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Abstract <p><b>Objective:</b> The fungicidal activity of 86 monoterpene indole alkaloids (MIAs) derived from plants was evaluated to identify novel lead compounds with antifungal potential. <b>Methods:</b> In this study, both <i>in vitro</i> and <i>in vivo</i> antifungal assays were performed to assess the efficacy of the selected MIAs. <b>Results and Discussion:</b> Among the tested compounds, rhazinilam (<b>32</b>) and rhazinal (<b>33</b>) exhibited markedly stronger antifungal activity against <i>Aspergillus niger</i> than ketoconazole in preliminary screenings. Further evaluation using mycelial growth inhibition assays confirmed that both compounds were significantly more active than ketoconazole against <i>A. niger</i>, <i>B. dothidea</i>, and <i>F. oxysporum</i> f. sp. <i>cubense in vitro</i>. The IC<sub>50</sub> values for rhazinilam (<b>32</b>) were &lt; 5, &lt; 10, and 17.89 μg/mL, respectively; for rhazinal (<b>33</b>), the values were &lt; 2.5, &lt; 5, and &lt; 5 μg/mL, respectively. Moreover, <i>in vivo</i> tests on cucumber leaves demonstrated that at a concentration of 40 μg/mL, compounds (<b>32</b>) and (<b>33</b>) provided significant protection against <i>A. niger</i>, with protection rates of 77.27 and 100%, respectively, compared to 47.62% for ketoconazole. <b>Conclusions:</b> Rhazinilam (<b>32</b>) and rhazinal (<b>33</b>) demonstrated potent antifungal activity in both <i>in vitro</i> and <i>in vivo</i> experiments, highlighting their promise as lead candidates for the development of novel fungicidal agents.</p>

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Evaluation of Natural Monoterpene Indole Alkaloids as Potent Fungicide Candidates

  • 期刊论文

  • 发表日期：

    2025年6月3日

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  • Zhuoyi Wang,
  • Yanyan Chen,
  • Hean Liu,
  • Yueming Li,
  • Mingjie Zhang,
  • Yongyong Zhang,
  • Junwei Sun

摘要

Abstract

Objective: The fungicidal activity of 86 monoterpene indole alkaloids (MIAs) derived from plants was evaluated to identify novel lead compounds with antifungal potential. Methods: In this study, both in vitro and in vivo antifungal assays were performed to assess the efficacy of the selected MIAs. Results and Discussion: Among the tested compounds, rhazinilam (32) and rhazinal (33) exhibited markedly stronger antifungal activity against Aspergillus niger than ketoconazole in preliminary screenings. Further evaluation using mycelial growth inhibition assays confirmed that both compounds were significantly more active than ketoconazole against A. niger, B. dothidea, and F. oxysporum f. sp. cubense in vitro. The IC50 values for rhazinilam (32) were < 5, < 10, and 17.89 μg/mL, respectively; for rhazinal (33), the values were < 2.5, < 5, and < 5 μg/mL, respectively. Moreover, in vivo tests on cucumber leaves demonstrated that at a concentration of 40 μg/mL, compounds (32) and (33) provided significant protection against A. niger, with protection rates of 77.27 and 100%, respectively, compared to 47.62% for ketoconazole. Conclusions: Rhazinilam (32) and rhazinal (33) demonstrated potent antifungal activity in both in vitro and in vivo experiments, highlighting their promise as lead candidates for the development of novel fungicidal agents.