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Molecules, Volume 21, Issue 10 (October 2016)

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Cover Story (view full-size image) During recent decades, numerous studies were performed to evaluate the neuroprotective effects of [...] Read more.
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Open AccessCorrection Correction: Chae, H.S.; et al. Atractylodin Inhibits Interleukin-6 by Blocking NPM-ALK Activation and MAPKs in HMC-1. Molecules 2016, 21, 1169
Molecules 2016, 21(10), 1412; https://doi.org/10.3390/molecules21101412
Received: 12 October 2016 / Accepted: 19 October 2016 / Published: 25 October 2016
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Abstract
The authors wish to make the following correction to their paper [1].[...] Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Chemical Constituents from the Aerial Parts of Cyrtopodium paniculatum
Molecules 2016, 21(10), 1418; https://doi.org/10.3390/molecules21101418
Received: 17 September 2016 / Revised: 9 October 2016 / Accepted: 19 October 2016 / Published: 24 October 2016
Cited by 3 | Viewed by 1422 | PDF Full-text (1189 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
We report the first phytochemical study of the neotropical orchid Cyrtopodium paniculatum. Eight new compounds, including one phenanthrene 1, one 9,10-dihydro-phenanthrene 2, one hydroxybenzylphenanthrene 3, two biphenanthrenes 45, and three 9,10 dihydrophenanthrofurans 68,
[...] Read more.
We report the first phytochemical study of the neotropical orchid Cyrtopodium paniculatum. Eight new compounds, including one phenanthrene 1, one 9,10-dihydro-phenanthrene 2, one hydroxybenzylphenanthrene 3, two biphenanthrenes 45, and three 9,10 dihydrophenanthrofurans 68, together with 28 known phenolic compounds, mostly stilbenoids, were isolated from the CH2Cl2 extract of its leaves and pseudobulbs. The structures of the new compounds were established on the basis of extensive spectroscopic methods. Full article
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Open AccessArticle Exogenous Methyl Jasmonate and Salicylic Acid Induce Subspecies-Specific Patterns of Glucosinolate Accumulation and Gene Expression in Brassica oleracea L.
Molecules 2016, 21(10), 1417; https://doi.org/10.3390/molecules21101417
Received: 16 September 2016 / Revised: 18 October 2016 / Accepted: 19 October 2016 / Published: 24 October 2016
Cited by 7 | Viewed by 1750 | PDF Full-text (2653 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Glucosinolates have anti-carcinogenic properties. In the recent decades, the genetics of glucosinolate biosynthesis has been widely studied, however, the expression of specific genes involved in glucosinolate biosynthesis under exogenous phytohormone treatment has not been explored at the subspecies level in Brassica oleracea.
[...] Read more.
Glucosinolates have anti-carcinogenic properties. In the recent decades, the genetics of glucosinolate biosynthesis has been widely studied, however, the expression of specific genes involved in glucosinolate biosynthesis under exogenous phytohormone treatment has not been explored at the subspecies level in Brassica oleracea. Such data are vital for strategies aimed at selective exploitation of glucosinolate profiles. This study quantified the expression of 38 glucosinolate biosynthesis-related genes in three B. oleracea subspecies, namely cabbage, broccoli and kale, and catalogued associations between gene expression and increased contents of individual glucosinolates under methyl jasmonate (MeJA) and salicylic acid (SA) treatments. Glucosinolate accumulation and gene expression in response to phytohormone elicitation was subspecies specific. For instance, cabbage leaves showed enhanced accumulation of the aliphatic glucoiberin, progoitrin, sinigrin and indolic neoglucobrassicin under both MeJA and SA treatment. MeJA treatment induced strikingly higher accumulation of glucobrassicin (GBS) in cabbage and kale and of neoglucobrassicin (NGBS) in broccoli compared to controls. Notably higher expression of ST5a (Bol026200), CYP81F1 (Bol028913, Bol028914) and CYP81F4 genes was associated with significantly higher GBS accumulation under MeJA treatment compared to controls in all three subspecies. CYP81F4 genes, trans-activated by MYB34 genes, were expressed at remarkably high levels in all three subspecies under MeJA treatment, which also induced in higher indolic NGBS accumulation in all three subspecies. Remarkably higher expression of MYB28 (Bol036286), ST5b, ST5c, AOP2, FMOGS-OX5 (Bol031350) and GSL-OH (Bol033373) was associated with much higher contents of aliphatic glucosinolates in kale leaves compared to the other two subspecies. The genes expressed highly could be utilized in strategies to selectively increase glucosinolate compounds in B. oleracea subspecies. These results promote efforts to develop genotypes of B. oleracea and other species with enhanced levels of desired glucosinolates. Full article
(This article belongs to the Section Molecular Diversity)
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Open AccessCorrection Correction: Chae, H.S., et al. Anti-Inflammatory Effects of 6,8-Diprenyl-7,4′-dihydroxyflavanone from Sophora tonkinensis on Lipopolysaccharide-Stimulated RAW 264.7 Cells. Molecules. 2016, 21, 1049.
Molecules 2016, 21(10), 1413; https://doi.org/10.3390/molecules21101413
Received: 12 October 2016 / Accepted: 19 October 2016 / Published: 24 October 2016
Cited by 1 | Viewed by 965 | PDF Full-text (729 KB) | HTML Full-text | XML Full-text Figures

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Open AccessCommunication Original Synthesis of Fluorenyl Alcohol Derivatives by Reductive Dehalogenation Initiated by TDAE
Molecules 2016, 21(10), 1408; https://doi.org/10.3390/molecules21101408
Received: 19 September 2016 / Revised: 18 October 2016 / Accepted: 19 October 2016 / Published: 24 October 2016
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Abstract
We report here a novel and easy-to-handle reductive dehalogenation of 9-bromofluorene in the presence of arylaldehydes and dicarbonyl derivatives to give the corresponding fluorenyl alcohol derivatives and Darzens epoxides as by-products in tetrakis(dimethylamino)ethylene (TDAE) reaction conditions. The reaction is believed to proceed via
[...] Read more.
We report here a novel and easy-to-handle reductive dehalogenation of 9-bromofluorene in the presence of arylaldehydes and dicarbonyl derivatives to give the corresponding fluorenyl alcohol derivatives and Darzens epoxides as by-products in tetrakis(dimethylamino)ethylene (TDAE) reaction conditions. The reaction is believed to proceed via two successive single electron transfers to generate the fluorenyl anion which was able to react with different electrophiles. A mechanistic study was conducted to understand the formation of the epoxide derivatives. Full article
(This article belongs to the Section Organic Chemistry)
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Open AccessArticle Naturally Occurring Cinnamic Acid Sugar Ester Derivatives
Molecules 2016, 21(10), 1402; https://doi.org/10.3390/molecules21101402
Received: 30 September 2016 / Revised: 30 September 2016 / Accepted: 12 October 2016 / Published: 24 October 2016
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Abstract
Cinnamic acid sugar ester derivatives (CASEDs) are a class of natural product with one or several phenylacrylic moieties linked with the non-anomeric carbon of a glycosyl skeleton part through ester bonds. Their notable anti-depressant and brains protective activities have made them a topic
[...] Read more.
