RESUMEN
Background: The gastrointestinal parasite Giardia lamblia causes giardiasis. Its treatment with standard drugs produces side effects and improper treatment can generate resistant strains. New antigiardial compounds are needed. An analysis was done to identify the antigiardial activity of Morinda royoc, a plant used in traditional Mayan medicine to treat stomach and bowel pain. We aimed to assess the efficacy of M. royoc roots against G. lamblia and their effect on cells viability. Methods: A methanol extract was done of the root and then fractionated. The extract and fractions were tested in vitro on G. lamblia trophozoites and their effect on cell viability was quantified by flow cytometry. The active extract and fractions were analyzed by gas chromatography-mass spectrometry and high-performance liquid chromatography. Results: The hexane fraction exhibited potent activity against G. lamblia (IC50 = 0.08 µg/mL). Its principal component was an anthraquinone-type compound. None of the fractions were toxic to human promyelocytic leukemia, chronic myelogenous leukemia and human mononuclear cells. Conclusion: The medicinal plant M. royoc contains promising bioactive agents with antigiardial activity and deserves further research.
RESUMEN
The in vivo antifibrotic effect of a fucoidan extract (FE) from Sargassum fluitans Borgesen was evaluated in a carbon tetrachloride-induced liver damage model in rats over twelve weeks. Chemical analysis showed the FE to contain carbohydrates, sulfates, uronic acids, protein, phenols, and to have a molecular weight of ~60 kDa. Physiological, biochemical, histological and genetic assays were done. Daily oral administration of FE (50 mg/kg) reduced liver enzymatic activity, liver infiltration of inflammatory cells, collagen fiber deposition and gene expression cytokines such as interleukin beta 1 (IL-ß1), tumor necrosis factor alpha (TNF-α), transforming growth factor beta 1 (TGF-ß1), Smad-3, Smad-2, collagen 1 alpha 1 (col1α1) and tissue inhibitor of metalloproteinase 1 (TIMP-1). It also increased RNA expression of Smad-7 and metalloproteinase 2 and 9 (MMP2 and MMP9). The fucoidan extract exhibited an antifibrotic effect mediated by the inhibiting TGF-ß1/Smad pathway, as well as anti-inflammatory effects.
Asunto(s)
Cirrosis Hepática/tratamiento farmacológico , Extractos Vegetales/farmacología , Polisacáridos/química , Sargassum/química , Animales , Tetracloruro de Carbono/toxicidad , Intoxicación por Tetracloruro de Carbono/tratamiento farmacológico , Intoxicación por Tetracloruro de Carbono/genética , Intoxicación por Tetracloruro de Carbono/patología , Modelos Animales de Enfermedad , Regulación de la Expresión Génica/efectos de los fármacos , Humanos , Hígado/efectos de los fármacos , Cirrosis Hepática/inducido químicamente , Cirrosis Hepática/patología , Extractos Vegetales/química , Polisacáridos/farmacología , Ratas , Transducción de Señal/efectos de los fármacos , Proteínas Smad/genética , Proteína smad3/genética , Factor de Crecimiento Transformador beta/genética , Factor de Crecimiento Transformador beta1/genéticaRESUMEN
One of the leading causes of death worldwide, cirrhosis, is a liver condition characterized by chronic necrosis, inflammation, and fibrosis. Hepatoprotective compounds, such as antioxidants, can prevent fibrosis. Macroalgae (seaweed) contain high amounts of antioxidant compounds and are plentiful; indeed, species such as Sargassum fluitans Borgesen (Phaeophyceae) carpet many beaches in the Caribbean Basin. An in vivo assay was done evaluating the possible hepatoprotective effect of a Sargassum fluitans ethanol extract. Two murine liver damage models were employed: acetaminophen (APAP) in Balb/c mice to induce acute damage; carbon tetrachloride (CCl4) in Wistar rats to induce chronic damage. Serum liver enzyme levels and relative liver weight were measured, and histopathological and immunohistochemical analyses of liver tissue sections were done. Both APAP and CCl4 significantly raised serum enzyme marker enzymes. Administration of 50 mg/kg S. Fluitans ethanol extract reduced this APAP- and CCl4-induced elevation to normal levels. This effect was corroborated by the extract's inhibition of inflammation and fibrosis in liver tissue observed in the histopathological analysis. The analyzed S. fluitans ethanol extract exhibited an in vivo hepatoprotective effect in acute and chronic liver injury models.
Asunto(s)
Enfermedad Aguda/terapia , Enfermedad Hepática Inducida por Sustancias y Drogas/tratamiento farmacológico , Enfermedad Crónica/terapia , Hígado/efectos de los fármacos , Extractos Vegetales/farmacología , Sustancias Protectoras/farmacología , Sargassum/química , Acetaminofén/farmacología , Adulto , Animales , Antioxidantes/farmacología , Tetracloruro de Carbono/farmacología , Etanol/química , Humanos , Inflamación/tratamiento farmacológico , Cirrosis Hepática/tratamiento farmacológico , Pruebas de Función Hepática/métodos , Ratones , Ratones Endogámicos BALB C , Ratas Wistar , Adulto JovenRESUMEN
Serjania goniocarpa is a plant used in Mayan traditional medicine as a remedy for the treatment of cancer-like symptoms. Bio-guided fractionation of the methanol extract of the leaves led to the isolation of an α- and ß-amyrin mixture, palmitic acid, phytol and the new sesterterpene goniocarpic acid whose structure was elucidated by IR, GC-MS, and NMR spectroscopic analyses. Goniocarpic acid exhibited cytotoxic and antiproliferative activity against several cancer cell lines.