Molecules

6 pages, 1593 KiB

Open AccessArticle

Sunflower-Like Nanostructure with Built-In Hotspots for Alpha-Fetoprotein Detection

by Xiaoyu Zhao, Aonan Zhu, Yaxin Wang, Yongjun Zhang and Xiaolong Zhang

Molecules 2021, 26(4), 1197; https://doi.org/10.3390/molecules26041197 - 23 Feb 2021

Cited by 8 | Viewed by 2460

In the present study, a sunflower-like nanostructure array composed of a series of synaptic nanoparticles and nanospheres was manufactured through an efficient and low-cost colloidal lithography technique. The primary electromagnetic field contribution generated by the synaptic nanoparticles of the surface array structures was [...] Read more.

In the present study, a sunflower-like nanostructure array composed of a series of synaptic nanoparticles and nanospheres was manufactured through an efficient and low-cost colloidal lithography technique. The primary electromagnetic field contribution generated by the synaptic nanoparticles of the surface array structures was also determined by a finite-difference time-domain software to simulate the hotspots. This structure exhibited high repeatability and excellent sensitivity; hence, it was used as a surface-enhanced Raman spectroscopy (SERS) active substrate to achieve a rapid detection of ultra-low concentrations of Alpha-fetoprotein (AFP). This study demonstrates the design of a plasmonic structure with strong electromagnetic coupling, which can be used for the rapid detection of AFP concentration in clinical medicine. Full article

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23 pages, 6774 KiB

Open AccessReview

Microwaves as “Co-Catalysts” or as Substitute for Catalysts in Organophosphorus Chemistry

by György Keglevich

Molecules 2021, 26(4), 1196; https://doi.org/10.3390/molecules26041196 - 23 Feb 2021

Cited by 7 | Viewed by 2834

Abstract

The purpose of this review is to summarize the importance of microwave (MW) irradiation as a kind of catalyst in organophosphorus chemistry. Slow or reluctant reactions, such as the Diels-Alder cycloaddition or an inverse-Wittig type reaction, may be performed efficiently under MW irradiation. [...] Read more.

The purpose of this review is to summarize the importance of microwave (MW) irradiation as a kind of catalyst in organophosphorus chemistry. Slow or reluctant reactions, such as the Diels-Alder cycloaddition or an inverse-Wittig type reaction, may be performed efficiently under MW irradiation. The direct esterification of phosphinic and phosphonic acids, which is practically impossible on conventional heating, may be realized under MW conditions. Ionic liquid additives may promote further esterifications. The opposite reaction, the hydrolysis of P-esters, has also relevance among the MW-assisted transformations. A typical case is when the catalysts are substituted by MWs, which is exemplified by the reduction of phosphine oxides, and by the Kabachnik–Fields condensation affording α-aminophosphonic derivatives. Finally, the Hirao P–C coupling reaction may serve as an example, when the catalyst may be simplified under MW conditions. All of the examples discussed fulfill the expectations of green chemistry. Full article

(This article belongs to the Special Issue Catalysts for a Green Chemistry: A Themed Issue Honoring Professor Roger Sheldon for His Contribution in the Field of the Green Chemistry with the Introduction of the E Factor)

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15 pages, 342 KiB

Open AccessFeature PaperReview

Versatile Use of Chitosan and Hyaluronan in Medicine

by Katarína Valachová and Ladislav Šoltés

Molecules 2021, 26(4), 1195; https://doi.org/10.3390/molecules26041195 - 23 Feb 2021

Cited by 29 | Viewed by 4865

Abstract

Chitosan is industrially acquired by the alkaline N-deacetylation of chitin. Chitin belongs to the β-N-acetyl-glucosamine polymers, providing structure, contrary to α-polymers, which provide food and energy. Another β-polymer providing structure is hyaluronan. A lot of studies have been performed on [...] Read more.

Chitosan is industrially acquired by the alkaline N-deacetylation of chitin. Chitin belongs to the β-N-acetyl-glucosamine polymers, providing structure, contrary to α-polymers, which provide food and energy. Another β-polymer providing structure is hyaluronan. A lot of studies have been performed on chitosan to explore its industrial use. Since chitosan is biodegradable, non-toxic, bacteriostatic, and fungistatic, it has numerous applications in medicine. Hyaluronan, one of the major structural components of the extracellular matrix in vertebrate tissues, is broadly exploited in medicine as well. This review summarizes the main areas where these two biopolymers have an impact. The reviewed areas mostly cover most medical applications, along with non-medical applications, such as cosmetics. Full article

(This article belongs to the Special Issue Chitin and Chitosan: Derivatives and Applications)

14 pages, 3105 KiB

Open AccessArticle

Chromatin Accessibility Is Associated with Artemisinin Biosynthesis Regulation in Artemisia annua

by Limeng Zhou, Yingzhang Huang, Qi Wang and Dianjing Guo

Molecules 2021, 26(4), 1194; https://doi.org/10.3390/molecules26041194 - 23 Feb 2021

Cited by 8 | Viewed by 3260

Abstract

Glandular trichome (GT) is the dominant site for artemisinin production in Artemisia annua. Several critical genes involved in artemisinin biosynthesis are specifically expressed in GT. However, the molecular mechanism of differential gene expression between GT and other tissue types remains elusive. Chromatin [...] Read more.

Glandular trichome (GT) is the dominant site for artemisinin production in Artemisia annua. Several critical genes involved in artemisinin biosynthesis are specifically expressed in GT. However, the molecular mechanism of differential gene expression between GT and other tissue types remains elusive. Chromatin accessibility, defined as the degree to which nuclear molecules are able to interact with chromatin DNA, reflects gene expression capacity to a certain extent. Here, we investigated and compared the landscape of chromatin accessibility in Artemisia annua leaf and GT using the Assay for Transposase-Accessible Chromatin using sequencing (ATAC-seq) technique. We identified 5413 GT high accessible and 4045 GT low accessible regions, and these GT high accessible regions may contribute to GT-specific biological functions. Several GT-specific artemisinin biosynthetic genes, such as DBR2 and CYP71AV1, showed higher accessible regions in GT compared to that in leaf, implying that they might be regulated by chromatin accessibility. In addition, transcription factor binding motifs for MYB, bZIP, C2H2, and AP2 were overrepresented in the highly accessible chromatin regions associated with artemisinin biosynthetic genes in glandular trichomes. Finally, we proposed a working model illustrating the chromatin accessibility dynamics in regulating artemisinin biosynthetic gene expression. This work provided new insights into epigenetic regulation of gene expression in GT. Full article

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17 pages, 1184 KiB

Open AccessArticle

Effect of Power Ultrasound Treatment on Free and Glycosidically-Bound Volatile Compounds and the Sensorial Profile of Red Wines

by Rodrigo Oliver Simancas, María Consuelo Díaz-Maroto, María Elena Alañón Pardo, Paula Pérez Porras, Ana Belén Bautista-Ortín, Encarna Gómez-Plaza and María Soledad Pérez-Coello

Molecules 2021, 26(4), 1193; https://doi.org/10.3390/molecules26041193 - 23 Feb 2021

Cited by 26 | Viewed by 3159

Abstract

This study presents the effect of the application of high-power ultrasound to crushed grapes, at a winery-scale, on the content of varietal volatile compounds (free and glycosidically-bound) in musts and on the overall aroma of wines. Two different frequencies (20 kHz and 28 [...] Read more.

