RESUMO
Pathogenic Acanthamoeba strains are causative agents of Granulomatous Amoebic Encephalitis (GAE) and Acanthamoeba keratitis (AK) worldwide. The existence of the cyst stage complicates Acanthamoeba therapy as it is highly resistant to antibiotics and physical agents. The aim of this study was to investigate the activity of Limouni olive leaf cultivar against the trophozoite stage of Acanthamoeba. The ethyl acetate and methanol extracts of this variety were tested against Acanthamoeba castellanii Neff. The ethyl acetate extract of olive leaf was the most active showing an IC50 of 5.11±0.71µg/ml of dry extract. Bio-guided fractionation of this extract was conducted and led to the identification of three active compounds namely oleanolic and maslinic acids and oleuropein which could be used for the development of novel therapeutic approaches against Acanthamoeba infections.
Assuntos
Acanthamoeba castellanii/efeitos dos fármacos , Olea/química , Extratos Vegetais/farmacologia , Acanthamoeba castellanii/crescimento & desenvolvimento , Bioensaio , Cromatografia em Gel , Concentração Inibidora 50 , Testes de Sensibilidade Parasitária , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Trofozoítos/efeitos dos fármacos , Trofozoítos/crescimento & desenvolvimento , TunísiaRESUMO
Protozoan diseases, such as leishmaniasis, are a cause of considerable morbidity throughout the world, affecting millions every year. In this study, two triterpenic acids (maslinic and oleanolic acids) were isolated from Tunisian olive leaf extracts and their in vitro activity against the promastigotes stage of Leishmania (L.) infantum and Leishmania (L.) amazonensis was investigated. Maslinic acid showed the highest activity with an IC50 of 9.32 ± 1.654 and 12.460 ± 1.25 µg/ml against L. infantum and L. amazonensis, respectively. The mechanism of action of these drugs was investigated by detecting changes in the phosphatidylserine (PS) exposure, the plasma membrane permeability, the mitochondrial membrane potential and the ATP level production in the treated parasites. By using the fluorescent probe SYTOX® Green, both triterpenic acids showed that they produce a time-dependent plasma membrane permeabilization in the treated Leishmania species. In addition, spectrofluorimeteric data revealed the surface exposure of PS in promastigotes. Both molecules reduced the mitochondrial membrane potential and decreased the ATP levels to 15% in parasites treated with IC90 for 24h. We conclude that the triterpenic acids tested in this study, show potential as future therapeutic alternative against leishmaniasis. Further studies are needed to confirm this.
Assuntos
Leishmania/efeitos dos fármacos , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Olea/química , Ácido Oleanólico/farmacologia , Extratos Vegetais/farmacologia , Trifosfato de Adenosina/metabolismo , Antiprotozoários/farmacologia , Permeabilidade da Membrana Celular , Estrutura Molecular , Folhas de Planta/química , Triterpenos/farmacologiaRESUMO
Los parásitos intestinales son un grave problema de salud pública donde la alta prevalencia está asociado a la falta de educación sanitaria, hábitos higiénicos e infraestructura inadecuada. El presente trabajo es un estudio descriptivo de corte transversal, donde el universo de trabajo son todos los niños de la Escuela Sapecho A (Gestión 2016-2017), trabajo que involucro a estudiantes de pregrado y de post grado de la Facultad de Ciencia Farmacéuticas y Bioquímicas, donde a través de estudios coproparasitológicos (técnica de Ritchie) se pudo observar que la mayoría de la población, entre 78,24 y 88,4%, se encontraba infectada por uno o más parásitos (HelmintosProtozoos). Luego de realizar una desparasitación masiva con albendazol (400mg/Dos dosis) se llegó a una reducción respecto a los helmintos de 53,5 y 65,2% respectivamente en cada gestión, sin embargo, este no fue efectivo contra los protozoos. Para alcanzar un éxito en el tratamiento se debe tratar al grupo familiar y dar énfasis al componente educativo de higiene y limpieza.