Cinnamic acid sugar ester derivatives (CASEDs) are a class of natural product with one or several phenylacrylic moieties linked with the non-anomeric carbon of a glycosyl skeleton part through ester bonds. Their notable anti-depressant and brains protective activities have made them a topic of great interest over the past several decades. In particular the compound 3′,6-disinapoylsucrose, the index component of Yuanzhi (a well-known Traditional Chinese Medicine or TCM), presents antidepressant effects at a molecular level, and has become a hotspot of research on new lead drug compounds. Several other similar cinnamic acid sugar ester derivatives are reported in traditional medicine as compounds to calm the nerves and display anti-depression and neuroprotective activity. Interestingly, more than one third of CASEDs are distributed in the family Polygalaceae. This overview discusses the isolation of cinnamic acid sugar ester derivatives from plants, together with a systematic discussion of their distribution, chemical structures and properties and pharmacological activities, with the hope of providing references for natural product researchers and draw attention to these interesting compounds. Full article
(This article belongs to the Section Medicinal Chemistry)
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Open AccessReview Development and Applications of the Copper-Catalyzed Azide-Alkyne Cycloaddition (CuAAC) as a Bioorthogonal Reaction
Molecules 2016, 21(10), 1393; https://doi.org/10.3390/molecules21101393
Received: 29 September 2016 / Revised: 14 October 2016 / Accepted: 15 October 2016 / Published: 24 October 2016
Cited by 20 | Viewed by 2643 | PDF Full-text (3330 KB) | HTML Full-text | XML Full-text
Abstract
The emergence of bioorthogonal reactions has greatly broadened the scope of biomolecule labeling and detecting. Of all the bioorthogonal reactions that have been developed, the copper-catalyzed azide-alkyne cycloaddition (CuAAC) is the most widely applied one, mainly because of its relatively fast kinetics and
[...] Read more.
The emergence of bioorthogonal reactions has greatly broadened the scope of biomolecule labeling and detecting. Of all the bioorthogonal reactions that have been developed, the copper-catalyzed azide-alkyne cycloaddition (CuAAC) is the most widely applied one, mainly because of its relatively fast kinetics and high efficiency. However, the introduction of copper species to in vivo systems raises the issue of potential toxicity. In order to reduce the copper-induced toxicity and further improve the reaction kinetics and efficiency, different strategies have been adopted, including the development of diverse copper chelating ligands to assist the catalytic cycle and the development of chelating azides as reagents. Up to now, the optimization of CuAAC has facilitated its applications in labeling and identifying either specific biomolecule species or on the omics level. Herein, we mainly discuss the efforts in the development of CuAAC to better fit the bioorthogonal reaction criteria and its bioorthogonal applications both in vivo and in vitro. Full article
(This article belongs to the Special Issue Recent Advances in CuAAC Click Chemistry)
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Open AccessArticle Isobutylhydroxyamides from Zanthoxylum bungeanum and Their Suppression of NO Production
Molecules 2016, 21(10), 1416; https://doi.org/10.3390/molecules21101416
Received: 18 September 2016 / Revised: 8 October 2016 / Accepted: 10 October 2016 / Published: 23 October 2016
Cited by 5 | Viewed by 1472 | PDF Full-text (628 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Four new unsaturated aliphatic acid amides, named zanthoamides A–D (14), and eight known ones—tetrahydrobungeanool (5), ZP-amide A (6), ZP-amide B (7), ZP-amide C (8), ZP-amide D (9), ZP-amide E
[...] Read more.
Four new unsaturated aliphatic acid amides, named zanthoamides A–D (14), and eight known ones—tetrahydrobungeanool (5), ZP-amide A (6), ZP-amide B (7), ZP-amide C (8), ZP-amide D (9), ZP-amide E (10), bugeanumamide A (11), and (2E,7E,9E)-N-(2-hydroxy-2-methylpropyl)-6,11-dioxo-2,7,9-dodecatrienamide (12)—were isolated from the pericarps of Zanthoxylum bungeanum. The structures of these compounds were elucidated by extensive use of spectroscopic methods, including HRESIMS, 1D and 2D NMR analyses and comparison with previously reported data. Compound 4 contained a rare C6 fatty acid unit with an acetal group. Results revealed that compounds 1, 5, 6, and 12 showed inhibitory effects on nitric oxide (NO) production in LPS-stimulated RAW 264.7 macrophages, with IC50values of 48.7 ± 0.32, 27.1 ± 1.15, 49.8 ± 0.38, and 39.4 ± 0.63 µM, respectively, while the other compounds were inactive (IC50 > 60 μM). They could contribute to the anti-inflammatory effects of Z. bungeanum by suppression of NO production. Full article
(This article belongs to the collection Bioactive Compounds)
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Open AccessArticle Design, Synthesis and Biological Evaluation of 6-(2,6-Dichloro-3,5-dimethoxyphenyl)-4-substituted-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors
Molecules 2016, 21(10), 1407; https://doi.org/10.3390/molecules21101407
Received: 10 September 2016 / Revised: 13 October 2016 / Accepted: 17 October 2016 / Published: 23 October 2016
Cited by 4 | Viewed by 1738 | PDF Full-text (3971 KB) | HTML Full-text | XML Full-text
Abstract
Tyrosine kinase fibroblast growth factor receptor (FGFR), which is aberrant in various cancer types, is a promising target for cancer therapy. Here we reported the design, synthesis, and biological evaluation of a new series of 6-(2,6-dichloro-3,5-dimethoxyphenyl)-4-substituted-1H-indazole derivatives as potent FGFR inhibitors.
[...] Read more.
