Department of Regenerative Medicine, Faculty of Medicine, Medical University of Warsaw, 02-091 Warsaw, Poland.
Department of Molecular Biochemistry, Faculty of Chemistry, University of Gdansk, 80-308 Gdansk, Poland.
Molecules. 2024 Feb 1;29(3):678. doi: 10.3390/molecules29030678.
The fusion of penetrating peptides (PPs), e.g., cell penetration peptides (CPPs) or antimicrobial peptides (AMPs), together with antimicrobial agents is an expanding research field. Specific AMPs, such as lactoferricin B (LfcinB), have demonstrated strong antibacterial, antifungal, and antiparasitic activity, as well as valuable anticancer activity, proving beneficial in the development of anticancer conjugates. The resulting conjugates offer potential dual functionality, acting as both an anticancer and an antimicrobial agent. This is especially necessary in cancer treatment, where microbial infections pose a critical risk. Leukemic cells frequently exhibit altered outer lipid membranes compared to healthy cells, making them more sensitive to compounds that interfere with their membrane. In this study, we revisited and reanalyzed our earlier research on LfcinB and its conjugates. Furthermore, we carried out new experiments with a specific focus on cell proliferation, changes in membrane asymmetric phosphatidylserine location, intracellular reactive oxygen species (ROS) generation, mitochondrial functions, and in vitro bacterial topoisomerase inhibition.
穿透肽（PPs）的融合，例如细胞穿透肽（CPPs）或抗菌肽（AMPs）与抗菌剂的融合，是一个不断发展的研究领域。特定的 AMPs，如乳铁蛋白衍生抗菌肽 B（LfcinB），表现出强大的抗菌、抗真菌和抗寄生虫活性，以及有价值的抗癌活性，在抗癌缀合物的开发中证明是有益的。由此产生的缀合物具有潜在的双重功能，既可以作为抗癌剂，也可以作为抗菌剂。在癌症治疗中，这一点尤其必要，因为微生物感染构成了关键的风险。与健康细胞相比，白血病细胞经常表现出改变的外部脂质膜，这使它们对干扰其膜的化合物更加敏感。在这项研究中，我们重新审视和重新分析了我们之前关于 LfcinB 及其缀合物的研究。此外，我们进行了新的实验，特别关注细胞增殖、膜不对称磷脂酰丝氨酸位置的变化、细胞内活性氧（ROS）的产生、线粒体功能以及体外拓扑异构酶抑制。
