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https://www.readbyqxmd.com/read/28644704/numerical-analysis-of-time-dependent-inhibition-kinetics-comparison-between-rat-liver-microsomes-and-rat-hepatocyte-data-for-mechanistic-model-fitting
#1
Chuong Pham, Swati Nagar, Ken Korzekwa
Time dependent inhibition (TDI) may confound drug interaction predictions. Recently, models were generated for an array of TDI kinetic schemes using numerical analysis of microsomal assays. Additionally, a distinct terminal inactivation step was identified for certain mechanism based inhibitors (MBI) following reversible metabolite intermediate complex (MIC) formation. Longer hepatocyte incubations potentially allow analysis of slow TDI and terminal inactivation. In the experiments presented here, we compared the quality of TDI parameterization by numerical analysis between hepatocyte and microsomal data...
June 23, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
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
#2
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/28642934/evaluation-of-the-antibacterial-and-antifungal-properties-of-phragmanthera-capitata-sprengel-balle-loranthaceae-a-mistletoe-growing-on-rubber-tree-using-the-dilution-techniques
#3
Franklin Uangbaoje Ohikhena, Olubunmi Abosede Wintola, Anthony Jide Afolayan
The alarming increase in multidrug resistance of pathogenic microorganisms to conventional drugs in recent years has prompted the search for new leads in alternative remedies in natural products. Hence, this study was aimed at evaluating the antimicrobial properties of Phragmanthera capitata, a parasitic mistletoe growing on rubber trees. The in vitro antimicrobial activities of the acetone, methanol, ethanol, and aqueous extracts were investigated using five gram-negative and five gram-positive bacteria and four fungi...
2017: TheScientificWorldJournal
https://www.readbyqxmd.com/read/28642751/in-vitro-antimicrobial-activity-of-chlorquinaldol-against-microorganisms-responsible-for-skin-and-soft-tissue-infections-comparative-evaluation-with-gentamicin-and-fusidic-acid
#4
Monica Bortolin, Alessandro Bidossi, Elena De Vecchi, Maura Avveniente, Lorenzo Drago
Skin and soft tissue infections (SSTIs) are a major therapeutic challenge for clinicians. The emergence of pathogens with decreased susceptibility to available therapies has become an emerging problem often associated with treatment failure. Hence, there is an urgent need for novel broad-spectrum antimicrobial agents. The purpose of this study was to assess the feasibility of chlorquinaldol as an alternative approach to currently used topical antibiotics for the treatment of skin and soft tissue infections...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28642571/pharmacokinetic-and-pharmacodynamic-modeling-of-cyadox-against-clostridium-perfringens-in-swine
#5
Lei Yan, Shuyu Xie, Dongmei Chen, Yuanhu Pan, Yanfei Tao, Wei Qu, ZhenLi Liu, Zonghui Yuan, Lingli Huang
The purpose of this study was to evaluate the activity of cyadox against Clostridium perfringens in swine and optimize the dosage regimen using ex vivo pharmacokinetic-pharmacodynamic (PK-PD) modeling. After oral administration, the ileum fluid of pigs containing the free cyadox was collected by implanted ultrafiltration probes. The Tmax, AUC24h, and CL/F of free cyadox in the ileum fluid were 1.96 h, 106.40 μg/h/mL, and 0.27 L/kg/h, respectively. Cyadox displayed a concentration-dependent killing action against C...
June 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28641919/prevalence-of-candida-africana-and-candida-dubliniensis-in-vulvovaginal-candidiasis-first-turkish-candida-africana-isolates-from-vulvovaginal-candidiasis
#6
G Hazirolan, H U Altun, R Gumral, N C Gursoy, B Otlu, B Sancak
INTRODUCTION: Candida africana and C. dubliniensis are closely related species of C. albicans. Current phenotypic methods are not suitable to accurately distinguish all the species belonging to the C. albicans complex. Several molecular-based methods have recently been designed for discriminating among closely related Candida species. The aim of this study was to establish the prevalence of C. dubliniensis and C. africana in vulvovaginal samples with phenotypic and genotypic methods...
