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Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry

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https://www.readbyqxmd.com/read/28644421/antibacterial-effect-of-a-4x-cu-tio%C3%A2-coating-simulating-acute-periprosthetic-infection-an-animal-model
#1
Andreas Mauerer, Stefanie Stenglein, Stefan Schulz-Drost, Christoph Schörner, Dominic Taylor, Sebastian Krinner, Frank Heidenau, Werner Adler, Raimund Forst
The purpose of our study was to investigate the antibacterial effect of a spacer (Ti6Al4V) coated with 4x Cu-TiO₂ in an animal model simulating an acute periprosthetic infection by Staphylococcus aureus. Ti6Al4 bolts contaminated with Staphylococcus aureus were implanted into the femoral condyle of rabbits (n = 36) divided into 3 groups. After one week in group 1 (control) the bolts were removed without any replacement. In group2 Ti6Al4V bolts with a 4x Cu-TiO₂ coating and in group 3 beads of a gentamicin-PMMA chain were imbedded into the borehole...
June 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28644411/on-the-reaction-of-carbonyl-diphosphonic-acid-with-hydroxylamine-and-o-alkylhydroxylamines-unexpected-degradation-of-p-c-p-bridge
#2
Olga A Khomich, Dmitry V Yanvarev, Roman A Novikov, Alexey B Kornev, Elina Puljulla, Jouko Vepsäläinen, Alex R Khomutov, Sergey N Kochetkov
Derivatives of methylenediphosphonic acid possess wide spectra of biological activities and are used in enzymology as research tools as well as in practical medicine. Carbonyl diphosphonic acid is a promising starting building block for synthesis of functionally substituted methylenediphosphonates. Investigation of the interaction of carbonyl diphosphonic acid with hydroxylamine clearly demonstrates that it is impossible to isolate oxime within the pH range 2-12, while only cyanophosphonic and phosphoric acids are the products of the fast proceeding Beckmann-like fragmentation...
June 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28644410/enhanced-antibacterial-activity-of-ent-labdane-derivatives-of-salvic-acid-7%C3%AE-hydroxy-8-17-ent-labden-15-oic-acid-effect-of-lipophilicity-and-the-hydrogen-bonding-role-in-bacterial-membrane-interaction
#3
Javier Echeverría, Alejandro Urzúa, Loreto Sanhueza, Marcela Wilkens
In the present study, the antibacterial activity of several ent-labdane derivatives of salvic acid (7α-hydroxy-8(17)-ent-labden-15-oic acid) was evaluated in vitro against the Gram-negative bacterium Escherichia coli and the Gram-positive bacteria Staphylococcus aureus and Bacillus cereus. For all of the compounds, the antibacterial activity was expressed as the minimum inhibitory concentration (MIC) in liquid media and minimum inhibitory amount (MIA) in solid media. Structure activity relationships (SAR) were employed to correlate the effect of the calculated lipophilicity parameters (logPow) on the inhibitory activity...
June 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28644406/an-updated-review-on-marine-anticancer-compounds-the-use-of-virtual-screening-for-the-discovery-of-small-molecule-cancer-drugs
#4
REVIEW
Verónica Ruiz-Torres, Jose Antonio Encinar, María Herranz-López, Almudena Pérez-Sánchez, Vicente Galiano, Enrique Barrajón-Catalán, Vicente Micol
Marine secondary metabolites are a promising source of unexploited drugs that have a wide structural diversity and have shown a variety of biological activities. These compounds are produced in response to the harsh and competitive conditions that occur in the marine environment. Invertebrates are considered to be among the groups with the richest biodiversity. To date, a significant number of marine natural products (MNPs) have been established as antineoplastic drugs. This review gives an overview of MNPs, both in research or clinical stages, from diverse organisms that were reported as being active or potentially active in cancer treatment in the past seventeen years (from January 2000 until April 2017) and describes their putative mechanisms of action...
June 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28644401/the-investigation-of-electrochemistry-behaviors-of-tyrosinase-based-on-directly-electrodeposited-grapheneon-choline-gold-nanoparticles
#5
Yaping He, Xiaohui Yang, Quan Han, Jianbin Zheng
A novel catechol (CA) biosensor was developed by embedding tyrosinase (Tyr) onto in situ electrochemical reduction graphene (EGR) on choline-functionalized gold nanoparticle (AuNPs-Ch) film. The results of UV-Vis spectra indicated that Tyr retained its original structure in the film, and an electrochemical investigation of the biosensor showed a pair of well-defined, quasi-reversible redox peaks with Epa = -0.0744 V and Epc = -0.114 V (vs. SCE) in 0.1 M, pH 7.0 sodium phosphate-buffered saline at a scan rate of 100 mV/s...