Tyrosine kinase fibroblast growth factor receptor (FGFR), which is aberrant in various cancer types, is a promising target for cancer therapy. Here we reported the design, synthesis, and biological evaluation of a new series of 6-(2,6-dichloro-3,5-dimethoxyphenyl)-4-substituted-1H-indazole derivatives as potent FGFR inhibitors. The compound 6-(2,6-dichloro-3,5-dimethoxyphenyl)-N-phenyl-1H-indazole-4-carboxamide (10a) was identified as a potent FGFR1 inhibitor, with good enzymatic inhibition. Further structure-based optimization revealed that 6-(2,6-dichloro-3,5-dimethoxyphenyl)-N-(3-(4-methylpiperazin-1-yl)phenyl)-1H-indazole-4-carboxamide (13a) is the most potent FGFR1 inhibitor in this series, with an enzyme inhibitory activity IC50 value of about 30.2 nM. Full article
(This article belongs to the Special Issue Kinase Inhibitor Chemistry)
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Open AccessArticle Laurus nobilis, Zingiber officinale and Anethum graveolens Essential Oils: Composition, Antioxidant and Antibacterial Activities against Bacteria Isolated from Fish and Shellfish
Molecules 2016, 21(10), 1414; https://doi.org/10.3390/molecules21101414
Received: 25 July 2016 / Revised: 7 October 2016 / Accepted: 17 October 2016 / Published: 22 October 2016
Cited by 8 | Viewed by 2063 | PDF Full-text (703 KB) | HTML Full-text | XML Full-text
Abstract
Several bacterial strains were isolated from wild and reared fish and shellfish. The identification of these strains showed the dominance of the Aeromonas hydrophila species in all seafood samples, followed by Staphylococcus spp., Vibrio alginolyticus, Enterobacter cloacae, Klebsiella ornithinolytica, Klebsiella
[...] Read more.
Several bacterial strains were isolated from wild and reared fish and shellfish. The identification of these strains showed the dominance of the Aeromonas hydrophila species in all seafood samples, followed by Staphylococcus spp., Vibrio alginolyticus, Enterobacter cloacae, Klebsiella ornithinolytica, Klebsiella oxytoca and Serratia odorifera. The isolates were studied for their ability to produce exoenzymes and biofilms. The chemical composition of the essential oils from Laurus nobilis leaves, Zingiber officinale rhizomes and Anethum graveolens aerial parts was studied by GC and GC/MS. The essential oils’ antioxidant and antibacterial activities against the isolated microorganisms were studied. Low concentrations of the three essential oils were needed to inhibit the growth of the selected bacteria and the lowest MBCs values were obtained for the laurel essential oil. The selected essential oils can be used as a good natural preservative in fish food due to their antioxidant and antibacterial activities. Full article
(This article belongs to the collection Recent Advances in Flavors and Fragrances)
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Open AccessArticle Potential Anticancer Effects of Polyphenols from Chestnut Shell Extracts: Modulation of Cell Growth, and Cytokinomic and Metabolomic Profiles
Molecules 2016, 21(10), 1411; https://doi.org/10.3390/molecules21101411
Received: 20 September 2016 / Revised: 18 October 2016 / Accepted: 18 October 2016 / Published: 21 October 2016
Cited by 5 | Viewed by 1475 | PDF Full-text (1519 KB) | HTML Full-text | XML Full-text
Abstract
In this study, a hydroalcoholic chestnut shell extract was characterized and tested on six different human cell lines. Gallic, ellagic, and syringic acids were the most abundant non-condensed compounds in the chestnut extract, as determined by high performance liquid chromatography (HPLC). Tannins were
[...] Read more.
In this study, a hydroalcoholic chestnut shell extract was characterized and tested on six different human cell lines. Gallic, ellagic, and syringic acids were the most abundant non-condensed compounds in the chestnut extract, as determined by high performance liquid chromatography (HPLC). Tannins were mainly represented by condensed monomeric units of epigallocatechin and catechin/epicatechin. After 48 h of treatment, only the human hepatoblastoma HepG2 cells reached an inhibition corresponding to IC50 with an increase of apoptosis and mitochondrial depolarization. The cytokinome evaluation before and after treatment revealed that the vascular endothelial growth factor (VEGF) and the tumor necrosis factor (TNF)-α decreased after the treatment, suggesting a potential anti-angiogenic and anti-inflammatory effect of this extract. Moreover, the metabolome evaluation by 1H-NMR evidenced that the polyphenols extracted from chestnut shell (PECS) treatment affected the levels of some amino acids and other metabolites. Overall, these data highlight the effects of biomolecules on cell proliferation, apoptosis, cell cycle and mitochondrial depolarization, and on cytokinomics and metabolomics profiles. Full article
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Open AccessArticle A Fast and Robust UHPLC-MRM-MS Method to Characterize and Quantify Grape Skin Tannins after Chemical Depolymerization
Molecules 2016, 21(10), 1409; https://doi.org/10.3390/molecules21101409
Received: 30 September 2016 / Revised: 18 October 2016 / Accepted: 19 October 2016 / Published: 21 October 2016
Cited by 6 | Viewed by 1965 | PDF Full-text (2288 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
A rapid, sensitive, and selective analysis method using ultra high performance liquid chromatography coupled with triple-quadrupole mass spectrometry (UHPLC-QqQ-MS) has been developed for the characterization and quantification of grape skin flavan-3-ols after acid-catalysed depolymerization in the presence of phloroglucinol (phloroglucinolysis). The compound detection
[...] Read more.
A rapid, sensitive, and selective analysis method using ultra high performance liquid chromatography coupled with triple-quadrupole mass spectrometry (UHPLC-QqQ-MS) has been developed for the characterization and quantification of grape skin flavan-3-ols after acid-catalysed depolymerization in the presence of phloroglucinol (phloroglucinolysis). The compound detection being based on specific MS transitions in Multiple Reaction Monitoring (MRM) mode, this fast gradient robust method allows analysis of constitutive units of grape skin proanthocyanidins, including some present in trace amounts, in a single injection, with a throughput of 6 samples per hour. This method was applied to a set of 214 grape skin samples from 107 different red and white grape cultivars grown under two conditions in the vineyard, irrigated or non-irrigated. The results of triplicate analyses confirmed the robustness of the method, which was thus proven to be suitable for high-throughput and large-scale metabolomics studies. Moreover, these preliminary results suggest that analysis of tannin composition is relevant to investigate the genetic bases of grape response to drought. Full article
(This article belongs to the Special Issue Flavonoids: From Structure to Health Issues)
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Open AccessArticle Capsaicin Suppresses Cell Proliferation, Induces Cell Cycle Arrest and ROS Production in Bladder Cancer Cells through FOXO3a-Mediated Pathways
Molecules 2016, 21(10), 1406; https://doi.org/10.3390/molecules21101406
Received: 7 September 2016 / Revised: 13 October 2016 / Accepted: 18 October 2016 / Published: 21 October 2016
Cited by 6 | Viewed by 2795 | PDF Full-text (6916 KB) | HTML Full-text | XML Full-text
Abstract
Capsaicin (CAP), a highly selective agonist for transient receptor potential vanilloid type 1 (TRPV1), has been widely reported to exhibit anti-oxidant, anti-inflammation and anticancer activities. Currently, several therapeutic approaches for bladder cancer (BCa) are available, but accompanied by unfavorable outcomes. Previous studies reported
[...] Read more.