This study presents the effect of the application of high-power ultrasound to crushed grapes, at a winery-scale, on the content of varietal volatile compounds (free and glycosidically-bound) in musts and on the overall aroma of wines. Two different frequencies (20 kHz and 28 kHz) were tested and the combination of grape sonication and different maceration times on wine aroma was also evaluated. The volatile compounds were isolated by solid phase extraction and analyzed by gas chromatography-mass spectrometry, carrying out a sensory evaluation of wines by quantitative descriptive analysis. Sonication produced an increase in the concentration of free varietal compounds such as C₆ alcohols, terpenes and norisoprenoids in musts and also in wines made by 48 h of skin maceration, being less efficient in the extraction of the bound fraction. Fermentation compounds were also positively affected by ultrasound treatment, although this effect was variable depending on the frequency used, the maceration time and the type of compound. All the wines made from sonicated grapes had better scores in the evaluated olfactory attributes with respect to the control wines. Our results indicate that sonication could produce an increase in the content of some volatile compounds of sensory relevance, obtaining wines with an aroma quality similar or higher than those elaborated with longer maceration times. Full article

(This article belongs to the Special Issue 25th Anniversary of Molecules—Recent Advances in Flavours and Fragrances in Foods)

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13 pages, 13504 KiB

Open AccessArticle

Induction of Low Temperature Tolerance in Wheat by Pre-Soaking and Parental Treatment with Melatonin

by Hua Zhang, Lei Liu, Zongshuai Wang, Guozhong Feng, Qiang Gao and Xiangnan Li

Molecules 2021, 26(4), 1192; https://doi.org/10.3390/molecules26041192 - 23 Feb 2021

Cited by 30 | Viewed by 3003

Abstract

Low temperatures seriously depress germination and seedling establishment in wheat and it is of great significance to explore approaches to improve wheat tolerance to low temperatures. In this study, the effects of seed pre-soaking and parental treatment with melatonin on seed germination and [...] Read more.

Low temperatures seriously depress germination and seedling establishment in wheat and it is of great significance to explore approaches to improve wheat tolerance to low temperatures. In this study, the effects of seed pre-soaking and parental treatment with melatonin on seed germination and low temperature tolerance during the early growing stage in wheat were studied. The results showed that pre-soaking with melatonin increased the germination rate, improved antioxidant capacity and accelerated starch degradation under low temperature, which alleviated low temperature-induced damage to the chloroplasts in coleoptiles of wheat seedlings. Parental melatonin treatment during grain filling stage significantly decreased the grain weight. Seeds from parental melatonin-treated plants showed higher germination rates and higher antioxidant enzyme activity than the control seeds under low temperature. In addition, parental treatment with melatonin modulated the activities of carbohydrate metabolism enzymes, which contributes to enhanced low temperature tolerance in wheat offspring. It was suggested that both seed pre-soaking and parental treatment with melatonin could be the effective approaches for low temperature tolerance induction in wheat. Full article

(This article belongs to the Special Issue Melatonin as an Antioxidant and a Functionally Pleiotropic Molecule: Synthesis, Metabolism and Activities in Organisms II)

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18 pages, 1243 KiB

Open AccessFeature PaperReview

Therapeutic Intervention of COVID-19 by Natural Products: A Population-Specific Survey Directed Approach

by Christian R. Gomez, Ingrid Espinoza, Fazlay S. Faruque, Md. Mahbub Hasan, Khondaker Miraz Rahman, Larry A. Walker and Ilias Muhammad

Molecules 2021, 26(4), 1191; https://doi.org/10.3390/molecules26041191 - 23 Feb 2021

Cited by 6 | Viewed by 4451

Abstract

To date very few promising leads from natural products (NP) secondary metabolites with antiviral and immunomodulatory properties have been identified for promising/potential intervention for COVID-19. Using in-silico docking studies and genome based various molecular targets, and their in vitro anti-SARS CoV-2 activities against [...] Read more.

To date very few promising leads from natural products (NP) secondary metabolites with antiviral and immunomodulatory properties have been identified for promising/potential intervention for COVID-19. Using in-silico docking studies and genome based various molecular targets, and their in vitro anti-SARS CoV-2 activities against whole cell and/or selected protein targets, we select a few compounds of interest, which can be used as potential leads to counteract effects of uncontrolled innate immune responses, in particular those related to the cytokine storm. A critical factor for prevention and treatment of SARS-CoV-2 infection relates to factors independent of viral infection or host response. They include population-related variables such as concurrent comorbidities and genetic factors critically relevant to COVID-19 health disparities. We discuss population risk factors related to SARS-CoV-2. In addition, we focus on virulence related to glucose-6-phosphate dehydrogenase deficiency (G6PDd), the most common human enzymopathy. Review of data on the response of individuals and communities with high prevalence of G6PDd to NP, prompts us to propose the rationale for a population-specific management approach to rationalize design of therapeutic interventions of SARS-CoV-2 infection, based on use of NP. This strategy may lead to personalized approaches and improve disease-related outcomes. Full article

(This article belongs to the Special Issue Natural Products Chemists: Leaving Our Lab in Covid-19 Emergency)

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21 pages, 40551 KiB

Open AccessArticle

Slow Relaxation of the Magnetization in Anilato-Based Dy(III) 2D Lattices

by Samia Benmansour, Antonio Hernández-Paredes, María Bayona-Andrés and Carlos J. Gómez-García

Molecules 2021, 26(4), 1190; https://doi.org/10.3390/molecules26041190 - 23 Feb 2021

Cited by 13 | Viewed by 2779

Abstract

The search for two- and three-dimensional materials with slow relaxation of the magnetization (single-ion magnets, SIM and single-molecule magnets, SMM) has become a very active area in recent years. Here we show how it is possible to prepare two-dimensional SIMs by combining Dy(III) [...] Read more.

The search for two- and three-dimensional materials with slow relaxation of the magnetization (single-ion magnets, SIM and single-molecule magnets, SMM) has become a very active area in recent years. Here we show how it is possible to prepare two-dimensional SIMs by combining Dy(III) with two different anilato-type ligands (dianions of the 3,6-disubstituted-2,5-dihydroxy-1,4-benzoquinone: C₆O₄X₂²⁻, with X = H and Cl) in dimethyl sulfoxide (dmso). The two compounds prepared, formulated as: [Dy₂(C₆O₄H₂)₃(dmso)₂(H₂O)₂]·2dmso·18H₂O (1) and [Dy₂(C₆O₄Cl₂)₃(dmso)₄]·2dmso·2H₂O (2) show distorted hexagonal honeycomb layers with the solvent molecules (dmso and H₂O) located in the interlayer space and in the hexagonal channels that run perpendicular to the layers. The magnetic measurements of compounds 1, 2 and [Dy₂(C₆O₄(CN)Cl)₃(dmso)₆] (3), a recently reported related compound, show that the three compounds present slow relaxation of the magnetization. In compound 1 the SIM behaviour does not need the application of a DC field whereas 2 and 3 are field-induced SIM (FI-SIM) since they show slow relaxation of the magnetization when a DC field is applied. We discuss the differences observed in the crystal structures and magnetic properties based on the X group of the anilato ligands (H, Cl and Cl/CN) in 1–3 and in the recently reported derivative [Dy₂(C₆O₄Br₂)₃(dmso)₄]·2dmso·2H₂O (4) with X = Br, that is also a FI-SIM. Full article

