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https://www.readbyqxmd.com/read/28651259/new-biguanides-as-anti-diabetic-agents-part-i-synthesis-and-evaluation-of-1-substituted-biguanide-derivatives-as-anti-diabetic-agents-of-type-ii-diabetes-insulin-resistant
#1
Samir Y Abbas, Wahid M Basyouni, Khairy A M El-Bayouk, Wael M Tohamy, Hanan F Aly, Azza Arafa, Mahmoud S Soliman
New 1-substituted-biguanide hydrochloride salts were synthesized via reacting benzo[1,3-d]dioxol-5-amine, phenylhydrazine, N,N-dimethylhydrazinecarboxamide, benzohydrazide and 2-phenyl acetohydrazide with dicyandiamide in acidic medium. Structures of the obtained biguanide salts were characterized by spectroscopic tools. The synthesized compounds were screened for their anti-diabetic activity with standard metformin drug. Oral treatment of hyperglycemic rats with the synthesized biguanide derivatives significantly decreased the elevated blood glucose level...
June 26, 2017: Drug Research
https://www.readbyqxmd.com/read/28651231/evaluation-of-in-vitro-anticancer-activity-of-1-8-cineole-containing-n-hexane-extract-of-callistemon-citrinus-curtis-skeels-plant-and-its-apoptotic-potential
#2
Sowndarya Sampath, Vidhya Veeramani, Gopal Shankar Krishnakumar, Udhayakumar Sivalingam, Suguna Lakshmi Madurai, Rose Chellan
Plants are the source of a variety of secondary metabolites, which are often used in the anticancer activity. Discovering new anticancer drug from herbal source is more important in both biological and pharmacological activities. Hence, the objective of this study is to identify the anticancer agent in Callistemon citrinus (Curtis) Skeels (CC) for the treatment of cancer. Very recently we have reported an increased antioxidant activity in the ethanolic and methanolic extracts (EE and ME) of CC but significantly reduced activity (rather increased cytotoxicity), in the n-hexane extract (HE)...
June 23, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28651154/new-comprehensive-studies-of-a-gold-iii-dithiocarbamate-complex-with-proven-anticancer-properties-aqueous-dissolution-with-cyclodextrins-pharmacokinetics-and-upstream-inhibition-of-the-ubiquitin-proteasome-pathway
#3
Marianna F Tomasello, Chiara Nardon, Valeria Lanza, Giuseppe Di Natale, Nicolò Pettenuzzo, Stefano Salmaso, Danilo Milardi, Paolo Caliceti, Giuseppe Pappalardo, Dolores Fregona
The gold(III)-dithiocarbamate complex AuL12 (dibromo [ethyl-N-(dithiocarboxy-kS,kS')-N-methylglycinate] gold(III)), is endowed with promising in vitro/in vivo antitumor activity and toxicological profile. Here, we report our recent strategies to improve its water solubility and stability under physiological conditions along with our efforts for unravelling its tangled mechanism of action. We used three types of α-cyclodextrins (CDs), namely β-CD, Me-β-CD and HP-β-CD to prepare aqueous solutions of AuL12...
June 19, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28651105/heterogeneous-epigenetic-regulation-of-hace1-in-burkitt-lymphoma-derived-cells
#4
Abdelilah Bouzelfen, Hafid Kora, Marion Alcantara, Philippe Bertrand, Jean-Baptiste Latouche, Fabrice Jardin
We examined the consequences of 3-deazaneplanocin A (DZNep) on HACE1 expression in human Burkitt- Lymphoma-derived cells to investigate fundamental molecular mechanisms that control its expression. We treated the human Burkitt- Lymphoma-derived cells lines Ramos and Raji with DZNep and examined HACE1 mRNA expression by RT-PCR. We also studied the effect of DZNep on the methylation of lysine 9 and 27 of histone 3 (H3K27me3 and H3K9me2) associated with the CpG88 and CpG177 islands of the HACE1 promoters by chromatin immunoprecipitation and quantitative PCR...
June 16, 2017: Leukemia Research
https://www.readbyqxmd.com/read/28651041/interaction-of-vivo-acac-2-with-human-serum-transferrin-and-albumin
#5
João Costa Pessoa, Isabel Correia, Ielyzaveta Chorna, Isabel Cavaco, Somnath Roy, Maxim L Kuznetsov, Nádia Ribeiro, Gonçalo Justino, Fernanda Marques, Teresa Santos Silva, Marino Santos, Hugo M Santos, José L Capelo, James Doutch
[VO(acac)2] is a remarkable vanadium compound and has potential as a therapeutic drug. It is important to clarify how it is transported in blood, but the reports addressing its binding to serum proteins have been contradictory. We use several spectroscopic and mass spectrometric techniques (ESI and MALDI-TOF), small-angle X-ray scattering and size exclusion chromatography (SEC) to characterize solutions containing [VO(acac)2] and either human serum apotransferrin (apoHTF) or albumin (HSA). DFT and modeling protein calculations are carried out to disclose the type of binding to apoHTF...
