Recently, researchers at SHVRI CAAS have developed a novel antibacterial compound, offering a promising new strategy to combat drug-resistant bacterial infections. The findings have been published in the top journal Bioorganic Chemistry.
α-Mangostin, a bioactive natural product isolated from mangosteen peel, is considered a highly potential antibacterial scaffold due to its anti-inflammatory, anti-tumor, and anti-bacterial activities. Nevertheless, its further development is constrained by inherent limitations, such as inadequate anti-biofilm efficacy, significant hemolytic property, and a relatively narrow antibacterial spectrum. Herein, we report a pharmacophore-oriented strategy to develop a candidate compound that addresses these issues. The resulting compound demonstrates a dual-mechanism antibacterial action: it directly attacks pathogens by disrupting the cell membrane and causing content leakage, and concurrently triggers lethal oxidative stress. Additionally, it resolves existing drug resistance through the potent inhibition and elimination of bacterial biofilms.
Discovery of α-mangostin derivative 7-8 based on pharmacophore-oriented and its dual-effect mechanism against methillin-resistant Staphylococcus aureus strains.
Dr. Tang Qun and Dr. Zhang Haiyang from SHVRI CAAS, are the first authors of this paper, with Prof. Zhou Wen and Prof. Wang Chunmei serving as corresponding authors. The research was supported by grants from the National Natural Science Foundation of China and the 14th Five-Year National Key Research and Development Program.
Original article link: https://doi.org/10.1016/j.bioorg.2025.109108
