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https://www.readbyqxmd.com/read/29458147/sessein-and-isosessein-with-anti-inflammatory-antibacterial-and-antioxidant-activity-isolated-from-salvia-sessei-benth
#1
Abraham Gómez-Rivera, Manasés González-Cortazar, Maribel Herrera-Ruíz, Alejandro Zamilpa, Verónica Rodríguez-López
ETHNOPHARMACOLOGICAL RELEVANCE: Salvia sessei Benth, popularly known as "pipilolxochitl" or "sabanito", is a plant utilized in Mexico in traditional medicine for the treatment of erysipela. To date, only one report, to our knowledge, has been found in which a royleanone-type diterpene of the aerial parts of the species was isolated but, again to our knowledge, studies have not been conducted on the pharmacological activity of extracts and compounds isolated from this plant...
February 16, 2018: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29458133/artesunate-derived-monomeric-dimeric-and-trimeric-experimental-drugs-their-unique-mechanistic-basis-and-pronounced-antiherpesviral-activity
#2
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
#3
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/29458017/synergistic-and-additive-effects-of-atra-in-combination-with-different-anti-tumor-compounds
#4
REVIEW
Eduarda Schultze, Tiago Collares, Caroline Lucas, Fabiana K Seixas
All-trans retinoic acid (ATRA), a derivative of vitamin A, has been shown to potentiate cancer chemotherapy due to its ability to induce signals for cell differentiation or death, and inhibit cell proliferation. The combination of ATRA with taxoids, kinase inhibitors, natural compounds, retinoids, ER or HER2 inhibitors, chemotherapeutic drugs, proteasome inhibitors and nanoformulations of tretinoin have demonstrated additive or synergistic effects in anti-cancer activities. The mechanisms by which the compounds exert their synergistic effects depend on the tumor and the cell type...
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
#5
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/29457975/fluorescent-dna-probing-nanoscale-mno2-adsorption-dissolution-by-thiol-and-nanozyme-activity
#6
Liu Wang, Zhicheng Huang, Yibo Liu, Jian Wu, Juewen Liu
Manganese dioxide (MnO2) is an interesting material due to its excellent biocompatibility and magnetic properties. Adsorption of DNA to MnO2 is potentially interest for drug delivery and sensing applications. However, little fundamental understanding is known about their interactions. In this work, carboxyfluorescein (FAM)-labeled DNA oligonucleotides were used to explore the effect of salt concentration, pH, and DNA sequence and length for adsorption by MnO2, and comparisons were made with graphene oxide (GO)...
February 19, 2018: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/29457887/synthesis-of-highly-substituted-imidazole-uracil-containing-molecules-via-ugi-4cr-and-passerini-3cr
#7
Rudrakshula Madhavachary, Tryfon Zarganes-Tzitzikas, Pravin Patil, Katarzyna Kurpiewska, Justyna Kalinowska-Tłuścik, Alexander Dömling
The synthesis of uracil/thymine containing tetra/tri-substituted imidazoles were demonstrated using Ugi/Passerini-reaction fol-lowed by a post-cyclization reaction sequence. The approach enables the one-pot facile construction of diverse compounds in moderate to excellent yields (47-82%). The 5-fluorouracil and 5-methyluracil moieties afford potentially bioactive molecules with drug-like properties. These scaffolds are being utilized in the screening deck of the European Lead Factory.
February 19, 2018: ACS Combinatorial Science
https://www.readbyqxmd.com/read/29457761/degradation-of-anti-inflammatory-drugs-in-municipal-wastewater-by-heterogeneous-photocatalysis-and-electro-fenton-process
#8
Minerva Villanueva-Rodríguez, Ricardo Bello-Mendoza, Aracely Hernández-Ramírez, Edgar J Ruiz-Ruiz
Non-steroidal anti-inflammatory drugs (NSAID) are compounds frequently found in municipal wastewater and their degradation by conventional wastewater treatment plants (WWTP) is generally incomplete. This study compared the efficiency of two advanced oxidation processes, namely heterogeneous photocatalysis (HP) and electro-Fenton (EF), in the degradation of a mixture of common NSAID (diclofenac, ibuprofen and naproxen) dissolved in either deionized water or effluent from a WWTP. Both processes were effective in degrading the NSAID mixture and the trend of degradation was as follows, diclofenac>naproxen>ibuprofen...
February 19, 2018: Environmental Technology
https://www.readbyqxmd.com/read/29457608/redox-responsive-ucnps-dpa-conjugated-ngo-peg-bpei-dox-for-imaging-guided-ptt-and-chemotherapy-for-cancer-treatment
#9
Arif Gulzar, Jiating Xu, Liangge Xu, Piaoping Yang, Fei He, Dan Yang, Guanghui An, Mohd Bismillah Ansari
The disulfide bond (-S-S-) is an enormously valuable functional group in a variety of chemical and biological agents that display effective reactivity or biological activities (e.g., antitumor activities). The disulfide bonds prevalent in proteins are somewhat oxidizing in the extracellular space; however, such disulfide bonds can rarely be found inside cells because of disulfide cleavage reactions facilitated by abundant free cellular thiols, including glutathione (GSH), which is the most important common thiol-containing small molecule...
