journal
MENU ▼
Read by QxMD icon Read
search

Pharmaceuticals

journal
https://www.readbyqxmd.com/read/29786643/controlled-deactivation-cb1-receptor-ligands-as-a-novel-strategy-to-lower-intraocular-pressure
#1
Sally Miller, Shashank Kulkarni, Alex Ciesielski, Spyros P Nikas, Ken Mackie, Alexandros Makriyannis, Alex Straiker
Nearly half a century has passed since the demonstration that cannabis and its chief psychoactive component Δ⁸-THC lowers intraocular pressure (IOP). Elevated IOP remains the chief hallmark and therapeutic target for glaucoma, a condition that places millions at risk of blindness. It is likely that Δ⁸-THC exerts much of its IOP-lowering effects via the activation of CB1 cannabinoid receptors. However, the initial promise of CB1 as a target for treating glaucoma has not thus far translated into a credible therapeutic strategy...
May 22, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29772843/the-role-of-trp-channels-in-the-metastatic-cascade
#2
REVIEW
Benedikt Fels, Etmar Bulk, Zoltán Pethő, Albrecht Schwab
A dysregulated cellular Ca2+ homeostasis is involved in multiple pathologies including cancer. Changes in Ca2+ signaling caused by altered fluxes through ion channels and transporters (the transportome) are involved in all steps of the metastatic cascade. Cancer cells thereby "re-program" and "misuse" the cellular transportome to regulate proliferation, apoptosis, metabolism, growth factor signaling, migration and invasion. Cancer cells use their transportome to cope with diverse environmental challenges during the metastatic cascade, like hypoxic, acidic and mechanical cues...
May 17, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29772761/high-concentrations-of-sodium-chloride-improve-microbicidal-activity-of-ibuprofen-against-common-cystic-fibrosis-pathogens
#3
Adrián J Muñoz, Roxana V Alasino, Ariel G Garro, Valeria Heredia, Néstor H García, David C Cremonezzi, Dante M Beltramo
Ibuprofen (IBU-H), a widely used anti-inflammatory, also shows a marked antimicrobial effect against several bacterial species, including those involved in cystic fibrosis such as Pseudomona aeruginosa , methicillin resistant Staphylococcus aureus and Burkholderia cepacia complex. Additionally, our results show significant synergy between water soluble Na-ibuprofen (IBU-Na) and ionic strength. Salt concentrations above 0.5 M modify the zeta potential promoting the action of Na-IBU; thus, with 1 M sodium chloride, IBU-Na is ten times more efficient than in the absence of ionic strength, and the minimum effective contact time is reduced from hours to minutes...
May 17, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29758017/the-effects-of-dabigatran-and-rivaroxaban-on-markers-of-polymorphonuclear-leukocyte-activation
#4
Guy A Richards, Annette Theron, Gregory Tintinger, Ronald Anderson
Dabigatran is an oral direct thrombin inhibitor, and rivaroxaban, a factor Xa inhibitor. Dabigatran has been implicated in the etiology of acute coronary syndromes and as these occur following inflammatory changes in the endothelium, we investigated the inflammatory potential of these agents in vitro. In order to do so, polymorphonuclear leukocytes (PMNL) were isolated from heparinized venous blood from non-smoking, healthy adults and exposed to dabigatran or rivaroxaban (0.5⁻10 µM). Generation of reactive oxygen species (ROS), elastase release, cytosolic Ca2+ fluxes, neutrophil extracellular trap (NET) formation and cell viability were measured using chemiluminescence, spectrophotometric and flow cytometric procedures respectively...
May 14, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29757952/novel-n4-like-bacteriophages-of-pectobacterium-atrosepticum
#5
Colin Buttimer, Hanne Hendrix, Alan Lucid, Horst Neve, Jean-Paul Noben, Charles Franz, Jim O'Mahony, Rob Lavigne, Aidan Coffey
Pectobacterium atrosepticum is an economically important phytopathogen that is responsible for potato blackleg and soft rot, and for which current control strategies are limited. In this study, stem samples of potato crops exhibiting blackleg were taken from three farms in Co. Cork, Ireland, and they were found to be infected with P. atrosepticum . Three closely related bacteriophages (phages) that are specific to this phytopathogen were isolated and characterized, namely vB_PatP_CB1, vB_PatP_CB3, and vB_PatP_CB4 (abbreviated as CB1, CB3, and CB4)...