Capsaicin (CAP), a highly selective agonist for transient receptor potential vanilloid type 1 (TRPV1), has been widely reported to exhibit anti-oxidant, anti-inflammation and anticancer activities. Currently, several therapeutic approaches for bladder cancer (BCa) are available, but accompanied by unfavorable outcomes. Previous studies reported a potential clinical effect of CAP to prevent BCa tumorigenesis. However, its underlying molecular mechanism still remains unknown. Our transcriptome analysis suggested a close link among calcium signaling pathway, cell cycle regulation, ROS metabolism and FOXO signaling pathway in BCa. In this study, several experiments were performed to investigate the effects of CAP on BCa cells (5637 and T24) and NOD/SCID mice. Our results showed that CAP could suppress BCa tumorigenesis by inhibiting its proliferation both in vitro and in vivo. Moreover, CAP induced cell cycle arrest at G0/G1 phase and ROS production. Importantly, our studies revealed a strong increase of FOXO3a after treatment with CAP. Furthermore, we observed no significant alteration of apoptosis by CAP, whereas Catalase and SOD2 were considerably upregulated, which could clear ROS and protect against cell death. Thus, our results suggested that CAP could inhibit viability and tumorigenesis of BCa possibly via FOXO3a-mediated pathways. Full article
(This article belongs to the Special Issue Capsaicin)
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Open AccessArticle The Inhibition Effect of Cell DNA Oxidative Damage and LDL Oxidation by Bovine Colostrums
Molecules 2016, 21(10), 1378; https://doi.org/10.3390/molecules21101378
Received: 11 August 2016 / Revised: 4 October 2016 / Accepted: 19 October 2016 / Published: 21 October 2016
Cited by 1 | Viewed by 1062 | PDF Full-text (1789 KB) | HTML Full-text | XML Full-text
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In the present study, we investigated the effect of bovine colostrums on inhibition of DNA oxidative damage and low density lipoprotein (LDL) oxidation in vitro. Results showed that whey and skimmed milk exhibited not only higher inhibitory activities of oxidative damage of deoxyribose
[...] Read more.
In the present study, we investigated the effect of bovine colostrums on inhibition of DNA oxidative damage and low density lipoprotein (LDL) oxidation in vitro. Results showed that whey and skimmed milk exhibited not only higher inhibitory activities of oxidative damage of deoxyribose but also an inhibitory effect on the breakdown of supercoiled DNA into open circular DNA and linear DNA. The quantities of 8-OH-2′-dG formed under whey, caseins and skimmed milk treatment were 0.24, 0.24 and 1.24 μg/mL, respectively. The quantity of malondialdehyde formed through LDL oxidation induced by copprous ion was significantly decreased as colostrums protein solutions were added, in which whey and caseins led to a more significant decrease than skimmed milk. The formation of conjugated dienes could be inhibited by treatment with colostrums protein solutions. Whey exhibited the longest lag time of conjugated dienes formation among the colostrums proteins. The lag time of the whey was 2.33 times that of the control. From the results of foregoing, the bovine colostrums protein has potential value in the inhibition of DNA oxidation damage and LDL oxidation. Full article
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Open AccessArticle Identification of Novel Human Breast Carcinoma (MDA-MB-231) Cell Growth Modulators from a Carbohydrate-Based Diversity Oriented Synthesis Library
Molecules 2016, 21(10), 1405; https://doi.org/10.3390/molecules21101405
Received: 18 August 2016 / Revised: 12 October 2016 / Accepted: 15 October 2016 / Published: 20 October 2016
Cited by 1 | Viewed by 1389 | PDF Full-text (7033 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
The application of a cell-based growth inhibition on a library of skeletally different glycomimetics allowed for the selection of a hexahydro-2H-furo[3,2-b][1,4]oxazine compound as candidate inhibitors of MDA-MB-231 cell growth. Subsequent synthesis of analogue compounds and preliminary biological studies validated
[...] Read more.
The application of a cell-based growth inhibition on a library of skeletally different glycomimetics allowed for the selection of a hexahydro-2H-furo[3,2-b][1,4]oxazine compound as candidate inhibitors of MDA-MB-231 cell growth. Subsequent synthesis of analogue compounds and preliminary biological studies validated the selection of a valuable hit compound with a novel polyhydroxylated structure for the modulation of the breast carcinoma cell cycle mechanism. Full article
(This article belongs to the Special Issue Diversity Oriented Synthesis 2016)
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Open AccessReview Effects of Saponins on Lipid Metabolism: A Review of Potential Health Benefits in the Treatment of Obesity
Molecules 2016, 21(10), 1404; https://doi.org/10.3390/molecules21101404
Received: 3 August 2016 / Revised: 11 October 2016 / Accepted: 12 October 2016 / Published: 20 October 2016
Cited by 10 | Viewed by 2663 | PDF Full-text (2258 KB) | HTML Full-text | XML Full-text
Abstract
Obesity is one of the greatest public health problems. This complex condition has reached epidemic proportions in many parts of the world, and it constitutes a risk factor for several chronic disorders, such as hypertension, cardiovascular diseases and type 2 diabetes. In the
[...] Read more.
Obesity is one of the greatest public health problems. This complex condition has reached epidemic proportions in many parts of the world, and it constitutes a risk factor for several chronic disorders, such as hypertension, cardiovascular diseases and type 2 diabetes. In the last few decades, several studies dealt with the potential effects of natural products as new safe and effective tools for body weight control. Saponins are naturally-occurring surface-active glycosides, mainly produced by plants, whose structure consists of a sugar moiety linked to a hydrophobic aglycone (a steroid or a triterpene). Many pharmacological properties have been reported for these compounds, such as anti-inflammatory, immunostimulant, hypocholesterolemic, hypoglycemic, antifungal and cytotoxic activities. The aim of this review is to provide an overview of recent studies about the anti-obesity therapeutic potential of saponins isolated from medicinal plants. Results on the in vitro and in vivo activity of this class of phytochemicals are here presented and discussed. The most interesting findings about their possible mechanism of action and their potential health benefits in the treatment of obesity are reported, as well. Full article
(This article belongs to the Special Issue Natural Products in Anti-Obesity Therapy)
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Open AccessArticle Seasonal Dynamics of Metabolites in Needles of Taxus wallichiana var. mairei
Molecules 2016, 21(10), 1403; https://doi.org/10.3390/molecules21101403
Received: 7 September 2016 / Revised: 13 October 2016 / Accepted: 16 October 2016 / Published: 20 October 2016
Cited by 5 | Viewed by 1099 | PDF Full-text (2811 KB) | HTML Full-text | XML Full-text
Abstract
Seasonal variations of the phytochemicals contents in needles of T. wallichiana var. mairei due to the effects of growth meteorological parameters were investigated in this study. The needles of T. wallichiana var. mairei were collected from different months and the contents of taxoids
[...] Read more.