June 26, 2017: Chemistry, An Asian Journal
https://www.readbyqxmd.com/read/28650900/a-high-throughput-hplc-ms-ms-assay-for-the-detection-quantification-and-simultaneous-structural-confirmation-of-136-drugs-and-metabolites-in-human-urine
#6
Jacek Klepacki, Baharak Davari, Marion Boulet, Ryan Lizarraga, Uwe Christians
BACKGROUND: Due to its superior sensitivity and specificity, multi-analyte high-performance liquid chromatography coupled with tandem mass spectrometry (HPLC-MS/MS) has become the gold standard in clinical toxicology. Although several qualitative and quantitative LC-MS/MS assays on various mass spectrometry platforms have been described in the literature, the majority of these methods either analyze only a limited number of compounds, and/or require tedious and time-consuming sample preparation...
June 22, 2017: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/28650662/glucose-restriction-combined-with-autophagy-inhibition-and-chemotherapy-in-hct-116-spheroids-decreases-cell-clonogenicity-and-viability-regulated-by-tumor-suppressor-genes
#7
Monica M Schroll, Gabriel J LaBonia, Katelyn R Ludwig, Amanda B Hummon
Drug resistance is a prevalent phenomenon that decreases the efficacy of cancer treatments and contributes to cancer progression and metastasis. Weakening drug resistant cancer cells prior to chemotherapy is a potential strategy to combat chemoresistance. One approach to damage resistant cancer cells is modulation of nutritional intake. The combination of nutrient restriction with targeted compound treatment results in pronounced molecular changes. This study provides valuable information about augmenting existing chemotherapeutic regimes with simultaneous glucose restriction and autophagy inhibition in colorectal cancer cells...
June 26, 2017: Journal of Proteome Research
https://www.readbyqxmd.com/read/28650661/triaryl-benzimidazoles-as-a-new-class-of-antibacterial-agents-against-resistant-pathogenic-microorganisms
#8
Pietro Picconi, Charlotte Hind, Shirin Jamshidi, Kazi Nahar, Melanie Clifford, Matthew E Wand, J Mark Sutton, K Miraz Rahman
A new class of non-toxic triaryl benzimidazole compounds, derived from existing classes of DNA minor groove binders, were designed, synthesized and evaluated for their antibacterial activity against multi-drug resistant (MDR) Gram-positive and Gram-negative species. Molecular modelling experiments suggest that the newly synthesized class cannot be accommodated within the minor groove of DNA, due to a change in the shape of the molecules. Compounds 8, 13 and 14 were found to be the most active of the series, with MICs in the range of 0...
June 26, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28650618/solution-and-solid-state-correlations-of-antimalarial-drug-actions-nmr-and-crystallographic-studies-of-drug-interactions-with-a-heme-model
#9
Erin L Dodd, Dagobert Tazoo, D Scott Bohle
Solution NMR has been used in tandem with a diamagnetic non-iron heme model compound as a simple and effective tool to rapidly probe the structures of the bound complexes formed between the metalloporphyrin and antimalarial drugs from the 4-aminoquinoline, 4-methylenehydroxylquinoline, and 8-aminoquinoline subfamilies. The ability of gallium(III) protoporphyrin IX to mimic heme chemistry is exploited. The 4-aminoquinolines quinacrine and amodiaquine and two novel 3-halo chloroquine analogues are found to bind to the metalloporphyrin through hydrogen-bonding and stacking interactions, while halofantrine and the 4-methylenehydroxylquinolines, quinine and mefloquine bind through the alcohol group of the drug...
June 26, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28650504/experimental-and-theoretical-studies-on-fluvastatin-primary-photoproduct-formation
#10
Dorota Jarmużek, Tomasz Pedzinski, Marcin Hoffmann, Tomasz Siodła, Kinga Salus, Donata Pluskota-Karwatka
Fluvastatin (FLV) belongs to the group of compounds referred to as statins, also known as 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors. Statins act as cholesterol-lowering agents and are among the most frequently prescribed drugs. They upregulate low-density lipoprotein receptors in the liver by binding to the active site of HMG-CoA reductase, which is the key enzyme in cholesterol biosynthesis. Statins have been detected as contaminants in natural waters and are susceptible to degradation upon exposure to light...
