Absorption and distribution of root, fruit, and foliar-applied 45 Ca in 'Clemenules' mandarin trees.

BACKGROUND: The mechanisms of calcium (Ca) absorption and transport in plants are still poorly understood. This study focused on assessing the absorption and distribution of Ca in different plant organs after root (soil), foliar, or fruit application to 6-year-old 'Clemenules' mandarin trees, grown in pots, using 45 Ca as a tracer. RESULTS: The rate of 45 Ca absorption and transportation in plant tissues varied according to the treatment method. The fruit and shoot Ca supply led to a rate of 97% to 98% 45 Ca retention in such organs. In Ca-treated fruits, 22% of the applied 45 Ca moved to the pulp and 78% remained in the flavedo and albedo. The fruit peel was examined by scanning electron microscopy and transmission electron microscopy (SEM and TEM) and variations were observed during fruit development. Following 45 Ca soil treatment, approximately 56% of 45 Ca activity was measured in the soil, with 19.5% determined in the roots, 14.6% in the trunks (90% in bark and sapwood and only 10% in heartwood), 9.6% in shoots, and 0.3% in fruits. CONCLUSION: Calcium mobility in 'Clemenules' mandarin trees is limited and depends on the mode of Ca fertilizer application. The distribution of Ca to and within the fruits may be limited during development because of structural and functional constraints. © 2020 Society of Chemical Industry.

Peptide multifunctionalized gold nanorods decrease toxicity of ß-amyloid peptide in a Caenorhabditis elegans model of Alzheimer's disease.

The properties of nanometric materials make nanotechnology a promising platform for tackling problems of contemporary medicine. In this work, gold nanorods were synthetized and stabilized with polyethylene glycols and modified with two kinds of peptides. The D1 peptide that recognizes toxic aggregates of Aß, a peptide involved in Alzheimer's disease (AD); and the Angiopep 2 that can be used to deliver nanorods to the mammalian central nervous system. The nanoconjugates were characterized using absorption spectrophotometry, dynamic light scattering, and transmission electron microscopy, among other techniques. We determined that the nanoconjugate does not affect neuronal viability; it penetrates the cells, and decreases aggregation of Aß peptide in vitro. We also showed that when we apply our nanosystem to a Caenorhabditis elegans AD model, the toxicity of aggregated Aß peptide is decreased. This work may contribute to the development of therapies for AD based on metallic nanoparticles.

Topical Anti-inflammatory Activity of New Hybrid Molecules of Terpenes and Synthetic Drugs.

The aim of the study was to assess changes in the activity of anti-inflammatory terpenes from Chilean medicinal plants after the formation of derivatives incorporating synthetic anti-inflammatory agents. Ten new hybrid molecules were synthesized combining terpenes (ferruginol (1), imbricatolic acid (2) and oleanolic acid (3)) with ibuprofen (4) or naproxen (5). The topical anti-inflammatory activity of the compounds was assessed in mice by the arachidonic acid (AA) and 12-O-tetradecanoyl phorbol 13-acetate (TPA) induced ear edema assays. Basal cytotoxicity was determined towards human lung fibroblasts, gastric epithelial cells and hepatocytes. At 1.4 µmol/mouse, a strong anti-inflammatory effect in the TPA assay was observed for oleanoyl ibuprofenate 12 (79.9%) and oleanoyl ibuprofenate methyl ester 15 (80.0%). In the AA assay, the best activity was observed for 12 at 3.2 µmol/mouse, with 56.8% reduction of inflammation, in the same range as nimesulide (48.9%). All the terpenyl-synthetic anti-inflammatory hybrids showed better effects in the TPA assay, with best activity for 6, 12 and 15. The cytotoxicity of the compounds 8 and 10 with a free COOH, was higher than that of 2. The derivatives from 3 were less toxic than the triterpene. Several of the new compounds presented better anti-inflammatory effect and lower cytotoxicity than the parent terpenes.

Gold nanoparticles as tracking devices to shed light on the role of caveolin-1 in early stages of melanoma metastasis.

