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1.
Iran J Parasitol ; 17(2): 259-267, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36032741

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.

2.
Nat Prod Res ; 36(18): 4714-4718, 2022 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-34747293

RESUMEN

A series of 15 novel 1,3-thiazole amide derivatives of the pentacyclic triterpene Ochraceolide A (1) was synthesized, characterized, and evaluated in vitro against three human cancer cell lines (MCF-7, MDA-MB-231 and SiHa) and a normal cell line (Vero). Synthetic derivatives were obtained by acylation of the 2-aminothiazole triterpene 2, previously reported. Remarkably, the 5-nitrofuramide derivative (2o) showed better cytotoxic and antiproliferative activity than compound 2 and the other derivatives against the three cancer cell lines with CC50 and IC50 values of 1.6-12.7 µM. Furthermore, butyramide derivative (2c) was approximately 25 times more selective than 2, as well as 3.4 times more selective than Docetaxel, against SiHa cells in the cytotoxic assay, while the phenyl amide derivatives were inactive against the three cancer cell lines.


Asunto(s)
Antineoplásicos , Triterpenos , Amidas/farmacología , Antineoplásicos/farmacología , Línea Celular Tumoral , Proliferación Celular , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Relación Estructura-Actividad , Tiazoles/farmacología , Triterpenos/farmacología
3.
Int J Biol Macromol ; 145: 500-509, 2020 Feb 15.
Artículo en Inglés | MEDLINE | ID: mdl-31874267

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/genética
4.
Biomed Res Int ; 2018: 6921845, 2018.
Artículo en Inglés | MEDLINE | ID: mdl-30671467

RESUMEN

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 Joven
5.
J Diet Suppl ; 14(2): 158-172, 2017 Mar 04.
Artículo en Inglés | MEDLINE | ID: mdl-27485995

RESUMEN

Several studies have shown the hepatoprotective effect of the consumption of coffee and tea, which is mainly attributed to caffeine. Many experimental studies have demonstrated this effect; however, these studies used high caffeine doses that are not related to human consumption. The aim of this study was to evaluate the hepatoprotective effect of low doses of caffeine on carbon tetrachloride (CCl4)-treated rats. Low doses of caffeine (CAFF) 5 and 10 mg/kg (CAFF5 and CAFF10) were evaluated in chronic liver damage induced by CCl4 (0.75 mL/kg) in rats. CAFF treatment was administered once a day and CCl4 administration was twice weekly for 10 weeks. Liver function tests (biochemical markers) and functional (sleeping time) and histological (hematoxylin-eosin and Masson trichrome stains) parameters were carried out at the end of damage treatment. Daily treatments of CAFF5 and CAFF10 exhibited a hepatoprotective effect supported by a decrease of alanine aminotransferase (ALT), aspartate aminotransferase (AST), and alkaline phosphatase (AP) serum activities and bilirubin serum levels compared with control and also restored serum albumin levels and liver glutathione (GSH). Moreover, CAFF prevented CCl4-induced prolongation in pentobarbital sleeping time and a decrease of liver fibrosis and cell death. Our results demonstrated that low doses of CAFF exert a hepatoprotective effect against CCl4 -induced liver damage in rats.


Asunto(s)
Cafeína/uso terapéutico , Intoxicación por Tetracloruro de Carbono/tratamiento farmacológico , Enfermedad Hepática Crónica Inducida por Sustancias y Drogas/tratamiento farmacológico , Cirrosis Hepática/tratamiento farmacológico , Sustancias Protectoras/uso terapéutico , Alanina Transaminasa/sangre , Fosfatasa Alcalina/sangre , Animales , Aspartato Aminotransferasas/sangre , Bilirrubina/sangre , Cafeína/administración & dosificación , Tetracloruro de Carbono , Intoxicación por Tetracloruro de Carbono/fisiopatología , Muerte Celular/efectos de los fármacos , Enfermedad Hepática Crónica Inducida por Sustancias y Drogas/fisiopatología , Relación Dosis-Respuesta a Droga , Glutatión/metabolismo , Hígado/efectos de los fármacos , Hígado/fisiopatología , Cirrosis Hepática/inducido químicamente , Cirrosis Hepática/fisiopatología , Pruebas de Función Hepática , Masculino , Sustancias Protectoras/administración & dosificación , Ratas , Ratas Wistar , Sueño/efectos de los fármacos
6.
Nat Prod Commun ; 10(9): 1513-6, 2015 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-26594746

RESUMEN

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.


Asunto(s)
Ácido Oleanólico/análogos & derivados , Sapindaceae/química , Sesquiterpenos/química , Sesquiterpenos/aislamiento & purificación , Sesterterpenos/química , Sesterterpenos/aislamiento & purificación , Línea Celular Tumoral , Humanos , Medicina Tradicional , Estructura Molecular , Ácido Oleanólico/química , Ácido Oleanólico/aislamiento & purificación , Extractos Vegetales/química , Hojas de la Planta/química
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