Evaluation studies on effects of quercetin with different concentrations on the physicochemical properties and in vitro digestibility of Tartary buckwheat starch.

The effects of polyphenols on the physicochemical properties and in vitro digestibility of Tartary buckwheat starch (TBS) remain scarce. In this study, the rheological, thermal properties, and in vitro digestibility of pregelatinized TBS (pre-TBS) with quercetin complexation at various concentrations were characterized. It was found that quercetin complexation increased the shearing resistance and viscosity of pre-TBS. Both SEM and TGA results revealed a more compact and stable structure of starch-quercetin complex in comparison to pre-TBS. The non-inclusive complex with higher crystallinity was formed through hydrogen bonds, which showed by XRD and FT-IR results. Additionally, complexes exhibited the lower digestion rate and digestion velocity constant, and the resistant starch content of complex (with 10% quercetin addition) was the highest. Therefore, quercetin complexation could improve the thermal and rheological properties, and decrease in vitro digestibility of pre-TBS, which could provide a theoretical basis for functional food development.

Antiproliferative Effect of Urera baccifera Leaves Against Ovarian Carcinoma Cell Line (OVCAR-3)

Abstract Natural products, especially phytochemicals, have been extensively studies and have exhibited important antiproliferative effects. The American native species Urera baccifera (L.) Gaudich. ex Wedd. (Urticaceae) is widely distributed in Brazil, where it is known as urtiga-vermelha or urtigão. The leaves are popularly used as anti-inflammatory, antirheumatic and in the treatment of gastric disorders. However, the antiproliferative potential of this plant against human tumor cells remain to be elucidated. In this study, we evaluated the antiproliferative effects of U. baccifera leaves extracts and fractions against a panel of human tumor cell lines in vitro besides a chemical evaluation of the most active sample by mass spectrometry (ESI-IT-MSn). The hydroalcoholic extract was inactive while dichloromethane extract showed moderate cytostatic activity against ovarian carcinoma cell line (OVCAR-3, GI50 = 1.5 μg/mL). More, the ethyl acetate and n-butanol fractions did not show important activity against tumour cell while the dichloromethane and hexane fractions showed moderate cytostatic activity against ovarian tumor cell line (OVCAR-3, GI50 = 12.7 and 9.4 μg/mL, respectively). Finally, the chemical profile evaluated by mass spectrometry (ESI-IT-MSn) allowed the detection of flavonoids in the HEU and hydroxylated fatty acid in DEU that can explain partially the biological effects observed. This is the first report of the antiproliferative effects of U. baccifera, and DEU has shown potential as a promising source of bioactive compounds.

The enhanced biomass and lipid accumulation in Coccomyxa subellipsoidea with an integrated treatment strategy initiated by brewery effluent and phytohormones.

Brewery effluent (BE) as an appreciable and sustainable resource presented new possibilities in low-cost algal biomass production, whereas the relatively low essential macronutrients hindered extensive applications as growth medium for microalgae cultivation. The objective of this study was to investigate the feasibility of an integrated treatment strategy initiated by BE coupling phytohormones in augmenting biomass and lipid accumulation in Coccomyxa subellipsoidea. Results revealed that BE coupling synthetic 1-naphthaleneacetic acid (NAA) accomplished the favorable lipid productivity of 481.76 mg/L/days, representing 6.80- to 9.71-fold more than that of single BE as well as standard Basal media. BE coupling NAA feeding also heightened the proportions of C16-C18 fatty acids (over 96%) and mono-unsaturated C18:1 (approximate 45%) which were prone to high-quality biofuels-making. Such profound lipids accumulation might be attributable to that BE coupling NAA treatment drove most of metabolic flux (i.e. acetyl-CoA) derived from TCA cycle and glycolysis flowing into lipid accumulation pathway. Concurrently, the complete removal of total nitrogen and total phosphorus by C. subellipsoidea with assistance of NAA were easily complied with the permissible dischargeable limits for BE. These present results strongly demonstrated that BE coupling NAA was a potential feeding strategy in boosting algal lipid productivity and further provided great possibilities in linking affordable algal biomass production with high-efficient biological contaminants removal.