AIM: To track early events during lung metastasis, we labeled cells expressing (B16F10CAV1) or lacking CAV1 (B16F10mock) with gold nanoparticles conjugated to the peptide TAT (AuNPs-PEG-TAT). METHODS: B16F10 expressing or lacking CAV1 were labeled with AuNPs-PEG-TAT. The physicochemical properties and cytotoxicity of these nanoparticles, as well as their effects on migration and invasiveness of B16F10 cells in vitro were evaluated. Ex vivo lung distribution of the labeled cells after tail vein injection into C57BL/6 mice was examined. RESULTS: AuNPs-PEG-TAT did not affect B16F10 viability, migration and invasiveness. The metastatic and tumorigenic capability of the labeled B16F10 was also not modified in comparison to unlabeled B16F10 cells. CAV1 expression favored the retention of B16F10 cells in the lungs of mice 2 h post injection, suggesting CAV1 promoted adherence to endothelial cells and transendothelial migration. CONCLUSIONS: We developed a protocol to label B16F10 cells with AuNPs-PEG-TAT that permits subsequent tracking of cells in mice. CAV1 overexpression was found to increase retention and transendothelial migration of B16F10 cells in the lung.

Anti-inflammatory activity and phenolic profile of propolis from two locations in Región Metropolitana de Santiago, Chile.

ETHNOPHARMACOLOGICAL RELEVANCE: Propolis has long been used as a popular folk medicine due to its wide spectrum of alleged biological and pharmaceutical properties. In Chile, propolis is widely used by folklore medicine as an anti-inflammatory agent; however, this property has not been demonstrated by scientific methods. AIM OF THE STUDY: The objective of this study was to determine the anti-inflammatory activity in vivo and in vitro and to establish the phenolic profile of propolis collected in two localities in Región Metropolitana de Santiago (RM), Chile. MATERIALS AND METHODS: Propolis was collected in the areas of Caleu and Buin, RM Chile. Following that, the samples were unwaxed to obtain the global ethanolic extracts of propolis (EEPs) and, from these, the serial extracts of dichloromethane (EEP-DCMs) and ethanol (EEP-EtOHs). The topic anti-inflammatory effect was evaluated through mice ear edema induced by arachidonic acid (AA) and 12-O-tetradecanoylphorbol-13-acetate (TPA) at a dose of 3 mg/ear. Nitric oxide (NO) measurements were determined spectrophotometrically (Greiss reagent) by the accumulation of nitrite in the medium of macrophages RAW 264.7 stimulated with the lipopolysaccharide (LPS, 1 µg/mL) for 20 h at different concentrations of the EEPs, EEP-DCMs and EEP-EtOHs (6.25-50.00 µg/mL). The content of total phenols and flavonoids were determined through the methods of Folin-Ciocalteau and AlCl3, respectively. The profile of phenolic compounds was determined by HPLC-UV-ESI-MS/MS. RESULTS: The EEP-EtOH (64%) and EEP (59%) of Buin were the most active in the inflammation induced by TPA and AA respectively, being the anti-inflammatory effect stronger than the same Caleu extracts. Regarding the release of NO, all the extracts from the Buin propolis inhibited significantly its release in a concentration-dependent manner, this inhibition was stronger than the extracts from Caleu propolis. CONCLUSIONS: Our research shows for the first time a comparative study of the topical in vivo activity of two Chilean propolis. Both propolis showed in vivo topical anti-inflammatory activity against AA and TPA, the most active was Buin propolis and this difference is due in part to the variations in total phenols and flavonoids content and the phenolic profile. The phenols and flavonoids content of Buin propolis was higher than Caleu propolis. The extracts from Buin propolis result in a lower release of NO.

Anti-inflammatory activity of animal oils from the Peruvian Amazon.

ETHNOPHARMACOLOGICAL RELEVANCE: Animal oils and fats from the fishes Electrophorus electricus and Potamotrygon motoro, the reptiles Boa constrictor, Chelonoidis denticulata (Geochelone denticulata) and Melanosuchus niger and the riverine dolphin Inia geoffrensis are used as anti-inflammatory agents in the Peruvian Amazon. The aim of the study was to assess the topic anti-inflammatory effect of the oils/fats as well as to evaluate its antimicrobial activity and fatty acid composition. MATERIALS AND METHODS: The oils/fats were purchased from a traditional store at the Iquitos market of Belen, Peru. The topic anti-inflammatory effect was evaluated by the mice ear edema induced by arachidonic acid (AA) and 12-O-tetradecanoylphorbol-13-acetate (TPA) at the dose of 3mg oil/ear. Indomethacine and nimesulide were used as reference anti-inflammatory drugs. The application resembles the traditional topical use of the oils. The antimicrobial effect of the oils/fats was assessed by the microdilution test against reference strains of Escherichia coli, Staphylococcus aureus and Salmonella enteritidis. The fatty acid composition of the oils/fats (as methyl esters) was determined by GC and GC-MS analysis after saponification. RESULTS: All oils/fats showed topic anti-inflammatory activity, with better effect in the TPA-induced mice ear edema assay. The most active drugs were Potamotrygon motoro, Melanosuchus niger and Geochelone denticulata. In the AA-induced assay, the best activity was found for Potamotrygon motoro and Electrophorus electricus oil. The oil of Electrophorus electricus also showed a weak antimicrobial effect with MIC values of 250 µg/mL against Escherichia coli ATCC 25922 and Salmonella enteritidis-MI. The main fatty acids in the oils were oleic, palmitic and linoleic acids. CONCLUSIONS: Topical application of all the oils/fats investigated showed anti-inflammatory activity in the mice ear edema assay. The effect can be related with the identity and composition of the fatty acids in the samples. This study gives support to the traditional use of animal oils/fats as ant-inflammatory agents in the Peruvian Amazon. However, new alternative should be encouraged due to the conservation status of several of the animal sources of the crude drugs.