May 14, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29751602/old-drugs-as-new-treatments-for-neurodegenerative-diseases
#6
REVIEW
Fernando Durães, Madalena Pinto, Emília Sousa
Neurodegenerative diseases are increasing in number, given that the general global population is becoming older. They manifest themselves through mechanisms that are not fully understood, in many cases, and impair memory, cognition and movement. Currently, no neurodegenerative disease is curable, and the treatments available only manage the symptoms or halt the progression of the disease. Therefore, there is an urgent need for new treatments for this kind of disease, since the World Health Organization has predicted that neurodegenerative diseases affecting motor function will become the second-most prevalent cause of death in the next 20 years...
May 11, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29747388/evaluation-of-anti-toxoplasma-gondii-effect-of-ursolic-acid-as-a-novel-toxoplasmosis-inhibitor
#7
Won Hyung Choi, In Ah Lee
This study was carried out to evaluate the anti-parasitic effect of ursolic acid against Toxoplasma gondii ( T. gondii ) that induces toxoplasmosis, particularly in humans. The anti-parasitic effects of ursolic acid against T. gondii -infected cells and T. gondii were evaluated through different specific assays, including immunofluorescence staining and animal testing. Ursolic acid effectively inhibited the proliferation of T. gondii when compared with sulfadiazine, and consistently induced anti- T. gondii activity/effect...
May 9, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29735913/2017-fda-peptide-harvest
#8
REVIEW
Othman Al Musaimi, Danah Al Shaer, Beatriz G de la Torre, Fernando Albericio
2017 was an excellent year in terms of new drugs (chemical entities and biologics) approved by the FDA, with a total of 46. In turn, one of the highlights was the number of peptides (six) included in this list. Here, the six peptides are analyzed in terms of chemical structure, synthetic strategy used for their production, source, therapeutic use, and mode of action.
May 7, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29734752/mitoxantrone-is-more-toxic-than-doxorubicin-in-sh-sy5y-human-cells-a-chemobrain-in-vitro-study
#9
Daniela Almeida, Rita Pinho, Verónica Correia, Jorge Soares, Maria de Lourdes Bastos, Félix Carvalho, João Paulo Capela, Vera Marisa Costa
The potential neurotoxic effects of anticancer drugs, like doxorubicin (DOX) and mitoxantrone (MTX; also used in multiple sclerosis), are presently important reasons for concern, following epidemiological data indicating that cancer survivors submitted to chemotherapy may suffer cognitive deficits. We evaluated the in vitro neurotoxicity of two commonly used chemotherapeutic drugs, DOX and MTX, and study their underlying mechanisms in the SH-SY5Y human neuronal cell model. Undifferentiated human SH-SY5Y cells were exposed to DOX or MTX (0...
May 5, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29734749/synthesis-and-structure-activity-relationships-of-cis-n-normetazocine-based-lp1-derivatives
#10
Lorella Pasquinucci, Carmela Parenti, Emanuele Amata, Zafiroula Georgoussi, Paschalina Pallaki, Valeria Camarda, Girolamo Calò, Emanuela Arena, Lucia Montenegro, Rita Turnaturi
(−)- cis - N -Normetazocine represents a rigid scaffold able to mimic the tyramine moiety of endogenous opioid peptides, and the introduction of different N -substituents influences affinity and efficacy of respective ligands at MOR (mu opioid receptor), DOR (delta opioid receptor), and KOR (kappa opioid receptor). We have previously identified LP1, a MOR/DOR multitarget opioid ligand, with an N -phenylpropanamido substituent linked to (−)- cis - N -Normetazocine scaffold. Herein, we report the synthesis, competition binding and calcium mobilization assays of new compounds 10 ⁻ 16 that differ from LP1 by the nature of the N -substituent...