Effects of lipid formulations on clove extract spray dried powders: comparison of physicochemical properties, storage stability and in vitro intestinal permeation.

Clove is an aromatic plant spice with potent antioxidant and anti-inflammatory activity. Eugenol is the main compound which contributes to such medicinal and nutritional benefits. To date, the formulation of unstable, volatile and poorly water-soluble compounds remains a challenging task. Lipid formulations can be used to improve physicochemical and biopharmaceutical properties of poorly soluble compounds. The aim of this study is to investigate the effects of lipids, such as Gelucire and Compritol on physicochemical properties; stability and in vitro intestinal permeation of spray dried powdered formulations loaded with clove's bioactive compounds. Results showed that eugenol retention in spray-dried powders could be correlated with antioxidant activity and with mass recovery after spray drying. Adding Gelucire but not Compritol to clove extract formulations, improved solubility of spray dried powders. Stability test in high humidity environment (63.5% RH) suggested that formulations including both Gelucire and Compritol were significantly more stable compared to the formulation without any lipid at the two tested temperatures (25 °C and 40 °C). This suggests that lipid additions to clove (Syzygium aromaticum) extract formulations provide protective effects for the spray dried powders in high-humidity environments. In addition, results from in vitro intestinal permeation studies suggested that eugenol uptake, was not being hindered by transporters nor was the absorption being affected by lipid formulations.

Fabrication, Physicochemical Characterization, and Performance Evaluation of Biodegradable Polymeric Microneedle Patch System for Enhanced Transcutaneous Flux of High Molecular Weight Therapeutics.

A revolutionary paradigm shift is being observed currently, towards the use of therapeutic biologics for disease management. The present research was focused on designing an efficient dosage form for transdermal delivery of α-choriogonadotropin (high molecular weight biologic), through biodegradable polymeric microneedles. Polyvinylpyrrolidone-based biodegradable microneedle arrays loaded with high molecular weight polypeptide, α-choriogonadotropin, were fabricated for its systemic delivery via transdermal route. Varied process and formulation parameters were optimized for fabricating microneedle array, which in turn was expected to temporally rupture the stratum corneum layer of the skin, acting as a major barrier to drug delivery through transdermal route. The developed polymeric microneedles were optimized on the basis of quality attributes like mechanical strength, axial strength, insertion ratio, and insertion force analysis. The optimized polymeric microneedle arrays were characterized for in vitro drug release studies, ex vivo drug permeation studies, skin resealing studies, and in vivo pharmacokinetic studies. Results depicted that fabricated polymeric microneedle arrays with mechanical strength of above 5 N and good insertion ratio exhibited similar systemic bioavailability of α-choriogonadotropin in comparison to marketed subcutaneous injection formulation of α-choriogonadotropin. Thus, it was ultimately concluded that the designed drug delivery system can serve as an efficient tool for systemic delivery of therapeutic biologics, with an added benefit of overcoming the limitations of parenteral delivery, achieving better patient acceptability and compliance.

Effect of dietary pomegranate seed oil on laying hen performance and physicochemical properties of eggs.

The objective of the study was to determine the effects of pomegranate seed oil, used as a source of punicic acid (CLnA) in the diets of laying hens, on the physicochemical properties of eggs. Forty Isa Brown laying hens (26weeks old) were equally subjected to 4 dietary treatments (n=10) and fed a commercial layer diet supplying 2.5% sunflower oil (control) or three levels (0.5, 1.0 and 1.5%) of punicic acid in the diets. After 12weeks of feeding the hens, eggs collection began. Sixty eggs - randomly selected from each group - were analysed for physicochemical properties. Eggs naturally enriched with CLnA preserve their composition and conventional properties in most of the analysed parameters (including chemical composition, physical as well as organoleptic properties). Dietary CLnA had positive impact on the colour of the eggs' yolk, whereas the hardness of hard-boiled egg yolks was not affected. Additionally, increasing dietary CLnA led to an increase not only the CLnA concentrations, but also CLA in egg-yolk lipids.