Seasonal variations of the phytochemicals contents in needles of T. wallichiana var. mairei due to the effects of growth meteorological parameters were investigated in this study. The needles of T. wallichiana var. mairei were collected from different months and the contents of taxoids (paclitaxel, 10-deacetylbaccatin III (10-DAB), baccatin III, cephalomannine, 10-deacetyltaxol (10-DAT)), flavones (ginkgetin, amentoflavone, quercetin) and polysaccharides were quantified by ultra performance liquid chromatography (UPLC) and the resonance light scattering (RIL) method. The content of taxoids gave the highest level of 1.77 ± 0.38 mg·g−1 in January, and the lowest value of 0.61 ± 0.08 mg·g−1 in September. Unlike taxoids, the content of flavonoids was the highest in August. The content of polysaccharides reached peak value of 28.52 ± 0.57 mg·g−1 in September, which was two times higher than the lowest content of 9.39 ± 0.17 mg·g−1 in January. The contents of paclitaxel, 10-DAB, 10-DAT and polysaccharides significantly depended on meteorological parameters. The mean of minimum temperature (R = −0.61) and length of daylight (R = −0.60) were significantly correlated to 10-DAB content, while 10-DAT level showed significant correlation with length of daylight (R = −0.70) and relative humidity (R = 0.70). In addition, temperature had significantly negative effect on the content of paclitaxel and a significantly positive effect on that of polysaccharides. This study enriched the knowledge on the accumulation pattern of metabolites and could help us to determine the collecting time of T. wallichiana var. mairei for medicinal use. Full article
(This article belongs to the Section Molecular Diversity)
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Open AccessArticle Curcumin Shows Antiviral Properties against Norovirus
Molecules 2016, 21(10), 1401; https://doi.org/10.3390/molecules21101401
Received: 3 September 2016 / Revised: 7 October 2016 / Accepted: 15 October 2016 / Published: 20 October 2016
Cited by 2 | Viewed by 1590 | PDF Full-text (4209 KB) | HTML Full-text | XML Full-text
Abstract
Phytochemicals provide environmentally friendly and relatively inexpensive natural products, which could potentially benefit public health by controlling human norovirus (HuNoV) infection. In this study, 18 different phytochemicals were evaluated for antiviral effects against norovirus using murine norovirus (MNV) as a model for norovirus
[...] Read more.
Phytochemicals provide environmentally friendly and relatively inexpensive natural products, which could potentially benefit public health by controlling human norovirus (HuNoV) infection. In this study, 18 different phytochemicals were evaluated for antiviral effects against norovirus using murine norovirus (MNV) as a model for norovirus biology. Among these phytochemicals, curcumin (CCM) was the most potent anti-noroviral phytochemical, followed by resveratrol (RVT). In a cell culture infection model, exposure to CCM or RVT for 3 days reduced infectivity of norovirus by 91% and 80%, respectively. To confirm the antiviral capability of CCM, we further evaluated its antiviral efficacy at various doses (0.25, 0.5, 0.75, 1, and 2 mg/mL) and durations (short-term: 10, 30, 60, and 120 min; long-term: 1, 3, 7, and 14 days). The anti-noroviral effect of CCM was verified to occur in a dose-dependent manner. Additionally, we evaluated the inhibitory effect of each phytochemical on the replication of HuNoV using a HuNoV replicon-bearing cell line (HG23). Neither CCM nor RVT had a strong inhibitory effect on HuNoV replication, which suggests that their antiviral mechanism may involve viral entry or other life cycle stages rather than the replication of viral RNA. Our results demonstrated that CCM may be a promising candidate for development as an anti-noroviral agent to prevent outbreaks of foodborne illness. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Blue Light Emitting Polyphenylene Dendrimers with Bipolar Charge Transport Moieties
Molecules 2016, 21(10), 1400; https://doi.org/10.3390/molecules21101400
Received: 13 September 2016 / Revised: 14 October 2016 / Accepted: 16 October 2016 / Published: 20 October 2016
Cited by 4 | Viewed by 1924 | PDF Full-text (2301 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Two light-emitting polyphenylene dendrimers with both hole and electron transporting moieties were synthesized and characterized. Both molecules exhibited pure blue emission solely from the pyrene core and efficient surface-to-core energy transfers when characterized in a nonpolar environment. In particular, the carbazole- and oxadiazole-functionalized
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Two light-emitting polyphenylene dendrimers with both hole and electron transporting moieties were synthesized and characterized. Both molecules exhibited pure blue emission solely from the pyrene core and efficient surface-to-core energy transfers when characterized in a nonpolar environment. In particular, the carbazole- and oxadiazole-functionalized dendrimer (D1) manifested a pure blue emission from the pyrene core without showing intramolecular charge transfer (ICT) in environments with increasing polarity. On the other hand, the triphenylamine- and oxadiazole-functionalized one (D2) displayed notable ICT with dual emission from both the core and an ICT state in highly polar solvents. D1, in a three-layer organic light emitting diode (OLED) by solution processing gave a pure blue emission with Commission Internationale de l’Éclairage 1931 CIE xy = (0.16, 0.12), a peak current efficiency of 0.21 cd/A and a peak luminance of 2700 cd/m2. This represents the first reported pure blue dendrimer emitter with bipolar charge transport and surface-to-core energy transfer in OLEDs. Full article
(This article belongs to the Special Issue Organic Light Emitting Diodes)
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Open AccessReview High-Pressure Design of Advanced BN-Based Materials
Molecules 2016, 21(10), 1399; https://doi.org/10.3390/molecules21101399
Received: 14 September 2016 / Revised: 3 October 2016 / Accepted: 12 October 2016 / Published: 20 October 2016
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Abstract
The aim of the present review is to highlight the state of the art in high-pressure design of new advanced materials based on boron nitride. Recent experimental achievements on the governing phase transformation, nanostructuring and chemical synthesis in the systems containing boron nitride
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The aim of the present review is to highlight the state of the art in high-pressure design of new advanced materials based on boron nitride. Recent experimental achievements on the governing phase transformation, nanostructuring and chemical synthesis in the systems containing boron nitride at high pressures and high temperatures are presented. All these developments allowed discovering new materials, e.g., ultrahard nanocrystalline cubic boron nitride (nano-cBN) with hardness comparable to diamond, and superhard boron subnitride B13N2. Thermodynamic and kinetic aspects of high-pressure synthesis are described based on the data obtained by in situ and ex situ methods. Mechanical and thermal properties (hardness, thermoelastic equations of state, etc.) are discussed. New synthetic perspectives, combining both soft chemistry and extreme pressure–temperature conditions are considered. Full article
