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Molecules, Volume 20, Issue 3 (March 2015), Pages 3496-5259

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Open AccessArticle Bacillus toyonensis Strain AEMREG6, a Bacterium Isolated from South African Marine Environment Sediment Samples Produces a Glycoprotein Bioflocculant
Molecules 2015, 20(3), 5239-5259; https://doi.org/10.3390/molecules20035239
Received: 26 February 2015 / Revised: 15 March 2015 / Accepted: 17 March 2015 / Published: 23 March 2015
Cited by 16 | PDF Full-text (1720 KB) | HTML Full-text | XML Full-text
Abstract
A bioflocculant-producing bacteria, isolated from sediment samples of a marine environment in the Eastern Cape Province of South Africa demonstrated a flocculating activity above 60% for kaolin clay suspension. Analysis of the 16S ribosomal deoxyribonucleic acid (rDNA) nucleotide sequence of the isolate in
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A bioflocculant-producing bacteria, isolated from sediment samples of a marine environment in the Eastern Cape Province of South Africa demonstrated a flocculating activity above 60% for kaolin clay suspension. Analysis of the 16S ribosomal deoxyribonucleic acid (rDNA) nucleotide sequence of the isolate in the GenBank database showed 99% similarity to Bacillus toyonensis strain BCT-7112 and it was deposited in the GenBank as Bacillus toyonensis strain AEMREG6 with accession number KP406731. The bacteria produced a bioflocculant (REG-6) optimally in the presence of glucose and NH4NO3 as the sole carbon and nitrogen source, respectively, initial medium pH of 5 and Ca2+ as the cation of choice. Chemical analysis showed that purified REG-6 was a glycoprotein mainly composed of polysaccharide (77.8%) and protein (11.5%). It was thermally stable and had strong flocculating activity against kaolin suspension over a wide range of pH values (3–11) with a relatively low dosage requirement of 0.1 mg/mL in the presence of Mn2+. Fourier transform infrared spectroscopy (FTIR) revealed the presence of hydroxyl, carboxyl and amide groups preferred for flocculation. Scanning electron microscopy (SEM) revealed that bridging was the main flocculation mechanism of REG-6. The outstanding flocculating performance of REG-6 holds great potential to replace the hazardous chemical flocculants currently used in water treatment. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Effect of Pulsed Electric Fields on the Flavour Profile of Red-Fleshed Sweet Cherries (Prunus avium var. Stella)
Molecules 2015, 20(3), 5223-5238; https://doi.org/10.3390/molecules20035223
Received: 25 November 2014 / Revised: 25 February 2015 / Accepted: 10 March 2015 / Published: 23 March 2015
Cited by 4 | PDF Full-text (1000 KB) | HTML Full-text | XML Full-text
Abstract
The aim of this research was to study the effect of pulsed electric fields (PEF) on the flavour profile of red-fleshed sweet cherries (Prunus avium variety Stella). The cherry samples were treated at a constant pulse frequency of 100 Hz, a constant
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The aim of this research was to study the effect of pulsed electric fields (PEF) on the flavour profile of red-fleshed sweet cherries (Prunus avium variety Stella). The cherry samples were treated at a constant pulse frequency of 100 Hz, a constant pulse width of 20 μs, different electric field strengths between 0.3 and 2.5 kV/cm and specific energy ranging from 31 to 55 kJ/kg. Volatile compounds of samples were analysed using an automated headspace solid phase microextraction (HS–SPME) method coupled with gas chromatography-mass spectrometry (GC–MS). A total of 33 volatile compounds were identified with benzaldehyde, hexanal, (E)-2-hexenal, (Z)-2-hexen-1-ol, and benzyl alcohol being the predominant volatiles in different PEF-treated samples. Aldehydes namely butanal, octanal, 2-octenal, and nonanal, and (Z)-2-hexen-1-ol increased significantly 24 h after PEF treatment at electric field strengths of more than 1.0 kV/cm. Samples incubated for 24 h after PEF treatment (S3) generated higher concentrations of volatiles than samples immediately after PEF treatments (S2). Quantitative results revealed that more flavour volatiles were released and associated with S3 samples after 24 h storage and S2 samples immediately after PEF both with the highest electric field intensities. Interestingly, this study found that the PEF treatments at the applied electric field strength and energy did not result in releasing/producing undesirable flavour compounds. Full article
(This article belongs to the Special Issue Aromas and Volatiles of Fruits)
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Open AccessArticle iso-Petromyroxols: Novel Dihydroxylated Tetrahydrofuran Enantiomers from Sea Lamprey (Petromyzon marinus)
Molecules 2015, 20(3), 5215-5222; https://doi.org/10.3390/molecules20035215
Received: 17 February 2015 / Revised: 17 March 2015 / Accepted: 18 March 2015 / Published: 23 March 2015
Cited by 3 | PDF Full-text (959 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
An enantiomeric pair of new fatty acid-derived hydroxylated tetrahydrofurans, here named iso-petromyroxols, were isolated from sea lamprey larvae-conditioned water. The relative configuration of iso-petromyroxol was elucidated with 1D and 2D NMR spectroscopic analyses. The ratio of enantiomers (er) in
[...] Read more.
