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https://www.readbyqxmd.com/read/28335571/3-substituted-n-benzylpyrazine-2-carboxamide-derivatives-synthesis-antimycobacterial-and-antibacterial-evaluation
#1
Lucia Semelková, Ondřej Janďourek, Klára Konečná, Pavla Paterová, Lucie Navrátilová, František Trejtnar, Vladimír Kubíček, Jiří Kuneš, Martin Doležal, Jan Zitko
A series of substituted N-benzyl-3-chloropyrazine-2-carboxamides were prepared as positional isomers of 5-chloro and 6-chloro derivatives, prepared previously. During the aminolysis of the acyl chloride, the simultaneous substitution of chlorine with benzylamino moiety gave rise to N-benzyl-3-(benzylamino)pyrazine-2-carboxamides as side products, in some cases. Although not initially planned, the reaction conditions were modified to populate this double substituted series. The final compounds were tested against four mycobacterial strains...
March 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28335560/serum-amyloid-a-production-is-triggered-by-sleep-deprivation-in-mice-and-humans-is-that-the-link-between-sleep-loss-and-associated-comorbidities
#2
Edson M de Oliveira, Bruna Visniauskas, Sergio Tufik, Monica L Andersen, Jair R Chagas, Ana Campa
Serum amyloid A (SAA) was recently associated with metabolic endotoxemia, obesity and insulin resistance. Concurrently, insufficient sleep adversely affects metabolic health and is an independent predisposing factor for obesity and insulin resistance. In this study we investigated whether sleep loss modulates SAA production. The serum SAA concentration increased in C57BL/6 mice subjected to sleep restriction (SR) for 15 days or to paradoxical sleep deprivation (PSD) for 72 h. Sleep restriction also induced the upregulation of Saa1...
March 21, 2017: Nutrients
https://www.readbyqxmd.com/read/28335544/combination-effect-of-antituberculosis-drugs-and-ethanolic-extract-of-selected-medicinal-plants-against-multi-drug-resistant-mycobacterium-tuberculosis-isolates
#3
Prabasiwi Nur Fauziyah, Elin Yulinah Sukandar, Dhyan Kusuma Ayuningtyas
Adverse drug reaction and resistance to antituberculosis drugs remain the causes of tuberculosis therapeutic failure. This research aimed to find the combination effect of standard antituberculosis drugs with Hibiscus sabdariffa L., Kaempferia galanga L., and Piper crocatum N.E. Br against multi-drug resistant (MDR) Mycobacterium tuberculosis isolates. Two MDR strains (i.e., isoniazid/ethambutol resistant and rifampicin/streptomycin resistant) of M. tuberculosis were inoculated in Löwenstein-Jensen medium containing a combination of standard antituberculosis drugs and ethanolic extracts of H...
March 20, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28335533/exploring-impacts-of-taxes-and-hospitality-bans-on-cigarette-prices-and-smoking-prevalence-using-a-large-dataset-of-cigarette-prices-at-stores-2001-2011-usa
#4
Lance S Ballester, Amy H Auchincloss, Lucy F Robinson, Stephanie L Mayne
In the USA, little is known about local variation in retail cigarette prices; price variation explained by taxes, bans, and area-level socio-demographics, and whether taxes and hospitality bans have synergistic effects on smoking prevalence. Cigarette prices 2001-2011 from chain supermarkets and drug stores (n = 2973) were linked to state taxes (n = 41), state and county bar/restaurant smoking bans, and census block group socio-demographics. Hierarchical models explored effects of taxes and bans on retail cigarette prices as well as county smoking prevalence (daily, non-daily)...
March 20, 2017: International Journal of Environmental Research and Public Health
https://www.readbyqxmd.com/read/28335529/effects-of-momordica-charantia-bitter-melon-on-ischemic-diabetic-myocardium
#5
Attila Czompa, Alexandra Gyongyosi, Kitti Szoke, Istvan Bak, Evelin Csepanyi, David D Haines, Arpad Tosaki, Istvan Lekli
Objective: A rat model is here used to test a hypothesis that Momordica charantia (Bitter melon (BM)) extract favorably alters processes in cardiovascular tissue and is systemically relevant to the pathophysiology of type 2 diabetes (T2DM) and related cardiovascular disease. Methods: Male Lean and Zucker Obese (ZO) rats were gavage-treated for six weeks with 400 mg/kg body weight bitter melon (BM) extract suspended in mucin-water vehicle, or with vehicle (Control). Animals were segregated into four treatment groups, 10 animals in each group, according to strain (Lean or ZO) and treatment (Control or BM)...