Topical anti-inflammatory activity of quillaic acid from Quillaja saponaria Mol. and some derivatives.

OBJECTIVES: Quillaic acid is the major aglycone of the widely studied saponins of the Chilean indigenous tree Quillaja saponaria Mol. The industrial availability of quillaja saponins and the extensive functionalization of this triterpenoid provide unique opportunities for structural modification and pose a challenge from the standpoint of selectivity in regard to one or the other secondary alcohol group, the aldehyde, and the carboxylic acid functions. The anti-inflammatory activity of this sapogenin has not been studied previously and it has never been used to obtain potential anti-inflammatory derivatives. METHODS: A series of quillaic acid derivatives were prepared and subjected to topical assays for the inhibition of inflammation induced by arachidonic acid or phorbol ester. KEY FINDINGS: Quillaic acid exhibited strong topical anti-inflammatory activity in both models. Most of its derivatives were less potent, but the hydrazone 8 showed similar potency to quillaic acid in the TPA assay. CONCLUSIONS: The structural modifications performed and the biological results suggest that the aldehyde and carboxyl groups are relevant to the anti-inflammatory activity in these models.

Antinociceptive activity of Quillaja saponaria Mol. saponin extract, quillaic acid and derivatives in mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Quillaja saponaria bark contains a high percentage of triterpene saponins and has been used for centuries as a cleansing and analgesic agent in Chilean folk medicine. AIM OF THE STUDY: The topical and systemic analgesic effects of a commercial partially purified saponin extract, 3ß,16α-dihydroxy-23-oxoolean-12-en-28-oic acid (quillaic acid), methyl 3ß,16α-dihydroxy-23-oxoolean-12-en-28-oate and methyl 4-nor-3,16-dioxoolean-12-en-28-oate. MATERIALS AND METHODS: The samples were assessed in mice using the topical tail-flick and i.p. hot-plate tests, respectively. RESULTS: All the samples showed activity in both analgesic tests in a dose-dependent manner. The most active against tail flick test was commercial partially purified saponin extract (EC50 27.9 mg%, w/v) and more than the ibuprofen sodium. On hot-plate test, methyl 4-nor-3, 16-dioxoolean-12-en-28-oate was the most active (ED50 12.2 mg/kg) and more than the ibuprofen sodium. CONCLUSIONS: The results of the present study demonstrated that Quillaja saponaria saponins, quillaic acid, its methyl ester, and one of the oxidized derivatives of the latter, elicit dose-dependent antinociceptive effects in two murine thermal models.

Comparative study of anti-inflammatory activity and qualitative-quantitative composition of triterpenoids from ten genotypes of Ugni molinae / Estudio comparativo de la actividad antiinflamatoria y composición química cualitativa y cuantitativa de triterpenoides de diez genotipos de Ugni molinae

The aim of this study was to assess the differences in qualitative-quantitative composition of triterpenoids and total phenolic contents, together with anti-inflammatory activity of Ugni molinae leaves obtained from ten genotypes. The ethyl acetate (EAE) and ethanol extracts (ETE) were obtained and analyzed. The plant genotypes were grown under same soil and climate conditions and under same agronomic management; the leaves were also harvested under the same conditions. Anti-inflammatory activity was evaluated by mice ear edema induced by 12-O-tetradecanoylphorbol-13-acetate (TPA) at a single dose of 200 mg/kg BW of each extract. Composition of triterpenoids and total phenolic contents was determined by HPLC-DAD and Folin-Ciocalteu method, respectively. Ugni molinae leaves of different plant genotypes exhibited significant differences in regard to their anti-inflammatory activity, as well as in qualitative-quantitative composition of triterpenoids and total phenolic content.

