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Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry

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https://www.readbyqxmd.com/read/29160852/the-complete-chloroplast-genome-sequences-of-aconitum-pseudolaeve-and-aconitum-longecassidatum-and-development-of-molecular-markers-for-distinguishing-species-in-the-aconitum-subgenus-lycoctonum
#1
Inkyu Park, Sungyu Yang, Goya Choi, Wook Jin Kim, Byeong Cheol Moon
Aconitum pseudolaeve Nakai and Aconitum longecassidatum Nakai, which belong to the Aconitum subgenus Lycoctonum, are distributed in East Asia and Korea. Aconitum species are used in herbal medicine and contain highly toxic components, including aconitine. A. pseudolaeve, an endemic species of Korea, is a commercially valuable material that has been used in the manufacture of cosmetics and perfumes. Although Aconitum species are important plant resources, they have not been extensively studied, and genomic information is limited...
November 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29160848/application-of-enzymatic-extracts-from-a-calb-standard-strain-as-biocatalyst-within-the-context-of-conventional-biodiesel-production-optimization
#2
Carlos Luna, Diego Luna, Felipa M Bautista, Rafael Estevez, Juan Calero, Alejandro Posadillo, Antonio A Romero, Enrique D Sancho
The application of biocatalysts in the transesterification process of triglycerides (TG) allows integrating the glycerol in the form of monoglyceride (MG), sharply increasing the yield and the environmental sustainability of the conventional biodiesel production process. This is known as Ecodiesel. To overcome the inconvenient of the high cost of the currently employed highly purified commercial enzymes, the use of scarcely purified extracts obtained from standard strains of the same species of commercial lipases currently applied in this process is being investigated...
November 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29160839/inkjet-printing-of-drug-loaded-mesoporous-silica-nanoparticles-a-platform-for-drug-development
#3
Henrika Wickström, Ellen Hilgert, Johan O Nyman, Diti Desai, Didem Şen Karaman, Thomas de Beer, Niklas Sandler, Jessica M Rosenholm
Mesoporous silica nanoparticles (MSNs) have shown great potential in improving drug delivery of poorly water soluble (BCS class II, IV) and poorly permeable (BCS class III, IV) drugs, as well as facilitating successful delivery of unstable compounds. The nanoparticle technology would allow improved treatment by reducing adverse reactions of currently approved drugs and possibly reintroducing previously discarded compounds from the drug development pipeline. This study aims to highlight important aspects in mesoporous silica nanoparticle (MSN) ink formulation development for digital inkjet printing technology and to advice on choosing a method (2D/3D) for nanoparticle print deposit characterization...
November 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29160837/application-of-an-ultrafine-shearing-method-for-the-extraction-of-c-phycocyanin-from-spirulina-platensis
#4
Jianfeng Yu
Cell disruption is an important step during the extraction of C-phycocyanin from Spirulina platensis. An ultrafine shearing method is introduced and combined with soaking and ultrasonication to disrupt the cell walls of S. platensis efficiently and economically. Five kinds of cell disruption method, including soaking, ultrasonication, freezing-thawing, soaking-ultrafine shearing and soaking-ultrafine shearing-ultrasonication were applied to break the cell walls of S. platensis. The effectiveness of cell breaking was evaluated based on the yield of the C-phycocyanin...
November 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29160833/taxon-and-site-specific-melatonin-catabolism
#5
REVIEW
Rüdiger Hardeland
Melatonin is catabolized both enzymatically and nonenzymatically. Nonenzymatic processes mediated by free radicals, singlet oxygen, other reactive intermediates such as HOCl and peroxynitrite, or pseudoenzymatic mechanisms are not species- or tissue-specific, but vary considerably in their extent. Higher rates of nonenzymatic melatonin metabolism can be expected upon UV exposure, e.g., in plants and in the human skin. Additionally, melatonin is more strongly nonenzymatically degraded at sites of inflammation...
