Antitrypanosomal Activity and Molecular Docking Studies of Lobetyolin From Lobelia rhynchopetalum Hemsl. Root Extract Against Trypanosoma congolense Field Isolates.

Currently available drugs for trypanosomiasis are few, and their use is limited by toxicity and growing resistance. This highlights the need for safer and more effective alternatives. In this study, the in vitro and in vivo antitrypanosomal activities of an 80% methanol root extract of Lobelia rhync...

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Publicado en:BioMed Research International Vol. 2026; pp. 1 - 16
Autores principales: Yimer, Selamawit, Tewelde, Eyael, Bisrat, Daniel, Tadesse, Solomon, Yeshak, Mariamawit Y., Shivahare, Rahul
Formato: equations & formulas pictorial research tables/charts Journal Article
Publicado: Wiley-Blackwell 2/4/2026
Acceso en línea:Ver este registro en EBSCOhost
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      dt: 2/4/2026
      vid: 2026
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      pub: Wiley-Blackwell
      place: Malden, Massachusetts
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        10.1155/bmri/2214310
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        atl: Antitrypanosomal Activity and Molecular Docking Studies of Lobetyolin From Lobelia rhynchopetalum Hemsl. Root Extract Against Trypanosoma congolense Field Isolates.
      aug:
        au:
          Yimer, Selamawit
          Tewelde, Eyael
          Bisrat, Daniel
          Tadesse, Solomon
          Yeshak, Mariamawit Y.
          Shivahare, Rahul
        affil: Department of Pharmacognosy,, School of Pharmacy,, College of Health Sciences,, Bahir Dar University,, Bahir Dar, Ethiopia, bdu.edu.et
      sug:
        subj:
          Protozoa Drug Effects
          Plant Extracts Pharmacodynamics
          Plant Roots
          Antiprotozoal Agents Pharmacodynamics
          Phytochemicals Pharmacodynamics
          Trypanosomiasis Drug Therapy
          Mice
          Animal Studies
          Models, Biological
          Molecular Docking Simulation
          In Vitro Studies
          In Vivo Studies
          Parasitemia Prevention and Control
          Oxidation-Reduction Drug Effects
          Plant Extracts Administration and Dosage
          Phytochemicals Administration and Dosage
          Ethiopia
          Descriptive Statistics
          Data Analysis Software
          One-Way Analysis of Variance
          Post Hoc Analysis
          Funding Source
      ab: Currently available drugs for trypanosomiasis are few, and their use is limited by toxicity and growing resistance. This highlights the need for safer and more effective alternatives. In this study, the in vitro and in vivo antitrypanosomal activities of an 80% methanol root extract of Lobelia rhynchopetalum and its major constituent were evaluated against Trypanosoma congolense field isolates. Phytochemical separation of the extract yielded lobetyolin (a polyacetylene compound), confirmed through spectroscopic analysis. At 4 mg/mL, both the crude extract and lobetyolin inhibited parasite motility, with lobetyolin acting slightly faster (25 min) than the extract (30 min). The blood incubation assay demonstrated dose‐dependent protection, with 4 mg/mL of DA, the lobetyolin‐rich extract, or pure lobetyolin preventing infection, while lower doses only delayed parasitemia. In vivo testing showed that lobetyolin at 100 mg/kg exhibited stronger activity than the crude extract at 400 mg/kg. Molecular docking demonstrated that lobetyolin binds strongly to the homology‐modeled trypanothione reductase (TR) enzyme of T. congolense, achieving a Glide score of −8.002 kcal/mol, which is close to that of the native ligand (−8.307 kcal/mol). This suggests that lobetyolin may inhibit TR, thereby disrupting the parasite′s redox balance essential for survival. Overall, these findings provide the first evidence supporting the antitrypanosomal activity of L. rhynchopetalum root extract and lobetyolin, providing scientific support to the plant′s traditional use. Further studies are needed to fully validate its therapeutic potential.
      pubtype: Academic Journal
      doctype:
        equations & formulas
        pictorial
        research
        tables/charts
        Journal Article
      ougenre: Article
    language: English
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