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https://www.readbyqxmd.com/read/28107695/antibacterial-activity-computational-analysis-and-host-toxicity-study-of-thymol-sulfonamide-conjugates
#1
Shasank S Swain, Sudhir K Paidesetty, Rabindra N Padhy
Methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin resistant Enterococcus faecalis (VRE) are notorious pathogenic multidrug resistant (MDR) bacteria in both hospital and community sectors, and today the first antibacterial drug sulfamethoxazole is ineffective. The monoterpene phenol, thymol was conjugated with seven sulfa drug derivatives individually, adopting the dye-azo synthesis protocol, and conjugates were characterized using spectral analysis techniques such as, UV, FTIR, MS, HPLC, (1)H NMR, (13)C NMR and SEM...
January 17, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28107663/antibacterial-anti-oxidant-electroactive-injectable-hydrogel-as-self-healing-wound-dressing-with-hemostasis-and-adhesiveness-for-cutaneous-wound-healing
#2
Xin Zhao, Hao Wu, Baolin Guo, Ruonan Dong, Yusheng Qiu, Peter X Ma
Injectable self-healing hydrogel dressing with multifunctional properties including anti-infection, anti-oxidative and conductivity promoting wound healing process will be highly desired in wound healing application and its design is still a challenge. We developed a series of injectable conductive self-healed hydrogels based on quaternized chitosan-g-polyaniline (QCSP) and benzaldehyde group functionalized poly(ethylene glycol)-co-poly(glycerol sebacate) (PEGS-FA) as antibacterial, anti-oxidant and electroactive dressing for cutaneous wound healing...
January 11, 2017: Biomaterials
https://www.readbyqxmd.com/read/28107379/experimental-and-in-silico-investigation-of-anti-microbial-activity-of-1-chloro-2-isocyanatoethane-derivatives-of-thiomorpholine-piperazine-and-morpholine
#3
Charles O Nwuche, Oguejiofo T Ujam, Akachukwu Ibezim, Ifeoma B Ujam
The Antibiogram properties of 1-chloro-2-isocyanatoethane derivatives of thiomorpholine (CTC), piperazine (CPC) and morpholine (CMC) were evaluated by the approved agar well diffusion, the minimum inhibitory concentration (MIC) and in silico techniques. A total of fourteen microbial cultures consisting of ten bacteria and four yeast strains were used in the biological study while affinity of the compounds for DNA gyrase, a validated antibacterial drug target, was investigated by docking method. Results indicate that both thiomorpholine and piperazine had zero activity against the Gram negative organisms tested...
2017: PloS One
https://www.readbyqxmd.com/read/28107121/a-case-based-approach-to-evaluate-the-potential-risks-associated-with-fluoroquinolones-and-steroids
#4
Timothy Nguyen, Karin Gelband
Fluoroquinolones (FQs) are a frequently prescribed class of antibacterial agents. FQs are widely used but may carry serious side effects particularly pronounced in older adults, and the Food and Drug Administration recently suggested FQs should not be routinely used in certain conditions if alternative options are available. Research has demonstrated that the risk of tendinitis and tendon rupture associated with FQs is one of the highest in older adults who are concurrently treated with steroids. Health care providers and pharmacists involved in the treatment of older adults should be aware of this potential drug interaction, which may lead to serious side effects and safety concerns...
November 1, 2016: Consultant Pharmacist: the Journal of the American Society of Consultant Pharmacists
https://www.readbyqxmd.com/read/28106929/conformational-analysis-of-an-antibacterial-cyclodepsipeptide-active-against-m-tuberculosis-by-a-combined-roe-and-rdc-analysis
#5
Maic Fredersdorf, Michael Kurz, Armin Bauer, Marc-Olivier Ebert, Carla Rigling, Laurie Lannes, Christina Thiele
Griselimycin (GM) and methylgriselimycin (MGM), naturally produced by microorganisms of the genus Streptomyces, are cyclic depsipeptides composed of ten amino acids. They exhibit antibacterial activity against mycobacterium species by inhibiting the sliding clamp of prokaryotic DNA polymerase III and are therefore considered as potential anti-tuberculosis drugs. The difference between both peptides is the presence of L -(R)-4-methylproline in MGM instead of L -proline in GM at position 8 of the amino acid sequence...
