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<p>The screening of antibiotics derived from microbial resources to combat vancomycin-resistant enterococci (VRE) revealed that a culture of marine-derived <i>Peribacillus</i> sp. KDM594 exhibited significant therapeutic efficacy in an infected in vivo-mimic silkworm model. Bioassay-guided purification led to the isolation of micrococcins P1 (<b>1</b>) and P2 (<b>2</b>), which exhibited potent antimicrobial activities against Gram-positive bacteria, including VRE, methicillin-resistant <i>Staphylococcus aureus</i> (MRSA), and <i>Mycobacterium</i> spp., with MIC values ranging from 0.25 to 8.0 µg ml<sup>−1</sup> using the microdilution method. In the silkworm models infected with VRE or MRSA, <b>1</b> and <b>2</b> exerted moderate therapeutic effects, with ED<sub>50</sub> values ranging from 3.2 to 51 µg larva<sup>−1</sup> g<sup>−1</sup>. Furthermore, a pharmacokinetic analysis revealed that <b>2</b> was metabolized to <b>1</b> in the silkworm hemolymph, and their elimination half-lives were 3.2 and 3.0 h, respectively. These results suggest that micrococcins are promising lead compounds for the development of anti-VRE and MRSA drugs.</p>

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Micrococcins from Peribacillus sp. KDM594; efficacy against vancomycin-resistant enterococci and drug metabolism in a silkworm model

  • 期刊论文

  • 发表日期：

    2025年6月11日

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  • Akiho Yagi,
  • Mayu Sato,
  • Katsuki Kikuchi,
  • Akito Taniguchi,
  • Takashi Fukuda,
  • Ryuji Uchida

摘要

The screening of antibiotics derived from microbial resources to combat vancomycin-resistant enterococci (VRE) revealed that a culture of marine-derived Peribacillus sp. KDM594 exhibited significant therapeutic efficacy in an infected in vivo-mimic silkworm model. Bioassay-guided purification led to the isolation of micrococcins P1 (1) and P2 (2), which exhibited potent antimicrobial activities against Gram-positive bacteria, including VRE, methicillin-resistant Staphylococcus aureus (MRSA), and Mycobacterium spp., with MIC values ranging from 0.25 to 8.0 µg ml−1 using the microdilution method. In the silkworm models infected with VRE or MRSA, 1 and 2 exerted moderate therapeutic effects, with ED50 values ranging from 3.2 to 51 µg larva−1 g−1. Furthermore, a pharmacokinetic analysis revealed that 2 was metabolized to 1 in the silkworm hemolymph, and their elimination half-lives were 3.2 and 3.0 h, respectively. These results suggest that micrococcins are promising lead compounds for the development of anti-VRE and MRSA drugs.