Evaluation of antioxidant activity and total phenolics of selected Czech honeys

Honey serves as a good source of natural antioxidants, which are effective in reducing the risk occurrence of heart disease, cancer, cataracts, different inflammatory processes and immune-system decline. In the fresh selected Czech honey samples originated mainly from the region North Moravia antioxidant activity and total polyphenol content were determined. A total of 40 honey samples (multifloral, lime, rape, raspberry, mixture and honeydew honeys) native to different stations gained in the period from May by August year 2006 were analysed. Total phenolics (TP) content was determined by the modified Folin-Ciocalteau method [TP was expressed as mg of gallic acid equivalent (GA eq.) per kg of honey]. For evaluation of the antioxidant activity (AOA) three different methods were used, the ferric reducing antioxidant power (FRAP) assay, the 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay and the 2,2′-azinobis(3-ethylbenzothiazolin)-6-sulfphonate (ABTS) assay. AOA was expressed in mg ascorbic acid equivalent (AA eq.) per kg of honey. The results indicated that TP and AOA in Czech honey varied greatly between the honey kinds, location and time of the harvest. Average TP ranged from 89.9 mg GA eq. kg^-1 in lime honey to 215.2 mg GA eq. kg⁻¹ in honeydew honey. Antioxidant activity determined by the DPPH, ABTS and FRAP methods was lowest in floral honeys. The highest values were obtained for honeydew and mixture honeys. ABTS and FRAP assays have been shown to be the optimal methods for AOA determination in honey. A positive linear correlation between AOA and TP was observed (in FRAP assay R² = 0.852). It indicates that phenolics are one of the main components responsible for antioxidant behaviour of honey. The obtained results support and extend complete knowledge about the content of bioactive phenolics and antioxidant activity in the Czech honeys.     

Association between Insertion-Deletion Polymorphism of the Angiotensin-Converting Enzyme Gene and Treatment Response to Antipsychotic Medications: A Study of Antipsychotic-Naïve First-Episode Psychosis Patients and Nonadherent Chronic Psychosis Patients

We investigated whether a functional insertion/deletion (I/D) polymorphism of angiotensin-converting enzyme (ACE) influenced antipsychotic treatment. At baseline, and after 8 weeks of treatment with various antipsychotic medications, we assessed patients’ Positive and Negative Syndrome Scale (PANSS) scores, PANSS factors, and metabolic-syndrome-related parameters (fasting plasma lipid and glucose levels, and body mass index). A total of 186 antipsychotic-naïve first-episode psychosis patients or nonadherent chronic psychosis individuals (99 males and 87 females) were genotyped by polymerase chain reaction analysis. The ACE-I/D polymorphism was significantly associated with changes in PANSS psychopathology only (p < 0.05). Compared to ACE-II homozygous males, ACE-DD homozygous and ACE-ID heterozygous males manifested significantly greater decreases in PANSS positive score, PANSS excitement factor, and PANSS cognitive factor. ACE-DD homozygous females manifested higher decreases in PANSS depression factor compared to ACE-II homozygous and ACE-ID heterozygous females. The polymorphism’s effect size was estimated as moderate to strong, while its contribution to the PANSS psychopathology ranged from ~5.4 to 8.7%, with the lowest contribution observed for PANSS positive score changes and the highest for PANSS depressive factor changes. Our results indicate that ACE-I/D polymorphism had a statistically significant but weak gender-specific impact on psychopathology data, and showed no association between ACE-I/D polymorphism and metabolic-syndrome-related parameters.     

Allosteric Modulation of Muscarinic Receptors by Cholesterol,Neurosteroids and Neuroactive Steroids

Muscarinic acetylcholine receptors are membrane receptors involved in many physiological processes. Malfunction of muscarinic signaling is a cause of various internal diseases, as well as psychiatric and neurologic conditions. Cholesterol, neurosteroids, neuroactive steroids, and steroid hormones are molecules of steroid origin that, besides having well-known genomic effects, also modulate membrane proteins including muscarinic acetylcholine receptors. Here, we review current knowledge on the allosteric modulation of muscarinic receptors by these steroids. We give a perspective on the research on the non-genomic effects of steroidal compounds on muscarinic receptors and drug development, with an aim to ultimately exploit such knowledge.     

Diastereoselective Synthesis of Novel Spiro-Phosphacoumarins and Evaluation of Their Anti-Cancer Activity

Herein we present the regio- and diastereoselective synthesis of novel pyrrolidine-fused spiro-dihydrophosphacoumarins via intermolecular [3 + 2] cycloaddition reaction. The presented approach is complementary to existing ones and provides an easy entry to the otherwise inaccessible derivatives. Additionally, the unprecedented pathway of the reaction of 4-hydroxycoumarin with azomethine ylides is described. The anti-cancer activity of the obtained compounds was tested in vitro, the most potent compound being 2.6-fold more active against the HuTu 80 cell line than the reference 5-fluorouracil, with a selectivity index > 32.     

Hydrolase-like properties of a cofactor-independent dioxygenase

Mechanistic promiscuity: The (2-alkyl)-3-hydroxy-4(1H)-quinolone-cleaving dioxygenase Hod has an α/β-hydrolase fold and a Ser/His/Asp triad in its active site. Isatoic anhydride, a suicide substrate of serine hydrolases, inactivates Hod by covalent modification of the active-site serine, thus indicating that the α/β-hydrolase fold can accommodate dioxygenase chemistry without completely abandoning hydrolase-like properties.     