(This article belongs to the Special Issue Recent Advances in Modern Inorganic Chemistry)

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2 pages, 173 KiB

Open AccessEditorial

Natural and Artificial Photoprotective Agents

by Diego Sampedro

Molecules 2021, 26(4), 1189; https://doi.org/10.3390/molecules26041189 - 23 Feb 2021

Viewed by 1828

Abstract

Sunlight has a long list of positive effects on living beings [...] Full article

(This article belongs to the Special Issue Natural and Artificial Photoprotective Agent)

19 pages, 8283 KiB

Open AccessArticle

Combined Therapy of A₁AR Agonists and A_2AAR Antagonists in Neuroinflammation

by Gabriella Marucci, Diego Dal Ben, Catia Lambertucci, Aleix Martí Navia, Andrea Spinaci, Rosaria Volpini and Michela Buccioni

Molecules 2021, 26(4), 1188; https://doi.org/10.3390/molecules26041188 - 23 Feb 2021

Cited by 13 | Viewed by 3133

Abstract

Alzheimer’s, Parkinson’s, and multiple sclerosis are neurodegenerative diseases related by neuronal degeneration and death in specific areas of the central nervous system. These pathologies are associated with neuroinflammation, which is involved in disease progression, and halting this process represents a potential therapeutic strategy. [...] Read more.

Alzheimer’s, Parkinson’s, and multiple sclerosis are neurodegenerative diseases related by neuronal degeneration and death in specific areas of the central nervous system. These pathologies are associated with neuroinflammation, which is involved in disease progression, and halting this process represents a potential therapeutic strategy. Evidence suggests that microglia function is regulated by A₁ and A_2A adenosine receptors (AR), which are considered as neuroprotective and neurodegenerative receptors, respectively. The manuscript’s aim is to elucidate the role of these receptors in neuroinflammation modulation through potent and selective A₁AR agonists (N⁶-cyclopentyl-2′- or 3′-deoxyadenosine substituted or unsubstituted in 2 position) and A_2AAR antagonists (9-ethyl-adenine substituted in 8 and/or in 2 position), synthesized in house, using N13 microglial cells. In addition, the combined therapy of A₁AR agonists and A_2AAR antagonists to modulate neuroinflammation was evaluated. Results showed that A₁AR agonists were able, to varying degrees, to prevent the inflammatory effect induced by cytokine cocktail (tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and interferon (IFN)-γ), while A_2AAR antagonists showed a good ability to counteract neuroinflammation. Moreover, the effect achieved by combining the two most effective compounds (1 and 6) in doses previously found to be non-effective was greater than the treatment effect of each of the two compounds used separately at maximal dose. Full article

(This article belongs to the Special Issue Synthesis and Identification of Small Compounds Active in Neurodegeneration)

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15 pages, 1013 KiB

Open AccessArticle

Impact of In Vitro Gastrointestinal Digestion on the Bioaccessibility of Phytochemical Compounds from Eight Fruit Juices

by Dasha Mihaylova, Ivelina Desseva, Magdalena Stoyanova, Nadezhda Petkova, Margarita Terzyiska and Anna Lante

Molecules 2021, 26(4), 1187; https://doi.org/10.3390/molecules26041187 - 23 Feb 2021

Cited by 33 | Viewed by 6317

Abstract

Fruits contain a number of useful substances including antioxidants. Their bio-accessibility after passing through the digestive tract is of primary importance when considering their benefits. In this respect, we investigated the effect of in vitro digestion on the phytochemicals of eight fruit juices. [...] Read more.

Fruits contain a number of useful substances including antioxidants. Their bio-accessibility after passing through the digestive tract is of primary importance when considering their benefits. In this respect, we investigated the effect of in vitro digestion on the phytochemicals of eight fruit juices. Freshly prepared juices from pomegranate, orange and grapefruit were used as well as commercially available juices from cherry, black grapes and aloe vera, blackberry and chokeberry, and two types of chokeberry and raspberries. Spectrophotometric and HPLC methods were used in order to analyse the sugar content, the total phenolic (TPC) and flavonoid contents (TFC), anthocyanins, phenolic acids and antioxidant activity. Principle component analysis was used to explain the differentiation among the types of fruit juice. Sugar recovery variation was between 4–41%. The bio-accessibility of TPC ranged from 13.52–26.49% and of flavonoids between 24.25–67.00%. The pomegranate juice and the juice of black grapes and aloe vera kept 58.12 and 50.36% of their initial anthocyanins content, while for the other samples less than 1.10% was established. As a result, a maximum of 30% remaining antioxidant activity was measured for some of the samples, but for most this was less than 10%. In conclusion, fruit juices are a rich source of biologically active substances, but a more detailed analysis of food transformation during digestion is needed. Full article

(This article belongs to the Special Issue Bioactive Compounds and Antioxidant Activity of Extracts from Different Natural Plants)

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16 pages, 2731 KiB

Open AccessArticle

Constructing an Efficient Bacillus subtilis Spore Display by Using Cohesin−Dockerin Interactions

by He Wang, Xiaomin Jiang, Yongchang Qian and Lianghong Yin

Molecules 2021, 26(4), 1186; https://doi.org/10.3390/molecules26041186 - 23 Feb 2021

Cited by 7 | Viewed by 2938

Abstract

Bacillus subtilis spore display has become a field of increasing interest in the past two decades. To improve the efficiency of B. subtilis spore display, its directed modification was performed based on the cellulosome architecture by introducing onto them divergent cohesin (Coh) modules [...] Read more.

Bacillus subtilis spore display has become a field of increasing interest in the past two decades. To improve the efficiency of B. subtilis spore display, its directed modification was performed based on the cellulosome architecture by introducing onto them divergent cohesin (Coh) modules that can specifically bind to the target enzyme bearing the matching dockerins (Doc). In this study, five different pairs of cohesins and dockerins, selected from four cellulolytic microbes, were examined for their capabilities in displaying a tetrameric enzyme β-galactosidase from Bacillus stearothermophilus IAM11001 on the surface of B. subtilis WB600 spores. Immunofluorescence microscopy, western blotting, dot blotting, and enzyme assay was applied to confirm its surface expression. All the resultant five Coh–Doc based spore display can hydrolyze o-nitrophenyl-β-D-galactopyranoside. Further, the optimized Coh–Doc based spore display exhibited the highest display efficiency. Overall, the results of current study may open new perspectives on the use of Coh–Doc interaction, which will find application in improving the efficiency of B. subtilis spore display. Full article

(This article belongs to the Special Issue Enzyme Immobilization Ⅳ)

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4 pages, 206 KiB

Open AccessEditorial

Algae and Microalgae and Their Bioactive Molecules for Human Health

by Benoît Chénais

Molecules 2021, 26(4), 1185; https://doi.org/10.3390/molecules26041185 - 23 Feb 2021

