Ratrey Poonam, Dalvi Sameer V, Mishra Abhijit
Materials Science and Engineering, Indian Institute of Technology Gandhinagar, Palaj, Gandhinagar 382355, India.
Chemical Engineering, Indian Institute of Technology Gandhinagar, Palaj, Gandhinagar 382355, India.
ACS Omega. 2020 Jul 23;5(30):19004-19013. doi: 10.1021/acsomega.0c02321. eCollection 2020 Aug 4.
Bacterial resistance to antimicrobial drugs is one of the biggest threats to human health and novel drugs, and strategies are needed to obviate this resistance crisis. An innovative strategy for designing novel antimicrobial drugs is based on the hybridization of an antimicrobial agent with a second functional entity. Here, we use a cell-penetrating peptide-octaarginine (R8) as the second functional entity and develop a complex or hybrid of R8 and curcumin that possibly targets the bacterial cell membrane. Minimum inhibitory concentration assays show that the antibacterial activity of the complex is enhanced in a synergistic manner and rapid killing kinetics are obtained, emphasizing a bactericidal mode of action. In addition, electron microscopy images reveal bacterial membrane disruption by the complex. The R8-curcumin complex also displays activity against HeLa cells.
细菌对抗菌药物的耐药性是对人类健康和新型药物的最大威胁之一，因此需要采取策略来消除这一耐药危机。设计新型抗菌药物的一种创新策略是基于抗菌剂与第二个功能实体的杂交。在这里，我们使用细胞穿透肽八聚精氨酸（R8）作为第二个功能实体，并开发了一种R8与姜黄素的复合物或杂化物，它可能靶向细菌细胞膜。最低抑菌浓度测定表明，该复合物的抗菌活性以协同方式增强，并获得了快速的杀菌动力学，强调了杀菌作用模式。此外，电子显微镜图像显示该复合物可破坏细菌膜。R8-姜黄素复合物对HeLa细胞也有活性。
