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https://www.readbyqxmd.com/read/29458207/co-spray-drying-of-hygroscopic-kanamycin-with-the-hydrophobic-drug-rifampicin-to-improve-the-aerosolization-of-kanamycin-powder-for-treating-respiratory-infections
#1
Mohammad A M Momin, Ian G Tucker, Colin S Doyle, John A Denman, Shubhra Sinha, Shyamal C Das
High dose delivery of drugs to the lung using a dry powder inhaler (DPI) is an emerging approach to combat drug-resistant local infections. To achieve this, highly aerosolizable powders are required. We hypothesized that co-spray-drying kanamycin, a hydrophilic hygroscopic antibiotic, with rifampicin, a hydrophobic antibiotic, would produce inhalable particles with surfaces enriched in rifampicin. Such particles would have higher aerosolization than kanamycin alone, and minimise the mass of powder for inhalation avoiding use of non-active excipients...
February 16, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29458205/developing-a-stable-aqueous-enteric-coating-formulation-with-hydroxypropyl-methylcellulose-acetate-succinate-hpmcas-mf-and-colloidal-silicon-dioxide-as-anti-tacking-agent
#2
Tanvi M Deshpande, Anisul Quadir, Sakae Obara, Ahmed Ibrahim, Stephen W Hoag
The purpose of this study was to use statistical design of experiments to develop a stable aqueous enteric coating formulation containing stabilizing excipients, such as polyethylene glycol that can minimize hydroxypropyl methylcellulose acetate succinate aggregation and minimize spray-nozzle clogging at elevated processing temperatures. The mechanisms of stabilization (i.e. charge stabilization and molecular interactions) were studied by performing zeta potential and FTIR studies. Electrostatic stabilization by sodium lauryl sulfate and hydrogen bonding by polyethylene glycol provided dispersion stability and yielded a stable aqueous coating formulation that prevented spray-nozzle clogging...
February 16, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29458160/gambogic-acid-sensitizes-breast-cancer-cells-to-trail-induced-apoptosis-by-promoting-the-crosstalk-of-extrinsic-and-intrinsic-apoptotic-signalings
#3
Shengpeng Wang, Yingqi Xu, Chenyang Li, Hongxun Tao, Anqi Wang, Chenyu Sun, Zhangfeng Zhong, Xu Wu, Peng Li, Yitao Wang
Due to the ability of tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) to induce cancer cell apoptosis selectively, TRAIL has attracted significant interest in the treatment of cancer. However, although TRAIL triggers apoptosis in a broad range of cancer cells, most primary cancers are often intrinsically TRAIL-resistant, or acquire resistance after TRAIL treatment, evocating new strategies to overcome TRAIL resistance. Gambogic acid (GA), an active constituent of Garcinia Hanburyi (Teng Huang in Chinese), has been applied for thousands of years for medicinal uses, however, the potential effect of GA in combating cancer resistance remains poorly investigated...
February 16, 2018: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/29458157/clostridium-innocuum-is-a-vancomycin-resistant-pathogen-that-may-cause-antibiotic-associated-diarrhea
#4
Ju-Hsin Chia, Ting-Shu Wu, Tsu-Lan Wu, Chyi-Liang Chen, Chih-Hsien Chuang, Lin-Hui Su, Hong-Jyun Chang, Chia-Chen Lu, An-Jing Kuo, Hsin-Chih Lai, Cheng-Hsun Chiu
OBJECTIVES: Clostridium innocuum can cause extra-intestinal infection in patients with underlying diseases. The role of C. innocuum in antibiotic-associated diarrhea (AAD) remains unknown. METHODS: Clinical information of 103 patients in which C. innocuum was isolated from was reviewed. We carried out cellular and animal experiments to examine the pathogenic potential of C. innocuum in AAD. RESULTS: Eighty-eight percent (91/103) of the 103 patients received antibiotics within 2 weeks of diarrhea onset...
