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Molecules, Volume 23, Issue 8 (August 2018)

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Cover Story (view full-size image) A viral protein R-derived 7-mer peptide with photo-reactive benzoylphenylalanyl and biotin residues [...] Read more.
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Open AccessReview Current Concepts and Treatments of Schizophrenia
Molecules 2018, 23(8), 2087; https://doi.org/10.3390/molecules23082087
Received: 26 July 2018 / Revised: 10 August 2018 / Accepted: 18 August 2018 / Published: 20 August 2018
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Abstract
Schizophrenia is a debilitating mental illness which involves three groups of symptoms, i.e., positive, negative and cognitive, and has major public health implications. According to various sources, it affects up to 1% of the population. The pathomechanism of schizophrenia is not fully understood
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Schizophrenia is a debilitating mental illness which involves three groups of symptoms, i.e., positive, negative and cognitive, and has major public health implications. According to various sources, it affects up to 1% of the population. The pathomechanism of schizophrenia is not fully understood and current antipsychotics are characterized by severe limitations. Firstly, these treatments are efficient for about half of patients only. Secondly, they ameliorate mainly positive symptoms (e.g., hallucinations and thought disorders which are the core of the disease) but negative (e.g., flat affect and social withdrawal) and cognitive (e.g., learning and attention disorders) symptoms remain untreated. Thirdly, they involve severe neurological and metabolic side effects and may lead to sexual dysfunction or agranulocytosis (clozapine). It is generally agreed that the interactions of antipsychotics with various neurotransmitter receptors are responsible for their effects to treat schizophrenia symptoms. In particular, several G protein-coupled receptors (GPCRs), mainly dopamine, serotonin and adrenaline receptors, are traditional molecular targets for antipsychotics. Comprehensive research on GPCRs resulted in the exploration of novel important signaling mechanisms of GPCRs which are crucial for drug discovery: intentionally non-selective multi-target compounds, allosteric modulators, functionally selective compounds and receptor oligomerization. In this review, we cover current hypotheses of schizophrenia, involving different neurotransmitter systems, discuss available treatments and present novel concepts in schizophrenia and its treatment, involving mainly novel mechanisms of GPCRs signaling. Full article
(This article belongs to the Section Medicinal Chemistry)
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Open AccessArticle Highly Effective Removal of Metal Cyanide Complexes and Recovery of Palladium Using Quaternary-Ammonium-Functionalized MOFs
Molecules 2018, 23(8), 2086; https://doi.org/10.3390/molecules23082086
Received: 12 June 2018 / Revised: 17 August 2018 / Accepted: 19 August 2018 / Published: 20 August 2018
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Abstract
In this study, quaternary-ammonium-functionalized metal–organic frameworks (MOFs) Et-N-Cu(BDC-NH2)(DMF), were prepared, characterized, and applied for the highly effective removal of metal cyanide complexes, including Pd(CN)42−, Co(CN)63, and Fe(CN)63. Batch
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In this study, quaternary-ammonium-functionalized metal–organic frameworks (MOFs) Et-N-Cu(BDC-NH2)(DMF), were prepared, characterized, and applied for the highly effective removal of metal cyanide complexes, including Pd(CN)42−, Co(CN)63, and Fe(CN)63. Batch studies were carried out, and the maximum adsorption capacities of Pd(II), Co(III), and Fe(III) reached 172.9, 101.0, and 102.6, respectively. Adsorption was rapid, and equilibrium was established within 30 min. Et-N-Cu(BDC-NH2)(DMF) exhibited high thermal and chemical stability. Furthermore, absorbed Pd(CN)42− was selectively recovered by two-step elution. First, Co(CN)63 and Fe(CN)63 were eluted with a 1.5 mol L−1 KCl solution. Elution rates of Co(CN)63 and Fe(CN)63 were greater than 98.0%, whereas the elution percentage of Pd(CN)42− was less than 2.0%. Second, >97.0% Pd(CN)42− on the loaded MOFs was eluted using a 2.0 mol L−1 KI solution. The recovery rate of Pd(CN)42− was greater than 91.0% after five testing cycles. Adsorption isotherms, kinetics models, and adsorption thermodynamics of Pd(CN)42− on Et-N-Cu(BDC-NH2) (DMF) were also systematically investigated. The Et-N-Cu(BDC-NH2) (DMF) absorbent exhibited a rapid, excellent ability for the adsorption of metal cyanide complexes. Full article
(This article belongs to the Section Green Chemistry)
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Open AccessArticle Phenanthrenes from Juncus Compressus Jacq. with Promising Antiproliferative and Anti-HSV-2 Activities
Molecules 2018, 23(8), 2085; https://doi.org/10.3390/molecules23082085
Received: 21 July 2018 / Revised: 13 August 2018 / Accepted: 16 August 2018 / Published: 20 August 2018
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Abstract
Juncaceae species are rich sources of phenanthrenes. The present study has focused on the isolation and structure determination of biologically active components from Juncus compressus. Eleven compounds (nine phenanthrenes and two flavonoids) have been isolated from the plant by the combination of
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Juncaceae species are rich sources of phenanthrenes. The present study has focused on the isolation and structure determination of biologically active components from Juncus compressus. Eleven compounds (nine phenanthrenes and two flavonoids) have been isolated from the plant by the combination of different chromatographic methods. Two compounds (compressins A (Compound 1) and B (Compound 2)) are novel natural products, while seven phenanthrenes (effusol (Compound 3), effususol (Compound 4), juncusol (Compound 5), 2-hydroxy-1-methyl-4-oxymethylene-5-vinyl-9,10-dihydrophenanthrene (Compound 6), 7-hydroxy-1-methyl-2-methoxy-5-vinyl-9,10-dihydrophenanthrene (Compound 7), effususin A (Compound 8), and dehydroeffusol (Compound 9)), and two flavonoids (apigenin (Compound 10) and luteolin (Compound 11) were isolated for the first time from the plant. Compressin B (Compound 2) is a dimeric phenanthrene, in which two juncusol monomers (Compound 5) are connecting through their C-3 atoms. The structure elucidation of the isolated compounds was carried out using 1D, 2D NMR spectroscopic methods and HR-MS measurements. In vitro investigation of the antiproliferative effect of the phenanthrenes on two cervical (HeLa and SiHa) and an ovarian human tumor cell line (A2780) revealed that compounds have remarkable antiproliferative activity, mainly on the HeLa cell line. Moreover, juncusol (Compound 5) proved to possess significant antiviral activity against the herpes simplex 2 virus (HSV-2). Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Synthesis and Evolution of Berberine Derivatives as a New Class of Antiviral Agents against Enterovirus 71 through the MEK/ERK Pathway and Autophagy
Molecules 2018, 23(8), 2084; https://doi.org/10.3390/molecules23082084
Received: 17 July 2018 / Revised: 14 August 2018 / Accepted: 16 August 2018 / Published: 20 August 2018
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Abstract
Taking berberine (BBR) as the lead, 23 new BBR derivatives were synthesized and examined for their antiviral activities against four different genotype enterovirus 71 (EV71) strains with a cytopathic effect (CPE) assay. Structure-activity relationship (SAR) studies indicated that introduction of a suitable substituent
[...] Read more.
