Department of BioMedical-Chemical Engineering, The Catholic University of Korea, 43 Jibong-ro, Wonmi-gu, Bucheon-si, Gyeonggi-do, 14662, Republic of Korea; Department of Biotechnology, The Catholic University of Korea, 43 Jibong-ro, Wonmi-gu, Bucheon-si, Gyeonggi-do, 14662, Republic of Korea.
Department of Gastroenterology, University of Ulsan College of Medicine, 88, Olympic-ro 43-gil, Songpa-gu, Seoul, Republic of Korea.
Biomaterials. 2024 Jul;308:122541. doi: 10.1016/j.biomaterials.2024.122541. Epub 2024 Mar 25.
Herein, we describe the 3'-sialyllactose-polyethyleneimine-chlorine e6 conjugate (3PC), meticulously engineered to effectively target Helicobacter bacteria (H. pylori) within the gastric environment. The composition of 3PC comprises polyethyleneimine, a cationic polymer, 3'-sialyllactose, which exhibits a specific binding affinity for H. pylori surface proteins, and a photosensitizer capable of generating oxygen radicals in response to specific wavelengths. The distinctive feature of 3PC lies in its capacity to enhance interaction with the anionic mucus layer facilitated by electrostatic forces. This interaction results in prolonged residence within the intestinal environment. The extended vacation in the intestinal milieu overcomes inherent limitations that have historically impeded conventional antibiotics from efficiently reaching and targeting H. pylori. 3PC can be harnessed as a potent tool for antibacterial photodynamic therapy, and its versatility extends to addressing the challenges posed by various antibiotic-resistant strains. The exceptional efficacy of 3PC in enhancing intestinal residence time and eradicating H. pylori has been robustly substantiated in animal models, particularly in mice. In summary, 3PC is a formidable agent capable of eradicating H. pylori, irrespective of its antibiotic resistance status, by efficiently penetrating and selectively targeting the mucus layer within the gastric environment.
在此，我们描述了 3'-唾液酸乳糖-聚乙烯亚胺-氯乙啶 6 缀合物（3PC），精心设计用于在胃环境中有效靶向幽门螺杆菌（H. pylori）。3PC 的组成包括聚乙烯亚胺，一种阳离子聚合物，3'-唾液酸乳糖，它对 H. pylori 表面蛋白具有特异性结合亲和力，以及一种光增敏剂，能够在特定波长下产生氧自由基。3PC 的独特之处在于它能够增强与带负电荷的粘液层的相互作用，这是通过静电力实现的。这种相互作用导致它在肠道环境中的停留时间延长。在肠道环境中的延长停留时间克服了传统抗生素有效到达和靶向 H. pylori 的固有局限性。3PC 可以用作一种强大的抗菌光动力治疗工具，其多功能性还扩展到解决各种抗生素耐药菌株带来的挑战。3PC 在增强肠道停留时间和根除 H. pylori 方面的卓越功效在动物模型中得到了有力证实，特别是在小鼠中。总之，3PC 是一种强大的药物，能够有效地穿透并选择性地靶向胃环境中的粘液层，从而根除 H. pylori，无论其抗生素耐药状态如何。