June 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28644391/molecular-structure-affinity-relationship-of-flavonoids-in-lotus-leaf-nelumbo-nucifera-gaertn-on-binding-to-human-serum-albumin-and-bovine-serum-albumin-by-spectroscopic-method
#6
Xiaosheng Tang, Ping Tang, Liangliang Liu
Lotus leaf has gained growing popularity as an ingredient in herbal formulations due to its various activities. As main functional components of lotus leaf, the difference in structure of flavonoids affected their binding properties and activities. In this paper, the existence of 11 flavonoids in lotus leaf extract was confirmed by High Performance Liquid Chromatography (HPLC) analysis and 11 flavonoids showed various contents in lotus leaf. The interactions between lotus leaf extract and two kinds of serum albumins (human serum albumin (HSA) and bovine serum albumin (BSA)) were investigated by spectroscopic methods...
June 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28644388/cellular-uptake-and-delivery-dependent-effects-of-tb-3-doped-hydroxyapatite-nanorods
#7
Yan Wei, Ying He, Xiyu Li, Haifeng Chen, Xuliang Deng
With the increasing interest in hydroxyapatite (HA) nanostructures for use in biomedicine, the systematic evaluation of their potential effects on biological systems is becoming critically important. In this work, we report the in vitro cellular uptake, in vivo tissue distributions and toxicity of Tb(3+)-doped HA (HA-Tb) after short-, intermediate-, and long-term exposure. Transmission electron microscopy analysis indicated that HA-Tb was taken up by cells via vesicle endocytosis. Cell proliferation and cytotoxicity assay, combined with confocal laser scanning microscopy, indicated excellent cell viability with no changes in cell morphology at the examined doses...
June 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28644385/ch-%C3%AF-interactions-in-carbohydrate-recognition
#8
REVIEW
Vojtěch Spiwok
Many carbohydrate-binding proteins contain aromatic amino acid residues in their binding sites. These residues interact with carbohydrates in a stacking geometry via CH/π interactions. These interactions can be found in carbohydrate-binding proteins, including lectins, enzymes and carbohydrate transporters. Besides this, many non-protein aromatic molecules (natural as well as artificial) can bind saccharides using these interactions. Recent computational and experimental studies have shown that carbohydrate-aromatic CH/π interactions are dispersion interactions, tuned by electrostatics and partially stabilized by a hydrophobic effect in solvated systems...
June 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28644383/use-of-ultrasonication-technology-for-the-increased-production-of-plant-secondary-metabolites
#9
REVIEW
Md Mohidul Hasan, Tufail Bashir, Hanhong Bae
Plant secondary metabolites (PSMs) provide taste, color, odor, and resistance to plants, and they are also used to treat cancer and cardiovascular diseases. Synthesis of PSMs in plants is stimulated in response to different forms of external stress. Use of ultrasonication (US) to clean or decontaminate fruits and vegetables leads to physical stress that finally results in the accumulation of PSMs. US can stimulate accumulation of taxol, ginsenoside saponins, shikonin, and resveratrol, e.g., up to 319-fold increase of resveratrol synthesis has been observed in grape due to US...
June 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28640230/total-flavonoids-of-drynariae-rhizoma-prevent-bone-loss-induced-by-hindlimb-unloading-in-rats
#10
Shuanghong Song, Ziyang Gao, Xujun Lei, Yinbo Niu, Yuan Zhang, Cuiqin Li, Yi Lu, Zhezhi Wang, Peng Shang
Drynariae Rhizoma is a kidney-tonifying herb that has a long history in clinical practice for the treatment of bone fractures and joint diseases in China. Flavonoids are considered to be its major active ingredients and are reported to ease bone loss in ovariectomized rats. However, the beneficial effects of the total flavonoids of Drynariae Rhizoma on osteoporosis caused by microgravity or mechanical inactivity remain unknown. This study assessed the effects of total Drynariae Rhizoma flavonoids (DRTF, Qihuang, Beijing, China, national medicine permit No...