An enantiomeric pair of new fatty acid-derived hydroxylated tetrahydrofurans, here named iso-petromyroxols, were isolated from sea lamprey larvae-conditioned water. The relative configuration of iso-petromyroxol was elucidated with 1D and 2D NMR spectroscopic analyses. The ratio of enantiomers (er) in the natural sample was measured by chiral-HPLC-MS/MS to be ca. 3:1 of (–)- to (+)-antipodes. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Selective C-Arylation of 2,5-Dibromo-3-hexylthiophene via Suzuki Cross Coupling Reaction and Their Pharmacological Aspects
Molecules 2015, 20(3), 5202-5214; https://doi.org/10.3390/molecules20035202
Received: 4 December 2014 / Revised: 6 February 2015 / Accepted: 16 February 2015 / Published: 23 March 2015
Cited by 5 | PDF Full-text (865 KB) | HTML Full-text | XML Full-text
Abstract
The present study reports the synthesis of various new derivatives based on 5-aryl-2-bromo-3-hexylthiophene with moderate-to-good yields via a palladium-catalyzed Suzuki cross-coupling reaction. This coupling method involved the reaction of 2,5-dibromo-3-hexylthiophene with several arylboronic acids in order to synthesize corresponding thiophene derivatives under controlled
[...] Read more.
The present study reports the synthesis of various new derivatives based on 5-aryl-2-bromo-3-hexylthiophene with moderate-to-good yields via a palladium-catalyzed Suzuki cross-coupling reaction. This coupling method involved the reaction of 2,5-dibromo-3-hexylthiophene with several arylboronic acids in order to synthesize corresponding thiophene derivatives under controlled and optimal reaction conditions. The different substituents (CH3, OCH3, Cl, F etc.) present on arylboronic acids are found to have significant electronic effects on the overall properties of new products. The synthesized thiophene molecules were studied for their haemolytic, biofilm inhibition and anti-thrombolytic activities, and almost all products showed potentially good properties. The compound 2-bromo-5-(3-chloro-4-fluorophenyl)-3-hexylthiophenein particular exhibited the highest values for haemolytic and bio-film inhibition activities among all newly synthesized derivatives. In addition, the compound 2-bromo-3-hexyl-5-(4-iodophenyl)thiophene also showed high anti-thrombolytic activity, suggesting the potential medicinal applications of these newly synthesized compounds. Full article
(This article belongs to the Section Medicinal Chemistry)
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Open AccessArticle Syntheses of Nickel (II) Complexes from Novel Semicarbazone Ligands with Chloroformylarylhydrazine, Benzimidazole and Salicylaldehyde Moieties
Molecules 2015, 20(3), 5184-5201; https://doi.org/10.3390/molecules20035184
Received: 30 January 2015 / Revised: 11 March 2015 / Accepted: 13 March 2015 / Published: 20 March 2015
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Abstract
This study addressed the design and syntheses of diverse ligands, which were then successfully treated with Ni (II) ion to afford a series of nickel complexes. α-Chloroformylarylhydrazine hydrochlorides 6 contain two different functional groups. One is a strong nucleophile, and the other is
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This study addressed the design and syntheses of diverse ligands, which were then successfully treated with Ni (II) ion to afford a series of nickel complexes. α-Chloroformylarylhydrazine hydrochlorides 6 contain two different functional groups. One is a strong nucleophile, and the other is a good electrophile. Therefore, it can be designed to react with several reagents to obtain diverse derivatives which can be used as ligands for metal complexes. Furthermore, benzimidazole and salicylaldehyde can provide electron donor sites, N and O electron donors, separately. Hence, the starting materials α-chloroformylarylhydrazine hydrochlorides 6 were first treated with 2-(aminomethyl)-benzimidazole (7) to give the corresponding semicarbazides 8. Then, the semicarbazides 8 reacted with various substituted salicylaldehydes 911 to afford the desired substituted-salicylaldehyde 2-aryl-4-substituted semicarbazones 1214, which could coordinate with nickel (II) ion to give the corresponding nickel complexes 1517. Full article