March 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28335526/oral-cyanocobalamin-is-effective-in-the-treatment-of-vitamin-b12-deficiency-in-crohn-s-disease
#6
Fernando Gomollón, Carla J Gargallo, Jose Fernando Muñoz, Raquel Vicente, Alberto Lue, Alberto Mir, Marta García-Alvarado, Marta Gracia, Santiago García-López
Cobalamin deficiency is common in patients with Crohn's disease (CD). Intramuscular cobalamin continues to be the standard therapy for the deficiency and maintenance treatment in these patients, although oral route has been demonstrated to be effective in other pathologies with impaired absorption. Our aims were to evaluate the efficacy of oral therapy in the treatment of cobalamin deficiency and in long-term maintenance in patients with Crohn's disease. We performed a multicenter retrospective cohort study that included 94 patients with Crohn's disease and cobalamin deficiency...
March 20, 2017: Nutrients
https://www.readbyqxmd.com/read/28335506/a-colorimetric-sensor-for-the-highly-selective-detection-of-sulfide-and-1-4-dithiothreitol-based-on-the-in-situ-formation-of-silver-nanoparticles-using-dopamine
#7
Lingzhi Zhao, Liu Zhao, Yanqing Miao, Chunye Liu, Chenxiao Zhang
Hydrogen sulfide (H₂S) has attracted attention in biochemical research because it plays an important role in biosystems and has emerged as the third endogenous gaseous signaling compound along with nitric oxide (NO) and carbon monoxide (CO). Since H₂S is a kind of gaseous molecule, conventional approaches for H₂S detection are mostly based on the detection of sulfide (S(2-)) for indirectly reflecting H₂S levels. Hence, there is a need for an accurate and reliable assay capable of determining sulfide in physiological systems...
March 20, 2017: Sensors
https://www.readbyqxmd.com/read/28335496/quantitative-analysis-of-the-kshv-transcriptome-following-primary-infection-of-blood-and-lymphatic-endothelial-cells
#8
A Gregory Bruce, Serge Barcy, Terri DiMaio, Emilia Gan, H Jacques Garrigues, Michael Lagunoff, Timothy M Rose
The transcriptome of the Kaposi's sarcoma-associated herpesvirus (KSHV/HHV8) after primary latent infection of human blood (BEC), lymphatic (LEC) and immortalized (TIME) endothelial cells was analyzed using RNAseq, and compared to long-term latency in BCBL-1 lymphoma cells. Naturally expressed transcripts were obtained without artificial induction, and a comprehensive annotation of the KSHV genome was determined. A set of unique coding sequence (UCDS) features and a process to resolve overlapping transcripts were developed to accurately quantitate transcript levels from specific promoters...
March 19, 2017: Pathogens
https://www.readbyqxmd.com/read/28335485/intra-amniotic-administration-of-raffinose-and-stachyose-affects-the-intestinal-brush-border-functionality-and-alters-gut-microflora-populations
#9
Sarina Pacifici, Jaehong Song, Cathy Zhang, Qiaoye Wang, Raymond P Glahn, Nikolai Kolba, Elad Tako
This study investigates the effectiveness of two types of prebiotics-stachyose and raffinose-which are present in staple food crops that are widely consumed in regions where dietary Fe deficiency is a health concern. The hypothesis is that these prebiotics will improve Fe status, intestinal functionality, and increase health-promoting bacterial populations in vivo (Gallus gallus). By using the intra-amniotic administration procedure, prebiotic treatment solutions were injected in ovo (day 17 of embryonic incubation) with varying concentrations of a 1...
March 19, 2017: Nutrients
https://www.readbyqxmd.com/read/28335484/energy-of-intramolecular-hydrogen-bonding-in-ortho-hydroxybenzaldehydes-phenones-and-quinones-transfer-of-aromaticity-from-ipso-benzene-ring-to-the-enol-system-s
#10
Danuta Rusinska-Roszak
Intramolecular hydrogen bonding (HB) is one of the most studied noncovalent interactions of molecules. Many physical, spectral, and topological properties of compounds are under the influence of HB, and there are many parameters used to notice and to describe these changes. Hitherto, no general method of measurement of the energy of intramolecular hydrogen bond (EHB) has been put into effect. We propose the molecular tailoring approach (MTA) for EHB calculation, modified to apply it to Ar-O-H∙∙∙O=C systems...