Taking berberine (BBR) as the lead, 23 new BBR derivatives were synthesized and examined for their antiviral activities against four different genotype enterovirus 71 (EV71) strains with a cytopathic effect (CPE) assay. Structure-activity relationship (SAR) studies indicated that introduction of a suitable substituent at the 9-position might be beneficial for potency. Among them, compound 2d exhibited most potent activities with IC50 values of 7.12–14.8 μM, similar to that of BBR. The effect of 2d was further confirmed in a dose-dependent manner both in RNA and protein level. The mechanism revealed that 2d could inhibit the activation of MEK/ERK signaling pathway. Meanwhile, it could suppress the EV71-induced autophagy by activating AKT and inhibiting the phosphorylation of JNK and PI3KIII proteins. We consider BBR derivatives to be a new family of anti-EV71 agents through targeting host components, with an advantage of broad-spectrum anti-EV71 potency. Full article
(This article belongs to the Special Issue Recent Advances in the Development of Antiviral Agents)
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Open AccessArticle Suppression of Hepatitis C Virus Genome Replication and Particle Production by a Novel Diacylglycerol Acyltransferases Inhibitor
Molecules 2018, 23(8), 2083; https://doi.org/10.3390/molecules23082083
Received: 19 June 2018 / Revised: 1 August 2018 / Accepted: 11 August 2018 / Published: 20 August 2018
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Abstract
Diacylglycerol acyltransferases (DGATs) play a critical role in the biosynthesis of endogenous triglycerides (TGs) and formation of lipid droplets (LDs) in the liver. In particular, one member of DGATs, DGAT-1 was reported to be an essential host factor for the efficient production of
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Diacylglycerol acyltransferases (DGATs) play a critical role in the biosynthesis of endogenous triglycerides (TGs) and formation of lipid droplets (LDs) in the liver. In particular, one member of DGATs, DGAT-1 was reported to be an essential host factor for the efficient production of hepatitis C virus (HCV) particles. By utilizing our previously characterized three different groups of twelve DGAT inhibitors, we found that one of the DGAT inhibitors, a 2-((4-adamantylphenoxy) methyl)-N-(furan-2-ylmethyl)-1H-benzo[d]imidazole-5-carboxam (10j) is a potent suppressor of both HCV genome replication and particle production. 10j was able to induce inhibition of these two critical viral functions in a mutually separate manner. Abrogation of the viral genome replication by 10j led to a significant reduction in the viral protein expression as well. Interestingly, we found that its antiviral effect did not depend on the reduction of TG biosynthesis by 10j. This suggests that the inhibitory activity of 10j against DGATs may not be directly related with its antiviral action. Full article
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Open AccessArticle Morphological, Release and Antibacterial Performances of Amoxicillin-Loaded Cellulose Aerogels
Molecules 2018, 23(8), 2082; https://doi.org/10.3390/molecules23082082
Received: 27 July 2018 / Revised: 9 August 2018 / Accepted: 14 August 2018 / Published: 20 August 2018
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Abstract
Cellulose has been widely used in the biomedical field. In this study, novel cellulose aerogels were firstly prepared in a NaOH-based solvent system by a facile casting method. Then amoxicillin was successfully loaded into cellulose aerogels with different loadings. The morphology and structure
[...] Read more.
Cellulose has been widely used in the biomedical field. In this study, novel cellulose aerogels were firstly prepared in a NaOH-based solvent system by a facile casting method. Then amoxicillin was successfully loaded into cellulose aerogels with different loadings. The morphology and structure of the cellulose aerogels were characterized using scanning electron microscopy (SEM) and Fourier transform infrared spectroscopy (FTIR). The drug release and antibacterial activities were also evaluated. The drug release results showed that cellulose aerogels have controlled amoxicillin release performance. In vitro antibacterial assay demonstrated that the cellulose aerogels exhibited excellent antibacterial activity with the amoxicillin dose-dependent activity. Therefore, the developed cellulose aerogels display controlled release behavior and efficient antibacterial performance, thus confirming their potential for biomedical applications. Full article
(This article belongs to the Special Issue Emerging Trends in Nanocelluloses)
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Open AccessArticle Comparative Transcriptome Profiling Reveals Defense-Related Genes against Meloidogyne incognita Invasion in Tobacco
Molecules 2018, 23(8), 2081; https://doi.org/10.3390/molecules23082081
Received: 29 July 2018 / Revised: 15 August 2018 / Accepted: 17 August 2018 / Published: 20 August 2018
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Abstract
Root-knot nematodes Meloidogyne incognita are one of the most destructive pathogens, causing severe losses to tobacco productivity and quality. However, the underlying resistance mechanism of tobacco to M. incognita is not clear. In this study, two tobacco genotypes, K326 and Changbohuang, which are
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Root-knot nematodes Meloidogyne incognita are one of the most destructive pathogens, causing severe losses to tobacco productivity and quality. However, the underlying resistance mechanism of tobacco to M. incognita is not clear. In this study, two tobacco genotypes, K326 and Changbohuang, which are resistant and susceptible to M. incognita, respectively, were used for RNA-sequencing analysis. An average of 35 million clean reads were obtained. Compared with their expression levels in non-infected plants of the same genotype, 4354 and 545 differentially expressed genes (DEGs) were detected in the resistant and susceptible genotype, respectively, after M. incognita invasion. Overall, 291 DEGs, involved in diverse biological processes, were common between the two genotypes. Genes encoding toxic compound synthesis, cell wall modification, reactive oxygen species and the oxidative burst, salicylic acid signal transduction, and production of some other metabolites were putatively associated with tobacco resistance to M. incognita. In particular, the complex resistance response needed to overcome M. incognita invasion may be regulated by several transcription factors, such as the ethylene response factor, MYB, basic helix–loop–helix transcription factor, and indole acetic acid–leucine-resistant transcription factor. These results may aid in the identification of potential genes of resistance to M. incognita for tobacco cultivar improvement. Full article
(This article belongs to the Section Chemical Biology)
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Open AccessFeature PaperReview Natural Cyclic Peptides as an Attractive Modality for Therapeutics: A Mini Review
Molecules 2018, 23(8), 2080; https://doi.org/10.3390/molecules23082080
Received: 30 July 2018 / Revised: 14 August 2018 / Accepted: 19 August 2018 / Published: 20 August 2018
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Abstract
Peptides are important biomolecules which facilitate the understanding of complex biological processes, which in turn could be serendipitous biological targets for future drugs. They are classified as a unique therapeutic niche and will play an important role as fascinating agents in the pharmaceutical
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Peptides are important biomolecules which facilitate the understanding of complex biological processes, which in turn could be serendipitous biological targets for future drugs. They are classified as a unique therapeutic niche and will play an important role as fascinating agents in the pharmaceutical landscape. Until now, more than 40 cyclic peptide drugs are currently in the market, and approximately one new cyclopeptide drug enters the market annually on average. Interestingly, the majority of clinically approved cyclic peptides are derived from natural sources, such as peptide antibiotics and human peptide hormones. In this report, the importance of cyclic peptides is discussed, and their role in drug discovery as interesting therapeutic biomolecules will be highlighted. Recently isolated naturally occurring cyclic peptides from microorganisms, sponges, and other sources with a wide range of pharmacological properties are reviewed herein. Full article
(This article belongs to the Special Issue Cyclic Peptides)
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Open AccessArticle Structure-Immunogenicity Relationship of α- and β-Tetrasaccharide Glycoforms from Bacillus anthracis Exosporium and Fragments Thereof
Molecules 2018, 23(8), 2079; https://doi.org/10.3390/molecules23082079
Received: 12 July 2018 / Revised: 1 August 2018 / Accepted: 17 August 2018 / Published: 20 August 2018
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Abstract
The tetrasaccharide (2-O-methyl-4-(3-hydroxy-3-methylbutamido)-4,6-dideoxy-α-d-glucopyranosyl-(1→3)-α-l-rhamnopyranosyl-(1→3)-α-l-rhamnopyranosyl-(1→2)-l-rhamnopyranose) from the major exosporium protein (BclA) of Bacillus anthracis has been proposed as a target for development of diagnostics and immune therapy or prophylaxis. While the immunodominant character of the
[...] Read more.
