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https://www.readbyqxmd.com/read/28231528/identification-of-uv-absorbing-extractables-from-rubber-closures-used-in-containers-of-injectable-powder-and-safety-assessment-of-leachables-in-the-drug
#1
Yulei Wei, Ying Wu, Tingli Zhu, Zhiyan Li, Yilan Zhang
Rubber closures have been of great concern to regulatory authorities on account of their potential safety risks to patients. The aim of our work is to provide part of data about the compatibility of the injectable powder and its packaging materials for the drug registration. In this report, methodologies were established to study the system of the preparation. Firstly, three major extractables were isolated by semi-preparative HPLC method combined with silica gel-based chromatographic methods. NMR spectra including 1D NMR ((1)H, (13)C, DEPT135) and 2D NMR (COSY, HSQC, HMBC) were introduced to identify the extractables, besides HPLC, GC-MS, ESI-MS/MS and HRMS...
February 16, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28230285/modeling-lung-surfactant-interactions-with-benzo-a-pyrene
#2
Jacek Korchowiec, Anna Stachowicz-Kusnierz, Sonia Trojan, Lukasz Cwiklik, Beata Korchowiec
By reducing surface tension of the air-water interface in alveoli, lung surfactant (LS) is crucial for proper functioning of the lungs. It also forms the first barrier against inhaled pathogens. In this study we inspect the interactions of LS models with a dangerous air pollutant, benzo[a]pyrene (BaP). DPPC, POPC and their 1:1 mixture are used as LS models. Pressure-area isotherms are employed to study macroscopic properties of the monolayers. We find that addition of BaP has a condensing effect, manifested by lowering the values of surface pressure and shifting the isotherms to smaller areas...
February 23, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28222603/synthesis-of-aza-oxa-and-thiaporphyrins-and-related-compounds
#3
Yoshihiro Matano
Chemical modification at the periphery with nitrogen or chalcogens is a highly promising strategy to diversify the optical, electrochemical, magnetic, and coordination properties of the porphyrin family. Indeed, various kinds of phthalocyanines and related benzo-annelated azaporphyrinoids have been synthesized, and their fundamental properties have been extensively investigated. However, the synthesis of heteroatom-containing porphyrins in which the peripheral methine groups are partially replaced with nitrogen or chalcogens remains a considerable challenge...
February 22, 2017: Chemical Reviews
https://www.readbyqxmd.com/read/28222397/a-novel-approach-towards-design-synthesis-and-evaluation-of-some-schiff-base-analogues-of-2-aminopyridine-and-2-aminobezothiazole-against-hepatocellular-carcinoma
#4
Shinu Chacko, Subir Samanta
Hepatocellular carcinoma is the most common primary malignancy of the liver with poor prognosis. In this study novel, Schiff's bases of 2-aminopyridine (SSSC-26 to 31) and 2-aminobenzothiazole (SSSC-32 to 37) were designed, synthesised and evaluated for antioxidant potential using DPPH method, and anti-hepatocellular carcinoma property using diethylnitrosamine (DEN) induced hepatocellular carcinoma rat model. The in-silico pharmacokinetic, rule of five and toxicity studies reveals that all the leads have an excellent intrinsic quality and sufficient structural features necessary for an oral activity...
February 18, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28222328/effects-of-cooking-methods-and-tea-marinades-on-the-formation-of-benzo-a-pyrene-in-grilled-pork-belly-samgyeopsal
#5
Keun-Cheol Park, HeeSoo Pyo, WooSeok Kim, Ki Sun Yoon
We investigated the effects of different grilling tools, temperatures, and tea marinades on the formation of benzo[a]pyrene in grilled pork belly as well as the antioxidant capacities of tea marinades. The least amount of benzo[a]pyrene was detected in modified charcoal-grilled pork belly (1.28μg/kg). The highest risk factors for the formation of benzo[a]pyrene are direct contact with flames and fat excess on the heating source. A modified charcoal grill can be used as an alternative grilling tool to meet consumer needs for safety and taste...
February 14, 2017: Meat Science
https://www.readbyqxmd.com/read/28221959/efficacy-of-ozonation-treatments-of-smoked-fish-for-reducing-its-benzo-a-pyrene-concentration-and-toxicity
#6
Irina Rozentale, Janis Ancans, Elena Bartkiene, Arturs Viksna, Vadims Bartkevics
Ozone is widely used in food processing, for example, to decompose mycotoxins or pesticide residues, to extend the shelf life of products, and for sanitation. The objective of this study was to assess the possibility of expanding the application of ozone for oxidative degradation of polycyclic aromatic hydrocarbons (PAHs). The evaluation was conducted by ozonation of a benzo[a]pyrene (BaP) standard solution and smoked fish (sprats) contaminated with PAHs. The effect of ozonation was immediate in the BaP solution; 89% of this toxic compound was decomposed after only 1 min of treatment...
