{"title":"Bio-guided identification of novel antiparasitic natural products from Gardenia imperialis K. Schum (Rubiaceae).","authors":"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","doi":"10.1007/s40199-026-00618-w","DOIUrl":null,"url":null,"abstract":"<p><strong>Background: </strong>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).</p><p><strong>Methods: </strong>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.</p><p><strong>Results: </strong>The leaf methanolic extract (GIlMeOH) exhibited broad-spectrum antiparasitic activity (IC₅₀ < 11 µg/mL) and low cytotoxicity (median cell cytotoxicity-CC<sub>50</sub> >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 5,7,3'-trihydroxy-6,4',5'-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 5,7,3'-trihydroxy-6,4',5'-trimethoxyflavone are reported here for the first time.</p><p><strong>Conclusion: </strong>The promising antiparasitic profile of the G. imperialis leaf extract and its isolated constituents, particularly and 5,7,3'-trihydroxy-6,4',5'-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>","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":"34 2","pages":""},"PeriodicalIF":2.8000,"publicationDate":"2026-06-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13280111/pdf/","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"DARU Journal of Pharmaceutical Sciences","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1007/s40199-026-00618-w","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
引用次数: 0
Abstract
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 5,7,3'-trihydroxy-6,4',5'-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 5,7,3'-trihydroxy-6,4',5'-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 5,7,3'-trihydroxy-6,4',5'-trimethoxyflavone (2), gradenin A (3), and salvigenin (4), warrants further investigation into their potential as novel and selective agents against the target parasitic diseases.
期刊介绍：
DARU Journal of Pharmaceutical Sciences is a peer-reviewed journal published on behalf of Tehran University of Medical Sciences. The journal encompasses all fields of the pharmaceutical sciences and presents timely research on all areas of drug conception, design, manufacture, classification and assessment.
The term DARU is derived from the Persian name meaning drug or medicine. This journal is a unique platform to improve the knowledge of researchers and scientists by publishing novel articles including basic and clinical investigations from members of the global scientific community in the forms of original articles, systematic or narrative reviews, meta-analyses, letters, and short communications.
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