January 20, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28106774/effects-of-long-term-water-aging-on-novel-anti-biofilm-and-protein-repellent-dental-composite
#6
Ning Zhang, Ke Zhang, Mary A S Melo, Michael D Weir, David J Xu, Yuxing Bai, Hockin H K Xu
The aims of this study were to: (1) synthesize an anti-biofilm and protein-repellent dental composite by combining 2-methacryloyloxyethyl phosphorylcholine (MPC) with quaternary ammonium dimethylaminohexadecyl methacrylate (DMAHDM); and (2) evaluate the effects of water-aging for 180 days on protein resistance, bacteria-killing ability, and mechanical properties of MPC-DMAHDM composite. MPC and DMAHDM were added into a resin composite. Specimens were stored in distilled water at 37 °C for 1, 30, 90, and 180 days...
January 18, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28106736/development-and-sequential-analysis-of-a-new-multi-agent-anti-acne-formulation-based-on-plant-derived-antimicrobial-and-anti-inflammatory-compounds
#7
Crina Saviuc, Bianca Ciubucă, Gabriela Dincă, Coralia Bleotu, Veronica Drumea, Mariana-Carmen Chifiriuc, Marcela Popa, Gratiela Gradisteanu Pircalabioru, Luminita Marutescu, Veronica Lazăr
The antibacterial and anti-inflammatory potential of natural, plant-derived compounds has been reported in many studies. Emerging evidence indicates that plant-derived essential oils and/or their major compounds may represent a plausible alternative treatment for acne, a prevalent skin disorder in both adolescent and adult populations. Therefore, the purpose of this study was to develop and subsequently analyze the antimicrobial activity of a new multi-agent, synergic formulation based on plant-derived antimicrobial compounds (i...
January 17, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28106379/sustainable-release-of-vancomycin-from-silk-fibroin-nanoparticles-for-treating-severe-bone-infections-in-a-rat-tibia-osteomyelitis-model
#8
Negar Hassani Besheli, Fatemeh Mottaghitalab, Masoud Eslami, Mahdi Gholami, Subhas C Kundu, David L Kaplan, Mehdi Farokhi
The successful treatment of bone infections is a major challenge in the field of orthopedics. There are some common methods for treating bone infections, including systemic antibiotic administration, local non-degradable drug vehicles, and surgical debridement and each of these approaches has advantages and disadvantages. In the present study, the antibiotic vancomycin (VANCO) was loaded in silk fibroin nanoparticles (SFNPs) and the complexes were then entrapped in silk scaffolds to form sustained drug delivery systems...
January 20, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28106348/a-biosurfactant-inspired-heptapeptide-with-improved-specificity-to-kill-mrsa
#9
Yuan Liu, Shuangyang Ding, Richard Dietrich, Erwin Märtlbauer, Kui Zhu
The emergence and rapid spread of methicillin-resistant Staphylococcus aureus (MRSA) poses a serious threat to public health. New antibiotics and strategies are urgently needed to combat S. aureus associated infections. Bacaucin, a novel cyclic lipopeptide from Bacillus subtilis CAU21, is reported. Bacaucin shows broad antibacterial activity against Gram-positive bacteria, but is also hemolytic and cytotoxic. However, bacaucin-1, a bacaucin-inspired ring-opened heptapeptide, shows specific antibacterial activity against MRSA by a membrane-disruptive mechanism without detectable toxicity to mammalian cells or induction of bacterial resistance...
February 1, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28104898/design-characterization-and-antimicrobial-activity-of-novel-antimicrobial-peptide-derived-from-bovine-lactophoricin
#10
Ji-Sun Kim, Ji-Ho Joeng, Yongae Kim
Lactophoricin (LPcin) which is a part of proteose peptone isolated from bovine milk is a cationic amphipathic α-helical antimicrobial peptide. Its truncated variants and mutated analogs were designed and their antimicrobial activities were evaluated by using various assays like broth dilution methods and disk diffusion methods as well as hemolysis assay. Three analogs of LPcin-C8 (LPcin-YK1), LPcin-T2&6W (LPcin-YK2), and LPcin-T2&6W-C8 (LPcin-YK3) that showed better antibiotic activities than LPcin were selected...