March 18, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28335476/inhibition-of-neoplastic-transformation-and-chemically-induced-skin-hyperplasia-in-mice-by-traditional-chinese-medicinal-formula-si-wu-tang
#11
Mandy M Liu, Kevin M Huang, Steven Yeung, Andy Chang, Suhui Zhang, Nan Mei, Cyrus Parsa, Robert Orlando, Ying Huang
Exploring traditional medicines may lead to the development of low-cost and non-toxic cancer preventive agents. Si-Wu-Tang (SWT), comprising the combination of four herbs, Rehmanniae, Angelica, Chuanxiong, and Paeoniae, is one of the most popular traditional Chinese medicines for women's diseases. In our previous studies, the antioxidant Nrf2 pathways were strongly induced by SWT in vitro and in vivo. Since Nrf2 activation has been associated with anticarcinogenic effects, the purpose of this study is to evaluate SWT's activity of cancer prevention...
March 18, 2017: Nutrients
https://www.readbyqxmd.com/read/28335470/design-of-new-benzo-h-chromene-derivatives-antitumor-activities-and-structure-activity-relationships-of-the-2-3-positions-and-fused-rings-at-the-2-3-positions
#12
Rawda M Okasha, Fawzia F Alblewi, Tarek H Afifi, Arshi Naqvi, Ahmed M Fouda, Al-Anood M Al-Dies, Ahmed M El-Agrody
A series of novel 4H-benzo[h]chromenes 4, 6-11, 13, 14; 7H-benzo[h]chromeno[2,3-d]pyrimidines 15-18, 20, and 14H-benzo[h]chromeno[3,2-e][1,2,4]triazolo[1,5-c]pyrimidine derivatives 19a-e, 24 was prepared. The structures of the synthesized compounds were characterized on the basis of their spectral data. Some of the target compounds were examined for their antiproliferative activity against three cell lines; breast carcinoma (MCF-7), human colon carcinoma (HCT-116) and hepatocellular carcinoma (HepG-2). The cytotoxic behavior has been tested using MTT assay and the inhibitory activity was referenced to three standard anticancer drugs: vinblastine, colchicine and doxorubicin...
March 18, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28335468/differential-degradation-and-detoxification-of-an-aromatic-pollutant-by-two-different-peroxidases
#13
Aysha Hamad Alneyadi, Iltaf Shah, Synan F AbuQamar, Syed Salman Ashraf
Enzymatic degradation of organic pollutants is a new and promising remediation approach. Peroxidases are one of the most commonly used classes of enzymes to degrade organic pollutants. However, it is generally assumed that all peroxidases behave similarly and produce similar degradation products. In this study, we conducted detailed studies of the degradation of a model aromatic pollutant, Sulforhodamine B dye (SRB dye), using two peroxidases-soybean peroxidase (SBP) and chloroperoxidase (CPO). Our results show that these two related enzymes had different optimum conditions (pH, temperature, H₂O₂ concentration, etc...
March 18, 2017: Biomolecules
https://www.readbyqxmd.com/read/28335466/a-specific-mixture-of-nutrients-suppresses-ovarian-cancer-a-2780-tumor-incidence-growth-and-metastasis-to-lungs
#14
Mohd Waheed Roomi, Tatiana Kalinovsky, Matthias Rath, Aleksandra Niedzwiecki
Ovarian cancer is the deadliest gynecological malignancy in women, and fifth leading cause of death. Despite advances made in chemotherapy and surgery, the average time of clinical remission is approximately 2 years and the 5-year survival rate is 45%. Thus, there is an urgent need for the development of a novel therapeutic approach to ovarian cancer treatment. We investigated the effect of a specific nutrient mixture (EPQ) containing ascorbic acid, lysine, proline, green tea extract, and quercetin on human ovarian cancer cell A-2780 in vivo and in vitro...
March 18, 2017: Nutrients
https://www.readbyqxmd.com/read/28335454/porcine-rotaviruses-epidemiology-immune-responses-and-control-strategies
#15
REVIEW
Anastasia N Vlasova, Joshua O Amimo, Linda J Saif
Rotaviruses (RVs) are a major cause of acute viral gastroenteritis in young animals and children worldwide. Immunocompetent adults of different species become resistant to clinical disease due to post-infection immunity, immune system maturation and gut physiological changes. Of the 9 RV genogroups (A-I), RV A, B, and C (RVA, RVB, and RVC, respectively) are associated with diarrhea in piglets. Although discovered decades ago, porcine genogroup E RVs (RVE) are uncommon and their pathogenesis is not studied well...
