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<p>Bioactivity-guided fractionation of an anti-<i>Trypanosoma cruzi</i> active extract from <i>Miconia willdenowii</i> Klotzsch ex Naudin, Melastomataceae, led to the isolation of one hydroquinone, miconidin, and a related quinone derivative, primin. The structures of these compounds were elucidated through detailed NMR and MS data analysis. Miconidin and primin demonstrated significant <i>in vitro</i> activity against the epimastigote forms of <i>T. cruzi</i>, with EC<sub>50</sub> values of 2.6 ± 2.4&#xa0;µM and 5.7 ± 2.1&#xa0;µM, respectively, compared to the reference drug benznidazole, which exhibited an EC<sub>50</sub> value of 39.5 ± 7.0&#xa0;µM. Both compounds showed low toxicity toward human primary skin fibroblasts (CCD-1059Sk), with CC<sub>50</sub> values exceeding 200&#xa0;µM. Furthermore, primin exhibited <i>in vivo</i> anti-<i>T. cruzi</i> activity, as evidenced by a reduction in parasitemia in the blood of treated mice. These findings suggest that miconidin and primin hold promise as prototypes for the development of novel therapeutic agents against Chagas disease.</p> Graphical Abstract <p></p>

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Antitrypanosomal Activity of Hydroquinone and Quinone Derivatives Isolated from Miconia willdenowii

  • 期刊论文

  • 发表日期：

    2025年1月19日

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  • Welton Rosa,
  • Bruna L. Silva,
  • Guilherme A. Ferreira Silva,
  • Daniel O. Miranda,
  • João L. Baldim,
  • Bianca B. Fernandes,
  • Patrícia Sartorelli,
  • Marisa Ionta,
  • Ivo S. Caldas,
  • João Henrique G. Lago,
  • Danielle F. Dias,
  • Daniela A. Chagas-Paula,
  • Marisi G. Soares

摘要

Bioactivity-guided fractionation of an anti-Trypanosoma cruzi active extract from Miconia willdenowii Klotzsch ex Naudin, Melastomataceae, led to the isolation of one hydroquinone, miconidin, and a related quinone derivative, primin. The structures of these compounds were elucidated through detailed NMR and MS data analysis. Miconidin and primin demonstrated significant in vitro activity against the epimastigote forms of T. cruzi, with EC50 values of 2.6 ± 2.4 µM and 5.7 ± 2.1 µM, respectively, compared to the reference drug benznidazole, which exhibited an EC50 value of 39.5 ± 7.0 µM. Both compounds showed low toxicity toward human primary skin fibroblasts (CCD-1059Sk), with CC50 values exceeding 200 µM. Furthermore, primin exhibited in vivo anti-T. cruzi activity, as evidenced by a reduction in parasitemia in the blood of treated mice. These findings suggest that miconidin and primin hold promise as prototypes for the development of novel therapeutic agents against Chagas disease.

Graphical Abstract