November 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29160827/organocatalytic-access-to-enantioenriched-spirooxindole-based-4-methyleneazetidines
#6
Giulia Rainoldi, Matteo Faltracco, Claudia Spatti, Alessandra Silvani, Giordano Lesma
This work describes the synthesis of enantioenriched spiro compounds, incorporating the azetidine and the oxindole motifs. The preparation relies on a formal [2 + 2] annulation reaction of isatin-derived N-tert-butylsulfonyl ketimines with allenoates. The asymmetric induction is secured by an organocatalytic strategy, exploiting a bifunctional cinchona-type β-isocupridine-based catalyst. Some post-transformation products, including unexpected spiropyrroline and 3,3-disubstituted oxindole derivatives, are also presented...
November 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29160824/microneedle-assisted-percutaneous-delivery-of-a-tetramethylpyrazine-loaded-microemulsion
#7
Qiang Zu, Yanyan Yu, Xiaolin Bi, Ren Zhang, Liuqing Di
This study examined the efficacy of the percutaneous delivery of a tetramethylpyrazine-loaded microemulsion (TMP-ME) on skin pretreated with microneedles (MN). The TMP-ME formulation was optimized in vitro with skin permeation experiments, using a uniform experimental design, guided by a pseudo-ternary phase diagram, in which the TMP skin permeation level and mean particle size were indices. The effects of MN pretreatment on skin permeation by TMP-ME were assessed using in vitro skin permeation, in vivo skin microdialysis, and pharmacokinetic studies in rats...
November 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29160822/how-secondary-and-tertiary-amide-moieties-are-molecular-stations-for-dibenzo-24-crown-8-in-2-rotaxane-molecular-shuttles
#8
Benjamin Riss-Yaw, Justine Morin, Caroline Clavel, Frédéric Coutrot
Interlocked molecular machines like [2]rotaxanes are intriguing aesthetic molecules. The control of the localization of the macrocycle, which surrounds a molecular axle, along the thread leads to translational isomers of very different properties. Although many moieties have been used as sites of interactions for crown ethers, the very straightforwardly obtained amide motif has more rarely been envisaged as molecular station. In this article, we report the use of secondary and tertiary amide moieties as efficient secondary molecular station in pH-sensitive molecular shuttles...
November 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29160816/optimization-of-goat-milk-with-ace-inhibitory-peptides-fermented-by-lactobacillus-bulgaricus-lb6-using-response-surface-methodology
#9
Guowei Shu, Xiaoyu Shi, He Chen, Zhe Ji, Jiangpeng Meng
In the present study, the incubation conditions of goat milk fermented by Lactobacillus bulgaricus LB6 were optimized to increase the angiotensin converting enzyme (ACE, EC 3.4.15.1) inhibitory activity by Box-Behnken design of response surface methodology. Incubation temperature, whey powder, and calcium lactate had significant effects on ACE inhibition rate and viable counts of LB6 during incubation. The results showed that optimal conditions of fermentation were found to be 37.05 °C, 0.8% (w/w) whey powder and 0...
November 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29160806/synthesis-of-nitrogen-heterocycles-using-samarium-ii-iodide
#10
REVIEW
Shicheng Shi, Michal Szostak
Nitrogen heterocycles represent vital structural motifs in biologically-active natural products and pharmaceuticals. As a result, the development of new, convenient and more efficient processes to N-heterocycles is of great interest to synthetic chemists. Samarium(II) iodide (SmI₂, Kagan's reagent) has been widely used to forge challenging C-C bonds through reductive coupling reactions. Historically, the use of SmI₂ in organic synthesis has been focused on the construction of carbocycles and oxygen-containing motifs...
November 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29160801/the-protective-effects-of-astaxanthin-on-the-ova-induced-asthma-mice-model
#11
Yun-Ho Hwang, Seong-Gyeol Hong, Seul-Ki Mun, Su-Jin Kim, Sung-Ju Lee, Jong-Jin Kim, Kyung-Yun Kang, Sung-Tae Yee
Although astaxanthin has a variety of biological activities such as anti-oxidant effects, inhibitory effects on skin deterioration and anti-inflammatory effects, its effect on asthma has not been studied. In this paper, the inhibitory effect of astaxanthin on airway inflammation in a mouse model of ovalbumin (OVA)-induced asthma was investigated. We evaluated the number of total cells, Th1/2 mediated inflammatory cytokines in bronchoalveolar lavage fluid (BALF) and airway hyperresponsiveness as well as histological structure...
