Zhong nan da xue xue bao. Yi xue ban = Journal of Central South University. Medical sciences · 2026
[Antibacterial activity and mechanism of the antiparasitic drug resorantel against Staphylococcus epidermidis].
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Guo Shaowei, Huang Guanqing, Xiao Dan, Lu Lihua, Li Mengna, Li Yimin, Wu Yong
Аннотация
OBJECTIVES: Staphylococcus epidermidis (S. epidermidis) is a common opportunistic pathogen in clinical settings. The widespread misuse of antibiotics has led to a continuous increase in its antimicrobial resistance, greatly complicating treatment. Drug repurposing, characterized by low cost, high safety, and short development cycles, represents an effective strategy for combating drug-resistant bacterial infections. This study aims to investigate the antibacterial activity of the antiparasitic drug resorantel against S. epidermidis and to preliminarily elucidate its antibacterial mechanism.
METHODS: The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of resorantel against S. epidermidis were determined using the broth microdilution method. Disk diffusion assays, 2, 3-Bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilid (XTT) assays, and time‑kill curves were employed to evaluate the susceptibility of S. epidermidis to resorantel. Serial induction experiments were conducted to assess the potential for resistance development. Crystal violet staining and XTT assays were used to evaluate the inhibitory and eradication effects of resorantel on biofilms. The checkerboard microdilution method was performed to investigate the combined effects of rafoxanide with conventional antibiotics. Antibacterial mechanisms were preliminarily explored by assessing membrane permeability, proton motive force, intracellular adenosine triphosphate (ATP) levels, and propidium iodide staining. Finally, a murine skin abscess model was established to evaluate the in vivo antibacterial activity of resorantel.
RESULTS: The MIC and MBC of resorantel against S. epidermidis were 2 μg/mL and 16 μg/mL, respectively. Disk diffusion assays demonstrated a pronounced antibacterial effect of resorantel against S. epidermidis. XTT assay results demonstrated that resorantel significantly reduced the viability of S. epidermidis (P<0.05). Time‑kill curve analysis indicated that even 1/4×MIC of resorantel effectively inhibited bacterial proliferation. After continuous exposure for 15 d, S. epidermidis did not develop resistance to resorantel. Crystal violet staining and XTT staining both revealed that 1 μg/mL resorantel significantly inhibited biofilm formation, while 2 μg/mL resorantel significantly reduced preformed biofilms (all P<0.05). Resorantel altered the proton motive force, inhibited intracellular ATP synthesis, and disrupted bacterial cell membrane integrity. In the murine skin abscess model, resorantel treatment significantly reduced the bacterial burden within abscess tissues (all P<0.05).
CONCLUSIONS: Resorantel exhibits both in vitro and in vivo antibacterial activity against S. epidermidis. Its antibacterial mechanism involves disruption of bacterial membrane integrity and proton motive force, as well as inhibition of intracellular ATP synthesis.
METHODS: The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of resorantel against S. epidermidis were determined using the broth microdilution method. Disk diffusion assays, 2, 3-Bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilid (XTT) assays, and time‑kill curves were employed to evaluate the susceptibility of S. epidermidis to resorantel. Serial induction experiments were conducted to assess the potential for resistance development. Crystal violet staining and XTT assays were used to evaluate the inhibitory and eradication effects of resorantel on biofilms. The checkerboard microdilution method was performed to investigate the combined effects of rafoxanide with conventional antibiotics. Antibacterial mechanisms were preliminarily explored by assessing membrane permeability, proton motive force, intracellular adenosine triphosphate (ATP) levels, and propidium iodide staining. Finally, a murine skin abscess model was established to evaluate the in vivo antibacterial activity of resorantel.
RESULTS: The MIC and MBC of resorantel against S. epidermidis were 2 μg/mL and 16 μg/mL, respectively. Disk diffusion assays demonstrated a pronounced antibacterial effect of resorantel against S. epidermidis. XTT assay results demonstrated that resorantel significantly reduced the viability of S. epidermidis (P<0.05). Time‑kill curve analysis indicated that even 1/4×MIC of resorantel effectively inhibited bacterial proliferation. After continuous exposure for 15 d, S. epidermidis did not develop resistance to resorantel. Crystal violet staining and XTT staining both revealed that 1 μg/mL resorantel significantly inhibited biofilm formation, while 2 μg/mL resorantel significantly reduced preformed biofilms (all P<0.05). Resorantel altered the proton motive force, inhibited intracellular ATP synthesis, and disrupted bacterial cell membrane integrity. In the murine skin abscess model, resorantel treatment significantly reduced the bacterial burden within abscess tissues (all P<0.05).
CONCLUSIONS: Resorantel exhibits both in vitro and in vivo antibacterial activity against S. epidermidis. Its antibacterial mechanism involves disruption of bacterial membrane integrity and proton motive force, as well as inhibition of intracellular ATP synthesis.