(This article belongs to the Special Issue Boron Nitride: Synthesis and Application)
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Open AccessArticle Improved Production and Antitumor Properties of Triterpene Acids from Submerged Culture of Ganoderma lingzhi
Molecules 2016, 21(10), 1395; https://doi.org/10.3390/molecules21101395
Received: 26 July 2016 / Revised: 9 October 2016 / Accepted: 16 October 2016 / Published: 20 October 2016
Cited by 3 | Viewed by 1131 | PDF Full-text (1915 KB) | HTML Full-text | XML Full-text
Abstract
Triterpene acids (TAs) are the major bioactive constituents in the medicinal fungus Ganoderma lingzhi. However, fermentative production of TAs has not been optimized for commercial use, and whether the TAs isolated from G. lingzhi submerged culture mycelia possess antitumor activity needs to
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Triterpene acids (TAs) are the major bioactive constituents in the medicinal fungus Ganoderma lingzhi. However, fermentative production of TAs has not been optimized for commercial use, and whether the TAs isolated from G. lingzhi submerged culture mycelia possess antitumor activity needs to be further proven. In this study, enhanced TA yield and productivity were attained with G. lingzhi using response surface methodology. The interactions of three variables were studied using a Box-Benhnken design, namely initial pH, dissolved oxygen (DO) and fermentation temperature. The optimum conditions were an initial pH of 5.9, 20.0% DO and 28.6 °C. These conditions resulted in a TA yield of 308.1 mg/L in a 5-L stirred bioreactor. Furthermore, the optimized conditions were then successfully scaled up to a production scale of 200 L, and maximum TA production and productivity of 295.3 mg/L and 49.2 mg/L/day were achieved, which represented 80.9% and 111.5% increases, respectively, compared with the non-optimized conditions. Additionally, the triterpene acid extract (TAE) from G. lingzhi mycelia was found to be cytotoxic to the SMMC-7721 and SW620 cell lines in vitro, and the TAE exhibited dose-dependent antitumor activity against the solid tumor sarcoma 180 in vivo. Chemical analysis revealed that the key active triterpene compounds, ganoderic acid T and ganoderic acid Me, predominated in the extract. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Structurally Related Monoterpenes p-Cymene, Carvacrol and Thymol Isolated from Essential Oil from Leaves of Lippia sidoides Cham. (Verbenaceae) Protect Mice against Elastase-Induced Emphysema
Molecules 2016, 21(10), 1390; https://doi.org/10.3390/molecules21101390
Received: 31 August 2016 / Revised: 4 October 2016 / Accepted: 12 October 2016 / Published: 20 October 2016
Cited by 8 | Viewed by 2944 | PDF Full-text (4248 KB) | HTML Full-text | XML Full-text
Abstract
Background: Chronic obstructive pulmonary disease (COPD) is characterized by irreversible airflow obstruction and inflammation. Natural products, such as monoterpenes, displayed anti-inflammatory and anti-oxidant activities and can be used as a source of new compounds to COPD treatment. Our aim was to evaluate, in
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Background: Chronic obstructive pulmonary disease (COPD) is characterized by irreversible airflow obstruction and inflammation. Natural products, such as monoterpenes, displayed anti-inflammatory and anti-oxidant activities and can be used as a source of new compounds to COPD treatment. Our aim was to evaluate, in an elastase-induced pulmonary emphysema in mice, the effects of and underlying mechanisms of three related natural monoterpenes (p-cymene, carvacrol and thymol) isolated from essential oil from leaves Lippia sidoides Cham. (Verbenaceae). Methods: Mices received porcine pancreatic elastase (PPE) and were treated with p-cymene, carvacrol, thymol or vehicle 30 min later and again on 7th, 14th and 28th days. Lung inflammatory profile and histological sections were evaluated. Results: In the elastase-instilled animals, the tested monoterpenes reduced alveolar enlargement, macrophages and the levels of IL-1β, IL-6, IL-8 and IL-17 in bronchoalveolar lavage fluid (BALF), and collagen fibers, MMP-9 and p-65-NF-κB-positive cells in lung parenchyma (p < 0.05). All treatments attenuated levels of 8-iso-PGF2α but only thymol was able to reduced exhaled nitric oxide (p < 0.05). Conclusion: Monoterpenes p-cymene, carvacrol and thymol reduced lung emphysema and inflammation in mice. No significant differences among the three monoterpenes treatments were found, suggesting that the presence of hydroxyl group in the molecular structure of thymol and carvacrol do not play a central role in the anti-inflammatory effects. Full article
(This article belongs to the Special Issue Natural Products and Inflammation)
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Open AccessArticle Proteome and Peptidome of Vipera berus berus Venom
Molecules 2016, 21(10), 1398; https://doi.org/10.3390/molecules21101398
Received: 3 August 2016 / Revised: 4 October 2016 / Accepted: 12 October 2016 / Published: 19 October 2016
Cited by 4 | Viewed by 1791 | PDF Full-text (1567 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Snake venom is a rich source of peptides and proteins with a wide range of actions. Many of the venom components are currently being tested for their usefulness in the treatment of many diseases ranging from neurological and cardiovascular to cancer. It is
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Snake venom is a rich source of peptides and proteins with a wide range of actions. Many of the venom components are currently being tested for their usefulness in the treatment of many diseases ranging from neurological and cardiovascular to cancer. It is also important to constantly search for new proteins and peptides with properties not yet described. The venom of Vipera berus berus has hemolytic, proteolytic and cytotoxic properties, but its exact composition and the factors responsible for these properties are not known. Therefore, an attempt was made to identify proteins and peptides derived from this species venom by using high resolution two-dimensional electrophoresis and MALDI ToF/ToF mass spectrometry. A total of 11 protein classes have been identified mainly proteases but also l-amino acid oxidases, C-type lectin like proteins, cysteine-rich venom proteins and phospholipases A2 and 4 peptides of molecular weight less than 1500 Da. Most of the identified proteins are responsible for the highly hemotoxic properties of the venom. Presence of venom phospholipases A2 and l-amino acid oxidases cause moderate neuro-, myo- and cytotoxicity. All successfully identified peptides belong to the bradykinin-potentiating peptides family. The mass spectrometry data are available via ProteomeXchange with identifier PXD004958. Full article
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Open AccessArticle Extract from Maize (Zea mays L.): Antibacterial Activity of DIMBOA and Its Derivatives against Ralstonia solanacearum
Molecules 2016, 21(10), 1397; https://doi.org/10.3390/molecules21101397
