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Antibiotics Pharmacology

Simon Trowitzsch, Robert Tampé
ATP-binding cassette (ABC) transporters constitute one of the largest family of integral membrane proteins, including importers, exporters, channels, receptors, and mechanotransducers, which fulfill a plethora of cellular tasks. ABC transporters are involved in nutrient uptake, hormone and xenobiotic secretion, ion and lipid homeostasis, antibiotic and multidrug resistance, as well as immunity, thus making them prime candidates for cellular regulation and pharmacological intervention. In recent years, divers structures of ABC transporters have been determined by X-ray crystallography or cryo-EM...
August 5, 2018: Journal of Molecular Biology
Andrea Novelli
Antibiotic resistance and new drugs in urologic setting: what we need to know? Urinary tract infections (UTIs) are among the most frequent infectious diseases, and represent an important public health problem with a substantial economic burden. In recent years the chemoresistance of the main uropathogens has significantly increased worldwide. Extended spectrum beta-lactamase (ESBL) production and multi-drug resistant (MDR) clones of Escherichia coli and Klebsiella pneumoniae are limiting available treatment options...
July 2018: Urologia
Ewa Grela, Milosz Wieczor, Rafal Luchowski, Joanna Zielińska, Angelika Barzycka, Wojciech Grudzinski, Katarzyna Nowak, Piotr Tarkowski, Jacek Czub, Wieslaw I Gruszecki
Amphotericin B is a lifesaving polyene antibiotic used in the treatment of systemic mycoses. Unfortunately, the pharmacological applicability of this drug is limited owing to its severe toxic side effects. At the same time, the lack of a well-defined mechanism of selectivity hampers the efforts to rationally design safer derivatives. As the drug primarily targets the biomembranes of both fungi and humans, new insights into the binding of amphotericin B to lipid membranes can be helpful in unveiling molecular mechanisms underlying both its pharmacological activity and toxicity...
August 6, 2018: Molecular Pharmaceutics
J Garrido-Mesa, F Algieri, A Rodríguez-Nogales, T Vezza, M P Utrilla, F Garcia, N Chueca, M E Rodriguez-Cabezas, N Garrido-Mesa, J Gálvez
OBJECTIVE: The use of immunomodulatory antibiotics to simultaneously target different factors involved in intestinal inflammatory conditions is an interesting but understudied pharmacological strategy. A great therapeutic potential has been obtained with minocycline and doxycycline in experimental colitis. Therefore, understanding the contribution of the different activities of immunomodulatory tetracyclines is crucial for the improvement and translation of their use into clinic. Design A comparative pharmacological study including tetracyclines and other antibiotic or immunomodulatory drugs was performed in 2,4-dinitrobenzene sulfonic acid (DNBS)-induced colitis in mice...
August 1, 2018: Biochemical Pharmacology
Zohra Nazir Kayani, Maryam Anwar, Zeb Saddiqe, Saira Riaz, Shahzad Naseem
The role of Ag dopant on ZnO thin films are studied. Ag doped ZnO thin films were deposited by sol-gel dip coating on glass substrates. The X-ray diffraction analysis shows hexagonal wurtzite with preferred orientation along the (101) plane. The crystallite size decreases from 33.40 nm to 28.37 nm with increase in silver doping percentage. Optical examination shows that the band gap decrease with an increase in the Ag doping in ZnO. The structural and optical results prove that Ag has substituted Zn in ZnO lattice...
July 25, 2018: Colloids and Surfaces. B, Biointerfaces
Amanda Karine de Sousa, Janaína Esmeraldo Rocha, Taciano Gonçalves de Souza, Thiago Sampaio de Freitas, Jaime Ribeiro-Filho, Henrique Douglas Melo Coutinho
The antimicrobial activity of psychotropic drugs, especially those of the class of mainly phenothiazines has been previously reported. Other drugs, including verapamil and trifluoperazine demonstrated to be effective against multidrug-resistant strains. Selective serotonin reuptake inhibitors (SSRIs) are antidepressant drugs that have presented significant activity against resistant bacterial resistance, but the antibacterial effect as well the antibiotic modulating properties of fluoxetine remain to be elucidated...
July 26, 2018: Microbial Pathogenesis
Józef Mierzwiński, Justyna Tyra, Karolina Haber, Maria Drela, Dariusz Paczkowski, Michael David Puricelli, Anna Sinkiewicz
INTRODUCTION: Acute mastoiditis remains the most common complication of acute otitis media. It may rarely appear also in cochlear implant patients. However, the treatment recommendations for this disease are not precisely defined or employed, and in the current literature the differences regarding both the diagnosis and management are relatively substantial. OBJECTIVE: The aim of this study was to determine a standard and safe procedure to be applied in case of pediatric acute mastoiditis...