June 22, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28640225/herb-drug-interaction-between-the-traditional-hepatoprotective-formulation-and-sorafenib-on-hepatotoxicity-histopathology-and-pharmacokinetics-in-rats
#11
Chin-Tsung Ting, Yung-Yi Cheng, Tung-Hu Tsai
Sorafenib has been used as a standard therapy for advanced hepatocellular carcinoma (HCC). In Asia, patients with HCC are potentially treated with the combination of sorafenib and Chinese herbal medicines to improve the efficiency and reduce the side effects of sorafenib. However, limited information about the herb-drug interactions is available. We hypothesize that the Chinese herbal medicine may exert hepatoprotective effects on the sorafenib-treated group. The aim of this study is to investigate the pharmacokinetic mechanism of drug-drug interactions of sorafenib including interacting with hepatoprotective formulation, Long-Dan-Xie-Gan-Tang formulation (LDXGT) and with two cytochrome P450 3A4 (CYP3A4) inhibitors, grapefruit juice and ketoconazole...
June 22, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28640222/albumin-and-hyaluronic-acid-coated-superparamagnetic-iron-oxide-nanoparticles-loaded-with-paclitaxel-for-biomedical-applications
#12
Elena Vismara, Chiara Bongio, Alessia Coletti, Ravit Edelman, Andrea Serafini, Michele Mauri, Roberto Simonutti, Sabrina Bertini, Elena Urso, Yehuda G Assaraf, Yoav D Livney
Super paramagnetic iron oxide nanoparticles (SPION) were augmented by both hyaluronic acid (HA) and bovine serum albumin (BSA), each covalently conjugated to dopamine (DA) enabling their anchoring to the SPION. HA and BSA were found to simultaneously serve as stabilizing polymers of Fe₃O₄·DA-BSA/HA in water. Fe₃O₄·DA-BSA/HA efficiently entrapped and released the hydrophobic cytotoxic drug paclitaxel (PTX). The relative amount of HA and BSA modulates not only the total solubility but also the paramagnetic relaxation properties of the preparation...
June 22, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28640221/use-of-chitosan-pva-hydrogels-with-copper-nanoparticles-to-improve-the-growth-of-grafted-watermelon
#13
Homero González Gómez, Francisca Ramírez Godina, Hortensia Ortega Ortiz, Adalberto Benavides Mendoza, Valentín Robledo Torres, Marcelino Cabrera De la Fuente
Modern agriculture requires alternative practices that improve crop growth without negatively affecting the environment, as resources such as water and arable land grow scarcer while the human population continues to increase. Grafting is a cultivation technique that allows the plant to be more efficient in its utilization of water and nutrients, while nanoscale material engineering provides the opportunity to use much smaller quantities of consumables compared to conventional systems but with similar or superior effects...
June 22, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28640218/studies-on-the-two-thymine-residues-in-the-catalytic-core-of-10-23-dnazyme-the-impact-on-the-catalysis-of-their-5-substituted-functional-groups
#14
Pengyu Li, Shanshan Du, Yang Li, Junlin He
In the 15-mer catalytic core of 10-23 DNAzyme, each residue contributes to the catalytic conformation differently. Here, the critically conserved T4 and the least conserved T8 were modified on their 5-position with hydroxyl, imidazolyl, and amino groups with a hydrogen-bonding ability. These external functional groups induced new interactions within the catalytic core, resulting in both negative and positive effects on the catalytic activity of 10-23 DNAzyme, and the different linkages could be used to modulate the effect of the functional groups...
June 22, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28640212/synthesis-and-in-vitro-anti-influenza-virus-evaluation-of-novel-sialic-acid-c-5-and-c-9-pentacyclic-triterpene-derivatives
#15
Xu Han, Long-Long Si, Yong-Ying Shi, Zi-Bo Fan, Shou-Xin Wang, Zhen-Yu Tian, Man Li, Jia-Qi Sun, Ping-Xuan Jiao, Fu-Xiang Ran, Yong-Min Zhang, De-Min Zhou, Su-Long Xiao
The emergence of drug resistant variants of the influenza virus has led to a great need to identify novel and effective antiviral agents. In our previous study, a series of sialic acid (C-2 and C-4)-pentacyclic triterpene conjugates have been synthesized, and a five-fold more potent antiviral activity was observed when sialic acid was conjugated with pentacyclic triterpene via C-4 than C-2. It was here that we further reported the synthesis and anti-influenza activity of novel sialic acid (C-5 and C-9)-pentacyclic triterpene conjugates...