Changes in physicochemical properties related to the texture of lotus rhizomes subjected to heat blanching and calcium immersion.

Pretreatments such as low temperature blanching and/or calcium soaking affect the cooked texture of vegetal food. In the work, lotus rhizomes (Nelumbo nucifera Gaertn.) were pretreated using the following 4 treatments, blanching at 40°C, blanching at 90°C, soaking in 0.5% CaCl2, and blanching at 40°C followed by immersion in 0.5% CaCl2. Subsequently, the cell wall material of pretreated samples was isolated and fractioned to identify changes in the degree of esterification (DE) and monosaccharide content of each section, and the texture of the lotus rhizomes in different pre-treatments was determined after thermal processing with different time. The results showed that the greatest hardness was obtained after blanching at 40°C in CaCl2, possibly attributing to the formation of a pectate calcium network, which maintains the integrity of cell walls. Furthermore, the content of galactose, rhamnose and arabinose decreased due to the breakage of sugar backbones and subsequent damage to cell walls. Our results may provide a reference for lotus rhizome processing.

Evaluation of physicochemical properties and intestinal permeability of six dietary polyphenols in human intestinal colon adenocarcinoma Caco-2 cells.

Phenolic compounds are common ingredients in many dietary supplements and functional foods. However, data concerning physicochemical properties and permeability of polyphenols on the intestinal epithelial cells are scarce. The aims of this study were to determine the experimental partition coefficient (Log P), and parallel artificial membrane permeability assay (PAMPA), to characterize the bi-directional transport of six phenolic compounds viz. caffeic acid, chrysin, gallic acid, quercetin, resveratrol and rutin in Caco-2 cells. The experimental Log P values of six polyphenols were correlated (R (2) = 0.92) well with the calculated Log P values. The apparent permeability (P app) range of all polyphenols in PAMPA for the apical (AP) to basolateral (BL) was 1.18 ± 0.05 × 10(-6) to 5.90 ± 0.16 × 10(-6) cm/s. The apparent Caco-2 permeability (P app) range for the AP-BL was 0.96 ± 0.03 × 10(-6) to 3.80 ± 0.45 × 10(-6) cm/s. The efflux ratio of P app (BL → AP) to P app (AP → BL) for all phenolics was <2, suggesting greater permeability in the absorptive direction. Six compounds exhibited strong correlations between Log P and PAMPA/Caco-2 cell monolayer permeation data. Dietary six polyphenols were poorly absorbed through PAMPA and Caco-2 cells, and their transepithelial transports were mainly by passive diffusion.

Low level of selenium increases the efficacy of 24-epibrassinolide through altered physiological and biochemical traits of Brassica juncea plants.

This study was conducted to provide an insight into the effect of Se (through soil) induced changes in Brassica juncea plants in the presence and absence of 24-epibrassinolide (EBL; foliar). The Se treatments showed dual response, 10 µM of Se significantly increased growth, water relations, photosynthetic attributes along with carbonic anhydrase activity whereas its higher concentrations proved inhibitory in concentration dependent manner. The follow-up application of EBL to the Se stressed plants improved growth, water relations, photosynthesis and simultaneously enhanced the various antioxidant enzymes viz. catalase, peroxidase and superoxide dismutase with the excess accumulation of proline. In addition to this, 10 µM Se increases the efficacy of 10(-8) M of EBL and both in combination showed maximum increase for the growth and photosynthetic traits of plants. On the other hand, the elevated level of antioxidant enzymes as well as proline could have conferred tolerance to the Se-stressed plants resulting in improved growth, water relations and photosynthesis.