January 20, 2017: Journal of Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28104533/antimicrobial-activity-of-stable-hemiaminals-against-porphyromonas-gingivalis
#11
Teresa Olczak, Michał Śmiga, Anna Kwiecień, Marcin Bielecki, Robert Wróbel, Mariusz Olczak, Zbigniew Ciunik
Porphyromonas gingivalis is a major etiologic agent and a key pathogen responsible for the development and progression of chronic periodontitis. Controlling the number of periodontal pathogens is one of the primary actions for maintaining oral health; therefore, active compounds with a capacity to exert antimicrobial activity have received considerable attention as they may represent potential new therapeutic agents for the treatment of chronic periodontitis. Heterocyclic compounds possessing 1,2,4- or 1,2,3-triazoles are known for several biological activities, including antibacterial properties...
January 16, 2017: Anaerobe
https://www.readbyqxmd.com/read/28104503/invasive-candida-krusei-infection-and-candida-vasculitis-of-a-leg-ulcer-in-an-immunocompetent-patient-a-case-report
#12
Jud Philipp, Valentin Thomas, Regauer Sigrid, Gary Thomas, Hackl Gerald, Rief Peter, Brodmann Marianne, Hafner Franz
A 71year old female Caucasian farmer without any known immunosuppression presented with a painful ulcer of her right lower leg after a trauma caused by a wood billet. There was no response to empirical antibacterial treatment. An ulcer biopsy showed an invasive Candida infection of the soft tissue and leucocytoclastic vasculitis. Voriconazole treatment was followed by wound healing. Invasive Candida infection and localized Candida vasculitis represent a rare cause of persisting leg ulcers. The similar clinical picture of chronic venous leg ulcers might blur the true cause and refractory cases should therefore promptly be processed by histopathological diagnostics...
January 16, 2017: International Journal of Infectious Diseases: IJID
https://www.readbyqxmd.com/read/28103929/chemical-composition-and-some-biological-activities-of-the-essential-oils-from-basil-ocimum-different-cultivars
#13
Arpi Avetisyan, Anahit Markosian, Margarit Petrosyan, Naira Sahakyan, Anush Babayan, Samvel Aloyan, Armen Trchounian
BACKGROUND: The plants belonging to the Ocimum genus of the Lamiaceae family are considered to be a rich source of essential oils which have expressed biological activity and use in different area of human activity. There is a great variety of chemotypes within the same basil species. Essential oils from three different cultivars of basil, O. basilicum var. purpureum, O. basilicum var. thyrsiflora, and O. citriodorum Vis. were the subjects of our investigations. METHODS: The oils were obtained by steam distillation in a Clevenger-type apparatus...
January 19, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28103779/flavone-analogues-as-antimicrobial-agents
#14
Kamlesh Kumar Naik, Sivakumar Thangavel, Afroze Alam
BACKGROUND: Most of the available antimicrobial drugs have developed resistance, some of them suffer from severe toxicity, side effects. So, there is a need to discover novel compound(s) which should not only be potent, but also less toxic and cost effective. OBJECTIVES: The aim of the study is to develop new synthetic antimicrobial agents (Anti-bacterial and anti-fungal) such as 3-substituted flavone/flavanone derivatives, which should be significantly potent with low toxicity...
January 18, 2017: Recent Patents on Inflammation & Allergy Drug Discovery
https://www.readbyqxmd.com/read/28103726/antibacterial-activities-of-chemical-constituents-from-the-aerial-parts-of-hedyotis-pilulifera
#15
Hoai Thi Nguyen, Duc Viet Ho, Hung Quoc Vo, Anh Tuan Le, Hien Minh Nguyen, Takeshi Kodama, Takuya Ito, Hiroyuki Morita, Ain Raal
CONTEXT: Hedyotis pilulifera (Pit.) T.N. Ninh (Rubiaceae) has been used in Vietnamese ethnomedicine; the methanol extract exhibited antibacterial activity in our preliminary screening. OBJECTIVES: In this study, compounds from H. pilulifera were isolated and their antibacterial activity in vitro was evaluated. MATERIALS AND METHODS: The aerial parts of H. pilulifera (1.4 kg) were extracted with MeOH, suspended in water and ethyl acetate extract was chromatographed on a silica gel column...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28103015/antimicrobial-activity-ame-resistance-and-translation-inhibition-studies-of-anthraquinone-neomycin-conjugates
#16
Natalya N Degtyareva, Changjun Gong, Sandra Story, Nathanael Levinson, Adegboyega K Oyelere, Keith D Green, Sylvie Garneau-Tsodikova, Dev Priya Arya
The antibacterial effects of aminoglycosides are based on their association with the A-site of bacterial ribosomal RNA and interference with the translational process in the bacterial cell, causing cell death. The clinical use of aminoglycosides is complicated by resistance and side effects, some of which arise from their interactions with the human mitochondrial 12S rRNA and its deafness-associated mutations, C1494U and A1555G. We report a rapid assay that allows screening of aminoglycoside compounds to these classes of rRNAs...