December 2016: Journal of Food Protection
https://www.readbyqxmd.com/read/28220698/copper-catalyzed-selenylation-of-imidazo-1-2-a-pyridines-with-selenium-powder-via-a-radical-pathway
#7
Pengfei Sun, Min Jiang, Wei Wei, Yuanyuan Min, Wen Zhang, Wanhui Li, Daoshan Yang, Hua Wang
A novel and efficient method for the synthesis of nitrogen heterocycle-fused benzo[b]selenophene and imidazo[1,2-a]pyridines has been initially developed through copper-catalyzed direct selenylation of 2-(2-bromophenyl)imidazo[1,2-a]pyridines via regioselective cleavage of C(sp2)-Br and C(sp2)-H bonds using readily available selenium powder as the selenylating reagents under ligand- and base-free conditions in air. Preliminary mechanistic investigations indicated that radical species were involved. The inexpensive and convenient copper-catalyzed approach provides a convenient and useful strategy for one-pot constructing biologically and optically interesting heterocycles containing benzo[b]selenophene and imidazo[1,2-a]pyridine motifs...
February 21, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28220149/chemical-characterization-of-mainstream-smoke-from-spectrum-variable-nicotine-research-cigarettes
#8
Yan S Ding, Patricia Richter, Bryan Hearn, Liqin Zhang, Roberto Bravo, Xizheng Yan, Jose J Perez, Michele Chan, Jared Hughes, Patrick Chen, Wayne Chen, Joshua Wong, Sydney Holmberg, Shakia Smith, Morgan Larango, Liza Valentín-Blasini, Clifford H Watson
OBJECTIVE: Our objective was to characterize mainstream smoke constituent deliveries from SPECTRUM variable nicotine research cigarettes under 2 machine smoking regimens. SPECTRUM cigarettes are manufactured by the 22nd Century company for the National Institute on Drug Abuse, National Institutes of Health to contain varying (including reduced) levels of nicotine. METHODS: Mainstream smoke constituent deliveries of "tar," nicotine, carbon monoxide, tobacco-specific nitrosamines (N'-nitrosonornicotine (NNN) and 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK)), benzo[a]pyrene, aromatic amines, and carbonyls were analyzed in 23 varieties of SPECTRUM cigarettes using ISO 17025 accredited methods...
December 1, 2017: Tobacco Regulatory Science
https://www.readbyqxmd.com/read/28218516/coumarin-based-thermally-activated-delayed-fluorescence-emitters-with-high-external-quantum-efficiency-and-low-efficiency-roll-off-in-the-devices
#9
Jia-Xiong Chen, Wei Liu, Cai-Jun Zheng, Kai Wang, Ke Liang, Yizhong Shi, Xue-Mei Ou, Xiao-Hong Zhang
Thermally activated delayed fluorescence (TADF) emitters have attracted much interest for their great applications in organic light emitting diodes (OLEDs), but the TADF OLEDs are limited by large efficiency roll-offs. In this study, we report two coumarin-based TADF emitters, 3-methyl-6-(10H-phenoxazin-10-yl)-1H-isochromen-1-one (PHzMCO) and 9-(10H-phenoxazin-10-yl)-6H-benzo[c]chromen-6-one (PHzBCO), with relatively high photoluminescence quantum yields (PLQYs) and extremely small singlet-triplet splittings...
February 20, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28217365/crystal-structure-of-the-cis-and-trans-polymorphs-of-bis-%C3%AE-2-1-3-benzo-thia-zol-2-yl-phenolato-%C3%AE%C2%BA-3-n-o-o-%C3%AE%C2%BA-3-o-n-o-bis-fac-tri-carbonyl-rhenium-i
#10
Maruthupandiyan Priyatharsini, Bhaskaran Shankar, Malaichamy Sathiyendiran, Navaneethakrishnan Srinivasan, Rajaputi Venkatraman Krishnakumar
The title dinuclear complex, [Re2(C13H8NOS)2(CO)6], crystallizes in two polymorphs where the 2-(1,3-benzo-thia-zol-2-yl)phenolate ligands and two carbonyl groups are trans- (I) or cis-arranged (II) with respect to the [Re2O2(CO)4] core. Polymorphs I and II exhibit a crystallographically imposed centre of symmetry and a twofold rotation axis, respectively. The structures may be described as being formed by two octa-hedrally distorted metal-coordinating units fused through μ-oxido bridges, leading to edge-sharing dimers...