El objetivo de este estudio fue establecer las diferencias en la composición cualitativa y cuantitativa de triterpenoides y en los contenidos totales de fenoles, junto con la actividad antiinflamatoria de las hojas de Ugni molinae provenientes de diez genotipos. Los extractos de acetato de etilo (EAE) y etanólicos (ETE) fueron obtenidos y analizados. Los genotipos fueron cultivados bajo las mismas condiciones edafo-climáticas y con el mismo manejo agronómico; las hojas fueron cosechadas bajo las mismas condiciones. La actividad antiinflamatoria fue evaluada en ratones a los que se les indujo un edema en la oreja mediante la aplicación del 12-O-tetradecanoilforbol-13 acetato (TPA) y los extractos fueron evaluados a una dosis única de 200 mg/kg de peso corporal. La composición en triterpenoides y los contenidos de fenoles totales fueron determinados por CLAE-DAD y por el método de Folin-Ciocalteu, respectivamente. Las hojas provenientes de los diferentes genotipos de U. molinae, exhibieron significativas diferencias en sus actividades antiinflamatorias, así como, en el contenido cualitativo y cuantitativo de triterpenoides y en el contenido de fenoles totales.

Topical anti-inflammatory activity of 2alpha-hydroxy pentacyclic triterpene acids from the leaves of Ugni molinae.

Leaf extracts of Ugni molinae Turcz. are used in the Chilean cosmetic industry on the assumption that they have decongestant, regenerative, and anti-aging properties. A bioassay-guided fractionation of this plant material showed that some extracts have potent anti-inflammatory activities. Further fractionation led to the isolation and identification of betulinic acid, a mixture of ursolic and oleanolic acids, and the 2alpha-hydroxy derivatives alphitolic, asiatic, and corosolic acids. The latter three were evaluated in vivo in the mouse ear assay for their topical anti-inflammatory activity, inducing inflammation with either arachidonic acid (AA) or 12-O-tetradecanoylphorbol-13 acetate (TPA). Only corosolic acid was active in the AA assay, with similar potency to nimesulide, but all three triterpene acids inhibited TPA-induced inflammation with potencies comparable to that of indomethacin.

Estructura alimentaria: valor nutritivo y aceptabilidad de preparaciones incluidas en la alimentación institucional del preescolar / Food structure, nutritive value and acceptability on meals offered in the institutional feeding of the preeschol children

El presente trabajo estudia la estructura alimentaria, valor nutritivo y aceptabilidad de las preparaciones ofrecidas en la alimentación institucional del preescolar chileno. La investigación se realizó en 426 niños de ambos sexos, de 2 a 3 años, que asistían a 16 Jardines de la Junta Nacional de Jardines Infantiles (JUNJI) en Santiago. La estructura alimentaria se definió como la contribución porcentual de los alimentos al contenido de energía, proteína, lípidos, hidratos de carbono y fibra cruda y se determinó de la composición alimentaria de las preparaciones. Se evaluaron 14 guisos con sus complementos (ensalada y postre). Se estudio la aceptabilidad de las preparaciones mediante la determinación del consumo por pesada diferencial, ofreciendo repetición en los guisos si el niño lo solicitaba. La conducta y preferencia alimentaria de los niños se estudió a través de las respuestas de un cuestionario contestado por el personal encargado de la alimentación del niño en el Jardín. En un 40% de los guisos el alimento predominante fue la papa y en un 30% el arroz; las leguminosas se proporcionaron con cereales. Se demuestra que los alimentos básicos contribuyen en una alta proporción a la estructura alimentaria de energía, hidratos de carbono, fibra. En cuanto a proteínas destaca el aporte de las leguminosas y de los alimentos de origen animal. El aceite vegetal fue un importante contribuyente de lípidos y energía en los guisos y el principal aportador en las ensaladas. El valor nutritivo de los guisos dependió de la estructura alimentaria. Los guisos con alimentos de origen animal y las combinaciones leguminosa-cereal mostraron los valores más altos de proteínas. Un 50% mostró valores de densidad energética (DE) mayores a 1 kcal/g, éstos fueron todos los guisos de leguminosa-cereal, y los que incluian alimentos de origen animal en cantidades importantes. Según la encuesta de conducta alimentaria los niños prefirieron los guisos con base en papas y en trigo, y dentro de cada grupo de preparaciones los más fluidos y con menor DE, lo que se corroboró experimentalmente en la determinación de consumo. La aceptabilidad de los guisos y de los alimentos del desayuno fue alta. Las ensaladas fueron rechazadas en promedio en un 57% y los postres en un 13%; valores que se obtuvieron ofreciendo repetición del guiso antes de la ensalada y postre. La aceptabilidad de los niños fue selectiva, siendo importante el rechazo demostrado por las ensaladas lo que amerita real