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Molecules, Volume 18, Issue 8 (August 2013), Pages 8712-10094

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Open AccessArticle Evaluation of Silica-H2SO4 as an Efficient Heterogeneous Catalyst for the Synthesis of Chalcones
Molecules 2013, 18(8), 10081-10094; https://doi.org/10.3390/molecules180810081
Received: 19 July 2013 / Revised: 5 August 2013 / Accepted: 7 August 2013 / Published: 20 August 2013
Cited by 12 | PDF Full-text (341 KB) | HTML Full-text | XML Full-text
Abstract
We report an efficient silica-H2SO4 mediated synthesis of a variety of chalcones that afforded the targeted compounds in very good yield compared to base catalyzed solvent free conditions as well as acid or base catalyzed refluxing conditions. Full article
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Open AccessArticle Modeling the Interaction of Dodecylphosphocholine Micelles with the Anticoccidial Peptide PW2 Guided by NMR Data
Molecules 2013, 18(8), 10056-10080; https://doi.org/10.3390/molecules180810056
Received: 19 July 2013 / Revised: 5 August 2013 / Accepted: 7 August 2013 / Published: 20 August 2013
Cited by 3 | PDF Full-text (1475 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Antimicrobial peptides are highly dynamic entities that acquire structure upon binding to a membrane interface. To better understand the structure and the mechanism for the molecular recognition of dodecylphosphocholine (DPC) micelles by the anticoccidial peptide PW2, we performed molecular dynamics (MD) simulations guided
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Antimicrobial peptides are highly dynamic entities that acquire structure upon binding to a membrane interface. To better understand the structure and the mechanism for the molecular recognition of dodecylphosphocholine (DPC) micelles by the anticoccidial peptide PW2, we performed molecular dynamics (MD) simulations guided by NMR experimental data, focusing on strategies to explore the transient nature of micelles, which rearrange on a millisecond to second timescale. We simulated the association of PW2 with a pre-built DPC micelle and with free-DPC molecules that spontaneously forms micelles in the presence of the peptide along the simulation. The simulation with spontaneous micelle formation provided the adequate environment which replicated the experimental data. The unrestrained MD simulations reproduced the NMR structure for the entire 100 ns MD simulation time. Hidden discrete conformational states could be described. Coulomb interactions are important for initial approximation and hydrogen bonds for anchoring the aromatic region at the interface, being essential for the stabilization of the interaction. Arg9 is strongly attached with phosphate. We observed a helix elongation process stabilized by the intermolecular peptide-micelle association. Full association that mimics the experimental data only happens after complete micelle re-association. Fast micelle dynamics without dissociation of surfactants leads to only superficial binding. Full article
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Open AccessCommunication Total Synthesis, Cytotoxic Effects of Damnacanthal, Nordamnacanthal and Related Anthraquinone Analogues
Molecules 2013, 18(8), 10042-10055; https://doi.org/10.3390/molecules180810042
Received: 22 May 2013 / Revised: 29 June 2013 / Accepted: 16 July 2013 / Published: 20 August 2013
Cited by 10 | PDF Full-text (317 KB) | HTML Full-text | XML Full-text
Abstract
Naturally occurring anthraquinones, damnacanthal (1) and nordamnacanthal (2) were synthesized with modified reaction steps and investigated for their cytotoxicity against the MCF-7 and K-562 cancer cell lines, respectively. Intermediate analogues 2-bromomethyl-1,3-dimethoxyanthraquinone (5, IC50 = 5.70 ±
