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<p>In this study, we aimed to design and synthesize a series of pentacyclic triterpenoids-triphenylphosphine (TPP) derivatives. A total of 22 derivatives were systematically synthesized and evaluated for their in vitro antibacterial activities against four pathogenic strains, namely, <i>S. aureus</i>, MRSA, <i>E. coli</i>, and <i>P. aeruginosa</i>, using the standard broth microdilution method. Notably, most derivatives demonstrated better antibacterial activity than the pentacyclic triterpenoids parent nucleus. Among them, Compound 1 performed the most potent antibacterial activity on MRSA (MIC = 0.78&#xa0;μM), which was significantly better than norfloxacin, penicillin, tobramycin, and tetracycline at the same concentration. In addition, according to the results of hemolysis test, chick chorioallantoic membrane (CAM) assay, zebrafish toxicity test, and acute toxicity test, Compound 1 exhibited higher selectivity and biosafety. Finally, the mechanistic results suggested that Compound 1 may exert its antibacterial activity by acting on key targets such as SasG, IcaB, and MurQ, thereby affecting the biofilm formation process.</p> Graphical Abstract <p></p>

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Design, synthesis, and biological evaluation of pentacyclic triterpenoids-triphenylphosphine derivatives as antibacterial agents to combat MRSA

  • 期刊论文

  • 发表日期：

    2026年7月13日

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  • Jinchai Qi,
  • Xueyan Li,
  • Desheng Cai,
  • Yuqin Yang,
  • Wenmin Pi,
  • Zijie Zhang,
  • Bing Xu,
  • Penglong Wang,
  • Haimin Lei

摘要

In this study, we aimed to design and synthesize a series of pentacyclic triterpenoids-triphenylphosphine (TPP) derivatives. A total of 22 derivatives were systematically synthesized and evaluated for their in vitro antibacterial activities against four pathogenic strains, namely, S. aureus, MRSA, E. coli, and P. aeruginosa, using the standard broth microdilution method. Notably, most derivatives demonstrated better antibacterial activity than the pentacyclic triterpenoids parent nucleus. Among them, Compound 1 performed the most potent antibacterial activity on MRSA (MIC = 0.78 μM), which was significantly better than norfloxacin, penicillin, tobramycin, and tetracycline at the same concentration. In addition, according to the results of hemolysis test, chick chorioallantoic membrane (CAM) assay, zebrafish toxicity test, and acute toxicity test, Compound 1 exhibited higher selectivity and biosafety. Finally, the mechanistic results suggested that Compound 1 may exert its antibacterial activity by acting on key targets such as SasG, IcaB, and MurQ, thereby affecting the biofilm formation process.

Graphical Abstract