Cited by 11 | Viewed by 3366

Abstract

The algae and microalgae are an extremely diverse group of organisms that contain many bioactive molecules, including pigments, polyunsaturated fatty acids, polysaccharides, polyphenol, etc [...] Full article

(This article belongs to the Special Issue Algae and Microalgae and Their Bioactive Molecules for Human Health)

16 pages, 1601 KiB

Open AccessArticle

Nutritional Value and Biological Activity of Gluten-Free Bread Enriched with Cricket Powder

by Przemysław Łukasz Kowalczewski, Małgorzata Gumienna, Iga Rybicka, Barbara Górna, Paulina Sarbak, Krzysztof Dziedzic and Dominik Kmiecik

Molecules 2021, 26(4), 1184; https://doi.org/10.3390/molecules26041184 - 23 Feb 2021

Cited by 46 | Viewed by 5521

Abstract

Cricket powder, described in the literature as a source of nutrients, can be a valuable ingredient to supplement deficiencies in various food products. Work continues on the implementation of cricket powder in products that are widely consumed. The aim of this study was [...] Read more.

Cricket powder, described in the literature as a source of nutrients, can be a valuable ingredient to supplement deficiencies in various food products. Work continues on the implementation of cricket powder in products that are widely consumed. The aim of this study was to obtain gluten-free bread with a superior nutritional profile by means of insect powder addition. Gluten-free breads enriched with 2%, 6%, and 10% of cricket (Acheta domesticus) powder were formulated and extensively characterized. The nutritional value, as well as antioxidant and β-glucuronidase activities, were assessed after simulated in vitro digestion. Addition of cricket powder significantly increased the nutritional value, both in terms of the protein content (exceeding two-, four-, and seven-fold the reference bread (RB), respectively) and above all mineral compounds. The most significant changes were observed for Cu, P, and Zn. A significant increase in the content of polyphenolic compounds and antioxidant activity in the enriched bread was also demonstrated; moreover, both values additionally increased after the digestion process. The total polyphenolic compounds content increased about five-fold from RB to bread with 10% CP (BCP10), and respectively about three-fold after digestion. Similarly, the total antioxidant capacity before digestion increased about four-fold, and after digestion about six-fold. The use of CP also reduced the undesirable activity of β-glucuronidase by 65.9% (RB vs. BCP10) in the small intestine, down to 78.9% in the large intestine. The influence of bread on the intestinal microflora was also evaluated, and no inhibitory effect on the growth of microflora was demonstrated, both beneficial (Bifidobacterium and Lactobacillus) and pathogenic (Enterococcus and Escherichia coli). Our results underscore the benefits of using cricket powder to increase the nutritional value and biological activity of gluten-free food products. Full article

(This article belongs to the Special Issue Emerging Protein Sources for Food Production and Human Nutrition)

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10 pages, 1621 KiB

Open AccessArticle

5-ALA Attenuates the Palmitic Acid-Induced ER Stress and Apoptosis in Bovine Mammary Epithelial Cells

by Mst Mamuna Sharmin, Md Aminul Islam, Itsuki Yamamoto, Shin Taniguchi and Shinichi Yonekura

Molecules 2021, 26(4), 1183; https://doi.org/10.3390/molecules26041183 - 23 Feb 2021

Cited by 6 | Viewed by 2719

Abstract

The conservation of mammary gland physiology by maintaining the maximum number of mammary epithelial cells (MECs) is of the utmost importance for the optimum amount of milk production. In a state of negative energy balance, palmitic acid (PA) reduces the number of bovine [...] Read more.

The conservation of mammary gland physiology by maintaining the maximum number of mammary epithelial cells (MECs) is of the utmost importance for the optimum amount of milk production. In a state of negative energy balance, palmitic acid (PA) reduces the number of bovine MECs. However, there is no effective strategy against PA-induced apoptosis of MECs. In the present study, 5-aminolevulinic acid (5-ALA) was established as a remedial agent against PA-induced apoptosis of MAC-T cells (an established line of bovine MECs). In PA-treated cells, the apoptosis-related genes BCL2 and BAX were down- and upregulated, respectively. The elevated expression of major genes of the unfolded protein response (UPR), such as CHOP, a proapoptotic marker (C/EBP homologous protein), reduced the viability of PA-treated MAC-T cells. In contrast, 5-ALA pretreatment increased and decreased BCL2 and BAX expression, respectively. Moreover, cleaved caspase-3 protein expression was significantly reduced in the 5-ALA-pretreated group in comparison with the PA group. The downregulation of major UPR-related genes, including CHOP, extended the viability of MAC-T cells pretreated with 5-ALA and also reduced the enhanced intensity of the PA-induced expression of phospho-protein kinase R-like ER kinase. Moreover, the enhanced expression of HO-1 (antioxidant gene heme oxygenase) by 5-ALA reduced PA-induced oxidative stress (OxS). HO-1 is not only protective against OxS but also effective against ER stress. Collectively, these findings offer new insights into the protective effects of 5-ALA against PA-induced apoptosis of bovine MECs. Full article

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13 pages, 8365 KiB

Open AccessArticle

Evaluation of the Antioxidant Capacities of Antarctic Macroalgae and Their Use for Nanoparticles Production

by N. González-Ballesteros, M. C. Rodríguez-Argüelles and M. Lastra-Valdor

Molecules 2021, 26(4), 1182; https://doi.org/10.3390/molecules26041182 - 23 Feb 2021

Cited by 12 | Viewed by 2613

Abstract

Macroalgae are sources of bioactive compounds that are interesting from both a chemical and a medical point of view. Although their use in biomedicine has increased significantly in recent years, tests conducted to date have been mostly related to species from temperate latitudes, [...] Read more.

Macroalgae are sources of bioactive compounds that are interesting from both a chemical and a medical point of view. Although their use in biomedicine has increased significantly in recent years, tests conducted to date have been mostly related to species from temperate latitudes, with the potential application of Antarctic biodiversity being minor. The wide variety of algae species present on Antarctic coastal areas can be a source of new antioxidants. Bearing this in mind, the brown macroalgae Desmarestia antarctica (DA) and the red Iridaea cordata (IC) were selected for the preparation of aqueous extracts with the aim of analyzing their antioxidant activity. This analysis was performed by determining reducing power, total phenolic content, and 2,2-diphenyl-1-picrylhydrazyl free radical scavenging activity. Furthermore, both extracts were employed to synthesize gold and silver nanoparticles. The nanomaterials were fully characterized by means of UV-Visible spectroscopy, transmission electron microscopy, Z potential measurements, and Fourier transform infrared spectroscopy, which confirmed the formation of stable, spherical nanoparticles with mean diameters of 13.7 ± 3.1 and 17.5 ± 3.7 nm for Ag@DA and Ag@IC and 12.6 ± 1.9 and 12.3 ± 1.6 nm for Au@DA and Au@IC. Antioxidant assays were performed after the synthesis of the nanomaterials to evaluate their possible synergistic effect with the extracts. The results suggest that polysaccharides and proteins may play a key role in the process of reduction and stabilization. Finally, for the sake of comparison, the results obtained for the Antarctic macroalgae Desmarestia menziesii and Palmaria decipiens have also been considered in the present work. Full article

(This article belongs to the Special Issue Gold Coordination Chemistry and Applications)

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13 pages, 3685 KiB

Open AccessArticle

Metabolite Differences of Polyphenols in Different Litchi Cultivars (Litchi chinensis Sonn.) Based on Extensive Targeted Metabonomics

by Nonghui Jiang, Huili Zhu, Wei Liu, Chao Fan, Feng Jin and Xu Xiang

Molecules 2021, 26(4), 1181; https://doi.org/10.3390/molecules26041181 - 23 Feb 2021

Cited by 23 | Viewed by 3545

Abstract

Litchi is an important fruit cultivated in tropical and subtropical areas with high nutritious and delicious flavor and the pulp is the main part of the fruit consumed. Previous studies found that litchi had high total phenol content and antioxidant activity, but most [...] Read more.