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Naturally occurring anthraquinones, damnacanthal (1) and nordamnacanthal (2) were synthesized with modified reaction steps and investigated for their cytotoxicity against the MCF-7 and K-562 cancer cell lines, respectively. Intermediate analogues 2-bromomethyl-1,3-dimethoxyanthraquinone (5, IC50 = 5.70 ± 0.21 and 8.50 ± 1.18 mg/mL), 2-hydroxymethyl-1,3-dimethoxyanthraquinone (6, IC50 = 12.10 ± 0.14 and 14.00 ± 2.13), 2-formyl-1,3-dimethoxyantharquinone (7, IC50 = 13.10 ± 1.02 and 14.80 ± 0.74), 1,3-dimethoxy-2-methylanthraquinone (4, IC50 = 9.40 ± 3.51 and 28.40 ± 2.33), and 1,3-dihydroxy-2-methylanthraquinone (3, IC50 = 25.60 ± 0.42 and 28.40 ± 0.79) also exhibited moderate cytotoxicity against MCF-7 and K-562 cancer cell lines, respectively. Other structurally related compounds like 1,3-dihydroxyanthraquinone (13a, IC50 = 19.70 ± 0.35 and 14.50 ± 1.28), 1,3-dimethoxyanthraquinone (13b, IC50 = 6.50 ± 0.66 and 5.90 ± 0.95) were also showed good cytotoxicity. The target compound damnacanthal (1) was found to be the most cytotoxic against the MCF-7 and K-562 cancer cell lines, with IC50 values of 3.80 ± 0.57 and 5.50 ± 1.26, respectively. The structures of all compounds were elucidated with the help of detailed spectroscopic techniques. Full article
(This article belongs to the Section Organic Chemistry)
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Open AccessArticle Volatile Aroma Compounds in Various Brewed Green Teas
Molecules 2013, 18(8), 10024-10041; https://doi.org/10.3390/molecules180810024
Received: 18 July 2013 / Revised: 7 August 2013 / Accepted: 14 August 2013 / Published: 20 August 2013
Cited by 19 | PDF Full-text (289 KB) | HTML Full-text | XML Full-text
Abstract
This study identifies and semi-quantifies aroma volatiles in brewed green tea samples. The objectives of this study were to identify using a gas chromatograph-mass spectrometer (GC-MS) paired with a headspace solid-phase micro-extraction (HS-SPME) the common volatile compounds that may be responsible for aroma/flavor
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This study identifies and semi-quantifies aroma volatiles in brewed green tea samples. The objectives of this study were to identify using a gas chromatograph-mass spectrometer (GC-MS) paired with a headspace solid-phase micro-extraction (HS-SPME) the common volatile compounds that may be responsible for aroma/flavor of the brewed liquor of a range of green tea samples from various countries as consumed and to determine if green teas from the same region have similarities in volatile composition when green tea samples are prepared for consumption. Twenty-four green tea samples from eight different countries were brewed as recommended for consumer brewing. The aroma volatiles were extracted by HS-SPME, separated on a gas chromatograph and identified using a mass spectrometer. Thirty-eight compounds were identified and the concentrations were semi-quantified. The concentrations were lower than those reported by other researchers, probably because this research examined headspace volatiles from brewed tea rather than solvent extraction of leaves. No relationship to country of origin was found, which indicates that other factors have a greater influence than country of origin on aroma. Full article
(This article belongs to the Special Issue Flavors and Fragrances)
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Open AccessArticle Antianxiety-Like Effects of Chimpi (Dried Citrus Peels) in the Elevated Open-Platform Test
Molecules 2013, 18(8), 10014-10023; https://doi.org/10.3390/molecules180810014
Received: 16 July 2013 / Revised: 9 August 2013 / Accepted: 16 August 2013 / Published: 20 August 2013
Cited by 6 | PDF Full-text (258 KB) | HTML Full-text | XML Full-text
Abstract
Dried citrus peels (Chimpi) is one of the most common natural medicines with qi (energy flow) rectifying and shi (dampness) drying actions, which originates from Citrus unshiu, and/or C. reticulata according to the definition of the pharmacopoeiae of Japan and China.