Antioxidants, phytochemicals, and cytotoxicity studies on Phaleria macrocarpa (Scheff.) Boerl seeds.

In recent years, the utilization of certain medicinal plants as therapeutic agents has drastically increased. Phaleria macrocarpa (Scheff.) Boerl is frequently used in traditional medicine. The present investigation was undertaken with the purpose of developing pharmacopoeial standards for this species. Nutritional values such as ash, fiber, protein, fat, and carbohydrate contents were investigated, and phytochemical screenings with different reagents showed the presence of flavonoids, glycosides, saponin glycosides, phenolic compounds, steroids, tannins, and terpenoids. Our results also revealed that the water fraction had the highest antioxidant activity compared to the methanol extract and other fractions. The methanol and the fractionated extracts (hexane, chloroform, ethyl acetate, and water) of P. macrocarpa seeds were also investigated for their cytotoxic effects on selected human cancer cells lines (MCF-7, HT-29, MDA-MB231, Ca Ski, and SKOV-3) and a normal human fibroblast lung cell line (MRC-5). Information from this study can be applied for future pharmacological and therapeutic evaluations of the species, and may assist in the standardization for quality, purity, and sample identification. To the best of our knowledge, this is the first report on the phytochemical screening and cytotoxic effect of the crude and fractionated extracts of P. macrocarpa seeds on selected cells lines.

Diphenyl diselenide-loaded nanocapsules: preparation and biological distribution.

Over the past years, organoselenium compounds have been aimed as targets of interest in organic synthesis. Diphenyl diselenide [(PhSe)2] is an important example of this class showing several pharmacological properties. However, the poor water-solubility and its low oral bioavailability may be considered an obstruction for the clinical utility of this compound. For this reason, the use of nanocapsules is a prominent approach to increase the bioavailability of lipophylic molecules. This study aims to prepare diphenyl diselenide-loaded nanocapsules with two different concentrations, by interfacial deposition of the preformed polymer in order to develop a system to improve its oral bioavailability. The drug-loaded nanocapsules with 1.56 and 5 mg ml−1 and unloaded nanocapsule suspensions presented macroscopic homogeneous aspect, as well as submicronic sizes, low polydispersity, negative zeta potentials and slightly acid or neutral pH values. The biological tests of selenium distribution in different tissues of mice show a higher bioavailability of the (PhSe)2 nanocapsules when compared with the free (PhSe)2, both administered by per oral route at the dose of 50 mg/kg, showing a prominent influence of the nanocarries systems for biological properties of this organochalcogenium compound.

The effects of Ca2SiO4-Ca3(PO4)2 ceramics on adult human mesenchymal stem cell viability, adhesion, proliferation, differentiation and function.

Bioceramic samples with osteogenic properties, suitable for use in the regeneration of hard tissue, were synthesized. The materials consisting of α-tricalcium phosphate (αTCP) and also αTCP doped with either 1.5 wt.% or 3.0 wt.% of dicalcium silicate (C2S) in the system Dicalcium Silicate-Tricalcium Phosphate (C2S-TCP) were obtained by solid state reaction. All materials were composed of a single phase, αTCP in the case of a pure material, or solid solution of C2S in αTCP (αTCPss) for the doped αTCP. Viability, proliferation and in vitro osteoinductive capacity were investigated by seeding, adult mesenchymal stem cells of human origin (ahMSCs) which were CD73(+), CD90(+), CD105(+), CD34(-) and CD45(-) onto the 3 substrates for 30 days. Results show a non-cytotoxic effect after applying an indirect apoptosis test (Annexin V/7-AAD staining), so ahMSCs adhered, spread, proliferated and produced extracellular matrix (Heparan-sulfate proteoglycan (HS) and osteopontin (OP)) on all the ceramics studied. Finally, the cells lost the cluster differentiation marker expression CD73, CD90 y CD105 characteristic of ahMSCs and they showed an osteoblastic phenotype (Alkaline phosphatase activity (ALP), Osteocalcin production (OC), Collagen type I expression (Col-I), and production of mineralization nodules on the extracellular matrix). These observations were more evident in the αTCP ceramic doped with 1.5 wt.% C2S, indicating osteoblastic differentiation as a result of the increased concentration of solid solution of C2S in αTCP (αTCPss). Overall, these results suggest that the ceramics studied are cytocompatible and they are able to induce osteoblastic differentiation of undifferentiated ahMSCs.