Litchi is an important fruit cultivated in tropical and subtropical areas with high nutritious and delicious flavor and the pulp is the main part of the fruit consumed. Previous studies found that litchi had high total phenol content and antioxidant activity, but most of them focused on the identification of single or a few phenolic components with a low throughput test, and the metabolic differences of cultivars are still unknown to a some extent. In this study we used widely targeted metabolome based on ultra-performance liquid chromatography coupled with mass spectrometry (UPLC-MS/MS) to analyze the polyphenol metabolites of five different genotypes of mature litchi fruit. A total of 126 polyphenol metabolites in eight categories were identified to reveal the composition and differences of polyphenol; 15 common differential metabolites and 20 specific differential metabolites to each cultivar were found for the first time. The results infer that flavonoids, flavonols, hydroxycinnamoyls and catechins are the main polyphenol metabolites of litchi pulp. Cluster analysis showed that there were three groups of polyphenols from high to low; early maturing Feizhixiao is a kind of high polyphenol content cultivars, especially in catechins, anthocyanins, flavonols, quinic acids and hydroxycinnamoyls. The polyphenols in the flesh of mature litchi are rich, and there are significant differences among cultivars; there was a level of correlation between the contents of phenolics and the maturity of litchi cultivars; the content of phenolics in early maturing litchi cultivars appeared higher than those of mid- to late-maturing cultivars. This experiment will provide significant reference information for cultivation, breeding, processing and consumption. Full article

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16 pages, 12186 KiB

Open AccessArticle

Chemical Fingerprinting of Cryptic Species and Genetic Lineages of Aneura pinguis (L.) Dumort. (Marchantiophyta, Metzgeriidae)

by Rafał Wawrzyniak, Wiesław Wasiak, Beata Jasiewicz, Alina Bączkiewicz and Katarzyna Buczkowska

Molecules 2021, 26(4), 1180; https://doi.org/10.3390/molecules26041180 - 22 Feb 2021

Cited by 4 | Viewed by 2191

Abstract

Aneura pinguis (L.) Dumort. is a representative of the simple thalloid liverworts, one of the three main types of liverwort gametophytes. According to classical taxonomy, A. pinguis represents one morphologically variable species; however, genetic data reveal that this species is a complex consisting [...] Read more.

Aneura pinguis (L.) Dumort. is a representative of the simple thalloid liverworts, one of the three main types of liverwort gametophytes. According to classical taxonomy, A. pinguis represents one morphologically variable species; however, genetic data reveal that this species is a complex consisting of 10 cryptic species (named by letters from A to J), of which four are further subdivided into two or three evolutionary lineages. The objective of this work was to develop an efficient method for the characterisation of plant material using marker compounds. The volatile chemical constituents of cryptic species within the liverwort A. pinguis were analysed by GC-MS. The compounds were isolated from plant material using the HS-SPME technique. Of the 66 compounds examined, 40 were identified. Of these 40 compounds, nine were selected for use as marker compounds of individual cryptic species of A. pinguis. A guide was then developed that clarified how these markers could be used for the rapid identification of the genetic lineages of A. pinguis. Multivariate statistical analyses (principal component and cluster analysis) revealed that the chemical compounds in A. pinguis made it possible to distinguish individual cryptic species (including genetic lineages), with the exception of cryptic species G and H. The classification of samples based on the volatile compounds by cluster analysis reflected phylogenetic relationships between cryptic species and genetic lineages of A. pinguis revealed based on molecular data. Full article

(This article belongs to the Collection Essential Oils)

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13 pages, 2630 KiB

Open AccessArticle

Quantification and Metabolite Identification of Sulfasalazine in Mouse Brain and Plasma Using Quadrupole-Time-of-Flight Mass Spectrometry

by Jangmi Choi, Min-Ho Park, Seok-Ho Shin, Jin-Ju Byeon, Byeong ill Lee, Yuri Park and Young G. Shin

Molecules 2021, 26(4), 1179; https://doi.org/10.3390/molecules26041179 - 22 Feb 2021

Cited by 3 | Viewed by 3662

Abstract

Sulfasalazine (SAS), an anti-inflammatory drug with potent cysteine/glutamate antiporter system xc-(SXC) inhibition has recently shown beneficial effects in brain-related diseases. Despite many reports related to central nervous system (CNS) effect of SAS, pharmacokinetics (PK) and metabolite identification studies in the brain for SAS [...] Read more.

Sulfasalazine (SAS), an anti-inflammatory drug with potent cysteine/glutamate antiporter system xc-(SXC) inhibition has recently shown beneficial effects in brain-related diseases. Despite many reports related to central nervous system (CNS) effect of SAS, pharmacokinetics (PK) and metabolite identification studies in the brain for SAS were quite limited. The aim of this study was to investigate the pharmacokinetics and metabolite identification of SAS and their distributions in mouse brain. Using in vivo brain exposure studies (neuro PK), the PK parameters of SAS was calculated for plasma as well as brain following intravenous and oral administration at 10 mg/kg and 50 mg/kg in mouse, respectively. In addition, in vivo metabolite identification (MetID) studies of SAS in plasma and brain were also conducted. The concentration of SAS in brain was much lower than that in plasma and only 1.26% of SAS was detected in mouse brain when compared to the SAS concentration in plasma (brain to plasma ratio (%): 1.26). In the MetID study, sulfapyridine (SP), hydroxy-sulfapyridine (SP-OH), and N-acetyl sulfapyridine (Ac-SP) were identified in plasma, whereas only SP and Ac-SP were identified as significant metabolites in brain. As a conclusion, our results suggest that the metabolites of SAS such as SP and Ac-SP might be responsible for the pharmacological effect in brain, not the SAS itself. Full article

(This article belongs to the Special Issue Analytical Techniques in Pharmaceutical and Biomedical Analysis)

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17 pages, 4153 KiB

Open AccessArticle

Enhancing the Potentiality of Trichoderma harzianum against Pythium Pathogen of Beans Using Chamomile (Matricaria chamomilla, L.) Flower Extract

by Abeer Abdulkhalek Ghoniem, Kamar M. Abd El-Hai, Ayman Y. El-khateeb, Noha M. Eldadamony, Samy F. Mahmoud and Ashraf Elsayed

Molecules 2021, 26(4), 1178; https://doi.org/10.3390/molecules26041178 - 22 Feb 2021

Cited by 18 | Viewed by 3266

Abstract

Our present study was designed to investigate the role of both Trichoderma harzianum and chamomile (Matricaria chamomilla L.) flower extract in mutual reaction against growth of Pythium ultimum. In vitro, the activity of chamomile extract was found to reduce the radial [...] Read more.