July 17, 2018: Brazilian Journal of Otorhinolaryngology
Michele Dei Cas, Riccardo Ghidoni
Polyphenols, chemically characterized by a polyhydroxylated phenolic structure, are well known for their widespread pharmacological properties: anti-inflammatory, antibiotic, antiseptic, antitumor, antiallergic, cardioprotective and others. Their distribution in food products is also extensive especially in plant foods such as vegetables, cereals, legumes, fruits, nuts and certain beverages. The latest scientific literature outlines a resilient interconnection between cancer modulation and dietary polyphenols by sphingolipid-mediated mechanisms, usually correlated with a modification of their metabolism...
July 21, 2018: Nutrients
I Kozlovska, S Kornaga, M Kykhtyn, Y Horiuk, S Karatieieva
Chronic anal fissures (CAF) are considered to be the illness with chronic course and characterized by frequent relapses. Although today the attention of researchers concerning the role of biofilm bacterial forms in pathogenesis of this pathology remains inadequate. Тherefore we investigated biofilms density of bacteria isolated from CAF and determined the current density possessing an optimal bactericidal effect on bacteria and destruct microbial biofilms. Bacteria isolated from CAF in monoculture manifest stronger adhesive properties and exopolysaccharide biofilm matrix in them is denser, which might provide better protection for microbe cells against environmental factors and antimicrobial drugs...
June 2018: Georgian Medical News
E A Pronkin
Urinary tract infections are among the most common infectious diseases. Due to high recurrence rates and the increasing resistance of uropathogens to antibacterial drugs, phytotherapy has become an important treatment option in modern urology. Phytotherapeutic medications are characterized by a wide spectrum of pharmacological action, efficacy, and low toxicity, thus allowing for a long term use for treating and preventing many chronic diseases without the risk of adverse effects. Medicinal plants that make up Phytolysin nefroCAPS contain substances that have a wide direct or indirect antimicrobial effect...
July 2018: Urologii︠a︡
Madher N AlFindee, Yagya P Subedi, Mariana C Fiori, Srinivasan Krishnan, Abbey Kjellgren, Guillermo A Altenberg, Cheng-Wei T Chang
Connexins hemichannels (HCs) from adjacent cells form gap junctional channels that mediate cell-to-cell communication. Abnormal opening of "free" undocked HCs can produce cell damage and participate in the mechanism of disorders such as cardiac infarct, stroke, deafness, skin diseases, and cataracts. Therefore, inhibitors of connexin HCs have great pharmacological potential. Antibiotic aminoglycosides (AGs) have been recently identified as connexin HC inhibitors, but their antibiotic effect is an issue for the treatment of disorders where infections do not play a role...
July 12, 2018: ACS Medicinal Chemistry Letters
Marinko Marušić, Antonio Klemenčić, Rosana Troskot Perić, Goran Hauser
Gastroesophageal variceal hemorrhage is the most important clinical event that results from portal hypertension. It is a lifethreatening condition that demands rapid and efficient treatment. The first step in bleeding control is hemodynamic stabilization and pharmacological treatment, which includes administration of vasoactive drugs and short-term antibiotic prophylaxis. After initial hemodynamic stabilization, endoscopic therapy should be performed. The first choice of endoscopic treatment for esophageal bleeding is endoscopic variceal ligation (EVL), or endoscopic injection sclerotherapy (EIS) if EVL cannot be performed...
April 2018: Acta Gastro-enterologica Belgica
Hani Z Asfour
Increasing extent of pathogenic resistance to drugs has encouraged the seeking for new anti-virulence drugs. Many pharmacological and pharmacognostical researches are performed to identify new drugs or discover new structures for the development of novel therapeutic agents in the antibiotic treatments. Although many phytochemicals show prominent antimicrobial activity, their power lies in their anti-virulence properties. Quorum sensing (QS) is a bacterial intercellular communication mechanism, which depends on bacterial cell population density and controls the pathogenesis of many organisms by regulating gene expression, including virulence determinants...