June 26, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28650495/syntheses-of-potent-teixobactin-analogues-against-methicillin-resistant-staphylococcus-aureus-mrsa-through-the-replacement-of-l-allo-enduracididine-with-its-isosteres
#11
Anish Parmar, Abhishek Iyer, Daniel G Lloyd, Charlotte S Vincent, Stephen H Prior, Annemieke Madder, Edward J Taylor, Ishwar Singh
The recently discovered cyclic depsipeptide, teixobactin, is a highly potent antibiotic against multi-drug resistant pathogens such as methicillin-resistant Staphylococcus aureus (MRSA) and Mycobaterium tuberculosis. It comprises of 4 D amino acids and a rare l-allo-enduracididine amino acid. The synthesis of a properly protected l-allo-enduracididine amino acid and its incorporation into teixobactin is time consuming, synthetically challenging and low yielding and is therefore a major bottleneck in the development of potent analogues of teixobactin...
June 26, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28650379/tenofovir-induced-toxicity-in-renal-proximal-tubular-epithelial-cells-involvement-of-mitochondria
#12
Lara Milián, José E Peris, Patricia Gandía, Isabel Andújar, Luis Pallardó, Jose L Górriz, Ana Blas-García
OBJECTIVE: In vivo studies suggest that mitochondria is involved in tenofovir-induced renal toxicity, but the underlying mechanisms are still unclear. The aim of the present study was to assess the effects of tenofovir and its prodrug, tenofovir disoproxil fumarate, on mitochondrial function and cell survival/viability in a renal proximal tubular cell line. DESIGN AND METHODS: We evaluated parameters of cellular proliferation/survival (cell count, cell cycle, viability) and mitochondrial function (oxygen consumption, mitochondrial membrane potential, reactive oxygen species production) in NRK52E cells...
June 23, 2017: AIDS
https://www.readbyqxmd.com/read/28650175/bioactive-peptide-natural-products-as-lead-structures-for-medicinal-use
#13
Tam Dang, Roderich D Süssmuth
The need for new drugs for the treatment of various diseases is enormous. From the previous century until the present, numerous peptide and peptide-derived natural products have been isolated from bacteria and fungi. Hence, microorganisms play a pivotal role as sources for novel drugs with an emphasis on anti-infective agents. Various disciplines from biology, chemistry, and medicine are involved in early stages of the search for peptide natural products including taxonomy, microbiology, bioanalytics, bioinformatics, and medicinal chemistry...
June 26, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28650160/discovery-of-novel-nucleotide-prodrugs-with-improved-potency-against-hcv-variants-carrying-ns5b-s282t-mutation
#14
Le Zhen, Liang Dai, Xiaoan Wen, Lan Yao, Xiaoliang Jin, Xiaowen Yang, Wenfeng Zhao, Sheng-Qi Yu, Haoliang Yuan, Guangji Wang, Hongbin Sun
Resistant HCV variants carrying NS5B S282T mutation confer reduced sensitivity to sofosbuvir, the sole marketed NS5B polymerase inhibitor. Based on the finding that 2'-α-F-2'-β-C-methylcytidine 5'-triphosphate (8) was more potent than sofosbuvir's active metabolite on inhibition of both wild-type and S282T mutant polymerase, a dual-prodrug approach has been established. Twenty-nine phosphoramidates with N4-modified cytosine were designed, synthesized, and evaluated for anti-HCV activity. The results showed that compounds 4c-4e, 4m (EC50 0...
June 26, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28649895/the-safety-and-efficacy-of-palbociclib-in-the-treatment-of-metastatic-breast-cancer
#15
Johannes Ettl, Nadia Harbeck
Palbociclib (Ibrance(®)) is the first-in-class CDK4/6 inhibitor which has been introduced into clinical practice for the treatment of hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative metastatic breast cancer (MBC). It is an orally administered drug, which acts by selectively inhibiting cyclin-dependant kinases CDK4 and CDK6. Given together with anti-estrogens like letrozole and fulvestrant it enhances the antiproliferative effect of these drugs without compromising the favorable toxicity profile of endocrine therapy...
June 26, 2017: Expert Review of Anticancer Therapy
https://www.readbyqxmd.com/read/28649663/addictive-neurons
#16
Sodikdjon A Kodirov
Since the reward center is considered to be the area tegmentalis ventralis of the hypothalamus, logically its neurons could mainly be responsible for addiction. However, the literature asserts that almost any neurons of CNS can respond to one or another addictive compound. Obviously not only addictive nicotine, but also alcohol, amphetamine, cannabis, cocaine, heroin and morphine may influence dopaminergic cells alone in VTA. Moreover, paradoxically some of these drugs ameliorate symptoms, counterbalance syndromes, cure diseases and improve health, not only those related to the CNS and in adults, but also almost all other organs and in children, e...
