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.

Nutritional Value and Antioxidant, Antimicrobial and Cytotoxic Activity of Wild Macrofungi.

Macrofungi are among the most promising sources of biologically active natural products with nutritional qualities and therapeutic values. In this work, the nutritional value of nine species of wild macrofungi from Ibague-Tolima (Colombia) was evaluated. In addition the antioxidant, antimicrobial and cytotoxic activities of an ethanol:water (70:30) extract of wild basidiomata were evaluated. The wild mushrooms' nutritional potential showed that the genus Pleurotus and Lentinus have the best protein percentages, with 18.4% and 18.5%. The nine extracts evaluated managed to stabilize the two radicals evaluated; however, lower IC50 was found for Phellinus gilvus and Ganoderma australe extracts. The results showed that Trametes coccinea, Pleurotus floridanus and Ganoderma australe extracts were the most effective as antimicrobials, with high inhibition percentages against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Klebsiella pneumoniae. Antifungal activity results against Rhizopus oryzae, Penicillium sp. and Aspergillus niger showed that the nine extracts were effective at the concentrations tested. Considering cell viability against isolated leukocytes, seven of the nine extracts showed percentages higher than 50% of cell viability. This research describes the nutritional value of nine wild macrofungi in Colombia and their potential for antimicrobial, cytotoxic and antioxidant activity.

Encapsulation of bioactive compounds from byproducts of two species of passionflowers: evaluation of the physicochemical properties and controlled release in a gastrointestinal model.

This study aimed to evaluate the release of active components with antioxidant and antihypertensive capacity from encapsulated extracts of the peel and seeds of Gulupa (Passiflora edulis f. edulis) and Cholupa (Passiflora maliformis) in an in vitro gastrointestinal digestion model. Microencapsulated extracts were prepared with enzymatically modified rice starch as the encapsulating material and ethanol extracts of seeds and peel of P. edulis f. edulis and P. maliformis as encapsulated material. Microcapsule characterization was performed by scanning electron microscopy with values of 4.54-5.13 µm and ξ potential values of -6.34 mV and -6.66 mV. Dynamic light scattering (DLS) analysis was conducted with polydispersion values from 1.33 to 1.51, and dispersion stability analysis was also conducted. The total phenol content and antioxidant activities (ABTS, DPPH, and FRAP) and ACE inhibitory activity (in vitro antihypertensive activity) were evaluated after each stage of digestion, with values greater than 80% of activity before gastrointestinal transit and with values greater than 55% activity after the end of gastrointestinal transit. Gastrointestinal evaluation of the encapsulated extracts was performed with an ex vivo model using pig intestines and simulating the conditions of digestion in three phases: the gastric (pH 2.0 with 1.0 M HCl +0.5 g/L pepsin), enteric (pH 8.0 with Krebs solution +1.0 mL/L bile) and final enteric (pH 7.5 Krebs solution only) phases. The microencapsulation of passionflower extracts showed good behavior against changes in pH and enzymatic activities throughout digestion, thus promoting a controlled release and targeted delivery of bioactive compounds, undergoing a paracellular mechanism through the intestinal barrier to preserve the antioxidant activity and ACE inhibitory that was shown by the extracts before encapsulation of the material.

Rice-Associated Rhizobacteria as a Source of Secondary Metabolites against Burkholderia glumae.

Various diseases, including bacterial panicle blight (BPB) and sheath rot, threaten rice production. It has been established that Burkholderia glumae (B. glumae) is the causative agent of the above mentioned pathologies. In the present study, antagonistic activity, growth promotion, and the metabolite profiles of two rhizobacteria, isolated in different paddy fields, were assessed against B. glumae. Strains were identified based on 16S rRNA gene sequences, and the phylogenetic analyses showed that both strains belong to the genus Enterobacter, with high similarity to the strain Enterobacter tabaci NR146667.2 (99%). The antagonistic activity was assessed with the disc diffusion method. Active fractions were isolated through a liquid/liquid extraction with ethyl acetate (EtOAc) from the fermentation media, and their antibacterial activities were evaluated following the Clinical and Laboratory Standards Institute (CLSI) guidelines. The Pikovskaya modified medium was used to test the ability of in vitro inorganic phosphorus solubilization, and BSB1 proved to be the best inorganic phosphorus solubilizer, with a solubilization index (SI) of 4.5 ± 0.2. The glass-column fractionation of the EtOAc extracted from BCB11 produced an active fraction (25.9 mg) that inhibited the growth of five B. glumae strains by 85-95%. Further, metabolomic analysis, based on GC-MS, showed 3-phenylpropanoic acid (3-PPA) to be the main compound both in this fraction (46.7%), and in the BSB1 extract (28.6%). This compound showed antibacterial activity against all five strains of B. glumae with a minimum inhibitory concentration (MIC) of 1000 mg/L towards all of them. The results showed that rice rhizosphere microorganisms are a source of compounds that inhibit B. glumae growth and are promising plant growth promoters (PGP).

