Clethra fimbriata hexanic extract triggers alteration in the energy metabolism in epimastigotes of Trypanosoma cruzi.

Chagas disease (ChD), caused by Trypanosoma cruzi, is endemic in American countries and an estimated 8 million people worldwide are chronically infected. Currently, only two drugs are available for therapeutic use against T. cruzi and their use is controversial due to several disadvantages associated with side effects and low compliance with treatment. Therefore, there is a need to search for new tripanocidal agents. Natural products have been considered a potential innovative source of effective and selective agents for drug development to treat T. cruzi infection. Recently, our research group showed that hexanic extract from Clethra fimbriata (CFHEX) exhibits anti-parasitic activity against all stages of T. cruzi parasite, being apoptosis the main cell death mechanism in both epimastigotes and trypomastigotes stages. With the aim of deepening the understanding of the mechanisms of death induced by CFHEX, the metabolic alterations elicited after treatment using a multiplatform metabolomics analysis (RP/HILIC-LC-QTOF-MS and GC-QTOF-MS) were performed. A total of 154 altered compounds were found significant in the treated parasites corresponding to amino acids (Arginine, threonine, cysteine, methionine, glycine, valine, proline, isoleucine, alanine, leucine, glutamic acid, and serine), fatty acids (stearic acid), glycerophospholipids (phosphatidylcholine, phosphatidylethanolamine and phosphatidylserine), sulfur compounds (trypanothione) and carboxylic acids (pyruvate and phosphoenolpyruvate). The most affected metabolic pathways were mainly related to energy metabolism, which was found to be decrease during the evaluated treatment time. Further, exogenous compounds of the triterpene type (betulinic, ursolic and pomolic acid) previously described in C. fimbriata were found inside the treated parasites. Our findings suggest that triterpene-type compounds may contribute to the activity of CFHEX by altering essential processes in the parasite.

Chemical Profile, Antibacterial Activity and Antibiotic-Modulating Effect of the Hexanic Zea Mays L. Silk Extract (Poaceae).

The present study aimed to determine the chemical profile and to evaluate the antibacterial activity and antibiotic-modulating action of the hexanic Zea mays silk extract in association with aminoglycosides. Standard Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923 and Pseudomonas aeruginosa ATCC 27853 strains, as well as multi-resistant Escherichia coli 27, Staphylococcus aureus 35, and Pseudomonas aeruginosa 31 strains, were used in this study. Phytochemical prospection revealed the presence of the following secondary metabolites: tannins, flavones, flavonoids, and xanthones, with the main chemical constituents being identified in plant extracts obtained with apolar organic solvents such as hexane. The extract presented a minimum inhibitory concentration (MIC) ≥1024 µg/mL against all the tested strains. The association of the extract with aminoglycoside antibiotics showed significant synergistic effects against Staphylococcus aureus and Pseudomonas aeruginosa, except for amikacin, which was antagonized by the extract against E. coli. These results indicate the Zea mays silk presents bioactive compounds with antibiotic-modulating properties. However, further research is required to characterize the effects of isolated compounds and determine their potential for drug development.

Schistosoma mansoni: In vivo evaluation of Phyllanthus amarus hexanic and ethanolic extracts.

Human schistosomiasis is an important neglected tropical disease caused by blood flukes of the genus Schistosoma and is responsible for more than 280,000 deaths annually. Treatment for this disease relies currently on a single drug, praziquantel (PZQ). Concerns regarding PZQ resistance and insensitivity of juvenile schistosomes have increased the interest in resorting to medicinal plants for alternative drug therapies. This study aimed to perform an in vivo schistosomicidal activity evaluation of crude hexanic (HE) and ethanolic (EE) extracts obtained from Phyllanthus amarus in mice infected with Schistosoma mansoni (BH strain). Mice were treated orally with a single dose of 100 or 250 mg/kg, on two different infection periods, 30 and 45 days post-infection (dpi). Parameters such as worm recovery, faecal egg count, intestinal tissue egg count and liver histopathology were evaluated. Treatment against young adult (30 dpi) and adult (45 dpi) worms were more effective compared to the control group treated with PZQ. At a concentration of 250 mg/kg (30 dpi) EE showed a 54.4% female reduction and a 61.2% total worm reduction whilst at a concentration of 100 mg/kg (45 dpi) HE showed a 40.6% female worm reduction and a 45.3% total worm reduction. Histopathological examination showed a granuloma decrease in both number and size for groups treated with 250 mg/kg of HE (45 dpi) or EE (30 or 45 dpi). From these results, it can be concluded that both hexanic and ethanolic extracts have antischistosomal activities, however, act differently according to the parasites age. The schistosomicidal activity results in groups treated 30 days post infection is extremely important since praziquantel does not show activity against the juvenile forms of Schistosoma.