January 19, 2017: ACS Infectious Diseases
https://www.readbyqxmd.com/read/28102765/pyrimidine-non-nucleoside-analogs-a-direct-synthesis-of-a-novel-class-of-n-substituted-amino-and-n-sulfonamide-derivatives-of-pyrimidines
#17
Galal H Elgemeie, Ali M Salah, Nermeen S Abbas, Hoda A Hussein, Reham A Mohamed
A convenient method for the regioselective synthesis of pyrimidine non-nucleoside analogs was developed. This study reports a novel and efficient method for the synthesis of a new type of N-substituted amino methylsulfanylpyrimidines and the corresponding pyrazolo[3,4-d]pyrimidines. This series of compounds was designed through the reaction of dimethyl N-cyanodithioiminocarbonate with 2-cyano-N'-(thiophen-2-yl-, furan-2-yl- and pyridin-4-ylmethylene)acetohydrazide and N'-(2-cyanoacetyl)arylsulfonohydrazides...
January 19, 2017: Nucleosides, Nucleotides & Nucleic Acids
https://www.readbyqxmd.com/read/28102305/structure-and-membrane-interactions-of-the-homodimeric-antibiotic-peptide-homotarsinin
#18
Rodrigo M Verly, Jarbas M Resende, Eduardo F C Junior, Mariana T Q de Magalhães, Carlos F C R Guimarães, Victor H O Munhoz, Marcelo Porto Bemquerer, Fábio C L Almeida, Marcelo M Santoro, Dorila Piló-Veloso, Burkhard Bechinger
Antimicrobial peptides (AMPs) from amphibian skin are valuable template structures to find new treatments against bacterial infections. This work describes for the first time the structure and membrane interactions of a homodimeric AMP. Homotarsinin, which was found in Phyllomedusa tarsius anurans, consists of two identical cystine-linked polypeptide chains each of 24 amino acid residues. The high-resolution structures of the monomeric and dimeric peptides were determined in aqueous buffers. The dimer exhibits a tightly packed coiled coil three-dimensional structure, keeping the hydrophobic residues screened from the aqueous environment...
January 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28102173/in-vitro-evaluation-of-the-antibacterial-and-osteogenic-activity-promoted-by-selenium-doped-calcium-phosphate-coatings
#19
Cosme Rodriguez-Valencia, Paula Freixeiro, Julia Serra, Carlos Ferreiros, Pio Gonzalez, Miriam Lopez-Alvarez
Selenium is an essential trace element present in 25 selenoenzymes, playing critical roles in a variety of physiological processes, such as anti-oxidative defense and the modulation of cell proliferation and differentiation. This paper characterizes selenium-doped calcium phosphate coatings and evaluates their effects on the osteogenic activity, the proliferation of osteosarcoma cells and biofilm formation. To do so, the structure and elemental composition of the obtained coatings were analyzed, in addition to their thicknesses, and they were compared to pure calcium phosphate coatings...
January 19, 2017: Biomedical Materials
https://www.readbyqxmd.com/read/28101884/lung-microdialysis-study-of-florfenicol-in-pigs-after-single-intramuscular-administration
#20
B Yang, J D Gao, X Y Cao, Q Y Wang, G Z Sun, J J Yang
For most bacterial lung infections, the concentration of unbound antimicrobial agent in lung interstitial fluid has been considered as the gold standard for estimating the antibacterial efficacy. In this study, the pharmacokinetics of florfenicol (FF) in porcine lung interstitial fluid was investigated after single intramuscular administration at two different doses (20 and 50 mg/kg). Twelve pigs underwent thoracotomy under general anesthesia. Then, the CMA/30 probe was implanted into the lung and perfused at 1 μL/min...
January 19, 2017: Journal of Veterinary Pharmacology and Therapeutics
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