Bioprospecting of Lacmellea standleyi fruits (lechemiel) / Bioprospección de frutos de Lacmellea standleyi (lechemiel)

Introduction: the idea to explore at least some of the regions diversity such as the Colombian Orinoco through bioprospecting study of Lacmellea standleyi (Woodson) Monach. arises as a consequence of ignorance of much of the floristic richness in Colombia and the potential relevance of much of this in the nutrition, health and industry. Objective: to evaluate the antioxidant potential, nutritional and phenolic content, antimicrobial activity, and safety degree of aqueous, ethanol, and ethyl acetate extracts of Lacmellea standleyi fruits in three different ripening stages. Methods: the nutritional value was evaluated using standardized methods to full fruit in its three ripening stages. Each of the extracts was chemically characterized by spectrophotometric assays. Antimicrobial activity was measured by the size of inhibition against strains of Staphylococcus aureus, Escherichia coli, and Candida parpsilosis; the acute toxicity of the fruits was measured through in vitro tests using Artemia salina as experimental model. Results: the results show that green fruits are suppliers of antioxidant compounds. Higher levels of nutrients are found in the intermediate state and mature fruit has attractive organoleptic properties and a relatively high nutrient content. Conclusions: the antioxidant capacity of Lacmellea standleyi fruits was evident in the three ripening stages, giving the plant a promising future in the pharmaceutical industry, standing out in this field the fruits in the green stage. Furthermore, the results suggest the application of the intermediate and mature fruits in the finished products development. The safety observed in the plant material warrants its use in human consumption.

Introducción: del desconocimiento de gran parte de la riqueza florística en Colombia y de la importancia que podría tener gran parte de esta en la nutrición, salud e industria, nace la idea de explorar, al menos en parte, la diversidad de regiones como la Orinoquía colombiana a través del estudio de bioprospección de los frutos de Lacmellea standleyi (Woodson) Monach. Objetivo: evaluar el potencial antioxidante, el contenido fenólico y nutricional, la actividad antimicrobiana y el grado de inocuidad de los extractos acuoso, etanólico y de acetato de etilo, de los frutos de Lacmellea standleyi en 3 estadios diferentes de maduración. Métodos: el valor nutricional se evaluó a través de métodos estandarizados, al fruto completo en sus 3 estadios de maduración; cada uno de los extractos se caracterizó químicamente a través de ensayos espectrofotométricos. La actividad antimicrobiana se midió mediante el tamaño del halo de inhibición frente a cepas de Staphylococcus aureus, Escherichia coli y Candida parpsilosis; la toxicidad aguda de los frutos se calculó mediante pruebas in vitro, usando como modelo experimental nauplios de Artemia salina. Resultados: se pudo evidenciar que los frutos verdes aportan compuestos antioxidantes. En el estado intermedio se encuentran los niveles más altos de nutrientes y el fruto maduro ostenta atractivas propiedades organolépticas y un contenido relativamente alto de nutrientes. Conclusiones: la capacidad antioxidante de los frutos de Lacmellea standleyi resultó evidente en los 3 estadios de maduración. Esto otorga al vegetal un futuro promisorio en la industria farmacológica, sobresaliendo en este campo los frutos en el estadio verde. Además, los resultados permiten sugerir la aplicación de los frutos en estado intermedio y maduro en la elaboración de productos alimenticios terminados. La inocuidad observada en el material vegetal garantizaría su uso en el consumo humano.

Valoración del potencial antioxidante de Mollinedia racemosa (romadizo) / Assessment of antioxidant potential of Mollinedia racemosa (romadizo)