Intestinal parasites are a serious public health problem where the high prevalence is associated with a lack of education, inadequate hygienic habits and sanitary infrastructure. The present work is a cross-sectional descriptive study, where the universe of work are the children of Sapecho A School (Management 2016-2017), work that involved undergraduate and post-graduate students of the Faculty of Pharmaceutical Science and Biochemistry where through coproparasitological studies (Ritchie's technique) it was observed that the majority of the population, between 78.24 and 88.4%, was infected by one or more parasites (Helminths-Protozoa). After performing a massive deworming treatment with albendazole (400mg/Two doses) a reduction was reached with respect to the helminths of 53.5 and 65.2%, respectively in each year, however this was not effective against the protozoa. To achieve a successful treatment, the family group must be treated and the educational component of hygiene and cleanliness should be emphasized.
Assuntos
Parasitos , Saúde Pública , Helmintos , Albendazol , HábitosRESUMO
El Instituto de Investigaciones Fármaco Bioquímicas (IIFB), de la Facultad de Ciencias Farmacéuticas y Bioquímicas, de la UMSA, desarrolla trabajos sobre la actividad leishmanicida, de los alcaloides totales (CAT) obtenidos de la corteza de la especie medicinal amazónica conocida como Evanta (Galipea longiflora) por los Pueblos Tacana, Tsimane y Mosetene. Como parte de las actividades del Proyecto UMSA-ASDI Biomoleculas de interés medicinal e industrial (antiparasitarios) hemos podido contar con la estadía, en el IIFB, de un investigador del Armauer Hansen Research Institute (AHRI) de Etiopia, lo que nos ha permitido desarrollar evaluaciones de CAT, Miltefocine y Amfotericina B, frente a cepas de Leishmania aethiopica, agente causante de las diversa formas de Leishmaniais cutánea en Etiopía. Un total de seis cepas, de L. aethiopica, fueron adaptadas a condiciones in vitro y mostraron un comportamiento homogéneo frente a CAT, cinco de estas cepas mostraron un valor promedio de IC50 = 8,68 ±1,56 mg/mL, valor algo inferior a los calculados para nuestras cepas de referencia, L. amazonensis y L. braziliensis con IC50 = 11,73 ± 4,32 mg/mL y IC50 = 12,28 ±- 2,95 mg/mL, respectivamente. Excepto por una cepa de L. aethiopica que mostro valores consistentemente más elevados que el resto con IC50= 14,37 ± 3,58 mg/mL. Como consecuencia de esta interacción científica, la Universidad Mayor de San Andrés (UMSA) ha firmado un Memorandum de Entendimiento para el desarrollo de investigaciones conjuntas, con el Armauer Hansen Research Institute (AHRI), dependiente del Ministerio de Salud de Etiopia y explorar la posibilidad de que nuestra experiencia de validación clínica con Evanta en el tratamiento de leishmaiasis cutánea, en Bolivia, podría ser replicada en Etiopía, donde se reportan entre 20,000 a 30,000 nuevos casos de Leismaniasis por año.
The Instituto de Investigaciones Fármaco Bioquímicas (IIFB), at the Faculty of Pharmaceutical and Biochemical Sciences, from UMSA, carry out work related to the leishmanicidal activity of the total alkaloids (CAT) obtained from the bark of the Amazonian medicinal species known as Evanta (Galipea longiflora) by the Tacana, Tsimane y Mosetene people. As part of the activities develop by the UMSA-ASDI Project Biomolecules of medicinal and industrial Interest (antiparasitic) we had a visit, in our laboratories at IIFB, of a researcher from The Armauer Hansen Research Institute (AHRI) from Ethiopia, during his stay we were able to carry out evaluations of CAT, Miltefocine and Anphotericin B, against strains of L. aethiopica, causative agent of the different manifestations of cutaneous leishmaniasis in Ethiopia. A total of six strains of L. aethiopica, were adapted to in vitro a conditions, at IIFB; and did show homogenous behavior against CAT. Five of the strains, showed an average calculated value for IC50 = 8.68 ±1.56 mg/mL, a value somewhat lower to the calculated for the reference strains L. amazonensis and L. braziliensis with IC50 = 11.73 ± 4.32 mg/mL and IC50 = 12.28 +/- 2.95 mg/mL, respectively. Except for one strain that showed values somewhat higher, to the other strains, consistently through our studies, with IC50 = 14.37 ± 3.58 mg/mL. As a consequence of our scientific interaction, the Universidad Mayor de San Andrés (UMSA) has signed a Memorandum of Understanding for the development of joint research with the Armauer Hansen Research Institute (AHRI) that belongs to the Ministry of Health in Ethiopia, and explore the possibilities to replicate the Bolivian clinical validation experience of Evanta in the treatment of cutaneous leishmaniasis, in Ethiopia where the annual incidence is estimated to be between 20, 000 to 30, 0000.