May 5, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29734693/iron-release-from-soybean-seed-ferritin-induced-by-cinnamic-acid-derivatives
#11
Xuejiao Sha, Hai Chen, Jingsheng Zhang, Guanghua Zhao
Plant ferritin represents a novel class of iron supplement, which widely co-exists with phenolic acids in a plant diet. However, there are few reports on the effect of these phenolic acids on function of ferritin. In this study, we demonstrated that cinnamic acid derivatives, as widely occurring phenolic acids, can induce iron release from holo soybean seed ferritin (SSF) in a structure-dependent manner. The ability of the iron release from SSF by five cinnamic acids follows the sequence of Cinnamic acid > Chlorogenic acid > Ferulic acid > p -Coumaric acid > Trans -Cinnamic acid...
May 4, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29710851/diagnostic-accuracy-of-protein-glycation-sites-in-long-term-controlled-patients-with-type-2-diabetes-mellitus-and-their-prognostic-potential-for-early-diagnosis
#12
Sandro Spiller, Yichao Li, Matthias Blüher, Lonnie Welch, Ralf Hoffmann
Current screening tests for type 2 diabetes mellitus (T2DM) identify less than 50% of undiagnosed T2DM patients and provide no information about how the disease will develop in prediabetic patients. Here, twenty-nine protein glycation sites were quantified after tryptic digestion of plasma samples at the peptide level using tandem mass spectrometry and isotope-labelled peptides as internal standard. The glycation degrees were determined in three groups, i.e., 48 patients with a duration of T2DM exceeding ten years, 48 non-diabetic individuals matched for gender, BMI, and age, and 20 prediabetic men...
April 30, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29710837/mechanism-of-the-dual-activities-of-human-cyp17a1-and-binding-to-anti-prostate-cancer-drug-abiraterone-revealed-by-a-novel-v366m-mutation-causing-17-20-lyase-deficiency
#13
Mónica Fernández-Cancio, Núria Camats, Christa E Flück, Adam Zalewski, Bernhard Dick, Brigitte M Frey, Raquel Monné, Núria Torán, Laura Audí, Amit V Pandey
The CYP17A1 gene regulates sex steroid biosynthesis in humans through 17α-hydroxylase/17,20 lyase activities and is a target of anti-prostate cancer drug abiraterone. In a 46, XY patient with female external genitalia, together with a loss of function mutation S441P, we identified a novel missense mutation V366M at the catalytic center of CYP17A1 which preferentially impaired 17,20 lyase activity. Kinetic experiments with bacterially expressed proteins revealed that V366M mutant enzyme can bind and metabolize pregnenolone to 17OH-pregnenolone, but 17OH-pregnenolone binding and conversion to dehydroepiandrosterone (DHEA) was impaired, explaining the patient’s steroid profile...
April 29, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29690576/nuc041-a-prodrug-of-the-dna-methytransferase-inhibitor-5-aza-2-2-difluorodeoxycytidine-nuc013-leads-to-tumor-regression-in-a-model-of-non-small-cell-lung-cancer
#14
Richard Daifuku, Sheila Grimes, Murray Stackhouse
5-aza-2′,2′-difluorodeoxycytidine (NUC013) has been shown to be significantly safer and more effective than decitabine in xenograft models of human leukemia and colon cancer. However, it suffers from a similar short half-life as other DNA methyltransferase inhibitors with a 5-azacytosine base, which is problematic for nucleosides that primarily target tumor cells in S phase. Because of the relative instability of 5-azanucleosides, a prodrug approach was developed to improve the pharmacology of NUC013. NUC013 was conjugated with trimethylsilanol (TMS) at the 3′ and 5′ position of the sugar, rendering the molecule hydrophobic and producing 3′,5′-di-trimethylsilyl-2′,2′-difluoro-5-azadeoxycytidine (NUC041)...
April 23, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29690513/research-progress-on-rolling-circle-amplification-rca-based-biomedical-sensing
#15
REVIEW
Lide Gu, Wanli Yan, Le Liu, Shujun Wang, Xu Zhang, Mingsheng Lyu
Enhancing the limit of detection (LOD) is significant for crucial diseases. Cancer development could take more than 10 years, from one mutant cell to a visible tumor. Early diagnosis facilitates more effective treatment and leads to higher survival rate for cancer patients. Rolling circle amplification (RCA) is a simple and efficient isothermal enzymatic process that utilizes nuclease to generate long single stranded DNA (ssDNA) or RNA. The functional nucleic acid unit (aptamer, DNAzyme) could be replicated hundreds of times in a short period, and a lower LOD could be achieved if those units are combined with an enzymatic reaction, Surface Plasmon Resonance, electrochemical, or fluorescence detection, and other different kinds of biosensor...