Our present study was designed to investigate the role of both Trichoderma harzianum and chamomile (Matricaria chamomilla L.) flower extract in mutual reaction against growth of Pythium ultimum. In vitro, the activity of chamomile extract was found to reduce the radial growth of Pythium ultimum up to 30% compared to the control. Whereas, the radial growth reduction effect of T. harzianum against P. ultimum reached 81.6% after 120 h. Data also showed the productivity of total phenolics and total flavonoids by T. harzianum, was 12.18 and 6.33 mg QE/100 mL culture filtrate, respectively. However, these compounds were determined in chamomile flower extract at concentrations of 75.33 and 24.29 mg QE/100 mL, respectively. The fractionation of aqueous extract of chamomile flower using HPLC provided several polyphenolic compounds such as pyrogallol, myricetin, rosemarinic acid, catechol, p-coumaric acid, benzoic acid, chlorogenic acid and other minor compounds. In vivo, the potentiality of T. harzianum with chamomile flower extract against Pythium pathogen of bean was investigated. Data obtained showed a reduction in the percentage of rotted seed and infected seedling up to 28 and 8%, respectively. Whereas, the survival increased up to 64% compared to other ones. There was also a significant promotion in growth features, total chlorophyll, carotenoids, total polyphenols and flavonoids, polyphenol-oxidase and peroxidase enzymes compared to other ones. To the best of our knowledge, there are no reported studies that included the mutual association of fungus, T. harzianum with the extract taken from the chamomile flower against P. ultimum, either in vitro or in vivo. In conclusion, the application of both T. harzianum and/or M. chamomilla extracts in the control of bean Pythium pathogen showed significant results. Full article

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11 pages, 1126 KiB

Open AccessArticle

Simultaneous Quantification of 3′- and 6′-Sialyllactose in Rat Plasma Using Liquid Chromatography-Tandem Mass Spectrometry and Its Application to a Pharmacokinetic Study

by Seok-In Jang, Han Young Eom, Jeong Ho Hwang, Lila Kim and Jong-Hwa Lee

Molecules 2021, 26(4), 1177; https://doi.org/10.3390/molecules26041177 - 22 Feb 2021

Cited by 4 | Viewed by 2419

Abstract

Sialyllactose (SL), an acidic oligosaccharide, has immune-protective effects against pathogens and helps with the development of the immune system and intestinal microorganisms. To elucidate the pharmacokinetic characterization after oral administration to rats, the simultaneous quantification method for 3′-SL and 6′-SL in rat plasma [...] Read more.

Sialyllactose (SL), an acidic oligosaccharide, has immune-protective effects against pathogens and helps with the development of the immune system and intestinal microorganisms. To elucidate the pharmacokinetic characterization after oral administration to rats, the simultaneous quantification method for 3′-SL and 6′-SL in rat plasma was validated, using liquid chromatography-tandem mass spectrometry (LC-MS/MS) in an electrospray ionization (ESI) mode. Several types of columns [C18, amide, and hydrophilic interaction liquid chromatography (HILIC) phase] were used to separate the peaks of 3′-SL and 6′-SL, which improved chromatographic selectivity. Ultimately, the HILIC phase column had a good peak shape and quick resolution, with a mobile phase comprising ammonium acetate buffer and acetonitrile obtained by gradient elution. In addition, the simultaneous quantification of 3′-SL and 6′-SL in rat plasma samples were adequately applied to pharmacokinetic study. Full article

(This article belongs to the Special Issue Bioanalysis and Biological Matrix Sampling)

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13 pages, 1073 KiB

Open AccessArticle

Validation of a Rapid Multiresidue Method for the Determination of Pesticide Residues in Vine Leaves. Comparison of the Results According to the Different Conservation Methods

by Salem Hayar, Rawan Zeitoun and Britt Marianna Maestroni

Molecules 2021, 26(4), 1176; https://doi.org/10.3390/molecules26041176 - 22 Feb 2021

Cited by 12 | Viewed by 2715

Abstract

The QuEChERS method was applied to the determination of pesticide residues in vine (Vitis vinifera) leaves by LC-MSMS. The method was validated in-house for 33 pesticides representing 17 different chemical groups, that are most commonly used in grape production. Recoveries for [...] Read more.

The QuEChERS method was applied to the determination of pesticide residues in vine (Vitis vinifera) leaves by LC-MSMS. The method was validated in-house for 33 pesticides representing 17 different chemical groups, that are most commonly used in grape production. Recoveries for the pesticides tested ranged from 75 to 104%, and repeatability and reproducibility relative standard deviations (RSD_r% and RSD_Rw%) were less than 20%. The method was applied to the analysis of pesticide residues in 17 market brands of vine leaves processed according to three different preservation methods and sampled from the Lebanese market. Dried vine leaves were more contaminated with pesticide residues than those preserved in brine or stuffed vine leaves. The systemic fungicides were the most frequently detected among all the phytosanitary compounds usually applied to grape production. Brine-preserved and stuffed vine leaves contained lower concentrations of the residues but still contained a cocktail of different pesticides. Full article

(This article belongs to the Special Issue Development of Analytical Methods to Analyze Pesticide Residues)

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13 pages, 9999 KiB

Open AccessArticle

Identification of Three Small Molecules That Can Selectively Influence Cellular Manganese Levels in a Mouse Striatal Cell Model

by Kyle J. Horning, Xueqi Tang, Morgan G. Thomas, Michael Aschner and Aaron B. Bowman

Molecules 2021, 26(4), 1175; https://doi.org/10.3390/molecules26041175 - 22 Feb 2021

Viewed by 2471

Abstract

Manganese (Mn) is a biologically essential metal, critical as a cofactor for numerous enzymes such a glutamine synthetase and kinases such as ataxia-telangiectasia mutated (ATM). Similar to other essential metals such as iron and zinc, proper levels of Mn need to be achieved [...] Read more.