(This article belongs to the Section Organic Chemistry)
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Open AccessArticle Influence of Pea Protein Aggregates on the Structure and Stability of Pea Protein/Soybean Polysaccharide Complex Emulsions
Molecules 2015, 20(3), 5165-5183; https://doi.org/10.3390/molecules20035165
Received: 28 November 2014 / Revised: 14 March 2015 / Accepted: 16 March 2015 / Published: 20 March 2015
Cited by 9 | PDF Full-text (2473 KB) | HTML Full-text | XML Full-text
Abstract
The applications of plant proteins in the food and beverage industry have been hampered by their precipitation in acidic solution. In this study, pea protein isolate (PPI) with poor dispersibility in acidic solution was used to form complexes with soybean soluble polysaccharide (SSPS),
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The applications of plant proteins in the food and beverage industry have been hampered by their precipitation in acidic solution. In this study, pea protein isolate (PPI) with poor dispersibility in acidic solution was used to form complexes with soybean soluble polysaccharide (SSPS), and the effects of PPI aggregates on the structure and stability of PPI/SSPS complex emulsions were investigated. Under acidic conditions, high pressure homogenization disrupts the PPI aggregates and the electrostatic attraction between PPI and SSPS facilitates the formation of dispersible PPI/SSPS complexes. The PPI/SSPS complex emulsions prepared from the PPI containing aggregates prove to possess similar droplet structure and similar stability compared with the PPI/SSPS emulsions produced from the PPI in which the aggregates have been previously removed by centrifugation. The oil droplets are protected by PPI/SSPS complex interfacial films and SSPS surfaces. The emulsions show long-term stability against pH and NaCl concentration changes. This study demonstrates that PPI aggregates can also be used to produce stable complex emulsions, which may promote the applications of plant proteins in the food and beverage industry. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Reduction of False Positives in Structure-Based Virtual Screening When Receptor Plasticity Is Considered
Molecules 2015, 20(3), 5152-5164; https://doi.org/10.3390/molecules20035152
Received: 5 February 2015 / Revised: 9 March 2015 / Accepted: 16 March 2015 / Published: 19 March 2015
Cited by 6 | PDF Full-text (2414 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Structure-based virtual screening for selecting potential drug candidates is usually challenged by how numerous false positives in a molecule library are excluded when receptor plasticity is considered. In this study, based on the binding energy landscape theory, a hypothesis that a true inhibitor
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Structure-based virtual screening for selecting potential drug candidates is usually challenged by how numerous false positives in a molecule library are excluded when receptor plasticity is considered. In this study, based on the binding energy landscape theory, a hypothesis that a true inhibitor can bind to different conformations of the binding site favorably was put forth, and related strategies to defeat this challenge were devised; reducing false positives when receptor plasticity is considered. The receptor in the study is the influenza A nucleoprotein, whose oligomerization is a requirement for RNA binding. The structural flexibility of influenza A nucleoprotein was explored by molecular dynamics simulations. The resultant distinctive structures and the crystal structure were used as receptor models in docking exercises in which two binding sites, the tail-loop binding pocket and the RNA binding site, were targeted with the Otava PrimScreen1 diversity-molecule library using the GOLD software. The intersection ligands that were listed in the top-ranked molecules from all receptor models were selected. Such selection strategy successfully distinguished high-affinity and low-affinity control molecules added to the molecule library. This work provides an applicable approach for reducing false positives and selecting true ligands from molecule libraries. Full article