February 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28216402/synthesis-of-novel-spiro-pyrazolo-4-3-d-pyrimidinones-and-spiro-benzo-4-5-thieno-2-3-d-pyrimidine-2-3-indoline-2-4-3h-diones-and-their-evaluation-for-anticancer-activity
#11
Ismail, Bhaskar Kuthati, Gangadhar Thalari, Venkatesham Bommarapu, Chaitanya Mulakayala, Suresh Kumar Chitta, Naveen Mulakayala
An efficient and novel method for the preparation of spiro[pyrazolo[4,3-d]pyrimidin]-7'(1'H)-ones by the condensation of 4-amino-1-methyl-3-propylpyrazole-5-carboxamide with ketones under mild conditions using catalytic InCl3 was reported. This method has been extended for the synthesis of novel spiro[benzo[4,5]thieno[2,3-d]pyrimidine-2,3'-indoline]-2',4(3H)-dione which are having potential applications in medicinal chemistry. All the synthesized compounds were evaluated for their anti-proliferative properties in vitro against cancer cell lines and several compounds were found to be active...
February 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28216010/uptake-of-benzo-a-pyrene-but-not-of-phenanthrene-is-inhibited-by-fatty-acids-in-intestinal-brush-border-membrane-vesicles-of-rainbow-trout-oncorhynchus-mykiss
#12
Stefan de Gelder, Liselot van Och, Jan Zethof, Thamar N M Pelgrim, Josef D Rasinger, Gert Flik, Marc H G Berntssen, Peter H M Klaren
Partial replacement of fish ingredients with vegetable ingredients has elevated levels of polycyclic aromatic hydrocarbons (PAHs) in Atlantic salmon reared on these feeds. PAH uptake in the intestinal tract is postulated to occur in association with lipid absorption and could well be affected by fatty acid composition. We therefore investigated the effects of a fish oil and vegetable oil fatty acid, eicosapentaenoic acid (EPA; 20:5n-3) and oleic acid (18:1n-9) respectively, on the uptake of benzo[a]pyrene (BaP) and phenanthrene (PHE) across the intestinal brush border membrane in the salmonid species rainbow trout (Oncorhynchus mykiss)...
February 12, 2017: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
https://www.readbyqxmd.com/read/28215082/development-of-a-quechers-based-method-for-determination-of-carcinogenic-2-nitrofluorene-and-1-nitropyrene-in-rice-grains-and-vegetables-a-comparative-study-with-benzo-a-pyrene
#13
Kailin Deng, Wan Chan
Nitrated polycyclic aromatic hydrocarbons (nitro-PAHs) are ubiquitous environmental pollutants attracting increasing attention because of their potent mutagenicity to humans. Previous studies of nitro-PAHs focused on investigating their formation mechanisms and detecting them in atmospheric environment; however, few studies have reported their occurrence in food samples, and regulations on nitro-PAHs are still lacking. We report in this study the development and application of a quick, easy, cheap, effective, rugged, and safe (QuEChERS) method for determination of nitro-PAHs in rice and vegetable samples...
February 23, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28209279/neolignan-and-megastigmane-glucosides-from-the-aerial-parts-of-isodon-japonicus-with-cell-protective-effects-on-bap-induced-cytotoxicity
#14
Takahiro Matsumoto, Seikou Nakamura, Souichi Nakashima, Tomoe Ohta, Keiko Ogawa, Masashi Fukaya, Junko Tsukioka, Tomohiro Hasei, Tetsushi Watanabe, Hisashi Matsuda
Six neolignan glucosides, named isodonosides I-VI, and a megastigmane glucoside named isodonmegastigmane I, were isolated together with 15 known compounds from the methanolic extract of aerial parts of Isodon japonicus cultivated in Tokushima, Japan. The chemical structures of the compounds were elucidated based on their MS and NMR spectroscopic analysis. The absolute configurations of the neolignan and megastigmane glucosides were determined by derivatizations, by ECD (electronic circular dicroism) Cotton effect approximation, and by the modified Mosher's method...
February 13, 2017: Phytochemistry
https://www.readbyqxmd.com/read/28208301/biomolecular-interaction-assays-identified-dual-inhibitors-of-glutaminase-and-glutamate-dehydrogenase-that-disrupt-mitochondrial-function-and-prevent-growth-of-cancer-cells
#15
Min Zhu, Jinzhang Fang, Jingjing Zhang, Zheng Zhang, Jianhui Xie, Yan Yu, Jennifer Jin Ruan, Zhao Chen, Wei Hou, Gensheng Yang, Weike Su, Benfang Helen Ruan
Glutaminase (KGA/isoenzyme GAC) is an emerging and important drug target for cancer. Traditional methods for assaying glutaminase activity are coupled with several other enzymes. Such coupled assays do not permit the direct and stringent characterization of specific glutaminase inhibitors. Ebselen was identified as a potent 9 nM KGA inhibitor in the KGA/glutamate oxidase (GO)/horse radish peroxidase (HRP) coupled assay but showed very weak activity in inhibiting the growth of glutamine-dependent cancer cells...