The tetrasaccharide (2-O-methyl-4-(3-hydroxy-3-methylbutamido)-4,6-dideoxy-α-d-glucopyranosyl-(1→3)-α-l-rhamnopyranosyl-(1→3)-α-l-rhamnopyranosyl-(1→2)-l-rhamnopyranose) from the major exosporium protein (BclA) of Bacillus anthracis has been proposed as a target for development of diagnostics and immune therapy or prophylaxis. While the immunodominant character of the anthrose residue has been previously elucidated, the role of the stereochemical configuration of the downstream rhamnose is unknown. Because the linkage of this residue to the GlcNAc bridging the glycan and the protein is lost during isolation of the tetrasaccharide, its α- and β-glycoforms have been synthesized. Herein, we prepared neoglycoconjugates from a series of fragments of the tetrasaccharide, including the complete α- and β-tetrasaccharide glycoforms, a 2-demethoxylated version of the α-tetrasaccharide, and the α- and β-trirhamnosides and CRM197. By immunization of mice, we showed that the anti α- and β-tetrasaccharide serum equally recognized both glycoforms. In contrast the sera produced following immunization with the α- and β-trirhamnoside fragments exhibited higher recognition for their own antigens than for their anomeric counterparts. The anti α- and β-tetrasaccharide sera recognized Sterne spores in a comparable fashion. ΔBclA spores not expressing the major exosporium protein were also recognized by the same sera, while mutants that produced the carbohydrate antigen with deletion of either rhamnose or anthrose were not. The tetrasaccharide could, therefore, be expressed in proteins other than BlcA. This work proves that α- and β-tetrasaccharide are equally potent immunogens. Full article
(This article belongs to the Special Issue Conjugate Vaccines from Carbohydrate Antigens)
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Open AccessArticle A Comparative Metabolomics Analysis Reveals the Tissue-Specific Phenolic Profiling in Two Acanthopanax Species
Molecules 2018, 23(8), 2078; https://doi.org/10.3390/molecules23082078
Received: 21 June 2018 / Revised: 24 July 2018 / Accepted: 24 July 2018 / Published: 20 August 2018
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Abstract
Acanthopanax senticosus (Rupr. Maxim.) Harms (ASH) and Acanthopanax sessiliflorus (Rupr. Maxim.) Seem (ASS), are members of the Araliaceae family, and both are used in Asian countries. These herbals have drawn much attention in recent years due to their strong biological activity, with innocuity
[...] Read more.
Acanthopanax senticosus (Rupr. Maxim.) Harms (ASH) and Acanthopanax sessiliflorus (Rupr. Maxim.) Seem (ASS), are members of the Araliaceae family, and both are used in Asian countries. These herbals have drawn much attention in recent years due to their strong biological activity, with innocuity and little side effects. However, the common and distinct mode of compound profiles between ASH and ASS is still unclear. In this study, a high performance liquid chromatograph-mass spectrometry (HPLC-MS) method was developed to simultaneously quantify the seven major active compounds, including protocatechuate, eleutheroside B, eleutheroside E, isofraxidin, hyperoside, kaempferol and oleanolic acid. Then the targeted metabolomics were conducted to identify 19 phenolic compounds, with tight relation to the above mentioned active compounds, including nine C6C3C6-type, six C6C3-type and four C6C1-type in the two Acanthopanax species studied here. The results showed that the seven active compounds presented a similar trend of changes in different tissues, with more abundant accumulation in roots and stems for both plants. From the view of plant species, the ASH plants possess higher abundance of compounds, especially in the tissues of roots and stems. For phenolics, the 19 phenols detected here could be clearly grouped into five main clusters based on their tissue-specific accumulation patterns. Roots are the tissue for the most abundance of their accumulations. C6C3C6-type compounds are the most widely existing type in both plants. In conclusion, the tissue- and species-specificity in accumulation of seven active compounds and phenolics were revealed in two Acanthopanax species. Full article
(This article belongs to the Special Issue Natural Product Isolation, Identification and Biological Activity)
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Open AccessArticle Origanum vulgare ssp. vulgare: Chemical Composition and Biological Studies
Molecules 2018, 23(8), 2077; https://doi.org/10.3390/molecules23082077
Received: 19 July 2018 / Revised: 14 August 2018 / Accepted: 15 August 2018 / Published: 19 August 2018
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Abstract
The biological properties and main phenolic compounds of the O. vulgare L. ssp. vulgare extract are described in the present paper. The polyphenolic compounds were analyzed by chromatographic and spectrophotometric techniques. The antioxidant potential was evaluated using several methods: CUPRAC (cupric ion reducing
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The biological properties and main phenolic compounds of the O. vulgare L. ssp. vulgare extract are described in the present paper. The polyphenolic compounds were analyzed by chromatographic and spectrophotometric techniques. The antioxidant potential was evaluated using several methods: CUPRAC (cupric ion reducing antioxidant capacity), FRAP (ferric reducing ability of plasma), inhibition of lipid peroxidation catalyzed by cytochrome c, and superoxide (SO) scavenging assays. The antimicrobial activity of the oregano extract was evaluated by means of agar-well diffusion assay. The hepatoprotective effect of the O. vulgare extract on CCl4-induced hepatotoxicity was evaluated in rats. Liver injury was estimated by determination of alanine aminotransaminase (ALT), aspartate aminotransaminase (AST), gamma-glutamyl transferase GGT, total protein and albumin concentrations, glutathione peroxidase (GPx), catalase (CAT), superoxide dismutase (SOD) and malondialdehyde (MDA). These values were improved by the administration of oregano extract. A specific phenolic profile was evidenced by these data, with large amounts of rosmarinic and chlorogenic acids. The oregano extract showed very strong antioxidant activity in good agreement with the phenolic content. Antimicrobial activity was good, especially against Salmonella enteritidis and Aspergillus niger strains. The high hepatoprotective, antioxidant and antimicrobial activity, along with polyphenol-rich content, can support the use of O. vulgare in therapy. We also expect our results to open new research directions for designing important new drug products, using indigenous plant material. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Using XRF and ICP-OES in Biosorption Studies