(This article belongs to the Special Issue Molecular Docking in Drug Design)
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Open AccessArticle Antiviral Activity of a Nanoemulsion of Polyprenols from Ginkgo Leaves against Influenza A H3N2 and Hepatitis B Virus in Vitro
Molecules 2015, 20(3), 5137-5151; https://doi.org/10.3390/molecules20035137
Received: 4 December 2014 / Revised: 2 March 2015 / Accepted: 10 March 2015 / Published: 19 March 2015
Cited by 2 | PDF Full-text (2204 KB) | HTML Full-text | XML Full-text
Abstract
In order to improve the bioavailability levels of polyprenols (derived from ginkgo leaves (GBP)) in the human body, a GBP nanoemulsion was prepared, and its antiviral activity was evaluated against influenza A H3N2 and hepatitis B virus in vitro. Methods: A GBP
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In order to improve the bioavailability levels of polyprenols (derived from ginkgo leaves (GBP)) in the human body, a GBP nanoemulsion was prepared, and its antiviral activity was evaluated against influenza A H3N2 and hepatitis B virus in vitro. Methods: A GBP nanoemulsion was prepared by inversed-phase emulsification (IPE). Next, we investigated the antiviral activity of the GBP nanoemulsion on influenza A H3N2 and hepatitis B virus in vitro by the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenlytetrezolium bromide) method. ELISA and the fluorescent quantitative PCR method were used to measure the content of HBsAg, HBeAg and DNA virus in human samples. Results: The GBP nanoemulsion exhibited uniformity at an average particle size 97 nm with a hydrophilic-lipophilic balance (HLB) of 9.5. GBP is non-toxic to normal cells, hepatitis B virus DNA, hepatitis B virus antigen and HepG2215. Furthermore, GBP could reach a 70% virucidal activity and a 74.9% protection rate (*** p < 0.001) on MDCK cells infected with H3N2 virus at a high concentration of 100 μg/mL. GBP had a good inhibition rate on HBsAg (52.11%, ** p < 0.01) at 50 μg/mL and Day 9 of incubation, and a 67.32% inhibition effect on HBeAg at a high concentration of 100 μg/mL and Day 9. GBP had good inhibition on HBV DNA with CT 18.6 and lower copies (** p < 0.01) at a middle concentration of 12.5 to 25 μg/mL. Conclusions: The GBP nanoemulsion was very stable and non-toxic and had very strong antiviral activity against influenza A H3N2 and hepatitis B virus in vitro. The inhibitory effects and reactive mechanisms were similar to the drug, 3TC; by lengthening the incubation time and increasing the drug concentration, GBP has promising potential as an antiviral drug. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Functional Characterization of Individual- and Mixed-Burgundian Saccharomyces cerevisiae Isolates for Fermentation of Pinot Noir
Molecules 2015, 20(3), 5112-5136; https://doi.org/10.3390/molecules20035112
Received: 8 January 2015 / Revised: 25 February 2015 / Accepted: 9 March 2015 / Published: 19 March 2015
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Abstract
Pinot noir has traditionally been fermented by native flora of multiple yeasts producing a complex combination of aromas and flavors. With the use of industrial dry yeasts, winemakers gained enological reliability and consistency in their wines, but lost diversity and complexity. This research
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Pinot noir has traditionally been fermented by native flora of multiple yeasts producing a complex combination of aromas and flavors. With the use of industrial dry yeasts, winemakers gained enological reliability and consistency in their wines, but lost diversity and complexity. This research evaluated the use of co-culturing yeasts to fulfill this dual role. Fermentations of Burgundian Saccharomyces cerevisiae isolates and their mixtures were evaluated for their enological characteristics and production of volatile compounds, at 22 °C and 27 °C. The novel isolates were genetically unique and enologically equivalent to the industrial strains. Analysis of variance and principal component analysis of 25 headspace volatiles