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<p><i>Candida</i> is a commensal fungus of clinical interest that commonly lives in oral cavity and intestine but can become an opportunist microrganism and cause severe infections. A serie of 10 aminochalcones were designed and synthetized to obtain compounds anti-<i>Candida</i> with potent and broad-spectrum activity. The most active compound <b>J34</b> demonstrated excellent in vitro activity against <i>Candida albicans</i>, <i>Candida tropicalis</i>, <i>Candida parapsilosis</i>, <i>Candida glabrata</i> and <i>Candida krusei</i> with minimum inhibitory concentration between 1.9 and 7.8&#xa0;µg/mL. The association of aminochalcone <b>J34</b> with amphotericin B demonstrated synergistic effect against <i>C. albicans</i>, with Fractional Inhibiroty Concentration Index (FICI) value of 0.5. Subinhibitory concentration of <b>J34</b> inhibited the <i>C. albicans</i> adhesion to human keratinocytes. Treatment with <b>J34</b> reduced <i>C. albicans</i> biofilm formation, as well as acts on preformed biofilm in concentration-dependent mode. Time-kill curve demonstrated that <b>J34</b> had fungicidal action after 12&#xa0;h of treatment. Preliminary mechanism of action study showed <b>J34</b> interacts with membrane ergosterol but does not act on fungal cell wall of <i>C. albicans</i>. In additon, in vivo studies using <i>Galleria mellonella</i> indicated low toxic effect of chalcone <b>J34</b> after 72&#xa0;h of treatment.</p>

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Synthesis and evaluation of the antifungal and antibiofilm potential of aminochalcones

  • 期刊论文

  • 发表日期：

    2025年1月20日

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  • Mayara Aparecida Rocha Garcia,
  • Janaína de Cássia Orlandi Sardi,
  • Mariana Bastos dos Santos,
  • Josy Golsoni Lazarini,
  • Pedro Luiz Rosalen,
  • Luis Octávio Regasini

摘要

Candida is a commensal fungus of clinical interest that commonly lives in oral cavity and intestine but can become an opportunist microrganism and cause severe infections. A serie of 10 aminochalcones were designed and synthetized to obtain compounds anti-Candida with potent and broad-spectrum activity. The most active compound J34 demonstrated excellent in vitro activity against Candida albicans, Candida tropicalis, Candida parapsilosis, Candida glabrata and Candida krusei with minimum inhibitory concentration between 1.9 and 7.8 µg/mL. The association of aminochalcone J34 with amphotericin B demonstrated synergistic effect against C. albicans, with Fractional Inhibiroty Concentration Index (FICI) value of 0.5. Subinhibitory concentration of J34 inhibited the C. albicans adhesion to human keratinocytes. Treatment with J34 reduced C. albicans biofilm formation, as well as acts on preformed biofilm in concentration-dependent mode. Time-kill curve demonstrated that J34 had fungicidal action after 12 h of treatment. Preliminary mechanism of action study showed J34 interacts with membrane ergosterol but does not act on fungal cell wall of C. albicans. In additon, in vivo studies using Galleria mellonella indicated low toxic effect of chalcone J34 after 72 h of treatment.