Manganese (Mn) is a biologically essential metal, critical as a cofactor for numerous enzymes such a glutamine synthetase and kinases such as ataxia-telangiectasia mutated (ATM). Similar to other essential metals such as iron and zinc, proper levels of Mn need to be achieved while simultaneously being careful to avoid excess levels of Mn that can be neurotoxic. A lifetime of occupational exposure to Mn can often lead to a Parkinsonian condition, also known as “manganism”, characterized by impaired gait, muscle spasms, and tremors. Despite the importance of its regulation, the mechanisms underlying the transport and homeostasis of Mn are poorly understood. Rather than taking a protein or gene-targeted approach, our lab recently took a high-throughput-screening approach to identify 41 small molecules that could significantly increase or decrease intracellular Mn in a neuronal cell model. Here, we report characterization of these small molecules, which we refer to as the “Mn toolbox”. We adapted a Fura-2-based assay for measuring Mn concentration and for measuring relative concentrations of other divalent metals: nickel, copper, cobalt, and zinc. Of these 41 small molecules, we report here the identification of three that selectively influence cellular Mn but do not influence the other divalent metals tested. The patterns of activity across divalent metals and the discovery of Mn-selective small molecules has potential pharmacological and scientific utility. Full article

(This article belongs to the Special Issue 25th Anniversary of Molecules - Featuring Element 25: Manganese and/or Other Metals)

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13 pages, 2547 KiB

Open AccessArticle

A Preliminary Study of FTIR Spectroscopy as a Potential Non-Invasive Screening Tool for Pediatric Precursor B Lymphoblastic Leukemia

by Radosław Chaber, Aneta Kowal, Paweł Jakubczyk, Christopher Arthur, Kornelia Łach, Renata Wojnarowska-Nowak, Krzysztof Kusz, Izabela Zawlik, Sylwia Paszek and Józef Cebulski

Molecules 2021, 26(4), 1174; https://doi.org/10.3390/molecules26041174 - 22 Feb 2021

Cited by 30 | Viewed by 3767

Abstract

Early detection of the most common pediatric neoplasm, B-cell precursor lymphoblastic leukemia (BCP-ALL), is challenging and requires invasive bone marrow biopsies. The purpose of this study was to establish new biomarkers for early screening to detect pediatric leukemia. In this small cohort study, [...] Read more.

Early detection of the most common pediatric neoplasm, B-cell precursor lymphoblastic leukemia (BCP-ALL), is challenging and requires invasive bone marrow biopsies. The purpose of this study was to establish new biomarkers for early screening to detect pediatric leukemia. In this small cohort study, Fourier transform infrared (FTIR) spectra were obtained from blood sera of 10 patients with BCP-ALL and were compared with the control samples from 10 children with some conditions other than neoplasm. Using various analytical approaches, including a new physical model, some significant differences were observable. The most important include: the different peak area ratio 2965/1645 cm⁻¹ (p = 0.002); the lower average percentage of both β-sheet and β-turn protein structures in the sera of BCP-ALL patients (p = 0.03); an AdaBoost-based predictive model for classifying healthy vs. BCP-ALL patients with 85% accuracy; and the phase shift of the first derivative in the spectral range 1050–1042 cm⁻¹ correlating with white blood cell (WBC) and blast cell count in BCP-ALL patients contrary to the samples obtained from healthy controls. Although verification in larger groups of patients will be necessary, these promising results suggest that FTIR spectroscopy may have future potential for the early screening of BCP-ALL. Full article

(This article belongs to the Special Issue Biomedical Applications of Infrared and Raman Spectroscopy)

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18 pages, 2136 KiB

Open AccessArticle

Synthesis of New Brassinosteroid 24-Norcholane Type Analogs Conjugated in C-3 with Benzoate Groups

by Karoll Ferrer, Katy Díaz, Miroslav Kvasnica, Andrés F. Olea, Mauricio Cuellar and Luis Espinoza

Molecules 2021, 26(4), 1173; https://doi.org/10.3390/molecules26041173 - 22 Feb 2021

Cited by 6 | Viewed by 2736

Abstract

The metabolism of brassinosteroid leads to structural modifications in the ring skeleton or the side alkyl chain. The esterification and glycosylation at C-3 are the most common metabolic pathways, and it has been suggested that conjugate brassinosteroids are less active or inactive. In [...] Read more.

The metabolism of brassinosteroid leads to structural modifications in the ring skeleton or the side alkyl chain. The esterification and glycosylation at C-3 are the most common metabolic pathways, and it has been suggested that conjugate brassinosteroids are less active or inactive. In this way, plants regulate the content of active brassinosteroids. In this work, the synthesis of brassinosteroid 24-norcholane type analogs conjugated at C-3 with benzoate groups, carrying electron donor and electron attractant substituents on the aromatic ring, is described. Additionally, their growth-promoting activities were evaluated using the Rice Lamina Inclination Test (RLIT) and compared with that exhibited by brassinolide (used as positive control) and non-conjugated analogs. The results indicate that at the lowest tested concentrations (10⁻⁸–10⁻⁷ M), all analogs conjugated at C-3 exhibit similar or higher activities than brassinolide, and the diasteroisomers with S configuration at C-22 are the more active ones. Increasing concentration (10⁻⁶ M) reduces the biological activities of analogs as compared to brassinolide. Full article

(This article belongs to the Special Issue Synthesis and Bioanalysis of Steroids and Steroid Biosynthesis Inhibitors)

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15 pages, 1113 KiB

Open AccessReview

Role of Gut Microbiota, Probiotics and Prebiotics in the Cardiovascular Diseases

by Anna Oniszczuk, Tomasz Oniszczuk, Marek Gancarz and Jolanta Szymańska

Molecules 2021, 26(4), 1172; https://doi.org/10.3390/molecules26041172 - 22 Feb 2021

Cited by 138 | Viewed by 15010

Abstract

In recent years, there has been a growing interest in identifying and applying new, naturally occurring molecules that promote health. Probiotics are defined as “live microorganisms which, when administered in adequate amounts, confer health benefits on the host”. Quite a few fermented products [...] Read more.

In recent years, there has been a growing interest in identifying and applying new, naturally occurring molecules that promote health. Probiotics are defined as “live microorganisms which, when administered in adequate amounts, confer health benefits on the host”. Quite a few fermented products serve as the source of probiotic strains, with many factors influencing the effectiveness of probiotics, including interactions of probiotic bacteria with the host’s microbiome. Prebiotics contain no microorganisms, only substances which stimulate their growth. Prebiotics can be obtained from various sources, including breast milk, soybeans, and raw oats, however, the most popular prebiotics are the oligosaccharides contained in plants. Recent research increasingly claims that probiotics and prebiotics alleviate many disorders related to the immune system, cancer metastasis, type 2 diabetes, and obesity. However, little is known about the role of these supplements as important dietary components in preventing or treating cardiovascular disease. Still, some reports and clinical studies were conducted, offering new ways of treatment. Therefore, the aim of this review is to discuss the roles of gut microbiota, probiotics, and prebiotics interventions in the prevention and treatment of cardiovascular disease. Full article

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16 pages, 1524 KiB

Open AccessArticle

Preliminary Investigation of the Antioxidant, Anti-Diabetic, and Anti-Inflammatory Activity of Enteromorpha intestinalis Extracts

by Biswajita Pradhan, Srimanta Patra, Chhandashree Behera, Rabindra Nayak, Bimal Prasad Jit, Andrea Ragusa and Mrutyunjay Jena

Molecules 2021, 26(4), 1171; https://doi.org/10.3390/molecules26041171 - 22 Feb 2021

Cited by 43 | Viewed by 4589

Abstract

Marine algae are a promising source of potent bioactive agents against oxidative stress, diabetes, and inflammation. However, the possible therapeutic effects of many algal metabolites have not been exploited yet. In this regard, we explored the therapeutic potential of Enteromorpha intestinalis extracts obtained [...] Read more.