November 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29160791/antimalarial-activity-of-acetylenic-thiophenes-from-echinops-hoehnelii-schweinf
#12
Helen Bitew, Wendimagegn Mammo, Ariaya Hymete, Mariamawit Yonathan Yeshak
Malaria is one of the world's most severe endemic diseases and due to the emergence of resistance to the currently available medicines, the need for new targets and relevant antimalarial drugs remains acute. The crude extract, four solvent fractions and two isolated compounds from the roots of Echinops hoehnelii were tested for their antimalarial activity using the standard four-day suppressive method in Plasmodium berghei-infected mice. The 80% methanol extract exhibited suppression of 4.6%, 27.8%, 68.5% and 78...
November 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29156652/comparison-of-the-chemical-profiles-and-antioxidant-activities-of-different-parts-of-cultivated-cistanche-deserticola-using-ultra-performance-liquid-chromatography-quadrupole-time-of-flight-mass-spectrometry-and-a-1-1-diphenyl-2-picrylhydrazyl-based-assay
#13
Xiaoming Wang, Jinfang Wang, Huanyu Guan, Rong Xu, Xiaomei Luo, Meifeng Su, Xiaoyan Chang, Wenting Tan, Jun Chen, Yue Shi
In this study, a sensitive ultra-performance liquid chromatography-photodiode array coupled to quadruple time-of-flight mass (UPLC-PDA-Q/TOF-MS) method and a 1,1-diphenyl-2- picrylhydrazyl (DPPH)-based assay were used to determine the chemical constituents and screen the antioxidant activity profiles of the methanol extracts of different parts of cultivated Cistanche deserticola (C. deserticola). First, qualitative and quantitative chemical composition analyses of the different parts of cultivated C. deserticola were conducted...
November 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29156646/inhibition-of-bcl-2-and-cox-2-protein-expression-after-local-application-of-a-new-carmustine-loaded-clinoptilolite-based-delivery-system-in-a-chemically-induced-skin-cancer-model-in-mice
#14
Cristina Mihaela Ghiciuc, Aurel Lulu Strat, Lacramioara Ochiuz, Catalina Elena Lupusoru, Maria Ignat, Aurelia Vasile, Alexandru Grigorovici, Iulian Stoleriu, Carmen Solcan
Our research has focused on in vitro and in vivo evaluations of a new Carmustine (BCNU)-loaded clinoptilolite-based delivery system. Two clinoptilolite ionic forms-hydrogen form (HCLI) and sodium form (NaCLI)-were prepared, allowing a loading degree of about 5-6 mg BCNU/g of zeolite matrix due to the dual porous feature of clinoptilolite. Clinoptilolite-based delivery systems released 35.23% of the load in 12 h for the BCNU@HCLI system and only 10.82% for the BCNU@NaCLI system. The BCNU@HCLI system was chosen to develop gel and cream semisolid dosage forms...
November 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29156637/synthesis-and-improved-cross-linking-properties-of-c5-modified-furan-bearing-pnas
#15
Joke Elskens, Alex Manicardi, Valentina Costi, Annemieke Madder, Roberto Corradini
Over the past decades, peptide nucleic acid/DNA (PNA:DNA) duplex stability has been improved via backbone modification, often achieved via introducing an amino acid side chain at the α- or γ-position in the PNA sequence. It was previously shown that interstrand cross-linking can further enhance the binding event. In this work, we combined both strategies to fine-tune PNA crosslinking towards single stranded DNA sequences using a furan oxidation-based crosslinking method; for this purpose, γ-l-lysine and γ-l-arginine furan-PNA monomers were synthesized and incorporated in PNA sequences via solid phase synthesis...
November 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29156630/anti-bacteria-and-microecosystem-regulating-effects-of-dental-implant-coated-with-dimethylaminododecyl-methacrylate
#16
Bolei Li, Yang Ge, Yao Wu, Jing Chen, Hockin H K Xu, Minggang Yang, Mingyun Li, Biao Ren, Mingye Feng, Michael D Weir, Xian Peng, Lei Cheng, Xuedong Zhou
The effects of dimethylaminododecyl methacrylate (DMADDM) modified titanium implants on bacterial activity and microbial ecosystem of saliva-derived biofilm were investigated for the first time. Titanium discs were coated with DMADDM solutions at mass fractions of 0 mg/mL (control), 1, 5 and 10 mg/mL, respectively. Biomass accumulation and metabolic activity of biofilms were tested using crystal violet assay and MTT (3-(4,5-Dimethyl-thiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. 16S rRNA gene sequencing was performed to measure the microbial community...
