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Background <p><i>Gardenia imperialis</i> K. Schum. is a medicinal plant used in traditional medicine to treat malaria and related symptoms. This bio-guided study aimed at identifying antiparasitic compounds from <i>G. imperialis</i> against the causative agents of malaria (<i>Plasmodium falciparum</i>), visceral leishmaniasis (<i>Leishmania donovani</i>), and sleeping sickness (<i>Trypanosoma brucei brucei</i>).</p> Methods <p>Crude methanolic extracts from the leaf and stem bark of <i>G. imperialis</i> were studied using liquid chromatography–mass spectrometry (LC–MS) and preparative medium/high-performance liquid chromatography (M/HPLC) guided by evidence of antiparasitic activity. The structures of the isolated compounds were elucidated using nuclear magnetic resonance (NMR) and MS. All the extracts, fractions, subfractions, and pure compounds were evaluated for antiparasitic activity. Cytotoxicity was tested against Vero and Raw264.7 mammalian cell lines.</p> Results <p>The leaf methanolic extract (GIlMeOH) exhibited broad-spectrum antiparasitic activity (IC₅₀ &lt; 11&#xa0;µg/mL) and low cytotoxicity (median cell cytotoxicity—CC<sub>50</sub> &gt;100&#xa0;µg/mL). The dereplication of the extract and isolation yielded fractions, subfractions, and four flavonoids with improved activity (IC₅₀ values ranging from 0.67 to 23.8&#xa0;µg/mL). Among the isolated flavonoids, gradenin A (3), salvigenin (4), hispidulin (1), and 5,7,3ʹ-trihydroxy-6,4ʹ,5ʹ-trimethoxyflavone (2) showed potent antitrypanosomal activity with IC₅₀ values of 2.8, 2.5, 16.6, and 9.7&#xa0;µg/mL, respectively. The antiparasitic activities of gradenin A, salvigenin, and 5,7,3ʹ-trihydroxy-6,4ʹ,5ʹ-trimethoxyflavone are reported here for the first time.</p> Conclusion <p>The promising antiparasitic profile of the <i>G. imperialis</i> leaf extract and its isolated constituents, particularly and 5,7,3ʹ-trihydroxy-6,4ʹ,5ʹ-trimethoxyflavone (2), gradenin A (3), and salvigenin (4), warrants further investigation into their potential as novel and selective agents against the target parasitic diseases.</p>

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Bio-guided identification of novel antiparasitic natural products from Gardenia imperialis K. Schum (Rubiaceae)

  • 期刊论文

  • 发表日期：

    2026年6月19日

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  • Christelle Wayoue Kom,
  • Sylvester Osei Bobbie,
  • Darline Dize,
  • Cyrille Armel Njanpa Ngansop,
  • Mariscal Brice Tchatat Tali,
  • Lauve Rachel Tchokouaha Yamthe,
  • Bill Baker,
  • Fabrice Fekam Boyom

摘要

Background

Gardenia imperialis K. Schum. is a medicinal plant used in traditional medicine to treat malaria and related symptoms. This bio-guided study aimed at identifying antiparasitic compounds from G. imperialis against the causative agents of malaria (Plasmodium falciparum), visceral leishmaniasis (Leishmania donovani), and sleeping sickness (Trypanosoma brucei brucei).

Methods

Crude methanolic extracts from the leaf and stem bark of G. imperialis were studied using liquid chromatography–mass spectrometry (LC–MS) and preparative medium/high-performance liquid chromatography (M/HPLC) guided by evidence of antiparasitic activity. The structures of the isolated compounds were elucidated using nuclear magnetic resonance (NMR) and MS. All the extracts, fractions, subfractions, and pure compounds were evaluated for antiparasitic activity. Cytotoxicity was tested against Vero and Raw264.7 mammalian cell lines.

Results

The leaf methanolic extract (GIlMeOH) exhibited broad-spectrum antiparasitic activity (IC₅₀ < 11 µg/mL) and low cytotoxicity (median cell cytotoxicity—CC50 >100 µg/mL). The dereplication of the extract and isolation yielded fractions, subfractions, and four flavonoids with improved activity (IC₅₀ values ranging from 0.67 to 23.8 µg/mL). Among the isolated flavonoids, gradenin A (3), salvigenin (4), hispidulin (1), and 5,7,3ʹ-trihydroxy-6,4ʹ,5ʹ-trimethoxyflavone (2) showed potent antitrypanosomal activity with IC₅₀ values of 2.8, 2.5, 16.6, and 9.7 µg/mL, respectively. The antiparasitic activities of gradenin A, salvigenin, and 5,7,3ʹ-trihydroxy-6,4ʹ,5ʹ-trimethoxyflavone are reported here for the first time.

Conclusion

The promising antiparasitic profile of the G. imperialis leaf extract and its isolated constituents, particularly and 5,7,3ʹ-trihydroxy-6,4ʹ,5ʹ-trimethoxyflavone (2), gradenin A (3), and salvigenin (4), warrants further investigation into their potential as novel and selective agents against the target parasitic diseases.