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Dried citrus peels (Chimpi) is one of the most common natural medicines with qi (energy flow) rectifying and shi (dampness) drying actions, which originates from Citrus unshiu, and/or C. reticulata according to the definition of the pharmacopoeiae of Japan and China. In this study, the pharmacological effects of their extracts and major chemical constituents hesperidin and its aglycone hesperetin on anxiety were examined with an anxiety model of elevated open-platform test using ICR male mice (6-week-old) and total duration of freezing was decreased in fluoxetine-treated mice, which is a simple and highly sensitive to the effects of serotonergic anxiolytics. Moreover, yokukansankachimpihange (YKH), a combination of yokukansan with Chimpi and Hange (Pinellia) was also examined because Chimpi is considered to play a crucial part in this formula against anxious symptoms in dementia patients. The results showed that Chimpi and YKH possess a significant anxiolytic-like effect similar to that of fluoxetine, suggesting that they might be similar to fluoxetine in their pharmacological actions through the serotonergic neurotransmission pathway. Moreover, it also suggested that the major chemical constituent, hesperidin could be an active principle attributed to the antianxiety-like effects with a direct and indirect role via its aglycone hesperetin. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Combination of Small Molecule Microarray and Confocal Microscopy Techniques for Live Cell Staining Fluorescent Dye Discovery
Molecules 2013, 18(8), 9999-10013; https://doi.org/10.3390/molecules18089999
Received: 26 June 2013 / Revised: 13 August 2013 / Accepted: 14 August 2013 / Published: 20 August 2013
Cited by 4 | PDF Full-text (4706 KB) | HTML Full-text | XML Full-text
Abstract
Discovering new fluorochromes is significantly advanced by high-throughput screening (HTS) methods. In the present study a combination of small molecule microarray (SMM) prescreening and confocal laser scanning microscopy (CLSM) was developed in order to discover novel cell staining fluorescent dyes. Compounds with high
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Discovering new fluorochromes is significantly advanced by high-throughput screening (HTS) methods. In the present study a combination of small molecule microarray (SMM) prescreening and confocal laser scanning microscopy (CLSM) was developed in order to discover novel cell staining fluorescent dyes. Compounds with high native fluorescence were selected from a 14,585-member library and further tested on living cells under the microscope. Eleven compartment-specific, cell-permeable (or plasma membrane-targeted) fluorochromes were identified. Their cytotoxicity was tested and found that between 1–10 micromolar range, they were non-toxic even during long-term incubations. Full article
(This article belongs to the Special Issue Reagents and Methods for Protein Target Identification)
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Open AccessArticle Enantio- and Periselective Nitroalkene Diels-Alder Reactions Catalyzed by Helical-Chiral Hydrogen Bond Donor Catalysts
Molecules 2013, 18(8), 9982-9998; https://doi.org/10.3390/molecules18089982
Received: 15 July 2013 / Revised: 13 August 2013 / Accepted: 14 August 2013 / Published: 19 August 2013
PDF Full-text (623 KB) | HTML Full-text | XML Full-text
Abstract
Helical-chiral double hydrogen bond donor catalysts promote the nitroalkene Diels-Alder reaction in an enantio- and periselective manner. This represents the first asymmetric catalytic nitroalkene Diels-Alder reaction via LUMO-lowering catalysis. To gain an insight into this new process, the substrate scope of our catalyst
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Helical-chiral double hydrogen bond donor catalysts promote the nitroalkene Diels-Alder reaction in an enantio- and periselective manner. This represents the first asymmetric catalytic nitroalkene Diels-Alder reaction via LUMO-lowering catalysis. To gain an insight into this new process, the substrate scope of our catalyst was investigated by exploiting readily available 5-substituted pentamethylcyclopentadienes. The catalyst was found to tolerate dienes with different steric demands as well as dienes substituted with heteroatoms. The synthetic utility of 5-substituted pentamethylcyclopentadienes is rather limited, and thus we have developed a three-step route to 1,4,5,5-tetrasubstituted cyclopentadienes from commercially available ketones. Full article
(This article belongs to the Special Issue Asymmetric Catalysis)
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Open AccessArticle Anti-Lung Cancer Activity through Enhancement of Immunomodulation and Induction of Cell Apoptosis of Total Triterpenes Extracted from Ganoderma luncidum (Leyss. ex Fr.) Karst.