2017: Therapeutic Targets for Neurological Diseases
https://www.readbyqxmd.com/read/28649446/phenotypic-profiling-of-cftr-modulators-in-patient-derived-respiratory-epithelia
#17
Saumel Ahmadi, Zoltan Bozoky, Michelle Di Paola, Sunny Xia, Canhui Li, Amy P Wong, Leigh Wellhauser, Steven V Molinski, Wan Ip, Hong Ouyang, Julie Avolio, Julie D Forman-Kay, Felix Ratjen, Jeremy A Hirota, Johanna Rommens, Janet Rossant, Tanja Gonska, Theo J Moraes, Christine E Bear
Pulmonary disease is the major cause of morbidity and mortality in patients with cystic fibrosis, a disease caused by mutations in the Cystic Fibrosis Transmembrane conductance Regulator (CFTR) gene. Heterogeneity in CFTR genotype-phenotype relationships in affected individuals plus the escalation of drug discovery targeting specific mutations highlights the need to develop robust in vitro platforms with which to stratify therapeutic options using relevant tissue. Toward this goal, we adapted a fluorescence plate reader assay of apical CFTR-mediated chloride conductance to enable profiling of a panel of modulators on primary nasal epithelial cultures derived from patients bearing different CFTR mutations...
April 14, 2017: NPJ Genomic Medicine
https://www.readbyqxmd.com/read/28649126/cis-stilbene-glucoside-in-polygonum-multiflorum-induces-immunological-idiosyncratic-hepatotoxicity-in-lps-treated-rats-by-suppressing-ppar-%C3%AE
#18
Ya-Kun Meng, Chun-Yu Li, Rui-Yu Li, Lan-Zhi He, He-Rong Cui, Ping Yin, Cong-En Zhang, Peng-Yan Li, Xiu-Xiu Sang, Ya Wang, Ming Niu, Ya-Ming Zhang, Yu-Ming Guo, Rong Sun, Jia-Bo Wang, Zhao-Fang Bai, Xiao-He Xiao
The root of Polygonum multiflorum Thunb (PM) has been used in China to treat a variety of diseases, such as constipation, early graying of the hair and hyperlipemia. Recent evidence shows that PM causes idiosyncratic drug-induced liver injury (IDILI) in humans. In this study, we investigated the molecular basis of PM-induced liver injury in a rat model of IDILI based on a non-hepatotoxic dose of LPS. SD rats were orally administered 3 potentially hepatotoxic compounds of PM: cis-stilbene glucoside (cis-SG, 50 mg/kg), trans-SG (50 mg/kg) or emodin (5 mg/kg), followed by injection of LPS (2...
June 26, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28649104/-aging-and-homeostasis-development-of-novel-adipor-targeted-drugs-with-exercise-mimicking-and-anti-aging-properties
#19
Miki Okada-Iwabu, Toshimasa Yamauchi, Masato Iwabu, Takashi Kadowaki
We have so far clarified that adiponectin, an adipocyte-secreted physiologically active substance, is decreased with the onset of obesity and that lifestyle-related diseases are primarily accounted for by the systemically decreased action of adiponectin/adiponectin receptors(AdipoRs). The activation of adiponectin/AdipoR has caloric restrictive and exercise-mimicking effects thus prolonging lifespan. We were the first in the world to succeed in identifying small-molecule compounds that serve as seed compounds for candidate AdipoR-activating drugs...
2017: Clinical Calcium
https://www.readbyqxmd.com/read/28649078/3-4-chlorophenyl-1-2-3-oxadiazol-3-ium-5-olate-and-its-4-formyl-analog-ultrasound-assisted-synthesis-and-in-vitro-anticancer-evaluation-against-human-tumor-cell-lines
#20
Sachin K Bhosale, Shreenivas R Deshpande, Rajendra D Wagh
The title compound, 3-(4-chlorophenyl)-4-formyl-[1, 2, 3] oxadiazol-3-ium-5-olate 5 was synthesized under ultrasonication by formylation of 3-(4-chlorophenyl)-[1, 2, 3] oxadiazol-3-ium-5-olate 4 and characterized by spectral studies. The ultrasonic method of synthesis was found to be simple, ecofriendly, economical, reduces reaction time and gave good yield when compared with traditional methods of synthesis. Anticancer activity of the compounds were tested against 60 human tumor cell lines and compared with standard drug vincristine sulphate...
March 2017: Pakistan Journal of Pharmaceutical Sciences
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