Received: 8 September 2016 / Revised: 10 October 2016 / Accepted: 15 October 2016 / Published: 19 October 2016
Cited by 1 | Viewed by 1828 | PDF Full-text (2353 KB) | HTML Full-text | XML Full-text
Abstract
Many cereals accumulate hydroxamic acids involved in defense of plant against various fungi, bacteria, and insects. 2,4-dihydroxy-7-methoxy-1,4-benzoxazine-3-one, commonly known as DIMBOA, is one of the principal cyclic hydroxamic acids in aqueous extracts of maize. The aim of this study was to evaluate the
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Many cereals accumulate hydroxamic acids involved in defense of plant against various fungi, bacteria, and insects. 2,4-dihydroxy-7-methoxy-1,4-benzoxazine-3-one, commonly known as DIMBOA, is one of the principal cyclic hydroxamic acids in aqueous extracts of maize. The aim of this study was to evaluate the antibacterial activity of the isolated DIMBOA and its derivatives 2-benzoxazolinone (BOA), 6-chloro-2-benzoxazolinone (CDHB), and 2-mercaptobenzothiazole (MBT) against Ralstonia solanacearum. MBT showed the strongest antibacterial activity, followed by CDHB and DIMBOA, with minimum inhibitory concentrations (MICs) of 50, 100 and 200 mg/L, respectively, better than the BOA with 300 mg/L. These compounds also significantly affect bacterial growth, reduce biofilm formation, and inhibit swarming motility within 24 h. This paper is the first to report the anti-R. solanacearum activity of DIMBOA from Z. mays. The bioassay and pot experiment results suggested that DIMBOA and its derivatives exhibit potential as a new matrix structure of designing target bactericide or elicitor for controlling tobacco bacterial wilt. Further studies must evaluate the efficacy of DIMBOA and its derivatives in controlling bacterial wilt under natural field conditions where low inoculum concentrations exist. Full article
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Open AccessArticle 20(S)-Protopanaxadiol Phospholipid Complex: Process Optimization, Characterization, In Vitro Dissolution and Molecular Docking Studies
Molecules 2016, 21(10), 1396; https://doi.org/10.3390/molecules21101396
Received: 17 July 2016 / Revised: 7 October 2016 / Accepted: 13 October 2016 / Published: 19 October 2016
Cited by 4 | Viewed by 1418 | PDF Full-text (3887 KB) | HTML Full-text | XML Full-text
Abstract
20(S)-Protopanaxadiol (PPD), a bioactive compound extracted from ginseng, possesses cardioprotective, neuroprotective, anti-inflammatory, antiestrogenic, anticancer and anxiolytic effects. However, the clinical application of PPD is limited by its weak aqueous solubility. In this study, we optimized an efficient method of preparing its
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20(S)-Protopanaxadiol (PPD), a bioactive compound extracted from ginseng, possesses cardioprotective, neuroprotective, anti-inflammatory, antiestrogenic, anticancer and anxiolytic effects. However, the clinical application of PPD is limited by its weak aqueous solubility. In this study, we optimized an efficient method of preparing its phospholipid complex (PPD-PLC) using a central composite design and response surface analysis. The prepared PPD-PLC was characterized by differential scanning calorimetric, powder X-ray diffraction, Fourier-transformed infrared spectroscopy and nuclear magnetic resonance analyses associated with molecular docking calculation. The equilibrium solubility of PPD-PLC in water and n-octanol increased 6.53- and 1.53-times, respectively. Afterwards, using PPD-PLC as the intermediate, the PPD-PLC-loaded dry suspension (PPD-PLC-SU) was prepared with our previous method. In vitro evaluations were conducted on PPD-PLC and PPD-PLC-SU, including dissolution behaviors and stability properties under different conditions. Results of in vitro dissolution behavior revealed the improved dissolution extents and rates of PPD-PLC and PPD-PLC-SU (p < 0.05). Results of the formulation stability investigation also exposed the better stability of PPD-PLC-SU compared with free PPD. Therefore, phospholipid complex technology is a useful formulation strategy for BCS II drugs, as it could effectively improve their hydrophilicity and lipophilicity. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Application of Super-Amphiphilic Silica-Nanogel Composites for Fast Removal of Water Pollutants
Molecules 2016, 21(10), 1392; https://doi.org/10.3390/molecules21101392
Received: 26 September 2016 / Revised: 13 October 2016 / Accepted: 15 October 2016 / Published: 19 October 2016
Cited by 2 | Viewed by 2183 | PDF Full-text (4743 KB) | HTML Full-text | XML Full-text
Abstract
This work first reports the preparation of super-amphiphilic silica-nanogel composites to reduce the contact angle of water to increase the diffusion of pollutant into adsorbents. In this respect, the silica nanoparticles were encapsulated into nanogels based on ionic and nonionic polyacrylamides by dispersion
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This work first reports the preparation of super-amphiphilic silica-nanogel composites to reduce the contact angle of water to increase the diffusion of pollutant into adsorbents. In this respect, the silica nanoparticles were encapsulated into nanogels based on ionic and nonionic polyacrylamides by dispersion polymerization technique. The morphologies and the dispersion stability of nanogel composites were investigated to clarify the ability of silica-nanogel composites to adsorb at different interfaces. The feasibility of silica polyacrylamide nanogel composites to act as a high-performance adsorbent for removal of methylene blue (MB) dye and heavy metals (Co2+ and Ni2+) from aqueous solution was investigated. The surface tension, contact angle, average pore size, and zeta potential of the silica-nanogel composites have been evaluated. The MB dye and heavy metal adsorption capacity achieved Qmax = 438–387 mg/g which is considerably high. The adsorption capacity results are explained from the changes in the morphology of the silica surfaces as recorded from scanning electron microscopy (SEM). Full article
(This article belongs to the Section Molecular Diversity)
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Open AccessReview The Potential of Secondary Metabolites from Plants as Drugs or Leads against Protozoan Neglected Diseases—Part III: In-Silico Molecular Docking Investigations
Molecules 2016, 21(10), 1389; https://doi.org/10.3390/molecules21101389
Received: 16 September 2016 / Revised: 6 October 2016 / Accepted: 12 October 2016 / Published: 19 October 2016
Cited by 7 | Viewed by 2232 | PDF Full-text (5610 KB) | HTML Full-text | XML Full-text
Abstract
Malaria, leishmaniasis, Chagas disease, and human African trypanosomiasis continue to cause considerable suffering and death in developing countries. Current treatment options for these parasitic protozoal diseases generally have severe side effects, may be ineffective or unavailable, and resistance is emerging. There is a