Molecules 2018, 23(8), 2076; https://doi.org/10.3390/molecules23082076
Received: 16 July 2018 / Revised: 13 August 2018 / Accepted: 13 August 2018 / Published: 19 August 2018
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Abstract
In this work, a method of recalculation of results of X-ray fluorescence (XRF) technique to Inductively Coupled Plasma-Optical Emission Spectroscopy (ICP-OES) method was elaborated for biosorption studies. Equations that calibrate XRF to ICP-OES were determined, as a biosorbent strawberry, blackcurrant and raspberry seeds
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In this work, a method of recalculation of results of X-ray fluorescence (XRF) technique to Inductively Coupled Plasma-Optical Emission Spectroscopy (ICP-OES) method was elaborated for biosorption studies. Equations that calibrate XRF to ICP-OES were determined, as a biosorbent strawberry, blackcurrant and raspberry seeds after supercritical CO2 extraction were used. ICP-OES showed a better precision and lower detection limits than XRF. The latter technique is cheaper, requires minimal sample preparation and gives faster results. Linear regression of the data gave almost 1:1 correlations without additional correction (for Cu r2 = 0.9998, Mn r2 = 0.807, Zn r2 = 0.979). Calibration and quantification of intensities of XRF was obtained using ICP-OES measurements after samples digestion with HNO3 in a microwave system. High positive correlations were estimated for Cu, Mn, Zn. It was demonstrated that XRF technique can be used together with other well established techniques (ICP-OES) to produce quantitative data from biosorption studies. Elaboration of cheap and quick analytical methodology is an important aspect in development of new processes and products based on biosorption process. Full article
(This article belongs to the Section Analytical Chemistry)
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Open AccessArticle Antimicrobial Photodynamic Therapy Mediated by Curcumin-Loaded Polymeric Nanoparticles in a Murine Model of Oral Candidiasis
Molecules 2018, 23(8), 2075; https://doi.org/10.3390/molecules23082075
Received: 14 July 2018 / Revised: 14 August 2018 / Accepted: 14 August 2018 / Published: 19 August 2018
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Abstract
Antimicrobial photodynamic therapy (aPDT) has been proposed as an alternative method for oral candidiasis (OC), while nanocarriers have been used to improve the water solubility of curcumin (CUR). The aim of this study is to encapsulate CUR in polymeric nanoparticles (NPs) and to
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Antimicrobial photodynamic therapy (aPDT) has been proposed as an alternative method for oral candidiasis (OC), while nanocarriers have been used to improve the water solubility of curcumin (CUR). The aim of this study is to encapsulate CUR in polymeric nanoparticles (NPs) and to evaluate its photodynamic effects on a murine model of OC. Anionic and cationic CUR-NP is synthesized using poly-lactic acid and dextran sulfate and then characterized. Female mice are immunosuppressed and inoculated with Candida albicans (Ca) to induce OC. aPDT is performed by applying CUR-NP or free CUR on the dorsum of the tongue, followed by blue light irradiation for five consecutive days. Nystatin is used as positive control. Afterward, Ca are recovered and cultivated. Animals are euthanized for histological, immunohistochemical, and DNA damage evaluation. Encapsulation in NP improves the water solubility of CUR. Nystatin shows the highest reduction of Ca, followed by aPDT mediated by free CUR, which results in immunolabelling of cytokeratins closer to those observed for healthy animals. Anionic CUR-NP does not show antifungal effect, and cationic CUR-NP reduces Ca even in the absence of light. DNA damage is associated with Ca infection. Consecutive aPDT application is a safe treatment for OC. Full article
(This article belongs to the Special Issue Nanomaterials for Phototherapeutic Applications)
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Open AccessFeature PaperPerspective The Fuzziness of the Molecular World and Its Perspectives
Molecules 2018, 23(8), 2074; https://doi.org/10.3390/molecules23082074
Received: 30 July 2018 / Revised: 16 August 2018 / Accepted: 17 August 2018 / Published: 19 August 2018
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Abstract
Scientists want to comprehend and control complex systems. Their success depends on the ability to face also the challenges of the corresponding computational complexity. A promising research line is artificial intelligence (AI). In AI, fuzzy logic plays a significant role because it is
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Scientists want to comprehend and control complex systems. Their success depends on the ability to face also the challenges of the corresponding computational complexity. A promising research line is artificial intelligence (AI). In AI, fuzzy logic plays a significant role because it is a suitable model of the human capability to compute with words, which is relevant when we make decisions in complex situations. The concept of fuzzy set pervades the natural information systems (NISs), such as living cells, the immune and the nervous systems. This paper describes the fuzziness of the NISs, in particular of the human nervous system. Moreover, it traces three pathways to process fuzzy logic by molecules and their assemblies. The fuzziness of the molecular world is useful for the development of the chemical artificial intelligence (CAI). CAI will help to face the challenges that regard both the natural and the computational complexity. Full article
(This article belongs to the Special Issue The Fuzziness in Molecular, Supramolecular, and Systems Chemistry)
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Open AccessArticle Preparation and Characterization of Antioxidative and UV-Protective Larch Bark Tannin/PVA Composite Membranes
Molecules 2018, 23(8), 2073; https://doi.org/10.3390/molecules23082073
Received: 17 July 2018 / Revised: 11 August 2018 / Accepted: 15 August 2018 / Published: 19 August 2018
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Abstract
In order to prepare functional materials for antioxidant and ultraviolet (UV)-protective green food packaging, condensed tannin, previously extracted from larch bark, was mixed with polyvinyl alcohol (PVA), and then the mixture was used to cast composite membranes. An antioxidative assay using 1,1-diphenyl-2-picrylhydrazyl (DPPH)—a
[...] Read more.
