2. Academic Validation
  3. 2,4-Diacetylphloroglucinol (DAPG) derivatives rapidly eradicate methicillin-resistant staphylococcus aureus without resistance development by disrupting membrane

2,4-Diacetylphloroglucinol (DAPG) derivatives rapidly eradicate methicillin-resistant staphylococcus aureus without resistance development by disrupting membrane

  • Eur J Med Chem. 2023 Sep 29:261:115823. doi: 10.1016/j.ejmech.2023.115823.
Yifan Zhong 1,  Xiaoli He 2,  Wenlan Tao 2,  Jizhou Feng 1,  Ruixue Zhang 1,  Hongzhi Gong 1,  Ziyi Tang 2,  Chao Huang 3,  Yun He 4
Affiliations

Affiliations

  • 1 School of Pharmaceutical Sciences, Chongqing Key Laboratory of Natural Product Synthesis and Drug Research, Chongqing University, Chongqing, 401331, PR China.
  • 2 Chongqing School, University of Chinese Academy of Sciences (UCAS Chongqing), Chongqing, PR China; Chongqing Institute of Green and Intelligent Technology, Chinese Academy of Sciences, Chongqing, PR China.
  • 3 School of Pharmaceutical Sciences, Chongqing Key Laboratory of Natural Product Synthesis and Drug Research, Chongqing University, Chongqing, 401331, PR China. Electronic address: chuang@cqu.edu.cn.
  • 4 School of Pharmaceutical Sciences, Chongqing Key Laboratory of Natural Product Synthesis and Drug Research, Chongqing University, Chongqing, 401331, PR China; Chongqing School, University of Chinese Academy of Sciences (UCAS Chongqing), Chongqing, PR China; BayRay Innovation Center, Shenzhen Bay Laboratory, Shenzhen, 518132, China. Electronic address: yun.he@cqu.edu.cn.
PMID: 37839345 DOI: 10.1016/j.ejmech.2023.115823
Abstract

Methicillin-resistant Staphylococcus aureus (MRSA) causes severe public health challenges throughout the world, and the multi-drug resistance (MDR) of MRSA to Antibiotics necessitates the development of more effective Antibiotics. Natural 2,4-diacetylphloroglucinol (DAPG), produced by Pseudomonas, displays moderate inhibitory activity against MRSA. A series of DAPG derivatives was synthesized and evaluated for their Antibacterial activities, and some showed excellent activities (MRSA MIC = 0.5-2 μg/mL). Among these derivatives, 7g demonstrated strong Antibacterial activity without resistance development over two months. Mechanistic studies suggest that 7g asserted its activity by targeting Bacterial cell membranes. In addition, 7g exhibited significant synergistic Antibacterial effects with oxacillin both in vitro and in vivo, with a tendency to eradicate MRSA biofilms. 7g is a promising lead for the treatment of MRSA.

Keywords

2,4-Diacetylphloroglucinol; Antimicrobial resistance; Biofilm; Cell membrane; MRSA; Synergy.

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