Molecules 2013, 18(8), 9966-9981; https://doi.org/10.3390/molecules18089966
Received: 14 June 2013 / Revised: 2 August 2013 / Accepted: 13 August 2013 / Published: 19 August 2013
Cited by 11 | PDF Full-text (592 KB) | HTML Full-text | XML Full-text
Abstract
Ganoderma luncidum (Leyss. ex Fr.) Karst. (GLK) has been used traditionally for the prevention and treatment of cancers or tumors for a long time in Traditional Chinese Medicine. The triterpenes as main effective components of GLK have been found to be beneficial for
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Ganoderma luncidum (Leyss. ex Fr.) Karst. (GLK) has been used traditionally for the prevention and treatment of cancers or tumors for a long time in Traditional Chinese Medicine. The triterpenes as main effective components of GLK have been found to be beneficial for the efficacy. The purpose of this study was to examine the anti-lung cancer activity of triterpenes of GLK in vitro and in vivo and to explore their anti-lung cancer effects and potential mechanisms. A549 cells and Lewis tumor-bearing mice were used to evaluate the inhibition effects of triterpenes on cell proliferation and tumor growth. The IC50 of triterpenes of GLK on A549 cells was 24.63 μg/mL. Triterpenes of GLK could significantly inhibit tumor growth in mice (30, 60 and 120 mg/kg). The immune organs indexes including spleen and thymus were increased remarkedly by the treatment with triterpenes. Moreover, they were able to stimulate the immune response by increasing the expressions of IL-6 and TNF-α. Flow cytometric analysis revealed that cell arrest caused by triterpenes treatment (7.5, 15 and 30 μg/mL) was in the G2/M phase in A549 cells. Triterpenes induced apoptosis by decreasing the expression of the antiapoptotic protein Bcl-2 and pro-caspase 9 and increasing the levels of cleaved-caspase 9. Our findings suggested that the triterpenes of GLK have anti-lung cancer activity in vitro and in vivo via enhancement of immunomodulation and induction of cell apoptosis. The study provides insights into the mechanism of GLK in the prevention and treatment of lung cancer. Full article
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Open AccessArticle Neuroprotective, Anti-Amyloidogenic and Neurotrophic Effects of Apigenin in an Alzheimer’s Disease Mouse Model
Molecules 2013, 18(8), 9949-9965; https://doi.org/10.3390/molecules18089949
Received: 21 June 2013 / Revised: 31 July 2013 / Accepted: 6 August 2013 / Published: 19 August 2013
Cited by 44 | PDF Full-text (607 KB) | HTML Full-text | XML Full-text
Abstract
Alzheimer’s disease (AD) is a neurodegenerative disorder characterized by extracellular senile plaques and intracellular neurofibrillary tangles in the brain. Amyloid-β peptides (Aβ) are considered to play a critical role in the onset and progression of AD. Apigenin (4',5,7-trihydroxyflavone) is a pharmacologically active agent.
