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<p>Globally, citrus fruits represent the most commercially significant category within the Rutaceae family, offering considerable nutritional benefits and playing a vital role in the world economy. However, citrus production faces serious threats from various plant diseases, such as greening, citrus decline, and gummosis. Among these, infection by <i>Xanthomonas axonopodis</i> pv. <i>citri</i> (<i>Xac</i>), a gram negative bacterial pathogen, leads to severe qualitative and quantitative losses, underscoring the urgent need for novel and environmentally friendly antibacterial agents. In this study, the antibacterial activity of compound <b>W2</b>, a series of phenylpiperazine derivatives linked by isopropanolamine and synthesized based on the principle of active fragment splicing employed in previous studies, against Xac bacteria was evaluated. Its efficacy was compared with that of two commonly used commercial bactericides—thiodiazole copper (<b>TC</b>) and bismerthiazol (<b>BT</b>). The results demonstrated that compound <b>W2</b> exhibited potent in vitro antibacterial activity, with an EC₅₀ value of 2.89&#xa0;µg/mL, substantially outperforming both <b>TC</b> (EC₅₀ = 56.22&#xa0;µg/mL) and <b>BT</b> (EC₅₀ = 51.48&#xa0;µg/mL). Further investigations revealed that <b>W2</b> strongly inhibited bacterial growth by inducing apoptosis and elevating intracellular reactive oxygen species levels. Scanning electron microscopy observations confirmed that <b>W2</b> caused clear morphological damage to <i>Xac</i> cells. Additionally, proteomic analysis indicated that the compound likely impairs virulence and motility in <i>Xac</i> through pathways involving two component systems and bacterial chemotaxis regulation. Preliminary in vivo assays also suggested that <b>W2</b> possesses both protective and curative effects against <i>Xac</i> infection. In conclusion, the phenol piperazine derivative <b>W2</b> shows promising potential as an effective and ecofriendly antibacterial agent for controlling citrus bacterial canker caused by <i>Xac</i>. Its multi modal action, combining direct antibacterial activity with virulence suppression, supports its further development as a candidate for integrated disease management in citrus cultivation.</p> Graphical abstract <p></p>

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Exploration of the mechanism of action of isopropanolamine derivatives against Xanthomonas axonopodis pv. citri

  • 期刊论文

  • 发表日期：

    2026年5月30日

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  • Mengting Liu,
  • Wenhang Wang,
  • Lihui Shao,
  • Jiao Meng,
  • Chengpeng Li,
  • Bingqian Liu,
  • Danping Chen,
  • Zhurui Li,
  • Chenchen Li,
  • Yunqiang Sun,
  • Zhenchao Wang

摘要

Globally, citrus fruits represent the most commercially significant category within the Rutaceae family, offering considerable nutritional benefits and playing a vital role in the world economy. However, citrus production faces serious threats from various plant diseases, such as greening, citrus decline, and gummosis. Among these, infection by Xanthomonas axonopodis pv. citri (Xac), a gram negative bacterial pathogen, leads to severe qualitative and quantitative losses, underscoring the urgent need for novel and environmentally friendly antibacterial agents. In this study, the antibacterial activity of compound W2, a series of phenylpiperazine derivatives linked by isopropanolamine and synthesized based on the principle of active fragment splicing employed in previous studies, against Xac bacteria was evaluated. Its efficacy was compared with that of two commonly used commercial bactericides—thiodiazole copper (TC) and bismerthiazol (BT). The results demonstrated that compound W2 exhibited potent in vitro antibacterial activity, with an EC₅₀ value of 2.89 µg/mL, substantially outperforming both TC (EC₅₀ = 56.22 µg/mL) and BT (EC₅₀ = 51.48 µg/mL). Further investigations revealed that W2 strongly inhibited bacterial growth by inducing apoptosis and elevating intracellular reactive oxygen species levels. Scanning electron microscopy observations confirmed that W2 caused clear morphological damage to Xac cells. Additionally, proteomic analysis indicated that the compound likely impairs virulence and motility in Xac through pathways involving two component systems and bacterial chemotaxis regulation. Preliminary in vivo assays also suggested that W2 possesses both protective and curative effects against Xac infection. In conclusion, the phenol piperazine derivative W2 shows promising potential as an effective and ecofriendly antibacterial agent for controlling citrus bacterial canker caused by Xac. Its multi modal action, combining direct antibacterial activity with virulence suppression, supports its further development as a candidate for integrated disease management in citrus cultivation.

Graphical abstract