February 19, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/29457543/greener-chemicals-for-the-future-qsar-modelling-of-the-pbt-index-using-eta-descriptors
#10
P De, K Roy
Persistent, bioaccumulative and toxic (PBT) chemicals symbolize a group of substances that are not easily degraded; instead, they accumulate in different organisms and exhibit an acute or chronic toxicity. The limited empirical data on PBT chemicals, the high cost of testing together with the regulatory constraints and the international push for reduced animal testing motivate a greater reliance on predictive computational methods like quantitative structure-activity relationship (QSAR) models in PBT assessment...
April 2018: SAR and QSAR in Environmental Research
https://www.readbyqxmd.com/read/29457449/catalytically-active-single-chain-polymeric-nanoparticles-exploring-their-functions-in-complex-biological-media
#11
Yiliu Liu, Silvia Pujals, Patrick J M Stals, Thomas Pauloehrl, Stanislav I Presolski, E W Meijer, Lorenzo Albertazzi, Anja R A Palmans
Dynamic single-chain polymeric nanoparticles (SCPNs) are intriguing, bioinspired architectures that result from the collapse or folding of an individual polymer chain into a nanometer-sized particle. Here we present a detailed biophysical study on the behavior of dynamic SCPNs in living cells and an evaluation of their catalytic functionality in such a complex medium. We first developed a number of delivery strategies that allowed the selective localization of SCPNs in different cellular compartments. Live/dead tests showed that the SCPNs were not toxic to cells while spectral imaging revealed that SCPNs provide a structural shielding and reduced the influence from the outer biological media...
February 19, 2018: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29457249/gut-bacteria-of-cockroaches-are-a-potential-source-of-antibacterial-compound-s
#12
Noor Akbar, Ruqaiyyah Siddiqui, Mazhar Iqbal, K Sagathevan, Naveed Ahmed Khan
Here, we hypothesized that the microbial gut flora of animals/pests living in polluted environments, produce substances to thwart bacterial infections. The overall aim of this study was to source microbes inhabiting unusual environmental niches for potential antimicrobial activity. Two cockroach species, Gromphadorhina portentosa (Madagascar) and Blaptica dubia (Dubia) were selected. The gut bacteria from these species were isolated and grown in RPMI 1640 and conditioned media were prepared. Conditioned media were tested against a panel of Gram-positive (Methicillin resistant Staphylococcus aureus, Streptococcus pyogenes, Bacillus cereus) and Gram-negative (Escherichia coli K1, Salmonella enterica, Serratia marcescens, Pseudomonas aeruginosa, Klebsiella pneumoniae) bacteria, as well as the protist pathogen, Acanthamoeba castellanii...
February 19, 2018: Letters in Applied Microbiology
https://www.readbyqxmd.com/read/29457201/validity-of-oral-fluid-test-for-delta-9-tetrahydrocannabinol-in-drivers-using-the-2013-national-roadside-survey-data
#13
Huiyan Jin, Sharifa Z Williams, Stanford T Chihuri, Guohua Li, Qixuan Chen
BACKGROUND: Driving under the influence of marijuana is a serious traffic safety concern in the United States. Delta 9-tetrahydrocannabinol (THC) is the main active compound in marijuana. Although blood THC testing is a more accurate measure of THC-induced impairment, measuring THC in oral fluid is a less intrusive and less costly method of testing. METHODS: We examined whether the oral fluid THC test can be used as a valid alternative to the blood THC test using a sensitivity and specificity analysis and a logistic regression, and estimate the quantitative relationship between oral fluid THC concentration and blood THC concentration using a correlation analysis and a linear regression on the log-transformed THC concentrations...
February 19, 2018: Injury Epidemiology
https://www.readbyqxmd.com/read/29457197/inactivation-of-the-indole-diterpene-biosynthetic-gene-cluster-of-claviceps-paspali-by-agrobacterium-mediated-gene-replacement
#14
László Kozák, Zoltán Szilágyi, Barbara Vágó, Annamária Kakuk, László Tóth, István Molnár, István Pócsi
The hypocrealean fungus Claviceps paspali is a parasite of wild grasses. This fungus is widely utilized in the pharmaceutical industry for the manufacture of ergot alkaloids, but also produces tremorgenic and neurotoxic indole-diterpene (IDT) secondary metabolites such as paspalitrems A and B. IDTs cause significant losses in agriculture and represent health hazards that threaten food security. Conversely, IDTs may also be utilized as lead compounds for pharmaceutical drug discovery. Current protoplast-mediated transformation protocols of C...