revealed differences among the yeasts and between the fermentation temperatures. Wines from the mixed-Burgundian isolates were most similar to one another and could be differentiated from the industrial strains at both 22 °C and 27 °C. Mixed-Burgundian wines at both temperatures had higher concentrations of ethyl esters and acetate esters, compared to the industrial strains which had higher concentrations of higher alcohols at 27 °C and higher concentration of other ethyl esters at 22 °C. Given the unique profiles of the co-cultured wines, this research offers winemakers a strategy for producing wines with unique and more complex characters without the risk of spontaneous fermentations. Full article
(This article belongs to the collection Wine Chemistry)
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Open AccessArticle Docking and Antiherpetic Activity of 2-Aminobenzo[de]-isoquinoline-1,3-diones
Molecules 2015, 20(3), 5099-5111; https://doi.org/10.3390/molecules20035099
Received: 27 January 2015 / Accepted: 9 March 2015 / Published: 19 March 2015
Cited by 4 | PDF Full-text (1044 KB) | HTML Full-text | XML Full-text
Abstract
As part of our search for new compounds having antiviral effects, the prepared 2-aminonaphthalimide series was examined for its activity against the herpes simplex viruses HSV-1 and HSV-2. This represents the first study of the antiviral effects of this class of compounds. The
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As part of our search for new compounds having antiviral effects, the prepared 2-aminonaphthalimide series was examined for its activity against the herpes simplex viruses HSV-1 and HSV-2. This represents the first study of the antiviral effects of this class of compounds. The new series of 2-amino-1H-benzo[de]isoquinoline-1,3-diones was examined against HSV-1 and HSV-2 using a cytopathic effect inhibition assay. In terms of effective concentration (EC50), furaldehyde, thiophene aldehyde and allyl isothiocyanide derivatives 1416 showed potent activity against HSV-1 (EC50 = 19.6, 16.2 and 17.8 μg/mL), compared to acyclovir as a reference drug (EC50 = 1.8 μg/mL). Moreover, 14 and 15 were found to exhibit valuable activity against HSV-2. Many of the tested compounds demonstrated weak to moderate EC50 values relative to their inactive parent compound (2-amino-1H-benzo[de]isoquinoline-1,3-dione), while compounds 7, 9, 13, 14, 15, 16, 21 and 22 were the most active set of antiviral compounds throughout this study. The cytotoxicity (CC50), EC50, and the selectivity index (SI) values were determined. In a molecular docking study, the ligand-receptor interactions of compounds 124 and their parent with the HSV-1 thymidine kinase active site were investigated using the Molegro Virtual Docker (MVD) software. Based on the potent anti-HSV properties of the previous naphthalimide condensate products, further exploration of this series of 2-amino-1H-benzo[de]isoquinoline-1,3-diones is warranted. Full article
(This article belongs to the Section Medicinal Chemistry)
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Open AccessArticle Determination of the Molecular Weight of Low-Molecular-Weight Heparins by Using High-Pressure Size Exclusion Chromatography on Line with a Triple Detector Array and Conventional Methods
Molecules 2015, 20(3), 5085-5098; https://doi.org/10.3390/molecules20035085
Received: 30 January 2015 / Revised: 6 March 2015 / Accepted: 12 March 2015 / Published: 19 March 2015
Cited by 6 | PDF Full-text (919 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
The evaluation of weight average molecular weight (Mw) and molecular weight distribution represents one of the most controversial aspects concerning the characterization of low molecular weight heparins (LMWHs). As the most commonly used method for the measurement of such parameters is high performance