Shelf stability, sensory qualities, and bioavailability of iron-fortified Nepalese curry powder.

BACKGROUND: The prevalence of iron-deficiency anemia in Nepal is almost 50% of the whole population. Curry powder is a promising vehicle for fortification due to its use in various meals. OBJECTIVE: To evaluate the bioavailability of different iron fortificants in curry powder and their effects on the qualities of curry powder. METHODS: The serving size of curry powder was evaluated in 40 Nepalese households and 10 restaurants. The powders were fortified with iron sources of different bioavailability. Sources with good bioavailability of iron--ferrous sulfate (FS), ferrous fumarate (FF), and sodium ferric ethylenediaminetetraacetic acid (NaFeEDTA)--were added to provide one-third of the recommended daily intake (RDI) of iron per serving. Elemental iron (H-reduced [HRI] and electrolytic [EEI]), which has poor bioavailability, was added to provide two-thirds of the RDI per serving. Both fortified and unfortified products were packed in either commercial packs or low-density polyethylene bags and stored at 40 +/- 2 degrees C under fluorescent light for 3 months. The stored products were analyzed for CIE color, peroxide value, thiobarbituric acid reactive substances, moisture, water activity, iron, and sensory qualities. The contents of phenolic compounds and phytate were analyzed, and iron bioavailability was determined by the Caco-2 cell technique. RESULTS: The serving size of curry powder was 4 g. Iron fortificants did not have adverse effects on the physical, chemical, and sensory qualities of curry powder packed in commercial packaging. After 3 months storage, HRI significantly affected darker colors of curry powder and the cooked dishes prepared with curry powder. The relative bioavailabilities of NaFeEDTA and EEI were 1.05 and 1.28 times that of FS, respectively. The cost of fortification with EEI was similar to that with FS and 4.6 times less than that with NaFeEDTA. CONCLUSIONS: It is feasible and economical to fortify Nepalese curry powder packed in commercial packaging with EEI.

Folic acid fortification through existing fortified foods: iodized salt and vitamin A-fortified sugar.

BACKGROUND: Folic acid fortification of cereal-grain products has markedly improved folate status and reduced the risks of neural tube defects and other chronic diseases in the populations participating in fortification programs. To more broadly extend its benefit to affected populations in developing countries, it would seem logical to incorporate folic acid fortification into existing or planned programs to minimize the incremental cost of this intervention. OBJECTIVE: To examine the feasibility of providing folic acid through ongoing programs for salt iodization and vitamin A fortification of sugar. METHODS: Folic acid was added to iodized salt and vitamin A-fortified sugar by various methods--direct blending as a powder, spraying onto the carriers as aqueous solution or suspension, or blending as a microencapsulated premix. The multiple fortified samples were subjected to a prolonged storage stability test, and the retentions of the added micronutrients were followed. RESULTS: Folic acid was generally stable when incorporated into Guatemalan iodized salt and vitamin A-fortified sugar. Even in the presence of encapsulated ferrous fumarate as an iron fortificant, samples retained > 80% in salt and approximately 70% in sugar samples respectively, after 9 months of storage at 40 degrees C and 60% relative humidity. The addition of folic acid as a dry premix made by extrusion was most effective in retaining both folic acid and the other added micronutrients. CONCLUSIONS: The fortification method had a pronounced impact on the stability of both folic acid and the other added micronutrients. Proper encapsulation may be required to ensure the stability of multiple fortified foods.