April 21, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29671806/enhancing-whole-phage-therapy-and-their-derived-antimicrobial-enzymes-through-complex-formulation
#16
REVIEW
Callum J Cooper, Shazeeda Koonjan, Anders S Nilsson
The resurgence of research into phage biology and therapy is, in part, due to the increasing need for novel agents to treat multidrug-resistant infections. Despite a long clinical history in Eastern Europe and initial success within the food industry, commercialized phage products have yet to enter other sectors. This relative lack of success is, in part, due to the inherent biological limitations of whole phages. These include (but are not limited to) reaching target sites at sufficiently high concentrations to establish an infection which produces enough progeny phages to reduce the bacterial population in a clinically meaningful manner and the limited host range of some phages...
April 19, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29671794/phytochemical-study-of-the-ecuadorian-species-lepechinia-mutica-benth-epling-and-high-antifungal-activity-of-carnosol-against-pyricularia-oryzae
#17
Jorge Ramírez, Gianluca Gilardoni, Erika Ramón, Solveig Tosi, Anna Maria Picco, Carlo Bicchi, Giovanni Vidari
The plant Lepechinia mutica (Benth.) Epling (family Lamiaceae) is endemic to Ecuador. In the present study, we report some major non-volatile secondary metabolites from the leaves and the chemistry of the essential oil distilled from the flowers. The main identified compounds were carnosol, viridiflorol, ursolic acid, oleanolic acid, chrysothol, and 5-hydroxy-4′,7-dimethoxy flavone. Their structures were determined by X-ray diffraction and NMR and MS techniques. The essential oil showed a chemical composition similar to that distilled from the leaves, but with some qualitative and quantitative differences regarding several minor compounds...
April 19, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29642542/antibody-drug-conjugates-for-cancer-therapy-chemistry-to-clinical-implications
#18
REVIEW
Nirnoy Dan, Saini Setua, Vivek K Kashyap, Sheema Khan, Meena Jaggi, Murali M Yallapu, Subhash C Chauhan
Chemotherapy is one of the major therapeutic options for cancer treatment. Chemotherapy is often associated with a low therapeutic window due to its poor specificity towards tumor cells/tissues. Antibody-drug conjugate (ADC) technology may provide a potentially new therapeutic solution for cancer treatment. ADC technology uses an antibody-mediated delivery of cytotoxic drugs to the tumors in a targeted manner, while sparing normal cells. Such a targeted approach can improve the tumor-to-normal tissue selectivity and specificity in chemotherapy...
April 9, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29642497/computational-modelling-of-large-scale-phage-production-using-a-two-stage-batch-process
#19
Konrad Krysiak-Baltyn, Gregory J O Martin, Sally L Gras
Cost effective and scalable methods for phage production are required to meet an increasing demand for phage, as an alternative to antibiotics. Computational models can assist the optimization of such production processes. A model is developed here that can simulate the dynamics of phage population growth and production in a two-stage, self-cycling process. The model incorporates variable infection parameters as a function of bacterial growth rate and employs ordinary differential equations, allowing application to a setup with multiple reactors...
April 8, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29562610/comparison-study-of-two-differently-clicked-18-f-folates-lipophilicity-plays-a-key-role
#20
Kathrin Kettenbach, Laura M Reffert, Hanno Schieferstein, Stefanie Pektor, Raphael Eckert, Matthias Miederer, Frank Rösch, Tobias L Ross
Within the last decade, several folate-based radiopharmaceuticals for Single Photon Emission Computed Tomography (SPECT) and Positron Emission Tomography (PET) have been evaluated; however, there is still a lack of suitable18 F-folates for clinical PET imaging. Herein, we report the synthesis and evaluation of two novel18 F-folates employing strain-promoted and copper-catalyzed click chemistry. Furthermore, the influence of both click-methods on lipophilicity and pharmacokinetics of the18 F-folates was investigated...
March 17, 2018: Pharmaceuticals
journal
journal
40955
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"