In order to prepare functional materials for antioxidant and ultraviolet (UV)-protective green food packaging, condensed tannin, previously extracted from larch bark, was mixed with polyvinyl alcohol (PVA), and then the mixture was used to cast composite membranes. An antioxidative assay using 1,1-diphenyl-2-picrylhydrazyl (DPPH)—a free radical scavenger—and starch–potassium iodide oxidation–discoloration analyses showed that the composite membranes have good antioxidative activities. The low UV transmission and protective effect of the composite films on vitamin E indicated the UV protection ability of the composite membranes. Both larch bark tannin and PVA are rich in hydroxyl groups; scanning electron microscopy analysis demonstrated their compatibility. Also, the mechanical and crystallization properties of the composite membranes did not significantly decrease with the addition of larch bark tannin. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Antihyperalgesic Activity of Atomoxetine on Diabetes-Induced Neuropathic Pain: Contribution of Noradrenergic and Dopaminergic Systems
Molecules 2018, 23(8), 2072; https://doi.org/10.3390/molecules23082072
Received: 20 July 2018 / Revised: 9 August 2018 / Accepted: 13 August 2018 / Published: 19 August 2018
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Abstract
Atomoxetine is a selective noradrenaline reuptake inhibitor drug. Based on the knowledge that agents increasing monoamine levels in the central nervous system have therapeutic potential for neuropathic pain, it is planned to investigate the possible efficacy of atomoxetine on diabetes-induced hyperalgesia, in this
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Atomoxetine is a selective noradrenaline reuptake inhibitor drug. Based on the knowledge that agents increasing monoamine levels in the central nervous system have therapeutic potential for neuropathic pain, it is planned to investigate the possible efficacy of atomoxetine on diabetes-induced hyperalgesia, in this study. Randall-Selitto (mechanical noxious stimuli) and Hargreaves (thermal noxious stimuli) tests were used to evaluate nociceptive perception of rats. Obtained data indicated that streptozotocin-induced diabetes causes significant decreases in the paw withdrawal threshold and paw withdrawal latency values of the animals, respectively. However, atomoxetine administered at 3 mg/kg/day for 7 and 14 days improved these diabetes-induced hyperalgesia responses. Furthermore, antihyperalgesic activity was antagonized with α-methyl-para-tyrosine methyl ester, phentolamine, propranolol, and sulpiride pre-treatments. The same effect was not reversed, however, by SCH 23390. These findings demonstrated, for the first time, that atomoxetine possesses significant antihyperalgesic activity on diabetes-induced neuropathic pain and this effect seems to be mediated by α- and β-adrenergic and D2/D3 dopaminergic receptors. Results of this present study seem to offer a new indication for an old drug; atomoxetine, but these preclinical data should first be confirmed with further well-designed clinical trials. Full article
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Open AccessArticle Green Tea Catechin Is an Alternative Immune Checkpoint Inhibitor that Inhibits PD-L1 Expression and Lung Tumor Growth
Molecules 2018, 23(8), 2071; https://doi.org/10.3390/molecules23082071
Received: 20 July 2018 / Revised: 15 August 2018 / Accepted: 16 August 2018 / Published: 18 August 2018
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Abstract
The anticancer activity of immune checkpoint inhibitors is attracting attention in various clinical sites. Since green tea catechin has cancer-preventive activity in humans, whether green tea catechin supports the role of immune checkpoint inhibitors was studied. We here report that (−)-epigallocatechin gallate (EGCG)
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The anticancer activity of immune checkpoint inhibitors is attracting attention in various clinical sites. Since green tea catechin has cancer-preventive activity in humans, whether green tea catechin supports the role of immune checkpoint inhibitors was studied. We here report that (−)-epigallocatechin gallate (EGCG) inhibited programmed cell death ligand 1 (PD-L1) expression in non–small-cell lung cancer cells, induced by both interferon (IFN)-γ and epidermal growth factor (EGF). The mRNA and protein levels of IFN-γ–induced PD-L1 were reduced 40–80% after pretreatment with EGCG and green tea extract (GTE) in A549 cells, via inhibition of JAK2/STAT1 signaling. Similarly, EGF-induced PD-L1 expression was reduced about 37–50% in EGCG-pretreated Lu99 cells through inhibition of EGF receptor/Akt signaling. Furthermore, 0.3% GTE in drinking water reduced the average number of tumors per mouse from 4.1 ± 0.5 to 2.6 ± 0.4 and the percentage of PD-L1 positive cells from 9.6% to 2.9%, a decrease of 70%, in lung tumors of A/J mice given a single intraperitoneal injection of 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK). In co-culture experiments using F10-OVA melanoma cells and tumor-specific CD3+ T cells, EGCG reduced PD-L1 mRNA expression about 30% in F10-OVA cells and restored interleukin-2 mRNA expression in tumor-specific CD3+ T cells. The results show that green tea catechin is an immune checkpoint inhibitor. Full article
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Open AccessArticle Valorization of Olive Pomace-Based Nutraceuticals as Antioxidants in Chemical, Food, and Biological Models
Molecules 2018, 23(8), 2070; https://doi.org/10.3390/molecules23082070
Received: 28 July 2018 / Revised: 11 August 2018 / Accepted: 17 August 2018 / Published: 18 August 2018
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Abstract
Waste remaining after the production of olive oil (olive pomace) is known to contain significant amounts of phenolic compounds that exert different types of biological activities, primarily acting as antioxidants. In this work, a sustainable approach that combines ultrasound-assisted extraction with food-grade solvents
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Waste remaining after the production of olive oil (olive pomace) is known to contain significant amounts of phenolic compounds that exert different types of biological activities, primarily acting as antioxidants. In this work, a sustainable approach that combines ultrasound-assisted extraction with food-grade solvents and encapsulation with different types of cyclodextrins was used to prepare olive pomace-based polyphenol rich extracts that were tested as antioxidants in various chemical, food, and biological model systems. Encapsulation with cyclodextrins had a significant positive impact on the chemical composition of obtained extracts and it positively affected their antioxidant activity. Observed effects can be explained by an increased content of polyphenols in the formulations, specific physical properties of encapsulated compounds improving their antioxidant activity in complex food/physiological environment, and enhanced interaction with natural substrates. Depending on the applied model, the tested samples showed significant antioxidant protection in the concentration range 0.1–3%. Among the investigated cyclodextrins, hydroxypropyl-β-cyclodextrin and randomly methylated-β-cyclodextrin encapsulated extracts showed particularly good antioxidant activity and were especially potent in oil-in-water emulsion systems (1242 mg/g and 1422 mg/g of Trolox equivalents, respectively), showing significantly higher antioxidant activity than Trolox (reference antioxidant). In other models, they provided antioxidant protection comparable to commonly used synthetic antioxidants at concentration levels of 2–3%. Full article
(This article belongs to the Special Issue Nutraceuticals and Their Medicinal Importance)
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Open AccessArticle Antioxidant Activity as Biomarker of Honey Variety
Molecules 2018, 23(8), 2069; https://doi.org/10.3390/molecules23082069
Received: 24 July 2018 / Revised: 14 August 2018 / Accepted: 17 August 2018 / Published: 18 August 2018
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Abstract