Introducción: Mollinedia racemosa (Schltdl.) Tul. (romadizo), es una especie usada por grupos indígenas y comunidades campesinas de la cuenca del Orinoco colombiano, empleada para tratar fiebres, dolores de cabeza y problemas de estómago, especialmente en el tratamiento del resfriado y como analgésico. Objetivo: evaluar el potencial antioxidante de las hojas de M. racemosa (romadizo). Métodos: se preparó un macerado etanólico de hojas (relación 1:15, vegetal/solvente), renovando el solvente cada 24 h hasta agotar la muestra. El extracto se filtró, se concentró a presión reducida y se almacenó (4 ºC). Se valoró el contenido de compuestos fenólicos, flavonoides y de flavonoles totales. Se estableció además la concentración de alcaloides que posee la planta. Asimismo, se evaluó la actividad antioxidante in vitro del vegetal midiendo la capacidad del extracto etanólico para estabilizar radicales DPPH (1,1-difenil-2-picrilhidracil) y ABTS (ácido 2,2'azinobis-[3 etilbenzotiazolina]-6-sulfónico), y la potencialidad para inhibir la peroxidación de un sistema lipídico. Resultados: el potencial antioxidante de M. racemosa mostró dependencia de la concentración aplicada, que a su vez está correlacionada con la diversidad y cantidad de constituyentes de naturaleza fenólica del vegetal. Concentraciones de 14,59 mg/mL y 17,32 mg/mL se requieren para inhibir 50 por ciento de la cantidad original utilizada de DPPH y ABTS, respectivamente. La actividad inhibitoria de la peroxidación lipídica alcanzó su máxima capacidad a las 360 h (15 d). Conclusiones: los resultados obtenidos permiten concluir que el extracto hidroalcohólico de las hojas de M. racemosa posee un efecto antioxidante y protector de un sistema lipídico.

Introduction: Mollinedia racemosa (Schltdl.) Tul. (romadizo), is one species used by indigenous and peasant communities in the Colombian Orinoco basin, to treat fever, headache and stomach problems, especially in the treatment of cold and as an analgesic. Objective: to evaluate the antioxidant potential of M. racemosa (romadizo) leaves. Methods: ethanolic macerate of leaves was prepared (ratio 1:15, plant/solvent), changing the solvent every 24 h until the sample was exhausted. The extract was filtered, concentrated under reduced pressure and stored (4°C). The content of phenolic compounds, flavonoids and total flavonols were assessed. The concentration of alkaloids of this plant was also established. Additionally, the in vitro antioxidant activity of plant was determined by measuring the ability of ethanol to stabilize radicals DPPH1 (1-diphenil-2-picrilhydracil) and ABTS (2,2'azinobis-[3 etilbenzotiazolin]-6-sulphonic acid) and the potential to inhibit lipid peroxidation. Results: the antioxidant potential of this plant depended on the applied concentration that in turn was correlated to the diversity and quantity of phenols present in the plant. Concentration rates of 14.59 and 17.32 µg/mL were required to inhibit 50 percent (IC50) of the original quantity of DPHH and ABTS respectively. The inhibitory capacity of lipidic peroxidation reached its maximum level after 360 hours (15 days). Conclusions: the results showed that the extract from M. racemosa leaves had antioxidant and protective effect in a lipidic system.

Climate influence on chemical composition and antioxidant activity of Justicia pectoralis Jacq. / Influencia del clima en la composición química y la actividad antioxidante de Justicia pectorales Jacq

In this paper, the influence of the altitude in the phenols and flavonoids contents and the antioxidant activity of the extracts of different polarities of Justicia pectoralis Jacq(Acanthaceae) was evaluated. There was found that the plants cultivated under the Ibagué-Tolima's climate and soil conditions, can be a source of antioxidant compounds, especially in water preparations. The chromatographic analysis revealed that J. pectoralis extracts have mainly flavonoids of the flavonone type, as apigenine. A greater (or The greatest) content of flavonoids was detected in the ethanolic extract of the plant samples grown at 1 265 m.a.s.l. (meters above sea level) (2 748,03 mg/L). The altitude level does not seem to have any influence on the functional properties, neither on the phytophenols content. The J. pectoralis Jacq can be considered one species with a high therapeutic potential and with good commercial opportunities.

En este trabajo se evaluó la influencia de la altitud en el contenido de fenoles y flavonoides y la actividad antioxidante de los extractos de diferentes polaridades provenientes de Justicia pectorales (Acanthaceae). Se halló que las plantas cultivadas en las condiciones del suelo y el clima de la zona Ibagué-Tolima pueden constituirse en compuestos antioxidantes, especialmente en preparados acuosos. El análisis cromatográfico reveló que los extractos de J. pectorales poseen en lo fundamental flavonoides del tipo flavona como es la apigenina. Un mayor contenido (sino el mayor) de flavonoides se detectó en el extracto etanol obtenido de las muestras de la planta cultivadas a 1 265 metros por encima del nivel del mar (2 748,03 mg/L). La altitud no parece influir en las propiedades funcionales, ni en el contenido de fitofenoles del extracto. La J. pectorales puede considerarse una especie de gran potencial terapéutico y buenas posibilidades de comercialización.