Assuntos
Parasitologia , Técnicas In Vitro , Leishmaniose Cutânea , Pesquisa , Academias e Institutos , AntiparasitáriosRESUMO
As part of our continuing search for bioactive natural products from plants, the present study was carried out in order to evaluate the gastroprotective properties of alkaloid extract and 2-phenylquinoline obtained from the bark of Galipea longiflora (Rutaceae). Anti-ulcer assays were performed using the following protocols in mice: nonsteroidal anti-inflammatory drug (NSAID)/bethanecol-induced ulcer, ethanol/HCl-induced ulcer, and stress-induced ulcer. The effects of the extract on gastric content volume, pH and total acidity were also evaluated, using the pylorus ligated model. Treatment using doses of 50, 125 and 250 mg/kg of G. longiflora alkaloid extract and positive controls (omeprazol or cimetidine) significantly diminished the lesion index, total lesion area, and percentage of lesion, in comparison with the negative control groups in all the models evaluated. Regarding the model of gastric secretion, a reduction in volume of gastric juice and total acidity was observed, as well as an increase in gastric pH. The main alkaloid of the plant, 2-phenylquinoline, was also evaluated in the ethanol-induced ulcer model. The results showed that at a dose of 50 mg/kg, it significantly inhibited ulcerative lesions. However, this effect was less than that of the alkaloid extract. All these results taken together show that G. longiflora displays gastroprotective activity, as evidenced by its significant inhibition of the formation of ulcers induced by different models. There are indications that mechanisms involved in anti-ulcer activity are related to a decrease in gastric secretion and an increase in gastric mucus content. Also, there is evidence of involvement of NO in the gastroprotector mechanisms. These effects may be attributed, at least in part, to the presence of some alkaloids, particularly 2-phenylquinoline.
Assuntos
Alcaloides/farmacologia , Extratos Vegetais/farmacologia , Quinolinas/farmacologia , Rutaceae/química , Úlcera Gástrica/prevenção & controle , Alcaloides/química , Animais , Antiulcerosos/química , Antiulcerosos/farmacologia , Betanecol/toxicidade , Relação Dose-Resposta a Droga , Etanol/toxicidade , Ácido Clorídrico/toxicidade , Indometacina/toxicidade , Camundongos , Estrutura Molecular , Casca de Planta/química , Extratos Vegetais/química , Quinolinas/química , Ratos , Ratos Wistar , Úlcera Gástrica/induzido quimicamenteRESUMO
El presente artículo describe la validación de un método de cuali-cuantificación de alcaloides quinolínicos por espectrofotometría UV con máximos de absorción de 330-335nm de longitud de onda. Para su cuantificación el extracto de alcaloides es disuelto en ácido clorhídrico 1N, al 0,05 %p/v y se preparan 12 diluciones 1:2. El método cumple con los requerimientos de exactitud y precisión con límites de detección y cuantificación entre 0,567-7,81 µg/mL y 1,72-7,81 µg/mL para los alcaloides quinolínicos respectivamente. Se obtuvieron respuestas lineales entre 0,2447,81 µg/mL con un coeficiente de determinación de 0,997. Se verificó la robustez del procedimiento aplicando tres variables, temperatura, luz UV y pH. (AU)