Honey variety is commonly defined by beekeepers based on nectar flow availability and the only laboratory method to provide verification is the melissopalynological analysis. Therefore, a quick and simple method for accurate assessment of honey variety is still being researched. The aim of
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Honey variety is commonly defined by beekeepers based on nectar flow availability and the only laboratory method to provide verification is the melissopalynological analysis. Therefore, a quick and simple method for accurate assessment of honey variety is still being researched. The aim of the study was to evaluate the antioxidant activity of honey as an indicator of variety through the use of multivariate statistical analysis. Materials for the study consisted of 90 samples of varietal Polish honeys (rape-12, tilia-10, goldenrod-11, dandelion-5, buckwheat-6, multifloral-17, nectar-honeydew-8 and coniferous honeydew-16 and leafy honeydew-5) obtained directly from apiaries. Honeys were investigated in aspect of antioxidant capacity by photochemiluminescence (PCL) methods using standard ACW and ACL kits. As the reference FRAP and DPPH methods were used. The total phenolics content (TPC) was determined through the Folin-Ciocalteu method. The strongest antioxidant activity was found for buckwheat, while the weakest was found for rape honeys regardless of the used method. Results of the used methods were positively correlated (r = 0.42 to 0.94). Analysis conducted by PCL method confirmed that the minor fraction of honey antioxidants exhibits hydrophobic properties. Clear separation of honey varieties using PCA and Clustering method indicate that antioxidant activity can be a useful parameter for determining the botanical origin of honey. Full article
(This article belongs to the Special Issue Antioxidants Chemistry and Applications)
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Open AccessArticle Beneficial Effect of Herbal Formulation KM1608 on Inflammatory Bowl Diseases: A Preliminary Experimental Study
Molecules 2018, 23(8), 2068; https://doi.org/10.3390/molecules23082068
Received: 17 July 2018 / Revised: 3 August 2018 / Accepted: 14 August 2018 / Published: 17 August 2018
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Abstract
Aucklandia lappa DC., Terminalia chebula Retz and Zingiber officinale Roscoe have been traditionally used in east Asia to treat chronic diarrhea and abdominal pain. This study aimed to evaluated the anti-inflammatory activity of KM1608, which is composed of three natural herbs in a
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Aucklandia lappa DC., Terminalia chebula Retz and Zingiber officinale Roscoe have been traditionally used in east Asia to treat chronic diarrhea and abdominal pain. This study aimed to evaluated the anti-inflammatory activity of KM1608, which is composed of three natural herbs in a mouse model of dextran sodium sulfate (DSS)-induced ulcerative colitis. The anti-inflammatory activity and underlying mechanism were assessed in vitro using LPS-treated RAW264.7 cells. The in vivo effect of KM1608 on DSS-induced colitis was examined after oral administration in mice. KM1608 significantly inhibited the inflammatory mediators such as nitric oxide, interleukin (IL)-6, monocyte chemotactic protein 1 (MCP-1) and tumor necrosis factor (TNF)-α in LPS-treated RAW264.7 cells. The inhibitory effect of KM1608 was attributed to the reduction of Akt phosphorylation in the LPS-treated cells. In the mouse model, oral administration of KM1608 significantly improved DSS-induced colitis symptoms, such as disease activity index (DAI), colon length, and colon weight, as well as suppressed the expression of IL-6, TNF-α, and myeloperoxidase (MPO) in the DSS-induced colitis tissues. Taken together, KM1608 improved colitis through the regulation of inflammatory responses, suggesting that KM1608 has potential therapeutic use in the treatment of inflammatory diseases. Full article
(This article belongs to the Special Issue Anti-Inflammatory Activity of Natural Products)
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Open AccessArticle Synthesis, Spectroscopic Analysis and Assessment of the Biological Activity of New Hydrazine and Hydrazide Derivatives of 3-Formylchromone
Molecules 2018, 23(8), 2067; https://doi.org/10.3390/molecules23082067
Received: 11 July 2018 / Revised: 12 August 2018 / Accepted: 15 August 2018 / Published: 17 August 2018
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Abstract
The hydrazine and hydrazide derivatives of benzo-γ-pyrones with fluorine substituents remain an unexplored group of chemical compounds. This preliminary study reports the synthesis, structural assessment, initial microbiological screening and biological testing of the synthesized compounds on cell lines using the XTT-assay. A series
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The hydrazine and hydrazide derivatives of benzo-γ-pyrones with fluorine substituents remain an unexplored group of chemical compounds. This preliminary study reports the synthesis, structural assessment, initial microbiological screening and biological testing of the synthesized compounds on cell lines using the XTT-assay. A series of 10 novel hydrazine and hydrazide derivatives of 3-formylchromone were synthesized and their structures determined. Structural assessment consisted of elemental analysis, IR, 1H-NMR, 13C-NMR, MS and crystallographic studies. Antimicrobial activity was tested on standard strains representing different groups of microorganisms. The tested compounds were found to inhibit microbial growth. Concentrations of 0.01–1250 µmol/L were found to influence cell proliferation, demonstrating antiproliferative and stimulation of proliferation against two cell lines: the L929 cell line (mouse fibroblast cell line) and the EA.hy926 cell line (the human umbilical vein, somatic cell hybrid). Full article
(This article belongs to the Section Medicinal Chemistry)
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Open AccessArticle A Polyphenol Rich Extract from Solanum melongena L. DR2 Peel Exhibits Antioxidant Properties and Anti-Herpes Simplex Virus Type 1 Activity In Vitro
Molecules 2018, 23(8), 2066; https://doi.org/10.3390/molecules23082066
Received: 2 August 2018 / Revised: 13 August 2018 / Accepted: 14 August 2018 / Published: 17 August 2018
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Abstract
DR2B and DR2C extracts, obtained by ethanolic maceration of peel from commercially and physiologically ripe aubergine berries, were studied for the antioxidative cytoprotective properties and anti-HSV-1 activity, in line with the evidence that several antioxidants can impair viral replication by maintaining reducing conditions
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DR2B and DR2C extracts, obtained by ethanolic maceration of peel from commercially and physiologically ripe aubergine berries, were studied for the antioxidative cytoprotective properties and anti-HSV-1 activity, in line with the evidence that several antioxidants can impair viral replication by maintaining reducing conditions in host cells. The antioxidative cytoprotective effects against tBOOH-induced damage were assessed in Caco2 cells, while antiviral activity was studied in Vero cells; polyphenolic fingerprints were characterized by integrated phytochemical methods. Results highlighted different compositions of the extracts, with chlorogenic acid and delphinidin-3-rutinoside as the major constituents; other peculiar phytochemicals were also identified. Both samples reduced reactive oxygen species (ROS) production and exhibited scavenging and chelating properties. DR2C partly counteracted the tBOOH-induced cytotoxicity, with a remarkable lowering of lactate metabolism under both normoxia and hypoxia; interestingly, it increased intracellular GSH levels. Furthermore, DR2C inhibited the HSV-1 replication when added for 24 h after viral adsorption, as also confirmed by the reduction of many viral proteins’ expression. Since DR2C was able to reduce NOX4 expression during HSV-1 infection, its antiviral activity may be correlated to its antioxidant properties. Although further studies are needed to better characterize DR2C activity, the results suggest this extract as a promising new anti-HSV-1 agent. Full article
(This article belongs to the Special Issue Natural Active Agents Against Bacteria, Fungi and Parasites)