The Influence of Drug Solubility and Particle Size on the Pellet Formulation in a Rotoprocessor

ABSTRACT

Pellets containing drugs of different properties were prepared in a Rotoprocessor in order to study changes in the formulation process and resulting pellet characteristics. Diltiazem hydrochloride, diclofenac sodium, and theophylline were chosen as model drugs. Pellet size distribution, sphericity, density, hardness, friability, and repose angle were determined using standard methods. The amount of water as a wetting agent necessary for successful pellet formulation was observed for each sample and changed depending on drug solubility, concentration, and particle size. The pelletization of freely soluble diltiazem hydrochloride required 24.8–23.1% of the wetting agent and its amount decreased as the drug concentration increased. The demand for water in the formulation of theophylline pellets was 31.0–34.4% and it increased with increasing drug concentration. The pellet samples containing both drugs were easy to prepare. However, the cohesion of micronized diclofenac sodium particles negatively influenced both the pellet size distribution and the formulation process itself. When the drug concentration exceeded 40%, it was not possible to produce pellets of an appropriate size and the process was not reproducible.     

Describing the sorption characteristics of a ternary system of benzene (1) and alcohol (2) in a nonporous polymer membrane (3) by the Flory–Huggins model

The Flory–Huggins equation was used to describe results of total and preferential sorption measurements for the binary liquid mixture of benzene (1) and alcohol (2) in one of two nonporous polymer membranes (3), low‐density polyethylene (LDPE) and Nafion membrane. The concentration dependence of binary and ternary interaction parameters was determined. The interaction parameters for the benzene – methanol binary mixture were obtained from binary vapor‐liquid equilibrium data in the literature to decrease the number of adjusted parameters. The results show that use of a ternary interaction parameter is necessary. Data treatment was performed assuming either no crystallinity or an average crystallinity typical for the studied membranes. Subsequently, the limiting activity coefficients of solutes in LDPE were calculated from the values of the interaction parameters and their values compared to values of the limiting activity coefficients of benzene and methanol in hypothetical liquid alkane with the same density as LDPE obtained by the UNIFAC method. POLYM. ENG. SCI., 55:1187–1195, 2015. © 2014 Society of Plastics Engineers     

Leg stiffness of sprinters using running-specific prostheses

Running-specific prostheses (RSF) are designed to replicate the spring-like nature of biological legs (bioL) during running. However, it is not clear how these devices affect whole leg stiffness characteristics or running dynamics over a range of speeds. We used a simple spring–mass model to examine running mechanics across a range of speeds, in unilateral and bilateral transtibial amputees and performance-matched controls. We found significant differences between the affected leg (AL) of unilateral amputees and both ALs of bilateral amputees compared with the bioL of non-amputees for nearly every variable measured. Leg stiffness remained constant or increased with speed in bioL, but decreased with speed in legs with RSPs. The decrease in leg stiffness in legs with RSPs was mainly owing to a combination of lower peak ground reaction forces and increased leg compression with increasing speeds. Leg stiffness is an important parameter affecting contact time and the force exerted on the ground. It is likely that the fixed stiffness of the prosthesis coupled with differences in the limb posture required to run with the prosthesis limits the ability to modulate whole leg stiffness and the ability to apply high vertical ground reaction forces during sprinting.     

Tocols of selected spring wheat (Triticum aestivum L.), einkorn wheat (Triticum monococcum L.) and wild emmer (Triticum dicoccum Schuebl [Schrank]) varieties

Wheat contributes significantly worldwide to antioxidant income with beneficial healthy effects. Two varieties of einkorn wheat (Triticum monococcum L. – Escana and Schwedisches Einkorn), two varieties of wild emmer [Triticum dicoccum Schuebl (Schrank)] (Rudico and Kahler Emmer) and three varieties of spring wheat (Triticum aestivum L. – Granny, Kärtner Früher and SW Kadrilj) were evaluated for tocols – tocopherols and tocotrienols by high performance liquid chromatography – electrospray ionisation tandem mass spectrometry (HPLC–ESI/MS/MS). Investigated emmer and einkorn wheat varieties have shown minor lower total tocols content in comparison with spring varieties, however significant typical levels of tocopherols and tocotrienols were found in these groups. In einkorn wheat varieties the major abundance of total tocols is represented by tocotrienols (Schwedisches Einkorn 65.0%, Escana 54.9%), in emmer wheat varieties the abundance of tocotrienols and tocopherols were similar (Rudico 48.9% of tocotrienols, Kahler Emmer 47.6%), whereas in spring bread wheat higher tocopherols (SW Kadrilj 54.5%, Kärtner Früher 60.2%, Granny 55.0%) were recorded.     

Light Quality and Intensity Modulate Cold Acclimation in Arabidopsis

Plant survival in temperate zones requires efficient cold acclimation, which is strongly affected by light and temperature signal crosstalk, which converge in modulation of hormonal responses. Cold under low light conditions affected Arabidopsis responses predominantly in apices, possibly because energy supplies were too limited for requirements of these meristematic tissues, despite a relatively high steady-state quantum yield. Comparing cold responses at optimal light intensity and low light, we found activation of similar defence mechanisms—apart from CBF1–3 and CRF3–4 pathways, also transient stimulation of cytokinin type-A response regulators, accompanied by fast transient increase of trans-zeatin in roots. Upregulated expression of components of strigolactone (and karrikin) signalling pathway indicated involvement of these phytohormones in cold responses. Impaired response of phyA, phyB, cry1 and cry2 mutants reflected participation of these photoreceptors in acquiring freezing tolerance (especially cryptochrome CRY1 at optimal light intensity and phytochrome PHYA at low light). Efficient cold acclimation at optimal light was associated with upregulation of trans-zeatin in leaves and roots, while at low light, cytokinin (except cis-zeatin) content remained diminished. Cold stresses induced elevation of jasmonic acid and salicylic acid (in roots). Low light at optimal conditions resulted in strong suppression of cytokinins, jasmonic and salicylic acid.