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Malaria, leishmaniasis, Chagas disease, and human African trypanosomiasis continue to cause considerable suffering and death in developing countries. Current treatment options for these parasitic protozoal diseases generally have severe side effects, may be ineffective or unavailable, and resistance is emerging. There is a constant need to discover new chemotherapeutic agents for these parasitic infections, and natural products continue to serve as a potential source. This review presents molecular docking studies of potential phytochemicals that target key protein targets in Leishmania spp., Trypanosoma spp., and Plasmodium spp. Full article
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Open AccessArticle Adsorption of Wine Constituents on Functionalized Surfaces
Molecules 2016, 21(10), 1394; https://doi.org/10.3390/molecules21101394
Received: 20 September 2016 / Revised: 13 October 2016 / Accepted: 15 October 2016 / Published: 18 October 2016
Cited by 2 | Viewed by 1469 | PDF Full-text (3583 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
The adsorption of macromolecules on solid surfaces is of great importance in the field of nanotechnology, biomaterials, biotechnological, and food processes. In the field of oenology adsorption of wine macromolecules such as polyphenols, polysaccharides, and proteins is much less desirable on membrane materials
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The adsorption of macromolecules on solid surfaces is of great importance in the field of nanotechnology, biomaterials, biotechnological, and food processes. In the field of oenology adsorption of wine macromolecules such as polyphenols, polysaccharides, and proteins is much less desirable on membrane materials because of fouling and reduced filtering performance. On the other hand, adsorption of these molecules on processing aids is very beneficial for achieving wine clarity and stability. In this article, the effect of surface chemical functionalities on the adsorption of white, rosé, and red wine constituents was evaluated. Allylamine, acrylic acid, and ethanol were selected as precursors for plasma polymerization in order to generate coatings rich in amine, carboxyl, and hydroxyl chemical groups, respectively. The surface chemical functionalities were characterized by X-ray photoelectron spectroscopy (XPS) and the ability of different surface chemical functionalities to adsorb wine constituents were characterized by quartz crystal microbalance with dissipation (QCM-D) and atomic force microscopy (AFM). The results demonstrated that the amine and carboxyl modified surfaces encourage adsorption of constituents from white wine. The hydroxyl modified surfaces have the ability to preferentially adsorb rosé wine constituents, whereas red wine adsorbed to the highest extent on acrylic acid surface. Full article
(This article belongs to the collection Wine Chemistry)
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Open AccessArticle Renal Protective Effects of 17β-Estradiol on Mice with Acute Aristolochic Acid Nephropathy
Molecules 2016, 21(10), 1391; https://doi.org/10.3390/molecules21101391
Received: 24 August 2016 / Revised: 5 October 2016 / Accepted: 13 October 2016 / Published: 18 October 2016
Cited by 4 | Viewed by 1837 | PDF Full-text (11987 KB) | HTML Full-text | XML Full-text
Abstract
Aristolochic acid nephropathy (AAN) is a progressive kidney disease caused by a Chinese herb containing aristolochic acid. Excessive death of renal tubular epithelial cells (RTECs) characterized the acute phase of AAN. Therapies for acute AAN were limited, such as steroids and angiotensin-receptor blockers
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Aristolochic acid nephropathy (AAN) is a progressive kidney disease caused by a Chinese herb containing aristolochic acid. Excessive death of renal tubular epithelial cells (RTECs) characterized the acute phase of AAN. Therapies for acute AAN were limited, such as steroids and angiotensin-receptor blockers (ARBs)/angiotensin-converting enzyme inhibitors (ACEIs). It was interesting that, in acute AAN, female patients showed relative slower progression to renal failure than males. In a previous study, female hormone 17β-estradiol (E2) was found to attenuate renal ischemia-reperfusion injury. Thus, the aim of this study was to investigate the potential protective role of E2 in acute AAN. Compared with male C57BL/6 mice of acute AAN, lower serum creatinine (SCr) and less renal injury, together with RTEC apoptosis in females, were found. Treatment with E2 in male AAN mice reduced SCr levels and attenuated renal tubular injury and RTEC apoptosis. In the mice kidney tissue and human renal proximal tubule cells (HK-2 cells), E2 both attenuated AA-induced cell apoptosis and downregulated the expression of phosphor-p53 (Ser15), p53, and cleaved-caspase-3. This study highlights that E2 exhibited protective effects on the renal injury of acute AAN in male mice by reducing RTEC apoptosis, which might be related to inhibiting the p53 signaling pathway. Full article
(This article belongs to the Section Medicinal Chemistry)
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Open AccessArticle Decrystallization of Crystals Using Gold “Nano-Bullets” and the Metal-Assisted and Microwave-Accelerated Decrystallization Technique
Molecules 2016, 21(10), 1388; https://doi.org/10.3390/molecules21101388
Received: 19 July 2016 / Revised: 4 October 2016 / Accepted: 7 October 2016 / Published: 18 October 2016
Cited by 1 | Viewed by 1762 | PDF Full-text (6151 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Gout is caused by the overproduction of uric acid and the inefficient metabolism of dietary purines in humans. Current treatments of gout, which include anti-inflammatory drugs, cyclooxygenase-2 inhibitors, and systemic glucocorticoids, have harmful side-effects. Our research laboratory has recently introduced an innovative approach
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Gout is caused by the overproduction of uric acid and the inefficient metabolism of dietary purines in humans. Current treatments of gout, which include anti-inflammatory drugs, cyclooxygenase-2 inhibitors, and systemic glucocorticoids, have harmful side-effects. Our research laboratory has recently introduced an innovative approach for the decrystallization of biological and chemical crystals using the Metal-Assisted and Microwave-Accelerated Evaporative Decrystallization (MAMAD) technique. In the MAMAD technique, microwave energy is used to heat and activate gold nanoparticles that behave as “nano-bullets” to rapidly disrupt the crystal structure of biological crystals placed on planar surfaces. In this study, crystals of various sizes and compositions were studied as models for tophaceous gout at different stages (i.e., uric acid as small crystals (~10–100 μm) and l-alanine as medium (~300 μm) and large crystals (~4400 μm). Our results showed that the use of the MAMAD technique resulted in the reduction of the size and number of uric acid and l-alanine crystals up to >40% when exposed to intermittent microwave heating (up to 20 W power at 8 GHz) in the presence of 20 nm gold nanoparticles up to 120 s. This study demonstrates that the MAMAD technique can be potentially used as an alternative therapeutic method for the treatment of gout by effective decrystallization of large crystals, similar in size to those that often occur in gout. Full article
(This article belongs to the Special Issue Gold Nanoparticles for Biomedical Applications)
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