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Open AccessArticle
Ionically Crosslinked Chitosan Membranes Used as Drug Carriers for Cancer Therapy Application
by , , , , , and
Materials 2018, 11(10), 2051; https://doi.org/10.3390/ma11102051 (registering DOI) -
Abstract
The aim of this paper was to prepare, by the freeze-drying method, ionically crosslinked chitosan membranes with different contents of pentasodium tripolyphosphate (TPP) and loaded with 1,4-naphthoquinone (NQ14) drug, in order to evaluate how the physical crosslinking affects NQ14 release from chitosan membranes
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The aim of this paper was to prepare, by the freeze-drying method, ionically crosslinked chitosan membranes with different contents of pentasodium tripolyphosphate (TPP) and loaded with 1,4-naphthoquinone (NQ14) drug, in order to evaluate how the physical crosslinking affects NQ14 release from chitosan membranes for cancer therapy application. The membranes were characterized by Fourier transform infrared spectroscopy (FTIR), wide-angle X-ray diffraction (WAXD), scanning electron microscopy (SEM), swelling degree, and through in vitro drug release and cytotoxicity studies. According to the results, the molecular structure, porosity and hydrophilicity of the chitosan membranes were affected by TPP concentration and, consequently, the NQ14 drug release behavior from the membranes was also affected. The release of NQ14 from crosslinked chitosan membranes decreased when the cross-linker TPP quantity increased. Thus, depending on the TPP amount, the crosslinked chitosan membranes would be a potential delivery system to control the release of NQ14 for cancer therapy application. Lastly, the inhibitory potential of chitosan membranes ionically crosslinked with TPP and loaded with NQ14 against the B16F10 melanoma cell line was confirmed through in vitro cytotoxicity studies assessed via MTT assay. The anti-proliferative effect of prepared membranes was directly related to the amount of cross-linker and among all membranes prepared, such that one crosslinked with 0.3% of TPP may become a potential delivery system for releasing NQ14 drug for cancer therapy. Full article
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Open AccessFeature PaperArticle
The Way to Ultrafast, High-Throughput Enantioseparations of Bioactive Compounds in Liquid and Supercritical Fluid Chromatography
by , , , , , , , and
Molecules 2018, 23(10), 2709; https://doi.org/10.3390/molecules23102709 (registering DOI) -
Abstract
Until less than 10 years ago, chiral separations were carried out with columns packed with 5 or 3 μm fully porous particles (FPPs). Times to resolve enantiomeric mixtures were easily larger than 30 min, or so. Pushed especially by stringent requirements from
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Until less than 10 years ago, chiral separations were carried out with columns packed with 5 or 3 μm fully porous particles (FPPs). Times to resolve enantiomeric mixtures were easily larger than 30 min, or so. Pushed especially by stringent requirements from medicinal and pharmaceutical industries, during the last years the field of chiral separations by liquid chromatography has undergone what can be defined a “true revolution”. With the purpose of developing ever faster and efficient method of separations, indeed, very efficient particle formats, such as superficially porous particles (SPPs) or Full article
Open AccessArticle
Believing in Women? Examining Early Views of Women among America’s Most Progressive Religious Groups
by and
Religions 2018, 9(10), 321; https://doi.org/10.3390/rel9100321 (registering DOI) -
Abstract
This paper examines views of women among the most prominent “progressive” American religious groups (as defined by those that liberalized early on the issue of birth control, circa 1929). We focus on the years between the first and second waves of the feminist
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This paper examines views of women among the most prominent “progressive” American religious groups (as defined by those that liberalized early on the issue of birth control, circa 1929). We focus on the years between the first and second waves of the feminist movement (1929–1965) in order to examine these views during a time of relative quiescence. We find that some groups indeed have a history of outspoken support for women’s equality. Using their modern-day names, these groups—the United Church of Christ, the Unitarian Universalist Association, and to a lesser extent, the Society of Friends, or Quakers—professed strong support for women’s issues, early and often. However, we also find that prominent progressive groups—the Protestant Episcopal Church, the Methodist Episcopal Church, and the United Presbyterian Church—were virtually silent on the issue of women’s rights. Thus, we conclude that birth control activism within the American religious field was not clearly correlated with an overall feminist orientation. Full article
Open AccessReview
Inhibitory-κB Kinase (IKK) α and Nuclear Factor-κB (NFκB)-Inducing Kinase (NIK) as Anti-Cancer Drug Targets
by , , and
Cells 2018, 7(10), 176; https://doi.org/10.3390/cells7100176 (registering DOI) -
Abstract
The cellular kinases inhibitory-κB kinase (IKK) α and Nuclear Factor-κB (NF-κB)-inducing kinase (NIK) are well recognised as key central regulators and drivers of the non-canonical NF-κB cascade and as such dictate the initiation and development of defined transcriptional responses associated with the liberation
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The cellular kinases inhibitory-κB kinase (IKK) α and Nuclear Factor-κB (NF-κB)-inducing kinase (NIK) are well recognised as key central regulators and drivers of the non-canonical NF-κB cascade and as such dictate the initiation and development of defined transcriptional responses associated with the liberation of p52-RelB and p52-p52 NF-κB dimer complexes. Whilst these kinases and downstream NF-κB complexes transduce pro-inflammatory and growth stimulating signals that contribute to major cellular processes, they also play a key role in the pathogenesis of a number of inflammatory-based conditions and diverse cancer types, which for the latter may be a result of background mutational status. IKKα and NIK, therefore, represent attractive targets for pharmacological intervention. Here, specifically in the cancer setting, we reflect on the potential pathophysiological role(s) of each of these kinases, their associated downstream signalling outcomes and the stimulatory and mutational mechanisms leading to their increased activation. We also consider the downstream coordination of transcriptional events and phenotypic outcomes illustrative of key cancer ‘Hallmarks’ that are now increasingly perceived to be due to the coordinated recruitment of both NF-κB-dependent as well as NF-κB–independent signalling. Furthermore, as these kinases regulate the transition from hormone-dependent to hormone-independent growth in defined tumour subsets, potential tumour reactivation and major cytokine and chemokine species that may have significant bearing upon tumour-stromal communication and tumour microenvironment it reiterates their potential to be drug targets. Therefore, with the emergence of small molecule kinase inhibitors targeting each of these kinases, we consider medicinal chemistry efforts to date and those evolving that may contribute to the development of viable pharmacological intervention strategies to target a variety of tumour types. Full article