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Open AccessArticle Two Classes of Pigments, Carotenoids and C-Phycocyanin, in Spirulina Powder and Their Antioxidant Activities
Molecules 2018, 23(8), 2065; https://doi.org/10.3390/molecules23082065
Received: 24 July 2018 / Revised: 14 August 2018 / Accepted: 15 August 2018 / Published: 17 August 2018
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Abstract
Arthrospira platensis is the widely available source of spirulina that contains distinctive natural pigments, including carotenoids and C-phycocyanin (C-PC). In this study, the major carotenoid and C-PC contents were determined in seven commercially available spirulina powder products and laboratory-prepared A. platensis trichomes (AP-1)
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Arthrospira platensis is the widely available source of spirulina that contains distinctive natural pigments, including carotenoids and C-phycocyanin (C-PC). In this study, the major carotenoid and C-PC contents were determined in seven commercially available spirulina powder products and laboratory-prepared A. platensis trichomes (AP-1) by an LC-DAD method and UV-Visible spectrometry, respectively. The correlation of these two pigment content levels with Hunter color coordinates and antioxidant activity was also evaluated. The L* value failed to show a significant correlation with pigment content, but a positive correlation was observed between a* values and the contents of total carotenoid and C-PC. As b* values decreased, the chlorophyll a and C-PC contents increased. AP-1 exhibited the highest content of total carotenoids, chlorophyll a and C-PC, and antioxidant activities among the samples. This observation could be related to degradation of these pigments during the mass production process. The carotenoid profiles suggested that the commercial spirulina powders originated from two different sources, A. platensis and A. maxima. Total carotenoid and C-PC content exhibited positive significant correlations with antioxidant activities measured by 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) assays. These results provide a strong scientific foundation for the establishment of standards for the commercial distribution of quality spirulina products. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessReview Gelatin as a Photosensitive Material
Molecules 2018, 23(8), 2064; https://doi.org/10.3390/molecules23082064
Received: 20 June 2018 / Revised: 4 July 2018 / Accepted: 9 July 2018 / Published: 17 August 2018
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Abstract
Because this issue journal is dedicated to Gelatin, here we present a few applications of gelatin in the field of optics. Optics is the science that studies the production, propagation, interaction and detection of light. Various materials sensitive to light (photosensitive) are used
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Because this issue journal is dedicated to Gelatin, here we present a few applications of gelatin in the field of optics. Optics is the science that studies the production, propagation, interaction and detection of light. Various materials sensitive to light (photosensitive) are used for detection of light, such as photomultipliers, CCDs, crystals, two dimensional (2D) materials and more. Among the 2D materials, the most popular for several centuries has been gelatin based photographic emulsion, which records spatial distributions of light. More recently (1970), films made of Gelatin with Dichromate (DCG) and dyes have been used. We describe some characteristics and applications of these two photosensitive materials. We also describe examples where gelatin is used as a Relative Humidity (RH) sensor and in the fabrication of optical elements based on gelatin. This article is intended for researchers outside the optics community. Full article
(This article belongs to the Special Issue Gelatin: Chemistry, Characterization, Application)
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Open AccessArticle Effect of Volatile Organic Chemicals in Chrysanthemum indicum Linné on Blood Pressure and Electroencephalogram
Molecules 2018, 23(8), 2063; https://doi.org/10.3390/molecules23082063
Received: 8 August 2018 / Revised: 16 August 2018 / Accepted: 16 August 2018 / Published: 17 August 2018
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Abstract
This study identified the volatile organic compounds in the essential oils that are extracted from Chrysanthemum indicum Linné (C. indicum Linné) and investigated the effects of the inhalation of these compounds. We detected a total of 41 volatile organic compounds, including 32
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This study identified the volatile organic compounds in the essential oils that are extracted from Chrysanthemum indicum Linné (C. indicum Linné) and investigated the effects of the inhalation of these compounds. We detected a total of 41 volatile organic compounds, including 32 hydrocarbons, four acids, three alcohols, two ketones, and one aldehyde. In a sniffing test, seven types of volatile organic compounds were identified. Furthermore, the volatile organic compounds in C. indicum Linné that were identified were found to be derived from 1,8-cineole and camphor. After inhalation of the essential oils, the subjects’ systolic blood pressure and heart rate decreased. This indicates that inhalation of the essential oils extracted from C. indicum Linné provides mental and physical relaxation. We examined the changes in electroencephalogram findings that are observed after C. indicum Linné essential oil inhalation. An increase in theta and alpha waves, which usually appear during relaxation, as well as a decrease in beta and gamma waves, which appear during brain activity such as excessive attention, were noted. These results indicate that C. indicum Linné essential oil inhalation helps to reduce blood pressure and may provide mental and physical relaxation. Full article
(This article belongs to the Special Issue Natural Product Isolation, Identification and Biological Activity)
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Open AccessArticle UPLC-QTOF/MS-Based Metabolomics Applied for the Quality Evaluation of Four Processed Panax ginseng Products
Molecules 2018, 23(8), 2062; https://doi.org/10.3390/molecules23082062
Received: 17 July 2018 / Revised: 2 August 2018 / Accepted: 14 August 2018 / Published: 17 August 2018
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Abstract
In the food industry and herbal markets, it is critical to control the quality of processed Panax ginseng products. In this study, ultra-performance liquid chromatography coupled to quadrupole time of flight mass spectrometry (UPLC-QTOF/MS)-based metabolomics was applied for the quality evaluation of white
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In the food industry and herbal markets, it is critical to control the quality of processed Panax ginseng products. In this study, ultra-performance liquid chromatography coupled to quadrupole time of flight mass spectrometry (UPLC-QTOF/MS)-based metabolomics was applied for the quality evaluation of white ginseng (WG), tae-geuk ginseng (TG), red ginseng (RG), and black ginseng (BG). Diverse metabolites including ginsenosides were profiled by UPLC-QTOF/MS, and the datasets of WG, TG, RG, and BG were then subjected to multivariate analyses. In principal component analysis (PCA), four processed ginseng products were well-differentiated, and several ginsenosides were identified as major components of each product. S-plot also characterized the metabolic changes between two processed ginseng products, and the major ginsenosides of each product were found as follows: WG (M-Rb1, M-Rb2, M-Rc, Re, Rg1), TG (Rb2, Rc, Rd, Re, Rg1), RG (Rb1, Rb2, Rc, Rd, Re, Rg1), and BG (Rd, Rk1, Rg5, Rg3). Furthermore, the quantitative contents of ginsenosides were evaluated from the four processed ginseng products. Finally, it was indicated that the proposed metabolomics approach was useful for the quality evaluation and control of processed ginseng products. Full article
(This article belongs to the Special Issue Technology for Natural Products Research)
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Open AccessArticle Aromatic Thioacetal-Bridged ROS-Responsive Nanoparticles as Novel Gene Delivery Vehicles
