ABSTRACT
Acanthamoeba are free living amoeba that have been isolated from different environments like soil, water, air dust. Moreover, they are also able to act as opportunist pathogens, mainly causing a fatal encephalitis and also keratitis in both human and animals. This study was aimed to evaluate the activity of the Medicines for Malaria Venture (MMV) compounds against the trophozoite stage of Acanthamoeba castellanii Neff. Sixteen compounds showed ≥90% inhibition of parasite growth in the initial screen (10⯵M). Those set were further evaluated to determine the inhibitor concentration that inhibit the 50% of the initial population and cytotoxicity against murine macrophages. Among the compounds included in the pathogen box, pentamidine and posaconazole were the most effective against this parasite with an of IC50 of 0.567⯱â¯0.04 and 0.630⯱â¯0.11, respectively.
Subject(s)
Acanthamoeba castellanii/drug effects , Amebicides/pharmacology , Amebicides/classification , Animals , Cell Line/drug effects , Cell Survival/drug effects , Dose-Response Relationship, Drug , Inhibitory Concentration 50 , Mice , Pentamidine/pharmacology , Triazoles/pharmacology , Trophozoites/drug effectsABSTRACT
A series of the natural constituents with amoebicidal activity isolated from several medicinal plants is shown. A list of the medicinal plants potentially active as amoebicide and/or against dysentery also is demonstrated. The present data grouping of the natural compounds and medicinal plants can be an important source of information for the selection of research plant material by the investigators interested in the discovery of new biologically active compounds as amoebicide.
Subject(s)
Amebicides/isolation & purification , Plants, Medicinal/chemistry , Amebicides/chemical synthesis , Amebicides/classification , Amebicides/pharmacology , Amebicides/therapeutic use , Animals , Brazil , Dysentery, Amebic/drug therapy , Entamoeba histolytica/drug effects , Humans , Molecular Structure , Phytotherapy , Plants, Medicinal/classificationABSTRACT
En conclusion, puede afirmarse que en la actualidad la amibiasis intestinal y hepatica, tiene un tratamiento muy especifico y efectivo en el 90-96%, gracias al descubrimiento del metronidazol y sus derivados actuales mas potentes y de vida media mas larga; algunas molestias dispepticas observadas en el 5% de los pacientes con este tipo de drogas se corrije facilmente si se administra concomitantemente Metoclopramida por via oral. Es aconsejable prolongar el tratamiento por 10 dias; la accion antabuse se debe explicar al paciente; para efectos de abstencion de alcohol durante el tiempo de tratamiento especifico. Las drogas luminales pracaticamente ya no se usan, ya que el metronidazol en dosis orales de 2 grs. al dia se elimina en las heces en cantidad de 14-120 mgrs por 100 grs de heces y marcando la droga con C 14, con dosis de 750 mg. al dia, aparece el 14% de la droga en las heces, lo cual significa la muy buena accion luminal de este tipo de droga amebicida. La forma parenteral del metronidazol y del ornidazol, esta indicada en las formas muy severas de infeccion amibiana intestinal o hepatica; debe recordarse la accion sobre anaerobioso del metronidazol y ornidazol por via I.V. en casos de sepsis. En casos de "amibiasis cronica", que no mejoran con tratamiento antiamibiano especifico, debe considerarse la posibilidad de un diagnostico de COLON IRRITABLE. Es probable que paralelamente en el transcurso de una amibiasis exista un cuadro de ALACTASIA; de ahi la marcada intolerancia a la leche de practicamente todos los pacientes con amibiasis.