February 7, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28206767/palladium-catalyzed-double-isocyanide-insertion-via-oxidative-n-o-cleavage-of-acetyl-oximes-syntheses-of-2h-pyrrol-2-imines
#16
Gopal Chandru Senadi, Ting-Yi Lu, Ganesh Kumar Dhandabani, Jeh-Jeng Wang
The palladium-catalyzed reaction of acetyl oximes with isocyanides was developed for the synthesis of 2H-pyrrol-2-imines. The key steps were (i) generation of an enamido-palladium(II) species, (ii) migratory double-isocyanide insertion, and (iii) cyclization. The scope of the synthesis of some 2H-pyrrol-2-imines was extended to the synthesis 1H-pyrrole-2,3-dione/1H-benzo[g]indole-2,3-dione derivatives via acid hydrolysis in a sequential one-pot manner.
February 16, 2017: Organic Letters
https://www.readbyqxmd.com/read/28205265/borylative-radical-cyclizations-of-benzo-3-4-cyclodec-3-ene-1-5-diynes-and-n-heterocyclic-carbene-boranes
#17
Takashi Watanabe, Daisuke Hirose, Dennis P Curran, Tsuyoshi Taniguchi
Borylative radical cyclization of benzo[3,4]cyclodec-3-ene-1,5-diynes to provide 5-borylated 6,7,8,9-tetrahydrobenzo[a]azulenes has been developed. The experimental results suggest that the reaction proceeds by a radical chain mechanism, and di-tert-butyl hyponitrite (TBHN) works as a good radical initiator to form boryl radicals from N-heterocyclic carbene-boranes (NHC-boranes). The present reaction is a rare model to illustrate addition of boryl radicals to alkynes.
February 16, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28205067/optical-electrochemical-and-thermal-studies-of-conjugated-polymers-synthesized-by-eutectic-melt-reaction
#18
Chinna Bathula, Kezia Buruga, Youngjong Kang, Imtiyaz Ahmed M Khazi
This paper reports on the synthesis of a novel donor-acceptor conjugated polymers, P1 and P2 by solvent free eutectic melt polymerization reaction. Triisopropylsilylethynyl(TIPS) substituted benzo[1,2-b:4,5-b']dithiophene(BDT) is used as donor, thienithiophene(TT) and thienopyrroledione(TPD) are utilized as acceptors for demonstrating eutectic polymerization. The most important fact in the solvent-free reaction between solid reactants actually proceeds through bulk liquid phases. Such liquid phases are possible due to the formation of eutectics between the reactants and product(s) and any evolution of heat...
February 15, 2017: Journal of Fluorescence
https://www.readbyqxmd.com/read/28203639/determination-of-kinetic-bioconcentration-in-mussels-after-short-term-exposure-to-polycyclic-aromatic-hydrocarbons
#19
Ledicia Rey-Salgueiro, Elena Martínez-Carballo, Antonio Cid, Jesús Simal-Gándara
The kinetic bioconcentration of N-heterocyclic aromatic hydrocarbons and polycyclic aromatic hydrocarbons in mussels (Mytilus galloprovincialis) after short waterborne exposure was studied. Benzo[a]pyrene (BaP), its analogue azaarene 10-azabenzo[a]pyrene (AzaBaP), and their mixture (Mix), were selected to monitor the changes in water concentrations over three days. Decay of both PAHs concentrations in water after 24 h of waterborne exposure to mussels at levels of 10 and 100 μg/L follows a first order kinetic with half-lives of 4-5 h, with residual levels of PAHs below 7%...
January 2017: Heliyon
https://www.readbyqxmd.com/read/28198919/natural-compounds-from-mexican-medicinal-plants-as-potential-drug-leads-for-anti-tuberculosis-drugs
#20
Rocio Gómez-Cansino, Silvia Laura Guzmán-Gutiérrez, María Guadalupe Campos-Lara, Clara Ines Espitia-Pinzón, Ricardo Reyes-Chilpa
In Mexican Traditional Medicine 187 plant species are used in the treatment of respiratory conditions that may be associated with tuberculosis. In this contribution, we review the ethnobotany, chemistry and pharmacology of 63 species whose extracts have been assayed for antimycobacterial activity in vitro. Among these, the most potent is Aristolochia brevipes (MIC= 12.5 µg/mL), followed by Aristolochia taliscana, Citrus sinensis, Chrysactinia mexicana, Persea americana, and Olea europaea (MIC<64 µg/mL)...
February 9, 2017: Anais da Academia Brasileira de Ciências
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