February 16, 2018: Clinical Microbiology and Infection
https://www.readbyqxmd.com/read/29458150/pink1-protects-auditory-hair-cells-and-spiral-ganglion-neurons-from-cisplatin-induced-ototoxicity-via-inducing-autophagy-and-inhibiting-jnk-signaling-pathway
#5
Qianqian Yang, Gaoying Sun, Haiyan Yin, Hongrui Li, Zhixin Cao, Jinghan Wang, Meijuan Zhou, Haibo Wang, Jianfeng Li
Phosphatase and tensin homologue (PTEN)-induced putative kinase 1 (PINK1) gene encodes a serine/threonine kinase, which acts as a molecular sensor of mitochondrial health necessary for mitochondrial quality control. The present study was designed to examine whether PINK1 expressed in C57BL/6 murine cochlea and HEI-OC1 cells and, if so, to investigate the possible mechanisms underlying the action of PINK1 in cisplatin-induced death of sensory hair cells (HCs) and spiral ganglion neurons (SGNs) in vitro. The expression pattern of PINK1, formation of parkin particles, and autophagy were determined by immunofluorescent staining...
February 16, 2018: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/29458133/artesunate-derived-monomeric-dimeric-and-trimeric-experimental-drugs-their-unique-mechanistic-basis-and-pronounced-antiherpesviral-activity
#6
Friedrich Hahn, Tony Fröhlich, Theresa Frank, Luca D Bertzbach, Stephan Kohrt, Benedikt B Kaufer, Thomas Stamminger, Svetlana B Tsogoeva, Manfred Marschall
Human cytomegalovirus (HCMV) is a major human pathogen and is associated with severe pathology, such as life-threatening courses of infection in immunocompromised individuals and neonates. Currently, antiviral therapy is still hampered by a considerable toxicity of the available drugs and induction of viral resistance. Recently, we and others reported the very potent antiviral activity of the broad antiinfective drug artesunate in vitro and in vivo. Here, we investigated further optimized analogs including monomeric, dimeric and trimeric derivatives belonging to this highly interesting chemical group of experimental drugs (sesquiterpenes/trioxanes) and compared these to the previously identified trimeric artesunate compound TF27...
February 16, 2018: Antiviral Research
https://www.readbyqxmd.com/read/29458130/impact-of-rna-polymerase-i-inhibitor-cx-5461-on-viral-kinase-dependent-and-independent-cytomegalovirus-replication
#7
Kristen N Westdorp, Scott S Terhune
Human cytomegalovirus (HCMV) infections cause congenital birth defects and disease in immunosuppressed individuals. Antiviral compounds can control infection yet their use is restricted due to concerns of toxicity and the emergence of drug resistant strains. We have evaluated the impact of an RNA Polymerase I (Pol I) inhibitor, CX-5461 on HCMV replication. CX-5461 inhibits Pol I-mediated ribosomal DNA transcription by binding G-quadruplex DNA structures and also activates cellular stress response pathways. The addition of CX-5461 at both early and late stages of the HCMV infection inhibited viral DNA synthesis and virus production...
February 16, 2018: Antiviral Research
https://www.readbyqxmd.com/read/29458121/the-paradox-of-marrow-adipose-tissue-in-anorexia-nervosa
#8
Pouneh K Fazeli, Anne Klibanski
Anorexia nervosa (AN) is a psychiatric disorder characterized by inappropriate nutrient intake resulting in low body weight. Multiple hormonal adaptations facilitate decreased energy expenditure in this state of caloric deprivation including non-thyroidal illness syndrome, growth hormone resistance, and hypogonadotropic hypogonadism. Although these hormonal adaptations confer a survival advantage during periods of negative energy balance, they contribute to the long-term medical complications associated with AN, the most common of which is significant bone loss and an increased risk of fracture...