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The evaluation of weight average molecular weight (Mw) and molecular weight distribution represents one of the most controversial aspects concerning the characterization of low molecular weight heparins (LMWHs). As the most commonly used method for the measurement of such parameters is high performance size exclusion chromatography (HP-SEC), the soundness of results mainly depends on the appropriate calibration of the chromatographic columns used. With the aim of meeting the requirement of proper Mw standards for LMWHs, in the present work the determination of molecular weight parameters (Mw and Mn) by HP-SEC combined with a triple detector array (TDA) was performed. The HP-SEC/TDA technique permits the evaluation of polymeric samples by exploiting the combined and simultaneous action of three on-line detectors: light scattering detectors (LALLS/RALLS); refractometer and viscometer. Three commercial LMWH samples, enoxaparin, tinzaparin and dalteparin, a γ-ray depolymerized heparin (γ-Hep) and its chromatographic fractions, and a synthetic pentasaccharide were analysed by HP-SEC/TDA. The same samples were analysed also with a conventional HP-SEC method employing refractive index (RI) and UV detectors and two different chromatographic column set, silica gel and polymeric gel columns. In both chromatographic systems, two different calibration curves were built up by using (i) γ-Hep chromatographic fractions and the corresponding Mw parameters obtained via HP-SEC/TDA; (ii) the whole γ-Hep preparation with broad Mw dispersion and the corresponding cumulative distribution function calculated via HP-SEC/TDA. In addition, also a chromatographic column calibration according to European Pharmacopoeia indication was built up. By comparing all the obtained results, some important differences among Mw and size distribution values of the three LMWHs were found with the five different calibration methods and with HP-SEC/TDA method. In particular, the detection of the lower molecular weight components turned out to be the most critical aspect. Whereas HP-SEC/TDA may underestimate species under 2 KDa when present in low concentration, other methods appeared to emphasize their content. Full article
(This article belongs to the Special Issue Glycosaminoglycans and Their Mimetics)
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Open AccessArticle Synthesis of Novel Dihydropyridothienopyrimidin-4,9-dione Derivatives
Molecules 2015, 20(3), 5074-5084; https://doi.org/10.3390/molecules20035074
Received: 27 January 2015 / Revised: 12 March 2015 / Accepted: 13 March 2015 / Published: 19 March 2015
Cited by 2 | PDF Full-text (707 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
A novel molecular scaffold, dihydropyridothienopyrimidin-4,9-dione, was synthesized from benzylamine or p-methoxybenzylamine in six steps involving successive ring closure to form a fused ring system composed of dihydropyridone, thiophene and pyrimidone. The pharmacological versatility of the dihydropyridothenopyrimidin-4,9-dione scaffold was demonstrated by inhibitory activity
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A novel molecular scaffold, dihydropyridothienopyrimidin-4,9-dione, was synthesized from benzylamine or p-methoxybenzylamine in six steps involving successive ring closure to form a fused ring system composed of dihydropyridone, thiophene and pyrimidone. The pharmacological versatility of the dihydropyridothenopyrimidin-4,9-dione scaffold was demonstrated by inhibitory activity against metabotropic glutamate receptor subtype 1 (mGluR1), which shows that the title compounds can serve as an interesting scaffold for the discovery of potential bioactive molecules for the treatment of human diseases. Full article
(This article belongs to the Section Organic Chemistry)
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Open AccessArticle Comparison of Two Species of Notopterygium by GC-MS and HPLC
Molecules 2015, 20(3), 5062-5073; https://doi.org/10.3390/molecules20035062
Received: 19 January 2015 / Revised: 2 March 2015 / Accepted: 4 March 2015 / Published: 19 March 2015
Cited by 7 | PDF Full-text (1579 KB) | HTML Full-text | XML Full-text
Abstract
Notopterygii Rhizoma et Radix (Qianghuo), including Notopterygium incisum Ting ex H. T. Chang (NI) and Notopterygium franchetii H. de Boiss (NF), is an important traditional Chinese medicine. Of these two plants, NI, is more commonly used and has a much higher price in
[...] Read more.