Molecules 2018, 23(8), 2061; https://doi.org/10.3390/molecules23082061
Received: 16 July 2018 / Revised: 10 August 2018 / Accepted: 11 August 2018 / Published: 17 August 2018
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Abstract
In this report, a series of polycations are designed and synthesized by conjugating reactive oxygen species (ROS)-responsive thioacetal-linkers to low molecular weight (LMW) polyethylenimine (PEI) via ring-opening polymerization. Their structure–activity relationships (SARs) as gene delivery vectors are systematically studied. Although the MWs of
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In this report, a series of polycations are designed and synthesized by conjugating reactive oxygen species (ROS)-responsive thioacetal-linkers to low molecular weight (LMW) polyethylenimine (PEI) via ring-opening polymerization. Their structure–activity relationships (SARs) as gene delivery vectors are systematically studied. Although the MWs of the target polymers are only ~9 KDa, they show good DNA binding ability. The formed polyplexes, which are stable toward serum but decomposed under ROS-conditions, have appropriate sizes (180~300 nm) and positive zeta-potentials (+35~50 mV). In vitro experiments reveal that these materials have low cytotoxicity, and higher transfection efficiency (TE) than controls. Furthermore, the title polymers exhibit excellent serum tolerance. With the present of 10% serum, the TE of the polymers even increases up to 10 times higher than 25 KDa PEI and 9 times higher than Lipofectamine 2000. The SAR studies also reveal that electron-withdrawing groups on the aromatic ring in 4a may benefit to balance between the DNA condensation and release for efficient gene transfection. Full article
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Open AccessReview Turning Stem Cells Bad: Generation of Clinically Relevant Models of Human Acute Myeloid Leukemia through Gene Delivery- or Genome Editing-Based Approaches
Molecules 2018, 23(8), 2060; https://doi.org/10.3390/molecules23082060
Received: 16 July 2018 / Revised: 9 August 2018 / Accepted: 14 August 2018 / Published: 17 August 2018
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Abstract
Acute myeloid leukemia (AML), the most common acute leukemia in the adult, is believed to arise as a consequence of multiple molecular events that confer on primitive hematopoietic progenitors unlimited self-renewal potential and cause defective differentiation. A number of genetic aberrations, among which
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Acute myeloid leukemia (AML), the most common acute leukemia in the adult, is believed to arise as a consequence of multiple molecular events that confer on primitive hematopoietic progenitors unlimited self-renewal potential and cause defective differentiation. A number of genetic aberrations, among which a variety of gene fusions, have been implicated in the development of a transformed phenotype through the generation of dysfunctional molecules that disrupt key regulatory mechanisms controlling survival, proliferation, and differentiation in normal stem and progenitor cells. Such genetic aberrations can be recreated experimentally to a large extent, to render normal hematopoietic stem cells “bad”, analogous to the leukemic stem cells. Here, we wish to provide a brief outline of the complementary experimental approaches, largely based on gene delivery and more recently on gene editing, employed over the last two decades to gain insights into the molecular mechanisms underlying AML development and progression and on the prospects that their applications offer for the discovery and validation of innovative therapies. Full article
(This article belongs to the Special Issue Gene Delivery)
Open AccessArticle Antimicrobial Properties of Spent Hops Extracts, Flavonoids Isolated Therefrom, and Their Derivatives
Molecules 2018, 23(8), 2059; https://doi.org/10.3390/molecules23082059
Received: 17 July 2018 / Revised: 13 August 2018 / Accepted: 15 August 2018 / Published: 17 August 2018
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Abstract
Hop cones preparations possess a wide range of biological activities including antimicrobial properties. In this work, we evaluated the effect of various organic extracts obtained from spent hops, as well as six hops flavonoids and their twenty natural and synthetic derivatives on human
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Hop cones preparations possess a wide range of biological activities including antimicrobial properties. In this work, we evaluated the effect of various organic extracts obtained from spent hops, as well as six hops flavonoids and their twenty natural and synthetic derivatives on human and plant microbial pathogens. Methylene chloride, acetone, ethyl acetate, and methanol were used as extractants. Seven flavonoids, among them two natural (α,β-dihydroxanthohumol and 8-prenylnaringenin) showed significant activity against methicillin sensitive and resistant Staphylococcus aureus and Staphylococcus epidermidis strains with the lowest MIC80 value of 0.5 µg/mL. The crude ethyl acetate, acetone, and methanol extracts from the spent hops exhibited antifungal activity against Fusarium oxysporum, F. culmorum, and F. semitectum with the lowest MIC50 of 0.5 mg/mL, while the methylene chloride extract exerted antifungal activity against Botrytis cinerea with the MIC50 of 1 mg/mL. The preparation obtained after the removal of xanthohumol from the spent hops crude extracts retained up to 95% of activity. These findings suggest that various spent hops extracts may be effective agents for the control of plant pathogens of economic importance, like Botrytis cinerea and Fusarium oxysporum, while some compounds from spent hops or their derivatives may become useful for staphylococcal infections. Full article
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Open AccessArticle Aqueous-Methanol Extracts of Orange-Fleshed Sweet Potato (Ipomoea batatas) Ameliorate Oxidative Stress and Modulate Type 2 Diabetes Associated Genes in Insulin Resistant C2C12 Cells
Molecules 2018, 23(8), 2058; https://doi.org/10.3390/molecules23082058
Received: 17 June 2018 / Revised: 6 August 2018 / Accepted: 8 August 2018 / Published: 17 August 2018
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Abstract
Edible plants such as sweet potato are sources of natural antioxidants that can be exploited in the management and treatment of insulin resistance. This present study investigated the effects of the extracts of an orange-fleshed sweet potato on oxidative stress biomarkers (glutathione status
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Edible plants such as sweet potato are sources of natural antioxidants that can be exploited in the management and treatment of insulin resistance. This present study investigated the effects of the extracts of an orange-fleshed sweet potato on oxidative stress biomarkers (glutathione status and lipid peroxidation) and activities of antioxidant enzymes (catalase, CAT and glutathione peroxidase, GPx) in palmitate-induced insulin resistant C2C12 cells. The intracellular antioxidant status of the cells was also measured using Ferric reducing antioxidant power (FRAP) and Trolox equivalent antioxidant capacity (TEAC) assays. Furthermore, this study determined the effect of the extracts on the regulation of some type 2 diabetes associated genes; glucose transporter 4 (glut4), Nuclear respiratory factor 1 (nrf1), Myocyte enhanced factor 2A (mef2a), Carnitine palmitoyltransferase 1 (cpt1) and Acetyl-CoA carboxylase 2 (acc2). The results showed a significant (p < 0.05) increase in intracellular GSH level, a significant reduction in the level of malonaldehyde and a significant improvement in the intracellular antioxidant status upon treatment of the insulin resistant cells with the extracts. The extracts were also able to positively modulate the expression levels of the type 2 diabetes associated genes. On the other hand, HPLC-MS analysis of the extracts showed the presence of polyphenols which could have contributed to the bioactivity of the extracts through their antioxidant effects. Full article
(This article belongs to the Special Issue The Antioxidant Capacities of Natural Products)
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