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Alzheimer’s disease (AD) is a neurodegenerative disorder characterized by extracellular senile plaques and intracellular neurofibrillary tangles in the brain. Amyloid-β peptides (Aβ) are considered to play a critical role in the onset and progression of AD. Apigenin (4',5,7-trihydroxyflavone) is a pharmacologically active agent. Even though some evidence suggests that it has potential neuroprotective effects, no preexisting study has reported any therapeutic effects of apigenin in AD models. In the present study, we examined the effects of apigenin on cognitive function in APP/PS1 double transgenic AD mice and explored its mechanism(s) of action. Three-month oral treatment with apigenin rescued learning deficits and relieved memory retention in APP/PS1 mice. Apigenin also showed effects affecting APP processing and preventing Aβ burden due to the down-regulation of BACE1 and β-CTF levels, the relief of Aβ deposition, and the decrease of insoluble Aβ levels. Moreover, apigenin exhibited superoxide anion scavenging effects and improved antioxidative enzyme activity of superoxide dismutase and glutathione peroxidase. In addition, apigenin restored neurotrophic ERK/CREB/BDNF pathway in the cerebral cortex. In conclusion, apigenin may ameliorate AD-associated learning and memory impairment through relieving Aβ burden, suppressing amyloidogenic process, inhibiting oxidative stress, and restoring ERK/CREB/BDNF pathway. Therefore, apigenin appears to represent an alternative medication for the prevention and/or therapy of AD. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Characterization and Bioactivity of Polysaccharides Obtained from Pine Cones of Pinus koraiensis by Graded Ethanol Precipitation
Molecules 2013, 18(8), 9933-9948; https://doi.org/10.3390/molecules18089933
Received: 8 June 2013 / Revised: 14 August 2013 / Accepted: 15 August 2013 / Published: 19 August 2013
Cited by 15 | PDF Full-text (284 KB) | HTML Full-text | XML Full-text
Abstract
Pinus koraiensis polysaccharides (PKP) were extracted by hot water from P. koraiensis pine cones. Five polysaccharide fractions named PKP-A, PKP-B, PKP-C, PKP-D and PKP-E were successfully separated at final ethanol concentrations of 30%, 50%, 60%, 70% and 80%, respectively. HPLC, FT-IR, GC-MS and
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Pinus koraiensis polysaccharides (PKP) were extracted by hot water from P. koraiensis pine cones. Five polysaccharide fractions named PKP-A, PKP-B, PKP-C, PKP-D and PKP-E were successfully separated at final ethanol concentrations of 30%, 50%, 60%, 70% and 80%, respectively. HPLC, FT-IR, GC-MS and automatic amino-acid analysis were applied to investigate their chemical characteristics. Monosaccharide component analysis indicated that the five fractions were all composed of d-ribose, l-rhamnose, l-arabinose, d-xylose, d-mannose, d-glucose and d-galactose, but their molar ratios were quite different. HPLC results revealed that the polysaccharides precipitated by higher concentrations of ethanol solution had lower molecular masses. Moreover, the antioxidant activities of the five fractions were studied on the basis of hydroxyl radical and ABTS radical scavenging tests. The five graded polysaccharide fractions exhibited good inhibitory power, and MTT tests in vitro showed the IC50 of PKP-A and PKP-E were 1,072.5 and 2,070.0 μg·mL−1, respectively. These results demonstrated that the PKP could be a potential source of natural antioxidants or dietary supplements. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Chemistry and Antiviral Activity of Arrabidaea pulchra (Bignoniaceae)
Molecules 2013, 18(8), 9919-9932; https://doi.org/10.3390/molecules18089919
Received: 26 April 2013 / Revised: 22 July 2013 / Accepted: 24 July 2013 / Published: 16 August 2013
Cited by 7 | PDF Full-text (907 KB) | HTML Full-text | XML Full-text
Abstract
The aim of the present work was to carry out a bioguided isolation of antiviral chemical constituents from an ethanol extract of leaves from Arrabidaea pulchra (Cham.) Sandwith (EEAPL) that had shown in vitro activity in a previous screening using DNA and RNA