Carboxymethyl cellulose coating and low-dose gamma irradiation improves storage quality and shelf life of pear (Pyrus communis L., Cv. Bartlett/William).

Carboxymethyl cellulose (CMC) coatings alone and in combination with gamma irradiation were tested for maintaining the storage quality and extending shelf life of pear. Matured green pears were CMC coated at levels 0.25% to 1.0% w/v and gamma irradiated at 1.5 kGy. The treated fruit including control was stored under ambient (temperature 25 ± 2 °C, RH 70%) and refrigerated (temperature 3 ± 1 °C, RH 80%) conditions. Irradiation alone at 1.5 kGy gave 8 and 4 d extension in shelf life of pear following 45 and 60 d of refrigeration, respectively. CMC coating at 1.0% w/v was effective in giving 6 and 2 d extension in shelf life of pear following 45 and 60 d of refrigeration, respectively. All combinatory treatments delayed the decaying of pear during postrefrigerated storage, but combination of 1.0% w/v CMC and 1.5 kGy irradiation proved significantly (P≤0.05) effective in maintaining the storage quality and delaying the decaying of pear. The above combinatory treatment gave an extension of 12 and 6 d in shelf life of pear during postrefrigerated storage at 25 ± 2 °C, RH 70% following 45 and 60 d of refrigeration.

Composition and antioxidant activity of Trigona carbonaria honey from Australia.

Stingless bees (Tribe Meliponini) are a diverse group of highly eusocial bees distributed throughout the tropics and subtropics. Trigona carbonaria honey, from Australia, was characterized by traditional physicochemical parameters (acidity, sugars, diastase, electrical conductivity, hydroxymethylfurfural, invertase, nitrogen, and water content) and other compositional factors (flavonoids, polyphenols, organic acids, and water activity), as well as total antioxidant capacity and radical scavenging activity. For the Australian T. carbonaria, the traditional analytical parameters were similar to those previously reported for neotropical stingless bee honey and confirm that honeys produced by Meliponini bees possess several physicochemical properties that are distinctly different from Apis mellifera honey, with higher values of moisture (26.5 +/- 0.8 g of water/100 g of honey), water activity (0.74 +/- 0.01), electrical conductivity (1.64 +/- 0.12 mS/cm), and free acidity (124.2 +/- 22.9 mEq/kg of honey) and a very low diastase activity (0.4 +/- 0.5 diastase number) and invertase activity (5.7 +/- 1.5 invertase number). The sugar spectrum was quite different from that of A. mellifera honey, with 20.3 +/- 2.9 g of maltose/100 g of honey. The values of pH (4.0 +/- 0.1), lactonic acidity (4.7 +/- 0.8 mEq/kg of honey), sucrose (1.8 +/- 0.4 g/100 g of honey), and fructose/glucose ratio (1.42 +/- 0.13) fell in the same ranges as those of A. mellifera honey. Citric (0.23 +/- 0.09) and malic (0.12 +/- 0.03) acid concentrations (in g/kg of honey) of T. carbonaria honeys were in the range described for A. mellifera honey. D-Gluconic was more concentrated (9.9 +/- 1.3 g/kg of honey), in the range of Italian Castanea, Thymus, Arbutus, and honeydew honeys. Flavonoid content was 10.02 +/- 1.59 mg of quercetin equivalents/100 g of honey, and polyphenol contents were 55.74 +/- 6.11 mg of gallic acid equivalents/100 g of honey. The antioxidant activity, expressed as percentage of 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) cation (ABTS(*+)) decolorization, was 233.96 +/- 50.95 microM Trolox equivalents, and free radical 1,1-diphenyl-2-picrylhydrazyl (DPPH(*)) depletion was 48.03 +/- 12.58 equivalents of ascorbic acid. All reported values are averages +/- standard deviation. The antioxidant activity can represent an important added value for T. carbonaria honey, to initiate a medicinal approach for both nutritional and pharmaceutical applications, besides further physicochemical characterization.