June 19, 2017: Journal de Mycologie Médicale
https://www.readbyqxmd.com/read/28641565/d-amino-acid-analogues-of-the-antimicrobial-peptide-cdt-exhibit-anti-cancer-properties-in-a549-a-human-lung-adenocarcinoma-cell-line
#7
Deborah L Heyl, Hedeel Guy Evans, Jeff Guthrie, Murali Jujjavarapu, Nathan Hendrickson, Anna Eitel, Yeji Park, Jennifer Garvey, Rebecca Newman, Daniel Esckilsen
The importance of the antitumor activity of some antimicrobial peptides is being increasingly recognized. The antimicrobial peptide, tachyplesin, has been shown to exhibit anticancer properties and a linear, cysteine deleted analogue (CDT), was found to retain its antibacterial function. We used sequence reversal and D-amino acids to synthesize four CDT analogues. We found that D-CDT exhibited the best bactericidal properties with the highest selectivity index. While the MIC was found to improve only modestly against S...
June 20, 2017: Protein and Peptide Letters
https://www.readbyqxmd.com/read/28641525/1-1%C3%AA-carbonyldiimidazole-cdi-mediated-facile-synthesis-structural-characterization-antimicrobial-activity-and-in-silico-studies-of-coumarin-3-carboxamide-derivatives
#8
Uzma Salar, Khalid Mohammed Khan, Muhammad Imran Fakhri, Shafqat Hussain, Saima Tauseef, Shagufta Ameer, Abdul Wadood, Huma Khan, Shahnaz Perveen
BACKGROUND: Despite of the availability of variety of antibacterial agents, re-emergance of pathogenic bacteria is still a serious medical concern. So, identification of new, safer, and selective antibacterial agents is the key interest in the medicinal chemistry research. METHOD: To explore the antimicrobial activity of coumarin-3-carboxamides for a range of bacterial and fungal strains, twenty eight derivatives were synthesized by the reaction of coumarin-3-carboxylic acid with a variety of aniline derivatives in the presence of 1,1ꞌ-carbonyldiimidazole (CDI)...
June 22, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28641267/a-cpu-mic-collaborated-parallel-framework-for-gromacs-on-tianhe-2-supercomputer
#9
Shaoliang Peng, Shunyun Yang, Wenhe Su, Xiaoyu Zhang, Tenglilang Zhang, Weiguo Liu, Xingming Zhao
Molecular Dynamics (MD) is the simulation of the dynamic behavior of atoms and molecules. As the most popular software for molecular dynamics, GROMACS cannot work on large-scale data because of limit computing resources. In this paper, we propose a CPU and Intel® Xeon Phi Many Integrated Core (MIC) collaborated parallel framework to accelerate GROMACS using the offload mode on a MIC coprocessor, with which the performance of GROMACS is improved significantly, especially with the utility of Tianhe-2 supercomputer...
June 16, 2017: IEEE/ACM Transactions on Computational Biology and Bioinformatics
https://www.readbyqxmd.com/read/28641057/child-anthropometry-data-quality-from-demographic-and-health-surveys-multiple-indicator-cluster-surveys-and-national-nutrition-surveys-in-the-west-central-africa-region-are-we-comparing-apples-and-oranges
#10
Daniel J Corsi, Jessica M Perkins, S V Subramanian
BACKGROUND: There has been limited work comparing survey characteristics and assessing the quality of child anthropometric data from population-based surveys. OBJECTIVE: To investigate survey characteristics and indicators of quality of anthropometric data in children aged 0-59 months from 23 countries in the West Central Africa region. METHODS: Using established methodologies and criteria to examine child age, sex, height, and weight, we conducted a comprehensive assessment and scoring of the quality of anthropometric data collected in 100 national surveys...
2017: Global Health Action
https://www.readbyqxmd.com/read/28640352/synthesis-and-evaluation-of-arylamidine-derivatives-for-new-antimicrobial-and-cytotoxic-activities
#11
Zenaide S Monte, Amanda M Silva, Gláucia M S Lima, Teresinha G DA Silva, Karla M R Marques, Maria D Rodrigues, Emerson P S Falcão, Sebastião J Melo
A series of arylamidines 3a-j was designed, synthesized and investigated for antimicrobial activity. Structures of the compounds were confirmed by IR, 1H-NMR and 13C-NMR and a 2D spectroscopic study was performed. A preliminary screening of the antimicrobial tests clearly showed that three out of ten arylamidines, viz, 3f, 3g and 3i, were effective against all the gram-negative bacteria: Klebsiella pneumoniae, Pseudomonas aeruginosa and Salmonella enteric; and against the yeast, candida albicans. Further, the Minimum Inhibitory Concentrations (MIC) against the bacteria and yeast were determined...