February 16, 2018: Bone
https://www.readbyqxmd.com/read/29458115/effect-of-acek-acesulfame-potassium-on-brain-function-under-dietary-restriction-in-mice
#9
Daisuke Ibi, Fumika Suzuki, Masayuki Hiramatsu
People preferably take zero or low-calorie beverages and foods with artificial sweeteners even though it has been recently suggested that long-term artificial sweetener use affects physiological functions. In addition, a lower body weight was considered to be more healthful, but an abnormally low body weight caused by an excessive diet has been reported to cause health problems. Acesulfame potassium (AceK) is one of the most commonly used for foods and beverages because of its resistance to thermal degradation and marked sweetness...
February 16, 2018: Physiology & Behavior
https://www.readbyqxmd.com/read/29458093/protective-efficacy-of-mucuna-pruriens-l-seed-meal-enriched-diet-on-growth-performance-innate-immunity-and-disease-resistance-in-oreochromis-mossambicus-against-aeromonas-hydrophila
#10
Mohamed Saiyad Musthafa, Syed Mohideen Asgari, Amitha Kurian, Elumalai Preetham, Abdul Rahman Jawahar Ali, Bilal Ahmad Paray, Mohammad K Al-Sadoon
The impact of Mucuna pruriens (L.) seed meal diet on growth performance, innate immune response, and disease resistance in Oreochromis mossambicus against Aeromonas hydrophila is reported for the first time. Infected O. mossambicus was fed with 2 g kg-1 , 4 g kg-1 , and 6 g kg-1 of M. pruriens seed meal diets significantly increased initial body weight (IBW) and final body weight (FBW) over control, for a period of 4 weeks. At 4 g kg-1 and 6 g kg-1 the enriched diet significantly (P < 0.05) enhanced the survival rate, weight gain (WG), protein efficiency ratio (PER), specific growth rate (SGR), feed conversion ratio (FCR), and feed efficiency (FE) when compared to the control; besides, from weeks 2-4 these diets significantly (P < 0...
February 16, 2018: Fish & Shellfish Immunology
https://www.readbyqxmd.com/read/29458088/antibiotics-use-among-palestine-refugees-attending-unrwa-primary-health-care-centers-in-jordan-a-cross-sectional-study
#11
Maysun Al Baz, Michael R Law, Rawan Saadeh
The irrational use of antibiotics is increasing in Jordanian refugee camps and consequently so too is bacterial resistance. About one-third of health expenditures at UNRWA health centers in Jordan are attributed to antibiotics. OBJECTIVE: We studied knowledge, attitude and behaviour of Palestine refugees attending UNRWA health centers in Jordan regarding antibiotic use in order to plan public health interventions accordingly. METHODS: A cross-sectional, interviewer-administered survey among 250 adult Palestine refugees at four different health centres was conducted...
February 16, 2018: Travel Medicine and Infectious Disease
https://www.readbyqxmd.com/read/29458065/nosocomial-ventriculitis-caused-by-a-meticillin-and-linezolid-resistant-clone-of-staphylococcus-epidermidis-in-neurosurgical-patients
#12
Carlos Rodríguez-Lucas, Javier Fernández, José Antonio Boga, Lucia López-Amor, Lorena Forcelledo, Eva Lázaro-López, M Rosario Rodicio
BACKGROUND: Post-neurosurgical ventriculitis is mainly caused by coagulase-negative staphylococci. The rate of linezolid resistant S. epidermidis (LRSE) is increasing worldwide. AIMS: To report clinical and microbiological data from a series of ventriculitis cases caused by LRSE in a Spanish hospital between 2013 and 2016. METHODS: LRSE ventriculitis cases were retrospectively reviewed in a Spanish hospital during a four-year period. Clinical/epidemiological data of the infected patients were reviewed, the isolates involved were typed by PFGE and MLST, and the molecular basis of linezolid resistance was determined...