Notopterygii Rhizoma et Radix (Qianghuo), including Notopterygium incisum Ting ex H. T. Chang (NI) and Notopterygium franchetii H. de Boiss (NF), is an important traditional Chinese medicine. Of these two plants, NI, is more commonly used and has a much higher price in the marketplace. To compare these two plants, a combination of gas chromatography-mass spectrometry (GC-MS) and high performance liquid chromatography (HPLC) was carried out, thus obtaining an overall characterization for both volatile and none-volatile compounds. Combined with hierarchical cluster analysis (HCA) and principal component analysis, GC-MS was successfully applied to distinguish NF and NI. The chemical constitutes of volatile oil in NI and NF were firstly compared in detail, and 1R-alpha-pinene, beta-pinene and 4-isopropyl-1-methyl-1,4-cyclohexadiene had great contribution to the discrimination. Fingerprints of 14 batches of Qinghuo samples were also established based on HPLC, and an obvious difference was found between the two species. The chromatographic fingerprints were further analyzed by similarity analysis and HCA. The present study is the first reported evaluation of two origins of Notopterygii Rhizoma et Radix by GC-MS and HPLC, which will facilitate quality control and its clinical application. Full article
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Open AccessArticle Design, Synthesis and Insecticidal Activity of Novel Phenylurea Derivatives
Molecules 2015, 20(3), 5050-5061; https://doi.org/10.3390/molecules20035050
Received: 28 February 2015 / Revised: 14 March 2015 / Accepted: 17 March 2015 / Published: 19 March 2015
Cited by 1 | PDF Full-text (692 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
A series of novel phenylurea derivatives were designed and synthesized according to the method of active groups linkage and the principle of aromatic groups bioisosterism in this study. The structures of the novel phenylurea derivatives were confirmed based on ESI-MS, IR and 1
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A series of novel phenylurea derivatives were designed and synthesized according to the method of active groups linkage and the principle of aromatic groups bioisosterism in this study. The structures of the novel phenylurea derivatives were confirmed based on ESI-MS, IR and 1H-NMR spectral data. All of the compounds were evaluated for the insecticidal activity against the third instars larvae of Spodoptera exigua Hiibner, Plutella xyllostella Linnaeus, Helicoverpa armigera Hubner and Pieris rapae Linne respectively, at the concentration of 10 mg/L. The results showed that all of the derivatives displayed strong insecticidal activity. Most of the compounds presented higher insecticidal activity against S. exigua than the reference compounds tebufenozide, chlorbenzuron and metaflumizone. Among the synthesized compounds, 3b, 3d, 3f, 4b and 4g displayed broad spectrum insecticidal activity. Full article
(This article belongs to the Section Organic Chemistry)
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Open AccessCommunication (−)-Tarchonanthuslactone Exerts a Blood Glucose-Increasing Effect in Experimental Type 2 Diabetes Mellitus
Molecules 2015, 20(3), 5038-5049; https://doi.org/10.3390/molecules20035038
Received: 8 December 2014 / Revised: 5 March 2015 / Accepted: 6 March 2015 / Published: 19 March 2015
Cited by 2 | PDF Full-text (995 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
A number of studies have proposed an anti-diabetic effect for tarchonanthuslactone based on its structural similarity with caffeic acid, a compound known for its blood glucose-reducing properties. However, the actual effect of tarchonanthuslactone on blood glucose level has never been tested. Here, we
[...] Read more.
A number of studies have proposed an anti-diabetic effect for tarchonanthuslactone based on its structural similarity with caffeic acid, a compound known for its blood glucose-reducing properties. However, the actual effect of tarchonanthuslactone on blood glucose level has never been tested. Here, we report that, in opposition to the common sense, tarchonanthuslactone has a glucose-increasing effect in a mouse model of obesity and type 2 diabetes mellitus. The effect is acute and non-cumulative and is present only in diabetic mice. In lean, glucose-tolerant mice, despite a slight increase in blood glucose levels, the effect was not significant. Full article
(This article belongs to the Section Medicinal Chemistry)
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