April 2017: Anais da Academia Brasileira de Ciências
https://www.readbyqxmd.com/read/28640317/octyl-gallate-a-food-additive-with-potential-beneficial-properties-to-treat-helicobacter-pylori-infection
#12
Vanessa Gonçalves Wolf, Cibele Bonacorsi, Maria Stella Gonçalves Raddi, Luiz Marcos da Fonseca, Valdecir Farias Ximenes
Helicobacter pylori infection is marked by intense production of reactive oxygen species (ROS) through the activation of neutrophils that are constantly attracted to the infected gastric mucosa. Here, gallic acid and its alkyl esters were evaluated as compounds able to act as antimicrobial agents and inhibitors of ROS released by H. pylori-activated neutrophils simultaneously. We found that the higher hydrophobicity caused by esterification of gallic acid led to a significant increase in its ability as a cytotoxic agent against H...
June 22, 2017: Food & Function
https://www.readbyqxmd.com/read/28638876/phytochemical-screening-antimicrobial-and-cytotoxicity-studies-of-ethanol-leaf-extract-of-aphaniasenegalensis-sapindaceae
#13
Alioune Dior Fall, Victor Patrick Bagla, Emmanuel Bassene, Jacobus Nicolaas Eloff
BACKGROUND: Aphania senegalensis (Sapindaceae) is commonly used in Senegalese traditional medicine to treat pain, inflammation, asthenia, bacterial and fungal infections. The aim of this study was to determine the type of phytochemical constituents present in the ethanol leaf extract and its antimicrobial activity against selected bacterial and fungal pathogens. MATERIALS AND METHODS: The ethanol leaf extract of A. senegalensis was evaluated for its cytotoxic effect in the MTT assay against Vero cells...
2017: African Journal of Traditional, Complementary, and Alternative Medicines: AJTCAM
https://www.readbyqxmd.com/read/28637339/emergence-of-ceftazidime-avibactam-non-susceptibility-in-an-mdr-klebsiella-pneumoniae-isolate
#14
Anna Both, Henning Büttner, Jiabin Huang, Markus Perbandt, Cristina Belmar Campos, Martin Christner, Florian P Maurer, Stefan Kluge, Christina König, Martin Aepfelbacher, Dominic Wichmann, Holger Rohde
Background: Avibactam is a novel broad-range β-lactamase inhibitor active against Ambler class A (including ESBL and KPC) and some Ambler class C and D (e.g. OXA-48) enzymes. We here report on the emergence of ceftazidime/avibactam resistance in clinical, multiresistant, OXA-48 and CTX-M-14-producing Klebsiella pneumoniae isolate DT12 during ceftazidime/avibactam treatment. Methods and results: Comparative whole-genome sequence analysis identified two SNPs in the CTX-M-14-encoding gene leading to two amino acid changes (P170S and T264I)...
June 16, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28637081/molecular-characterization-of-gluten-hydrolyzing-bacillus-spp-and-their-efficacy-and-biotherapeutic-potential-as-probiotics-using-caco-2-cell-line
#15
B S Rashmi, Gayathri Devaraja
AIM: To isolate and characterize indigenous gluten hydrolyzing bacteria from wheat sourdough and curd samples and further evaluation of their probiotic potentiality. METHODS AND RESULTS: Indigenous gluten hydrolyzing isolates GS 33, GS 143, GS 181 and GS 188 were identified as Bacillus spp. by molecular-typing methods and studied extensively for their functional and probiotic attributes. All the tested isolates could survive at pH 2 and toxicity of 0.3% bile and also exhibited cell-surface hydrophobicity and autoaggregation phenotype...
June 21, 2017: Journal of Applied Microbiology
https://www.readbyqxmd.com/read/28636756/chemical-composition-and-allelopathic-antibacterial-antifungal-and-antiacetylcholinesterase-activity-of-fish-mint-houttuynia-cordata-thunb-from-india
#16
Ram S Verma, Neeta Joshi, Rajendra C Padalia, Ved R Singh, Prakash Goswami, Ajay Kumar, Hina Iqbal, Rajesh K Verma, Debabrata Chanda, Amit Chauhan, Dharmendra Saikia
Fish-mint (Houttuynia cordata Thunb.), belongs to family Saururaceae has long been used as food and traditional herbal medicine. The present study was framed to assess the changes occurring in the essential-oil composition of Houttuynia cordata during annual growth and to evaluate allelopathic, antibacterial, antifungal and antiacetylcholinesterase activities. The essential-oil content ranged from 0.06-0.14% and 0.08-0.16% in aerial-parts and underground-stem, respectively. The essential oils were analysed by GC-FID, GC-MS and NMR ((1) H & (13) C)...