Actividad antibacteriana del extracto total de hojas de Cucurbita moschata Duchesne (Ahuyama) / Antibacterial activity of total extract from leaves of Cucurbita moschata Duchesne (ahuyama)

Introduction: Cucurbita moschata Duchesne (ahuyama) is grown across America as well as in the Middle East and Europe. It has been used as alternative medicine since ancient times. In the northern section of the department of Bolívar, Colombia, the plant is used by peasants to treat skin infections, hence our interest in conducting this study. Objective: Evaluate the antibacterial activity of total extract from leaves ofC. moschata against Staphylococcus aureus, Klebsiella pneumoniae and Escherichia coli. Methods: Fresh leaves of C. moschata were classified taxonomically using standard methods. The leaves were dried in an oven and pulverized in a blade mill. Extraction was performed by cold solid-liquid percolation and concentration in a rotary evaporator. Antibacterial activity of the ethanolic and hexanic extracts was evaluated in vitro against methicillin-resistant Staphylococcus aureus, Escherichia coli and Klebsiella pneumoniae, using the minimum inhibitory concentration (MIC) method, in compliance with guidelines from the Clinical and Laboratory Standards Institute (CLSI). Results: The hexanic extract caused significant inhibition from dilution 0.16 µg/mL for S. aureus strain ATCC 43300, and from dilution 19.5 µg/mL for strain ATCC 25923 (MSSA). The ethanolic and hexanic extracts significantly inhibited the growth of the clinical E. coli strain, whereas no significant inhibition was observed for K. pneumoniae at any of the concentrations tested. Conclusions: For the first time it was shown that the total hexanic extract of leaves of C. moschata had the greatest inhibition power against clinical strains of S. aureus and E. coli. The antimicrobial potential of this native species from the Colombian Caribbean has been recognized, and it is recommended to conduct assays with a larger number of human pathogens(AU)

Introducción: Cucurbita moschata Duchesne (Ahuyama) es cultivada en toda América, así como en Medio Oriente y Europa. Es utilizada desde la antigüedad como medicina alternativa. En la zona norte del departamento de Bolívar-Colombia es empleada por los campesinos para tratar infecciones en la piel, lo que generó el interés por desarrollar esta investigación. Objetivo: evaluar la actividad antibacteriana del extracto total de hojas de C. moschata frente a Staphylococcus aureus, Klebsiella pneumoniae y Escherichia coli. Métodos: hojas frescas de C. moschata fueron clasificadas taxonómicamente de acuerdo a métodos estándares. La obtención de los extractos se realizó por secado en horno, pulverización en molino de cuchilla, extracción por percolación sólido-líquido en frío y concentración en evaporador rotatorio. La actividad antibacteriana de los extractos etanólicos y hexánicos se evaluó in vitro frente a Staphylococcus aureus meticilino resistente, Escherichia coli y Klebsiella pneumoniae, mediante el método de Concentración Inhibitoria Mínima (CIM), siguiendo los lineamientos establecidos por Clinical and Laboratory Standards Institute (CLSI). Resultados: el extracto hexánico generó inhibición significativa desde la dilución 0,16 µg/mL para la cepa de S. aureus ATCC 43300. Para la cepa ATCC 25923 (MSSA) el extracto hexánico generó inhibición significativa desde la dilución 19,5 µg/mL. Los extractos etanólico y hexánico inhibieron significativamente el crecimiento de la cepa clínica de E. coli., mientras que para K. pneumoniae no hubo inhibición significativa en ninguna de las concentraciones evaluadas. Conclusiones: se demostró por primera vez que el extracto hexánico total de hojas de C. moschata tuvo el mayor poder de inhibición frente a las cepas clínicas de S. aureus y E. coli. Se reconoce el potencial antimicrobiano de esta especie autóctona de la costa del Caribe colombiano y se recomienda realizar ensayos en un número mayor de patógenos humanos(AU)