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The aim of the present work was to carry out a bioguided isolation of antiviral chemical constituents from an ethanol extract of leaves from Arrabidaea pulchra (Cham.) Sandwith (EEAPL) that had shown in vitro activity in a previous screening using DNA and RNA viruses. The activity of EEPAL was evaluated against the DNA viruses Human herpesvirus 1 (HSV-1) and Vaccinia virus Western Reserve (VACV-WR) as well as against the RNA viruses Murine encephalomyocarditis virus (EMCV), and Dengue virus 2 (DENV-2) by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) colorimetric assay. Cytotoxicity was determined in LLCMK2 and Vero cells and the Selectivity Indexes (SI) were calculated. The most potent effect was observed against DENV-2 (EC50 46.8 ± 1.6 µg mL−1; SI 2.7). For HSV-1 and VACV-WR EC50 values > 200 µg mL−1 were determined, while no inhibition of the cytopathic effect was observed with EMCV. Bioguided fractionation of EEAPL by partition between immiscible solvents followed by chromatography over a Sephadex LH20 column afforded two arylpropanoid glycosides, verbascoside (AP 1) and caffeoylcalleryanin (AP 2), along with a terpenoid, ursolic acid (AP 3). AP 1 and AP 3 exhibited similar anti-DENV-2 profiles, with SI values of 3.8 and 3.1, respectively, while AP 2 was the most effective anti-DENV-2 constituent, with a SI of 20.0. Our results show that A. pulchra leaves ethanol extract (EEAPL) affords compounds with antiviral activity, mainly against DENV-2. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Kinetics of Nitric Oxide and Oxygen Gases on Porous Y-Stabilized ZrO2-Based Sensors
Molecules 2013, 18(8), 9901-9918; https://doi.org/10.3390/molecules18089901
Received: 15 July 2013 / Revised: 8 August 2013 / Accepted: 13 August 2013 / Published: 16 August 2013
Cited by 4 | PDF Full-text (1926 KB) | HTML Full-text | XML Full-text
Abstract
Using impedance spectroscopy the electrical response of sensors with various porous Y-stabilized ZrO2 (YSZ) microstructures was measured for gas concentrations containing 0–100 ppm NO with 10.5%O2 at temperatures ranging from 600–700 °C. The impedance response increased substantially as the sensor porosity
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Using impedance spectroscopy the electrical response of sensors with various porous Y-stabilized ZrO2 (YSZ) microstructures was measured for gas concentrations containing 0–100 ppm NO with 10.5%O2 at temperatures ranging from 600–700 °C. The impedance response increased substantially as the sensor porosity increased from 46%–50%. Activation energies calculated based on data from the impedance measurements increased in magnitude (97.4–104.9 kJ/mol for 100 ppm NO) with respect to increasing YSZ porosity. Analysis of the oxygen partial pressure dependence of the sensors suggested that dissociative adsorption was the dominant rate limiting. The PWC/DNP theory level was used to investigate the gas-phase energy barrier of the 2NO+O2→2NO2 reaction on a 56-atom YSZ/Au model cluster using Density Functional Theory and Linear Synchronous Transit/Quadratic Synchronous Transit calculations. The reaction path shows oxygen surface reactions that begin with NO association with adsorbed O2 on a Zr surface site, followed by O2 dissociative adsorption, atomic oxygen diffusion, and further NO2 formation. The free energy barrier was calculated to be 181.7 kJ/mol at PWC/DNP. A qualitative comparison with the extrapolated data at 62% ± 2% porosity representing the YSZ model cluster indicates that the calculated barriers are in reasonable agreement with experiments, especially when the RPBE functional is used. Full article
(This article belongs to the Special Issue Gas Phase Reactions)
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Open AccessReview Breathing Some New Life into an Old Topic: Chalcogen-Nitrogen π-Heterocycles as Electron Acceptors
Molecules 2013, 18(8), 9850-9900; https://doi.org/10.3390/molecules18089850
Received: 3 July 2013 / Revised: 13 August 2013 / Accepted: 14 August 2013 / Published: 16 August 2013
Cited by 44 | PDF Full-text (2445 KB) | HTML Full-text | XML Full-text
Abstract