January 2018: Journal of microscopy and ultrastructure
Fatih Mehmet Kandemir, Serkan Yildirim, Sefa Kucukler, Cuneyt Caglayan, Amdia Mahamadu, Muhammet Bahaeddin Dortbudak
Vancomycin (VCM) is a glycopeptidic broad-spectrum antibiotic against methicillin-resistant Staphylococcus aureus, though it has some adverse effects, including nephrotoxicity, that limit its usefulness. Zingerone (ZO), a component of dry ginger root, has several pharmacological activities due to its antioxidant, anti-inflammatory and antiapoptotic properties. The aim of this study was to determine the therapeutic efficacy of ZO against VCM-induced oxidative stress, inflammation, apoptosis and kidney aquaporin 1 (AQP1) levels in rats...
September 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
S Reuter, G Deuschl, D Berg, A Helmers, D Falk, K Witt
INTRODUCTION: The deep brain stimulation (DBS) withdrawal syndrome (DBS-WDS) is a rare, life-threatening complication in Parkinson's disease (PD) patients with long disease duration and stimulation when stimulation is terminated for extended periods mostly due to infection of the DBS-hardware. METHODS, RESULTS: In five patients explantation became necessary because of infection after a mean of 11.4 years (range 4-15 years) of DBS and a mean disease duration of 24...
July 2, 2018: Parkinsonism & related Disorders
Jennifer Sherwin, Elizabeth Thompson, Kevin D Hill, Kevin Watt, Andrew J Lodge, Daniel Gonzalez, Christoph P Hornik
The ventricular assist device is being increasingly used as a "bridge-to-transplant" option in children with heart failure who have failed medical management. Care for this medically complex population must be optimised, including through concomitant pharmacotherapy. Pharmacokinetic/pharmacodynamic alterations affecting pharmacotherapy are increasingly discovered in children supported with extracorporeal membrane oxygenation, another form of mechanical circulatory support. Similarities between extracorporeal membrane oxygenation and ventricular assist devices support the hypothesis that similar alterations may exist in ventricular assist device-supported patients...
September 2018: Cardiology in the Young
Bettina Engel, Sylvia Schacher, Klaus Weckbecker, Annika Stausberg, Ingo Gräff
BACKGROUND: Gout or hyperuricemia are both well known and common diseases. The prevalence of gout is increasing worldwide. Thus, patients with gout are becoming more common. Although there are several published guidelines for the management of gout, actual treatment of gout is inconsistent with these guidelines in many respects. Gout is usually treated by general practitioners (GP) in Germany. The aim of our study was to show which patients present to the emergency department and to record how treatment and clinical diagnostic testing of gout patients is performed in the emergency department of a university hospital in Germany...
July 9, 2018: Zeitschrift Für Orthopädie und Unfallchirurgie
Ananda Kumar Konreddy, Grandhe Usha Rani, Kyeong Lee, Yongseok Choi
Drug repurposing is a safe and successful pathway to speed up the novel drug discovery and development processes compared with de novo drug discovery approaches. Drug repurposing uses FDA-approved drugs and drugs that failed in clinical trials, which have detailed information of potential toxicity, formulation, and pharmacology. Technical advancements in the informatics, genomics, and biological sciences account for the major success of drug repurposing in identifying secondary indications of existing drugs...
July 5, 2018: Current Medicinal Chemistry
Ibikunle Anibijuwon, Ifeoluwa Gbala, Jumai Abioye
Background: The decline in the production of new effective antibiotics coupled with the constantly evolving antimicrobial resistance remains a public health concern. This study thus evaluated the antibacterial and antifungal effects of the ethanolic, n-hexane and hot aqueous extracts of Carpolobialutea leaves. Methods: The extracts were tested using agar well diffusion method against selected clinical isolates: Pseudomonas aeruginosa, Salmonella typhi, Escherichia coli, Staphylococcus aureus and Candida albicans...
March 2018: Ethiopian Journal of Health Sciences
Sandra Morgado, Manuel Morgado, Ana I Plácido, Fátima Roque, Ana Paula Duarte
ETHNOPHARMACOLOGICAL RELEVANCE: Arbutus unedo L., the strawberry tree (Ericaceae family) is of increasing interest because of its common traditional, industrial, chemical and pharmaceutical uses. The plant is a typical evergreen plant of the Mediterranean basin, as well as of other regions with hot summers and mild rainy winters. This review covers the studies relevant to Arbutus unedo L. utilization in the current pharmacological therapy. MATERIALS AND METHODS: The available information on traditional uses, phytochemistry and biological activities of Arbutus unedo L...
July 4, 2018: Journal of Ethnopharmacology
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