June 22, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28640203/effect-of-solution-ph-on-the-adsorption-of-paracetamol-on-chemically-modified-activated-carbons
#16
Valentina Bernal, Alessandro Erto, Liliana Giraldo, Juan Carlos Moreno-Piraján
Paracetamol adsorption in acidic, neutral and basic media on three activated carbons with different chemistry surfaces was studied. A granular activated carbon (GAC) was prepared from coconut shell; starting from this sample, an oxidized activated carbon (GACo) was obtained by treating the GAC with a boiling solution of 6 M nitric acid, so to generate a greater number of oxygenated surface groups. In addition, a reduced activated carbon (GACr) was obtained by heating the GAC at 1173 K, to remove the oxygenated surface groups...
June 22, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28635656/screening-and-identification-of-the-metabolites-in-rat-plasma-and-urine-after-oral-administration-of-areca-catechu-l-nut-extract-by-ultra-high-pressure-liquid-chromatography-coupled-with-linear-ion-trap-orbitrap-tandem-mass-spectrometry
#17
Lulu Li, Zhiqiang Luo, Yang Liu, Hao Wang, Aoxue Liu, Guohua Yu, Mengwei Li, Ruirui Yang, Xinjing Chen, Jialian Zhu, Baosheng Zhao
Areca catechu L. nut, a well-known toxic traditional herbal medicine, has been widely used to treat various diseases in China and many other Asian countries for centuries. However, to date the in vivo absorption and metabolism of its multiple bioactive or toxic components still remain unclear. In this study, liquid chromatography coupled with tandem mass spectrometry was used to analyze the major components and their metabolites in rat plasma and urine after oral administration of Areca catechu L. nut extract (ACNE)...
June 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28635655/from-farm-to-pharma-an-overview-of-industrial-heparin-manufacturing-methods
#18
REVIEW
Jan-Ytzen van der Meer, Edwin Kellenbach, Leendert J van den Bos
The purification of heparin from offal is an old industrial process for which commercial recipes date back to 1922. Although chemical, chemoenzymatic, and biotechnological alternatives for this production method have been published in the academic literature, animal-tissue is still the sole source for commercial heparin production in industry. Heparin purification methods are closely guarded industrial secrets which are not available to the general (scientific) public. However by reviewing the academic and patent literature, we aim to provide a comprehensive overview of the general methods used in industry for the extraction of heparin from animal tissue...
June 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28635653/virtual-screening-against-phosphoglycerate-kinase-1-in-quest-of-novel-apoptosis-inhibitors
#19
Jie Xia, Bo Feng, Qianhang Shao, Yuhe Yuan, Xiang Simon Wang, Naihong Chen, Song Wu
Inhibition of apoptosis is a potential therapy to treat human diseases such as neurodegenerative disorders (e.g., Parkinson's disease), stroke, and sepsis. Due to the lack of druggable targets, it remains a major challenge to discover apoptosis inhibitors. The recent repositioning of a marketed drug (i.e., terazosin) as an anti-apoptotic agent uncovered a novel target (i.e., human phosphoglycerate kinase 1 (hPgk1)). In this study, we developed a virtual screening (VS) pipeline based on the X-ray structure of Pgk1/terazosin complex and applied it to a screening campaign for potential anti-apoptotic agents...
June 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28635648/deoxyelephantopin-and-isodeoxyelephantopin-as-potential-anticancer-agents-with-effects-on-multiple-signaling-pathways
#20
REVIEW
Tahir Mehmood, Amara Maryam, Hamed A Ghramh, Muhammad Khan, Tonghui Ma
Cancer is the 2nd leading cause of death worldwide. The development of drugs to target only one specific signaling pathway has limited therapeutic success. Developing chemotherapeutics to target multiple signaling pathways has emerged as a new prototype for cancer treatment. Deoxyelephantopin (DET) and isodeoxyelephantopin (IDET) are sesquiterpene lactone components of "Elephantopus scaber and Elephantopus carolinianus", traditional Chinese medicinal herbs that have long been used as folk medicines to treat liver diseases, diabetes, diuresis, bronchitis, fever, diarrhea, dysentery, cancer, and inflammation...
June 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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