February 19, 2018: Applied Microbiology and Biotechnology
https://www.readbyqxmd.com/read/29456818/synthesis-and-antiplasmodial-activity-of-novel-phenanthroline-derivatives-an-in-vivo-study
#15
Azar Tahghighi, Safoura Karimi, Arezoo Rafie Parhizgar, Sedigheh Zakeri
Objectives: Due to the rapid increased drug resistance to Plasmodium parasites, an urgent need to achieve new antiplasmodial drugs is felt. Therefore, in this study, the new synthetic phenanthroline derivatives were synthesized with antiplasmodial activity. Materials and Methods: A series of 1,10-phenanthroline derivatives containing amino-alcohol and amino-ether substituents were synthesized via facile procedures, starting with 5,6-epoxy-1,10-phenanthroline. Their antiplasmodial activity was then evaluated using Peter's 4-day suppressive test against Plasmodium berghei-infected mice (ANKA strain)...
February 2018: Iranian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/29456802/hts-by-nmr-for-the-identification-of-potent-and-selective-inhibitors-of-metalloenzymes
#16
Carlo Baggio, Linda Cerofolini, Marco Fragai, Claudio Luchinat, Maurizio Pellecchia
We have recently proposed a novel drug discovery approach based on biophysical screening of focused positional scanning libraries in which each element of the library contained a common binding moiety for the given target or class of targets. In this Letter, we report on the implementation of this approach to target metal containing proteins. In our implementation, we first derived a focused positional scanning combinatorial library of peptide mimetics (of approximately 100,000 compounds) in which each element of the library contained the metal-chelating moiety hydroxamic acid at the C-terminal...
February 8, 2018: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29456798/-18-f-radiolabeled-panobinostat-allows-for-positron-emission-tomography-guided-delivery-of-a-histone-deacetylase-inhibitor
#17
Harikrishna Kommidi, Umberto Tosi, Uday B Maachani, Hua Guo, Christopher S Marnell, Benedict Law, Mark M Souweidane, Richard Ting
Histone deacetylase (HDAC) inhibition is becoming an increasingly popular approach to treat cancer, as HDAC overexpression is common in many malignancies. The blood-brain barrier (BBB) prevents systemically delivered drugs from reaching brain at effective concentration, making small-molecule-HDAC inhibition in brain tumors particularly challenging. To circumvent the BBB, novel routes for administering therapeutics are being considered in the clinic, and a need exists for drugs whose deliveries can be directly imaged, so that effective delivery across the BBB can be monitored...
February 8, 2018: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29456540/kallikrein-kinin-system-suppresses-type-i-interferon-responses-a-novel-pathway-of-interferon-regulation
#18
Alecia Seliga, Michael Hweemoon Lee, Nicole C Fernandes, Viviana Zuluaga-Ramirez, Marta Didukh, Yuri Persidsky, Raghava Potula, Stefania Gallucci, Uma Sriram
The Kallikrein-Kinin System (KKS), comprised of kallikreins (klks), bradykinins (BKs) angiotensin-converting enzyme (ACE), and many other molecules, regulates a number of physiological processes, including inflammation, coagulation, angiogenesis, and control of blood pressure. In this report, we show that KKS regulates Type I IFN responses, thought to be important in lupus pathogenesis. We used CpG (TLR9 ligand), R848 (TLR7 ligand), or recombinant IFN-α to induce interferon-stimulated genes (ISGs) and proteins, and observed that this response was markedly diminished by BKs, klk1 (tissue kallikrein), or captopril (an ACE inhibitor)...
2018: Frontiers in Immunology
https://www.readbyqxmd.com/read/29456107/design-synthesis-and-discovery-of-5-1-3-diphenyl-1h-pyrazol-4-yl-methylene-pyrimidine-2-4-6-1h-3h-5h-triones-and-related-derivatives-as-novel-inhibitors-of-mpges-1
#19
Kai Ding, Ziyuan Zhou, Shuo Zhou, Yaxia Yuan, Kyungbo Kim, Ting Zhang, Xirong Zheng, Fang Zheng, Chang-Guo Zhan
Human mPGES-1 has emerged as a promising target in exploring a next generation of anti-inflammatory drugs, as selective mPGES-1 inhibitors are expected to discriminatively suppress the production of induced PGE2 without blocking the normal biosynthesis of other prostanoids including homeostatic PGE2 . Therefore, this therapeutic approach is believed to reduce the adverse effects associated with the application of traditional non-steroidal anti-inflammatory drugs (tNSAIDs) and selective COX-2 inhibitors (coxibs)...
February 8, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29455836/the-rigidins-isolation-bioactivity-and-total-synthesis-novel-pyrrolo-2-3-d-pyrimidine-analogues-using-multicomponent-reactions
#20
Aletta E van der Westhuyzen, Liliya V Frolova, Alexander Kornienko, Willem A L van Otterlo
Rigidins (2-6) are pyrrolopyrimidine alkaloids isolated from marine tunicates. Since their isolation, refinement of their total syntheses, and biochemical evaluation, interest toward this pyrrolo[2,3-d]pyrimidine scaffold as a medicinal candidate has been triggered. The derivatization of these natural products has led to the discovery of a novel range of 7-deazahypoxanthines, which exhibit extremely potent anticancer activity in human cancer cell lines. A major breakthrough toward the synthesis of rigidin and various rigidin analogues has been the application of multicomponent reactions (MCRs)...
2018: Alkaloids. Chemistry and Biology
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