February 16, 2018: Journal of Hospital Infection
https://www.readbyqxmd.com/read/29458045/aldose-reductase-inhibitor-fidarestat-prevents-doxorubicin-induced-endothelial-cell-death-and-dysfunction
#13
Himangshu Sonowal, Pabitra Pal, Kirtikar Shukla, Ashish Saxena, Satish K Srivastava, Kota V Ramana
Despite doxorubicin (Dox) being one of the most widely used chemotherapy agents for breast, blood and lung cancers, its use in colon cancer is limited due to increased drug resistance and severe cardiotoxic side effects that increase mortality associated with its use at high doses. Therefore, better adjuvant therapies are warranted to improve the chemotherapeutic efficacy and to decrease cardiotoxicity. We have recently shown that aldose reductase inhibitor, fidarestat, increases the Dox-induced colon cancer cell death and reduces cardiomyopathy...
February 16, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29458019/raffinose-from-costus-speciosus-attenuates-lipid-synthesis-through-modulation-of-ppars-srebp1c-and-improves-insulin-sensitivity-through-pi3k-akt
#14
Muthukumaran Padmanaban, Thiyagarajan Gopal, Arun Babu Rajendran, Baddireddi Subhadra Lakshmi
Among several metabolic disorders, the pathogenesis of insulin resistance is considered to be multifactorial. Raffinose, an oligosaccharide isolated from the rhizome of Costus speciosus showed ≤50% inhibition of lipid accumulation in differentiated HepG2 and 3T3-L1 cells through exhibiting partial agonism to PPARγ, and, an enhanced secretion of adiponectin in 3T3-L1 adipocytes. Raffinose was also observed to attenuate the expression of SREBP1c, ACC and FAS which are involved in the fatty acid synthesis. A corresponding upregulation of PPARα and ACO involved in fatty acid oxidation was observed in steatotic HepG2 hepatocytes and 3T3-L1 adipocytes...
February 16, 2018: Chemico-biological Interactions
https://www.readbyqxmd.com/read/29458018/5-chloro-n4-2-isopropylsulfonyl-phenyl-n2-2-methoxy-4-4-4-methylpiperazin-1-yl-methyl-1h-1-2-3-triazol-1-yl-phenyl-pyrimidine-2-4-diamine-wy-135-a-novel-alk-inhibitor-induces-cell-cycle-arrest-and-apoptosis-through-inhibiting-alk-and-its-downstream-pathways
#15
Mengting Han, Jiwei Shen, Lijing Wang, Yu Wang, Xin Zhai, Yao Li, Meiqiao Liu, Zengqiang Li, Daiying Zuo, Yingliang Wu
Anaplastic lymphoma kinase (ALK)-positive cancers have rising morbidity and mortality in recent years, and novel chemotherapeutic drugs with no drug resistance and high activity for treating ALK-positive cancers are needed urgently. In this study, we investigated the anti-cancer effect of 5-chloro-N4-(2-(isopropylsulfonyl)phenyl)-N2-(2-methoxy-4-(4-((4-methylpiperazin-1-yl)methyl)-1H-1,2,3-triazol-1-yl)phenyl)pyrimidine-2,4-diamine (WY-135), a novel ALK inhibitor, on nucleophosmin-anaplastic lymphoma kinase (NPM-ALK) positive cancer cell line Karpas299 and echinoderm microtubule associated protein like 4-anaplastic lymphoma kinase (EML4-ALK) positive cancer cell line H2228...
February 16, 2018: Chemico-biological Interactions
https://www.readbyqxmd.com/read/29458015/sulfenamide-and-sulfonamide-derivatives-of-metformin-can-exert-anti-coagulant-and-pro-fibrinolytic-properties
#16
Magdalena Markowicz-Piasecka, Kristiina M Huttunen, Łukasz Mateusiak, Elżbieta Mikiciuk-Olasik, Joanna Sikora
Type 2 diabetes mellitus (T2DM) is characterised not only by hyperglycaemia and insulin resistance but also an impaired balance between the processes of coagulation and fibrinolysis. The aim of this study was to examine the effects of metformin, a widely-used oral anti-diabetic drug, phenformin and eight sulfenamide and sulfonamide derivatives of metformin on several haemostasis parameters. Thrombin Time (TT) tests were performed according to the available commercial method. The activity of factor X was conducted based on deficient plasma factor X...
