Professor Liu Shouping’s Research Team: New Progress Made in the R&D of Drugs Against Antibiotic Resistant Bacteria Based on Mechanisms of Membrane Targeting Antibiotics
2021-03-04575Currently, as antibiotic resistance increases sharply, which is a serious threat to human health, it is urgent to develop new drugs against antibiotic resistant bacteria. Recently, PI Professor Liu Shouping of the respiratory pharmacology group and Associate Professor Lin Shuimu of the research team of anti-infective agents in medicinal chemistry of the Laboratory used natural kaempferol, sofalone, and the drug intermediate 4-glycidoxycarbazole as the nucleus, based on the design principles of biomimetic simulation of the molecular structure of natural antimicrobial peptides and the mechanisms of membrane-targeting antibiotics, to obtain a series of new antimicrobial drugs through structural optimization of system with flavone or carbazole as the cores, and a series of progress has been made. The research results show that these antimicrobial peptide mimics based on flavone or carbazole not only show good antibacterial activity, high sterilization rate, high safety, good stability, low cost of preparation, good druggability, etc., but also maintain excellent antibacterial activity in animals. It is hopefully a new type of antibacterial drugs based on a new mechanism of action and a new molecular framework can be developed, which can effectively deal with antibiotic resistance, to provide a new solution for the crisis in antibiotic resistance.
Related research results have been published in 2020, including four research papers: J Med Chem 2020, 63(11), 5797-5815, J Med Chem 2020, 63(17):9284-9299, Eur J Med Chem 2020, 202, 112596 and Biochim Biophys Acta Biomembr 2020, 1862, 183353. Two national invention patents in the research technology have been applied (application numbers: 201911257926.8 and 201911415794.7). The above-mentioned research, with the School of Pharmaceutical Sciences of Guangzhou Medical University as the first and corresponding author, is funded by the Youth Project of the National Natural Science Foundation of China and the High-level University Construction Project of Guangzhou Medical University.