June 21, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/28636609/genomic-and-phenotypic-characterisation-of-fluoroquinolone-resistance-mechanisms-in-enterobacteriaceae-in-durban-south-africa
#17
John Osei Sekyere, Daniel Gyamfi Amoako
Resistance to fluoroquinolones (FQ) is being increasingly reported and found to be mediated by efflux pumps, plasmid-mediated quinolone resistance genes (PMQR) and mutations in gyrA, gyrB, parC and parE. However, studies reporting on FQ resistance mechanisms (FQRM), particularly in Africa, are focused mostly on Salmonella. This study used a whole-genome-based approach to describe FQRM in forty-eight clinical Enterobacteriaceae isolates comprising of Klebsiella pneumoniae (n = 21), Serratia marcescens (n = 12), Enterobacter spp...
2017: PloS One
https://www.readbyqxmd.com/read/28636325/challenges-and-hallmarks-of-establishing-alkylacetylphosphonates-as-probes-of-bacterial-1-deoxy-d-xylulose-5-phosphate-synthase
#18
Sara Sanders, Ryan J Vierling, David Bartee, Alicia A DeColli, Mackenzie J Harrison, Joseph L Aklinski, Andrew T Koppisch, Caren L Freel Meyers
1-Deoxy-d-xylulose 5-phosphate (DXP) synthase catalyzes the thiamin diphosphate (ThDP)-dependent formation of DXP from pyruvate and d-glyceraldehyde 3-phosphate. DXP is at a metabolic branch point in bacteria, feeding into the methylerythritol phosphate pathway to indispensable isoprenoids and acting as a precursor for biosynthesis of essential cofactors in central metabolism, pyridoxal phosphate and ThDP, the latter of which is also required for DXP synthase catalysis. DXP synthase follows a unique random sequential mechanism and possesses an unusually large active site...
June 21, 2017: ACS Infectious Diseases
https://www.readbyqxmd.com/read/28634338/coumarin-benzimidazole-hybrids-as-a-potent-antimicrobial-agent-synthesis-and-biological-elevation
#19
L Ravithej Singh, Srinivasa Rao Avula, Sneha Raj, Akanksha Srivastava, Gopala Reddy Palnati, C K M Tripathi, Mukesh Pasupuleti, Koneni V Sashidhara
Molecular hybridization approach is an emerging tool in drug discovery for designing new pharmacophores with biological activity. A novel, new series of coumarin-benzimidazole hybrids were designed, synthesized and evaluated for their broad spectrum antimicrobial activity. Among all the synthesized molecules, compound (E)-3-(2-1H-benzo[d]imidazol-1-yl)-1-((4-chlorobenzyl)oxy)imino)ethyl)-2H-chromen-2-one showed the most promising broad spectrum antibacterial activity against Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis and Proteus vulgaris...
June 21, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28633894/synthesis-and-antibacterial-activity-of-5-methylphenanthridium-derivatives-as-ftsz-inhibitors
#20
Fang Liu, Henrietta Venter, Fangchao Bi, Susan J Semple, Jingru Liu, Chaobin Jin, Shutao Ma
5-Methylphenanthridium derivatives were designed, synthesized and evaluated for their in vitro antibacterial activity and cell division inhibitory activity against various Gram-positive and -negative bacteria. Among them, compounds 5A2, 5B1, 5B2, 5B3, 5C1 and 5C2 displayed the best on-target antibacterial activity with an MIC value of 4µg/mL against B. subtilis ATCC9372 and S. pyogenes PS, showing over 2-fold better activity than sanguinarine. The SARs showed that the 5-methylphenanthridium derivatives with the alkyl side chains at the 2-postion, especially the straight alkyl side chains exerted better on-target antibacterial activity...
June 3, 2017: Bioorganic & Medicinal Chemistry Letters
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