February 16, 2018: Chemico-biological Interactions
https://www.readbyqxmd.com/read/29458007/a-genomically-characterized-collection-of-high-grade-serous-ovarian-cancer-xenografts-for-preclinical-testing
#17
Paulina Cybulska, Jocelyn M Stewart, Azin Sayad, Carl Virtanen, Patricia A Shaw, Blaise Clarke, Natalie Stickle, Marcus Q Bernardini, Benjamin G Neel
High-grade serous ovarian cancer (HGSC) is the leading cause of morbidity and mortality from gynecologic malignancy. Overall survival remains low, due to the nearly ubiquitous emergence of platinum-resistance and the paucity of effective next-line treatments. Current cell culture-based models show limited similarity to HGSC and are therefore unreliable predictive models for pre-clinical evaluation of investigational drugs. This deficiency could help explain the low overall rate of successful drug development and the decades of largely unchanged approaches to HGSC treatment...
February 16, 2018: American Journal of Pathology
https://www.readbyqxmd.com/read/29457996/the-tyg-index-cutoff-point-and-its-association-with-body-adiposity-and-lifestyle-in-children
#18
Sarah A Vieira Ribeiro, Poliana C A Fonseca, Cristiana S Andreoli, Andréia Q Ribeiro, Helen H M Hermsdorff, Patrícia F Pereira, Silvia E Priore, Sylvia C C Franceschini
OBJECTIVE: To investigate the factors associated with insulin resistance in children aged 4-7 years, and to identify the cutoff point of the triglyceride-glucose index for the prediction of IR in this population. METHODS: A cross-sectional study was conducted with 403 children from a retrospective cohort. Insulin resistance was also evaluated in a sub-sample using the HOMA index. Four indicators of body adiposity were assessed: body mass index, waist-to-height ratio, and the percentages of total and central body fat...
February 16, 2018: Jornal de Pediatria
https://www.readbyqxmd.com/read/29457960/phylogenetic-relationships-and-acaricidal-effects-of-beauveria-bassiana-obtained-from-cattle-farm-soils-against-rhipicephalus-microplus
#19
Agustin Fernández-Salas, Miguel Angel Alonso Díaz, Rogelio Alejandro Alonso Morales, Roberto Lezama-Gutierrez, José Antonio Cervantes-Chávez
The objectives of the present study were to isolate Beauveria bassiana strains from cattle farms soils, to analyze the phylogenetic relationships among the isolated fungi strains, and to determine the acaricidal effect of B. bassiana isolates on Rhipicephalus microplus engorged ticks, resistant or susceptible to chemical acaricides. Six strains of Beauveria bassiana were obtained and isolated from cattle farms soils by Galleria bait method in Mexican tropics and the acaricidal effect was assessed against 2 populations of R...
February 19, 2018: Journal of Parasitology
https://www.readbyqxmd.com/read/29457957/synergistic-effect-of-entomopathogenic-fungus-fusarium-oxysporum-extract-in-combination-with-temephos-against-three-major-mosquito-vectors
#20
Perumal Vivekanandhan, Sengodan Karthi, Muthugounder S Shivakumar, Giovanni Benelli
Mosquito control using chemical insecticides is facing a major challenge due to development of insecticide resistance. Improving the efficiency of existing insecticides using synergistic secondary metabolites of biological origin is increasingly being researched. Herein, we evaluated the toxicity of Fusarium oxysporum extract alone and in binary combinations with temephos, on larvae and pupae of Anopheles stephensi, Aedes aegypti and Culex quinquefaciatus. F. oxysporum extract was characterized using TLC, FT-IR and GC-MS...
February 19, 2018: Pathogens and Global Health
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