Marine algae are a promising source of potent bioactive agents against oxidative stress, diabetes, and inflammation. However, the possible therapeutic effects of many algal metabolites have not been exploited yet. In this regard, we explored the therapeutic potential of Enteromorpha intestinalis extracts obtained from methanol, ethanol, and hexane, in contrasting oxidative stress. The total phenolic (TPC) and flavonoids (TFC) content were quantified in all extracts, with ethanol yielding the best values (about 60 and 625 mg of gallic acid and rutin equivalents per gram of extract, respectively). Their antioxidant potential was also assessed through DPPH^•, hydroxyl radical, hydrogen peroxide, and superoxide anion scavenging assays, showing a concentration-dependent activity which was greater in the extracts from protic and more polar solvents. The α-amylase and α-glucosidase activities were estimated for checking the antidiabetic capacity, with IC₅₀ values of about 3.8 µg/mL for the methanolic extract, almost as low as those obtained with acarbose (about 2.8 and 3.3 µg/mL, respectively). The same extract also showed remarkable anti-inflammatory effect, as determined by hemolysis, protein denaturation, proteinase and lipoxygenase activity assays, with respectable IC₅₀ values (about 11, 4, 6, and 5 µg/mL, respectively), also in comparison to commercially used drugs, such as acetylsalicylic acid. Full article

(This article belongs to the Section Medicinal Chemistry)

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15 pages, 3116 KiB

Open AccessArticle

The Antiproliferative and Apoptotic Effect of a Novel Synthesized S-Triazine Dipeptide Series, and Toxicity Screening in Zebrafish Embryos

by Azizah M. Malebari, Rakia Abd Alhameed, Zainab Almarhoon, Muhammad Farooq, Mohammad A. M. Wadaan, Anamika Sharma, Beatriz G. de la Torre, Fernando Albericio and Ayman El-Faham

Molecules 2021, 26(4), 1170; https://doi.org/10.3390/molecules26041170 - 22 Feb 2021

Cited by 7 | Viewed by 2804

Abstract

Several derivatives containing morpholine/piperidine, anilines, and dipeptides as pending moieties were prepared using s-triazine as a scaffold. These compounds were evaluated for their anticancer activity against two human breast cancer cell lines (MCF-7 and MDA-MB-231), a colon cancer cell line (HCT-116), and [...] Read more.

Several derivatives containing morpholine/piperidine, anilines, and dipeptides as pending moieties were prepared using s-triazine as a scaffold. These compounds were evaluated for their anticancer activity against two human breast cancer cell lines (MCF-7 and MDA-MB-231), a colon cancer cell line (HCT-116), and a non-tumorigenic cell line (HEK 293). Tamoxifen was used as a reference. Animal toxicity tests were carried out in zebrafish embryos. Most of these compounds showed a higher activity against breast cancer than colon cancer. Compound 3a—which contains morpholine, aniline, and glycylglycinate methyl ester—showed a high level of cytotoxicity against MCF-7 cells with IC₅₀ values of less than 1 µM. This compound showed a much lower level of toxicity against the non-tumorigenic HEK-293 cell line, and in the in vivo studies using zebrafish embryos. Furthermore, it induced cell cycle arrest at the G2/M phase, and apoptosis in MCF-7 cells. On the basis of our results, 3a emerges as a potential candidate for further development as a therapeutic drug to treat hormone receptor-positive breast cancer. Full article

(This article belongs to the Collection Efficient Pharmaceutical and Chemical Approaches for Anticancer Therapy: Design, Preliminary Evaluations, and Further Developments)

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39 pages, 9124 KiB

Open AccessReview

Challenges and Perspectives of Standard Therapy and Drug Development in High-Grade Gliomas

by Shalini Sundramurthi Chelliah, Ervin Ashley Lourdes Paul, Muhamad Noor Alfarizal Kamarudin and Ishwar Parhar

Molecules 2021, 26(4), 1169; https://doi.org/10.3390/molecules26041169 - 22 Feb 2021

Cited by 15 | Viewed by 5709

Abstract

Despite their low incidence rate globally, high-grade gliomas (HGG) remain a fatal primary brain tumor. The recommended therapy often is incapable of resecting the tumor entirely and exclusively targeting the tumor leads to tumor recurrence and dismal prognosis. Additionally, many HGG patients are [...] Read more.

Despite their low incidence rate globally, high-grade gliomas (HGG) remain a fatal primary brain tumor. The recommended therapy often is incapable of resecting the tumor entirely and exclusively targeting the tumor leads to tumor recurrence and dismal prognosis. Additionally, many HGG patients are not well suited for standard therapy and instead, subjected to a palliative approach. HGG tumors are highly infiltrative and the complex tumor microenvironment as well as high tumor heterogeneity often poses the main challenges towards the standard treatment. Therefore, a one-fit-approach may not be suitable for HGG management. Thus, a multimodal approach of standard therapy with immunotherapy, nanomedicine, repurposing of older drugs, use of phytochemicals, and precision medicine may be more advantageous than a single treatment model. This multimodal approach considers the environmental and genetic factors which could affect the patient’s response to therapy, thus improving their outcome. This review discusses the current views and advances in potential HGG therapeutic approaches and, aims to bridge the existing knowledge gap that will assist in overcoming challenges in HGG. Full article

(This article belongs to the Special Issue Anticancer Drug Discovery and Development)

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9 pages, 2413 KiB

Open AccessArticle

The Wound Healing Peptide, AES16-2M, Ameliorates Atopic Dermatitis In Vivo

by Myun Soo Kim, Jisun Song, Sunyoung Park, Tae Sung Kim, Hyun Jeong Park and Daeho Cho

Molecules 2021, 26(4), 1168; https://doi.org/10.3390/molecules26041168 - 22 Feb 2021

Cited by 8 | Viewed by 3151

Abstract

Peptide materials have recently been considered for use in various industrial fields. Because of their efficacy, safety, and low cost, therapeutic peptides are studied for various diseases, including atopic dermatitis (AD). AD is a common inflammatory skin disease impairing the patient’s quality of [...] Read more.

Peptide materials have recently been considered for use in various industrial fields. Because of their efficacy, safety, and low cost, therapeutic peptides are studied for various diseases, including atopic dermatitis (AD). AD is a common inflammatory skin disease impairing the patient’s quality of life. Various therapies, such as treatments with corticosteroids, calcineurin inhibitors, and antibody drugs, have been applied, but numerous side effects have been reported, including skin atrophy, burning, and infection. In the case of antibody drugs, immunogenicity against the drugs can be a problem. To overcome these side effects, small peptides are considered therapeutic agents. We previously identified the small wound healing peptide AES16-2M with a sequence of REGRT, and examined its effects on AD in this study. Interestingly, the administration of AES16-2M downregulated the AD disease score, ear thickness, serum IgE, and thymic stromal lymphopoietin (TSLP) in AD mice. The thickness of the epidermal layer was also improved by AES16-2M treatment. In addition, quantities of IL-4-, IL-13-, and IL-17-producing CD4 T cells from peripheral lymph nodes and spleens were reduced by injection of AES16-2M. Furthermore, the expression of TSLP was significantly reduced in AES16-2M-treated human keratinocytes. Therefore, these results suggest that AES16-2M can be a novel candidate for AD treatment. Full article

(This article belongs to the Special Issue Advances in Research of Short Peptides)

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