as 0.55 μg mL-1 can kill more than 98% of methicillin resistant Staphylococcus aureus (MRSA) on MRSA-infected full-thickness defect wounds of a mouse, and both TTII and TTIIS were effective in eliminating the bacteria and promoting wound healing.
摘要：
多药耐药(MDR)细菌由于缺乏杀死MDR细菌的有效和生物相容性药物而对公众健康构成严重威胁。光动力抗菌疗法由于其低诱导抗性而被广泛研究。然而,很少报道可以通过I型和II型机制有效产生活性氧（ROS）并且具有多种作用方式的光敏剂。解决这个问题，我们开发了一种近红外发射三苯胺吲哚碘乙烷（TTII）及其银（I）自组装（TTIS）聚集诱导发射（AIE）光敏剂，用于多模式细菌感染治疗。TTII可以有效地产生I型ROS·OH和II型ROS1O2。有趣的是,Ag(I)-π相互作用促进了TTIS效率的产生。此外，通过释放Ag+，TTIS启用光动力-Ag(I)双模式灭菌。因此,TTIS实现了抗菌活性的有效增强，对多重耐药大肠杆菌（MDR大肠杆菌）的1-2倍增强。浓度低至0.55μgmL-1的TTII和TTIS均可在MRSA感染的小鼠全层缺损伤口上杀死98％以上的耐甲氧西林金黄色葡萄球菌（MRSA），TTII和TTIS均能有效消除细菌并促进伤口愈合。