March 18, 2017: Viruses
https://www.readbyqxmd.com/read/28335450/assessment-of-radioactive-materials-and-heavy-metals-in-the-surface-soil-around-the-bayanwula-prospective-uranium-mining-area-in-china
#16
Haribala Bai, Bitao Hu, Chengguo Wang, Shanhu Bao, Gerilemandahu Sai, Xiao Xu, Shuai Zhang, Yuhong Li
The present work is the first systematic and large scale study on radioactive materials and heavy metals in surface soil around the Bayanwula prospective uranium mining area in China. In this work, both natural and anthropogenic radionuclides and heavy metals in 48 surface soil samples were analyzed using High Purity Germanium (HPGe) γ spectrometry and inductively coupled plasma-mass spectrometry (ICP-MS). The obtained mean activity concentrations of (238)U, (226)Ra, (232)Th, (40)K, and (137)Cs were 25.81 ± 9...
March 14, 2017: International Journal of Environmental Research and Public Health
https://www.readbyqxmd.com/read/28335434/induction-of-g2m-arrest-by-flavokawain-a-a-kava-chalcone-increases-the-responsiveness-of-her2-overexpressing-breast-cancer-cells-to-herceptin
#17
Danielle D Jandial, Lauren S Krill, Lixia Chen, Chunli Wu, Yu Ke, Jun Xie, Bang H Hoang, Xiaolin Zi
HER2/neu positive breast tumors predict a high mortality and comprise 25%-30% of breast cancer. We have shown that Flavokawain A (FKA) preferentially reduces the viabilities of HER2-overexpressing breast cancer cell lines (i.e., SKBR3 and MCF7/HER2) versus those with less HER2 expression (i.e., MCF7 and MDA-MB-468). FKA at cytotoxic concentrations to breast cancer cell lines also has a minimal effect on the growth of non-malignant breast epithelial MCF10A cells. FKA induces G2M arrest in cell cycle progression of HER2-overexpressing breast cancer cell lines through inhibition of Cdc2 and Cdc25C phosphorylation and downregulation of expression of Myt1 and Wee1 leading to increased Cdc2 kinase activities...
March 14, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28335422/association-between-coffee-consumption-and-its-polyphenols-with-cardiovascular-risk-factors-a-population-based-study
#18
Andreia Machado Miranda, Josiane Steluti, Regina Mara Fisberg, Dirce Maria Marchioni
Epidemiological studies have examined the effect of coffee intake on cardiovascular disease, but the benefits and risks for the cardiovascular system remain controversial. Our objective was to evaluate the association between coffee consumption and its polyphenols on cardiovascular risk factors. Data came from the "Health Survey of São Paulo (ISA-Capital)" among 557 individuals, in São Paulo, Brazil. Diet was assessed by two 24-h dietary recalls. Coffee consumption was categorized into <1, 1-3, and ≥3 cups/day...
March 14, 2017: Nutrients
https://www.readbyqxmd.com/read/28335421/pamam-dendrimers-cross-the-blood-brain-barrier-when-administered-through-the-carotid-artery-in-c57bl-6j-mice
#19
Bhairavi Srinageshwar, Sarah Peruzzaro, Melissa Andrews, Kayla Johnson, Allison Hietpas, Brittany Clark, Crystal McGuire, Eric Petersen, Jordyn Kippe, Andrew Stewart, Olivia Lossia, Abeer Al-Gharaibeh, Aaron Antcliff, Rebecca Culver, Douglas Swanson, Gary Dunbar, Ajit Sharma, Julien Rossignol
Drug delivery into the central nervous system (CNS) is challenging due to the blood-brain barrier (BBB) and drug delivery into the brain overcoming the BBB can be achieved using nanoparticles such as dendrimers. The conventional cationic dendrimers used are highly toxic. Therefore, the present study investigates the role of novel mixed surface dendrimers, which have potentially less toxicity and can cross the BBB when administered through the carotid artery in mice. In vitro experiments investigated the uptake of amine dendrimers (G1-NH₂ and G4-NH₂) and novel dendrimers (G1-90/10 and G4-90/10) by primary cortical cultures...
March 14, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28335396/optimization-of-conditions-for-cyanidin-3-oglucoside-c3g-nanoliposome-production-by-response-surface-methodology-and-cellular-uptake-studies-in-caco-2-cells
#20
Tisong Liang, Rongfa Guan, Haitao Shen, Qile Xia, Mingqi Liu
We aimed to optimize the formulation of C3G nanoliposomes using response surface methodology. Additionally, we evaluated the stability, particle change, and encapsulation efficiency (EE) of C3G nanoliposomes under different temperatures and storage durations, as well as in simulated gastrointestinal juice (SGF) and simulated intestinal fluid. The morphology of C3G nanoliposomes was observed by transmission electron microscope. The ability of C3G nanoliposomes to affect cancer cell morphology and inhibit cancer cell proliferation was studied with Caco-2 cells...
March 13, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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