Recent progress in the design, synthesis and characterization of chalcogen-nitrogen π-heterocycles, mostly 1,2,5-chalcogenadiazoles (chalcogen: S, Se and Te) and their fused derivatives, possessing positive electron affinity is discussed together with their use in preparation of charge-transfer complexes and radical-anion salts—candidate building blocks of
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Recent progress in the design, synthesis and characterization of chalcogen-nitrogen π-heterocycles, mostly 1,2,5-chalcogenadiazoles (chalcogen: S, Se and Te) and their fused derivatives, possessing positive electron affinity is discussed together with their use in preparation of charge-transfer complexes and radical-anion salts—candidate building blocks of molecule-based electrical and magnetic functional materials. Full article
(This article belongs to the Special Issue Chalcogen-Nitrogen Chemistry)
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Open AccessArticle ADIBO-Based “Click” Chemistry for Diagnostic Peptide Micro-Array Fabrication: Physicochemical and Assay Characteristics
Molecules 2013, 18(8), 9833-9849; https://doi.org/10.3390/molecules18089833
Received: 1 July 2013 / Revised: 25 July 2013 / Accepted: 6 August 2013 / Published: 16 August 2013
Cited by 12 | PDF Full-text (1150 KB) | HTML Full-text | XML Full-text
Abstract
Several azide-derivatized and fluorescently-labeled peptides were immobilized on azadibenzocyclooctyne (ADIBO)-activated slide surfaces via a strain-promoted alkyne-azide cycloaddition (SPAAC) reaction revealing excellent immobilization kinetics, good spot homogeneities and reproducible fluorescence signal intensities. A myc-peptide micro-array immunoassay showed an antibody limit-of-detection (LOD) superior to
[...] Read more.
Several azide-derivatized and fluorescently-labeled peptides were immobilized on azadibenzocyclooctyne (ADIBO)-activated slide surfaces via a strain-promoted alkyne-azide cycloaddition (SPAAC) reaction revealing excellent immobilization kinetics, good spot homogeneities and reproducible fluorescence signal intensities. A myc-peptide micro-array immunoassay showed an antibody limit-of-detection (LOD) superior to a microtiter plate-based ELISA. Bovine serum albumin (BSA) and dextran covalently attached via “click” chemistry more efficiently reduced non-specific binding (NSB) of fluorescently-labeled IgG to the microarray surface in comparison to immobilized hexanoic acid and various types of polyethylene glycol (PEG) derivatives. Confirmation of these findings via further studies with other proteins and serum components could open up new possibilities for human sample and microarray platform-based molecular diagnostic tests. Full article
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Open AccessArticle Eco-Friendly Synthesis and Antiproliferative Evaluation of Some Oxygen Substituted Diaryl Ketones
Molecules 2013, 18(8), 9818-9832; https://doi.org/10.3390/molecules18089818
Received: 26 June 2013 / Revised: 5 August 2013 / Accepted: 12 August 2013 / Published: 16 August 2013
Cited by 9 | PDF Full-text (320 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
A broad variety of oxygen-substituted diaryl ketones has been synthesized by solar energy-induced Friedel Crafts acylations of 1,4-benzo- and 1,4-naphthoquinones with benzaldehydes. The in vitro antiproliferative properties of the photoproducts were assessed on prostate (DU-145), bladder (T24) and breast (MCF7) human-derived tumor cell
[...] Read more.
A broad variety of oxygen-substituted diaryl ketones has been synthesized by solar energy-induced Friedel Crafts acylations of 1,4-benzo- and 1,4-naphthoquinones with benzaldehydes. The in vitro antiproliferative properties of the photoproducts were assessed on prostate (DU-145), bladder (T24) and breast (MCF7) human-derived tumor cell lines and compared to non-tumor mouse fibroblasts (Balb/3T3). Among the tested compounds, it was found that those containing a 3,4,5-trimethoxyphenyl A-ring, such as 12 and 22 are more active on DU-145, with EC50 values of 1.2 and 5.9 μM, respectively. By comparing their effects on the three cancer cell lines, the analogue 22 has the best mean selective index (2.4). Full article
(This article belongs to the Section Organic Chemistry)
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