November 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29156621/influence-of-shenxiong-glucose-injection-on-the-activities-of-six-cyp-isozymes-and-metabolism-of-warfarin-in-rats-assessed-using-probe-cocktail-and-pharmacokinetic-approaches
#17
Jia Sun, Yuan Lu, Yueting Li, Jie Pan, Chunhua Liu, Zipeng Gong, Jing Huang, Jiang Zheng, Lin Zheng, Yongjun Li, Ting Liu, Yonglin Wang
Shenxiong glucose injection (SGI), a traditional Chinese medicine (TCM) preparation, has been widely used for the treatment of various cardiovascular and cerebrovascular diseases for many years. We assessed the potential influences of SGI on the activities of six CYP enzymes (CYP1A2, CYP2C11, CYP2C19, CYP2D4, CYP2E1, and CYP3A2) and on the pharmacokinetics of warfarin in rats. We compared plasma pharmacokinetics of six probe drugs (caffeine/CYP1A2, tolbutamide/CYP2C11, omeprazole/CYP2C19, metoprolol/CYP2D4, chlorzoxazone/CYP2E1, and midazolam/CYP3A2) and of warfarin between control and SGI-pretreated groups, to estimate the effect on the relative activities of the six isozymes and warfarin metabolism...
November 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29156603/adding-an-artificial-tail-anchor-to-a-peptide-based-hiv-1-fusion-inhibitor-for-improvement-of-its-potency-and-resistance-profile
#18
Shan Su, Zhenxuan Ma, Chen Hua, Weihua Li, Lu Lu, Shibo Jiang
Peptides derived from the C-terminal heptad repeat (CHR) of human immunodeficiency virus type 1 (HIV-1) envelope protein transmembrane subunit gp41, such as T20 (enfuvirtide), can bind to the N-terminal heptad repeat (NHR) of gp41 and block six-helix bundle (6-HB) formation, thus inhibiting HIV-1 fusion with the target cell. However, clinical application of T20 is limited because of its low potency and genetic barrier to resistance. HP23, the shortest CHR peptide, exhibits better anti-HIV-1 activity than T20, but the HIV-1 strains with E49K mutations in gp41 will become resistant to it...
November 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29156590/enhancement-of-aggregation-induced-emission-by-introducing-multiple-o-carborane-substitutions-into-triphenylamine
#19
Kenta Nishino, Kyoya Uemura, Masayuki Gon, Kazuo Tanaka, Yoshiki Chujo
The enhancement of aggregation-induced emission (AIE) is presented on the basis of the strategy for improving solid-state luminescence by employing multiple o-carborane substituents. We synthesized the modified triphenylamines with various numbers of o-carborane units and compared their optical properties. From the optical measurements, the emission bands from the twisted intramolecular charge transfer (TICT) state were obtained from the modified triphenylamines. It was notable that emission efficiencies of the multi-substituted triphenylamines including two or three o-carborane units were enhanced 6- to 8-fold compared to those of the mono-substituted triphenylamine...
November 19, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29156575/synthesis-of-oxadiazole-thiadiazole-hybrids-and-their-anticandidal-activity
#20
Serkan Levent, Betül Kaya Çavuşoğlu, Begüm Nurpelin Sağlık, Derya Osmaniye, Ulviye Acar Çevik, Özlem Atlı, Yusuf Özkay, Zafer Asım Kaplancıklı
In the field of infection management, it is a major challenge to discover a potent and safe antifungal agent due to the emergence of resistant strains. Hence, the goal of this paper is to design and synthesize novel oxadiazole-thiadiazole hybrid compounds (6a-6s) and evaluate their antifungal activity. The structures of synthesized compounds were elucidated by various methods including FT-IR, ¹H-NMR, (13)C-NMR and HR-MS spectral data. Compounds were tested against four Candida species by broth microdilution assay...
November 18, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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