Actividad antibacteriana del extracto total de hojas de Cucurbita moschata Duchesne (Ahuyama) / Antibacterial activity of total extract from leaves of Cucurbita moschata Duchesne (ahuyama)

Introduction: Cucurbita moschata Duchesne (ahuyama) is grown across America as well as in the Middle East and Europe. It has been used as alternative medicine since ancient times. In the northern section of the department of Bolívar, Colombia, the plant is used by peasants to treat skin infections, hence our interest in conducting this study. Objective: Evaluate the antibacterial activity of total extract from leaves ofC. moschata against Staphylococcus aureus, Klebsiella pneumoniae and Escherichia coli. Methods: Fresh leaves of C. moschata were classified taxonomically using standard methods. The leaves were dried in an oven and pulverized in a blade mill. Extraction was performed by cold solid-liquid percolation and concentration in a rotary evaporator. Antibacterial activity of the ethanolic and hexanic extracts was evaluated in vitro against methicillin-resistant Staphylococcus aureus, Escherichia coli and Klebsiella pneumoniae, using the minimum inhibitory concentration (MIC) method, in compliance with guidelines from the Clinical and Laboratory Standards Institute (CLSI). Results: The hexanic extract caused significant inhibition from dilution 0.16 µg/mL for S. aureus strain ATCC 43300, and from dilution 19.5 µg/mL for strain ATCC 25923 (MSSA). The ethanolic and hexanic extracts significantly inhibited the growth of the clinical E. coli strain, whereas no significant inhibition was observed for K. pneumoniae at any of the concentrations tested. Conclusions: For the first time it was shown that the total hexanic extract of leaves of C. moschata had the greatest inhibition power against clinical strains of S. aureus and E. coli. The antimicrobial potential of this native species from the Colombian Caribbean has been recognized, and it is recommended to conduct assays with a larger number of human pathogens(AU)

Introducción: Cucurbita moschata Duchesne (Ahuyama) es cultivada en toda América, así como en Medio Oriente y Europa. Es utilizada desde la antigüedad como medicina alternativa. En la zona norte del departamento de Bolívar-Colombia es empleada por los campesinos para tratar infecciones en la piel, lo que generó el interés por desarrollar esta investigación. Objetivo: evaluar la actividad antibacteriana del extracto total de hojas de C. moschata frente a Staphylococcus aureus, Klebsiella pneumoniae y Escherichia coli. Métodos: hojas frescas de C. moschata fueron clasificadas taxonómicamente de acuerdo a métodos estándares. La obtención de los extractos se realizó por secado en horno, pulverización en molino de cuchilla, extracción por percolación sólido-líquido en frío y concentración en evaporador rotatorio. La actividad antibacteriana de los extractos etanólicos y hexánicos se evaluó in vitro frente a Staphylococcus aureus meticilino resistente, Escherichia coli y Klebsiella pneumoniae, mediante el método de Concentración Inhibitoria Mínima (CIM), siguiendo los lineamientos establecidos por Clinical and Laboratory Standards Institute (CLSI). Resultados: el extracto hexánico generó inhibición significativa desde la dilución 0,16 µg/mL para la cepa de S. aureus ATCC 43300. Para la cepa ATCC 25923 (MSSA) el extracto hexánico generó inhibición significativa desde la dilución 19,5 µg/mL. Los extractos etanólico y hexánico inhibieron significativamente el crecimiento de la cepa clínica de E. coli., mientras que para K. pneumoniae no hubo inhibición significativa en ninguna de las concentraciones evaluadas. Conclusiones: se demostró por primera vez que el extracto hexánico total de hojas de C. moschata tuvo el mayor poder de inhibición frente a las cepas clínicas de S. aureus y E. coli. Se reconoce el potencial antimicrobiano de esta especie autóctona de la costa del Caribe colombiano y se recomienda realizar ensayos en un número mayor de patógenos humanos(AU)