Open AccessFeature PaperArticle
Long-Term Effect on Bioactive Components and Antioxidant Activity of Thermal and High-Pressure Pasteurization of Orange Juice
by , , , , , and
Molecules 2018, 23(10), 2706; https://doi.org/10.3390/molecules23102706 (registering DOI) -
Abstract
The long-term effect of thermal pasteurization (TP) and high-pressure processing (HPP) of orange juices stored under refrigeration, on the bioactive components and antioxidant activity, was compared. Total phenolic content (TPC), flavonoid, anthocyanin, and carotenoid contents, the individual content of major phenolic components, and
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The long-term effect of thermal pasteurization (TP) and high-pressure processing (HPP) of orange juices stored under refrigeration, on the bioactive components and antioxidant activity, was compared. Total phenolic content (TPC), flavonoid, anthocyanin, and carotenoid contents, the individual content of major phenolic components, and the antioxidant activity, were evaluated in TP- and HPP-treated juices over a 36-day period. At day 0, no significant differences in TPC, and a decrease in carotenoid content after both treatments, were observed. TP caused a decrease of flavonoid and anthocyanin contents, while HPP increased flavonoid content. Three major phenolic components were identified: apigenin-6,8-di-C-glucoside, naringenin-7-O-rutinoside, and hesperetin-7-O-rutinoside, the latter increasing ca. 45% immediately after HPP. During storage, a decrease in TPC, and in the anthocyanin and carotenoid contents of both treated juices was observed, with higher anthocyanin and phenolic contents in HPP juices. A significant increase of hesperetin-7-O-rutinoside content was observed in HPP juice. Both treatments caused a decrease (26% and 13%, respectively) of antioxidant activity. Most of the kinetic profiles followed zero-order patterns, with HPP juices showing a considerably higher half-life than TP ones. These results clearly demonstrate the advantages of HPP for orange juice preservation allowing, also, their nutritional benefits to be enhanced by increasing the content of some bioactive components. Full article
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Open AccessArticle
Reprogramming Static Deformation Patterns in Mechanical Metamaterials
by and
Materials 2018, 11(10), 2050; https://doi.org/10.3390/ma11102050 (registering DOI) -
Abstract
This paper discusses an x-braced metamaterial lattice with the unusual property of exhibiting bandgaps in their deformation decay spectrum, and, hence, the capacity for reprogramming deformation patterns. The design of polarizing non-local lattice arising from the scenario of repeated zero eigenvalues of a
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This paper discusses an x-braced metamaterial lattice with the unusual property of exhibiting bandgaps in their deformation decay spectrum, and, hence, the capacity for reprogramming deformation patterns. The design of polarizing non-local lattice arising from the scenario of repeated zero eigenvalues of a system transfer matrix is also introduced. We develop a single mode fundamental solution for lattices with multiple degrees of freedom per node in the form of static Raleigh waves. These waves can be blocked at the material boundary when the solution is constructed with the polarization vectors of the bandgap. This single mode solution is used as a basis to build analytical displacement solutions for any applied essential and natural boundary condition. Subsequently, we address the bandgap design, leading to a comprehensive approach for predicting deformation pattern behavior within the interior of an x-braced plane lattice. Overall, we show that the stiffness parameter and unit-cell aspect ratio of the x-braced lattice can be tuned to completely block or filter static boundary deformations, and to reverse the dependence of deformation or strain energy decay parameter on the Raleigh wavenumber, a behavior known as the reverse Saint Venant’s edge effect (RSV). These findings could guide future research in engineering smart materials and structures with interesting functionalities, such as load pattern recognition, strain energy redistribution, and stress alleviation. Full article
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Open AccessFeature PaperArticle
A New Tool in the Quest for Biocompatible Phthalocyanines: Palladium Catalyzed Aminocarbonylation for Amide Substituted Phthalonitriles and Illustrative Phthalocyanines Thereof
by , , , and
Catalysts 2018, 8(10), 480; https://doi.org/10.3390/catal8100480 (registering DOI) -
Abstract
The amide peptide bond type linkage is one of the most natural conjugations available, present in many biological synthons and pharmaceutical drugs. Hence, aiming the direct conjugation of potentially biologically active compounds to phthalocyanines, herein we disclose a new strategy for direct modulation
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The amide peptide bond type linkage is one of the most natural conjugations available, present in many biological synthons and pharmaceutical drugs. Hence, aiming the direct conjugation of potentially biologically active compounds to phthalocyanines, herein we disclose a new strategy for direct modulation of phthalonitriles, inspired by an attractive synthetic strategy for the preparation of carboxamides based on palladium-catalyzed aminocarbonylation of aryl halides in the presence of carbon monoxide (CO) which, to our knowledge, has never been used to prepare amide-substituted phthalonitriles, the natural precursors for the synthesis of phthalocyanines. Some examples of phthalocyanines prepared thereof are also reported, along with their full spectroscopic characterization and photophysical properties initial assessment. Full article
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