keyword
MENU ▼
Read by QxMD icon Read
search

Drug compounding

keyword
https://www.readbyqxmd.com/read/29054093/the-role-of-pazopanib-on-tumour-angiogenesis-and-in-the-management-of-cancers-a-review
#1
REVIEW
Dinesh Kumar Chellappan, Jestin Chellian, Zhao Yin Ng, Yan Jinn Sim, Chiu Wei Theng, Joyce Ling, Mei Wong, Jia Hui Foo, Goh Jun Yang, Li Yu Hang, Saranyah Nathan, Yogendra Singh, Gaurav Gupta
Pazopanib is a relatively new compound to be introduced into the chemotherapy field. It is thought to have decent anti-angiogenic properties, which gives an additional hope for the treatment of certain types of cancers. A systematic review solely discussing about pazopanib and its anti-angiogenic effect is yet to be published to date, despite several relevant clinical trials being conducted over the recent years. In this review, we aim to investigate the mechanism of pazopanib's anti-angiogenic effect and its effectiveness in treating several cancers...
October 17, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29053625/traditional-uses-origins-chemistry-and-pharmacology-of-bombyx-batryticatus-a-review
#2
REVIEW
Meibian Hu, Zhijie Yu, Jiaolong Wang, Wenxiang Fan, Yujie Liu, Jianghua Li, He Xiao, Yongchuan Li, Wei Peng, Chunjie Wu
Bombyx batryticatus (B. batryticatus), a well-known traditional animal Chinese medicine, has been commonly used in China for thousands of years. The present paper reviewed advances in traditional uses, origin, chemical constituents, pharmacology and toxicity studies of B. batryticatus. The aim of the paper is to provide more comprehensive references for modern B. batryticatus study and application. In Traditional Chinese Medicine (TCM) culture, drugs containing B. batryticatus have been used to treat convulsions, headaches, skin prurigo, scrofula, tonsillitis and fever...
October 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29053620/self-nanoemulsifying-drug-delivery-systems-containing-plantago-lanceolata-an-assessment-of-their-antioxidant-and-antiinflammatory-effects
#3
Azin Kalantari, Dóra Kósa, Dániel Nemes, Zoltán Ujhelyi, Pálma Fehér, Miklós Vecsernyés, Judit Váradi, Ferenc Fenyvesi, Ákos Kuki, Sándor Gonda, Gábor Vasas, Rudolf Gesztelyi, Anayatollah Salimi, Ildikó Bácskay
The most important components of Plantago lanceolata L. leaves are catalpol, aucubin, and acteoside (=verbascoside). These bioactive compounds possess different pharmacological effects: anti-inflammatory, antioxidant, antineoplastic, and hepatoprotective. The aim of this study was to protect Plantago lanceolata extract from hydrolysis and to improve its antioxidant effect using self-nano-emulsifying drug delivery systems (SNEDDS). Eight SNEDDS compositions were prepared, and their physical properties, in vitro cytotoxicity, and in vivo AST/ALT values were investigated...
October 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29053578/treatment-with-synthetic-glucocorticoids-and-the-hypothalamus-pituitary-adrenal-axis
#4
REVIEW
Rosa Maria Paragliola, Giampaolo Papi, Alfredo Pontecorvi, Salvatore Maria Corsello
Chronic glucocorticoid (GC) treatment represents a widely-prescribed therapy for several diseases in consideration of both anti-inflammatory and immunosuppressive activity but, if used at high doses for prolonged periods, it can determine the systemic effects characteristic of Cushing's syndrome. In addition to signs and symptoms of hypercortisolism, patients on chronic GC therapy are at risk to develop tertiary adrenal insufficiency after the reduction or the withdrawal of corticosteroids or during acute stress...
October 20, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29053192/dissociation-of-nnos-from-psd-95-promotes-functional-recovery-after-cerebral-ischaemia-in-mice-through-reducing-excessive-tonic-gaba-release-from-reactive-astrocytes
#5
Yu-Hui Lin, Hai-Ying Liang, Ke Xu, Huan-Yu Ni, Jian Dong, Hui Xiao, Lei Chang, Hai-Yin Wu, Fei Li, Dong-Ya Zhu, Chun-Xia Luo
Mechanisms underlying functional recovery after stroke are little known, and effective drug intervention during the delayed stage is desirable. One potential drug target, the protein-protein interaction between neuronal nitric oxide synthase (nNOS) and postsynaptic density protein 95 (PSD-95), is critical to acute ischaemic damage and neurogenesis. We show that nNOS-PSD-95 dissociation induced by microinjection of a recombinant fusion protein Tat-nNOS-N1-133 or systemic administration of a small molecule ZL006 from days 4 to 10 after photothrombotic ischaemia in mice reduced excessive tonic inhibition in the peri-infarct cortex and ameliorated motor functional outcome...
October 20, 2017: Journal of Pathology
https://www.readbyqxmd.com/read/29053169/whole-body-physiologically-based-modelling-of-beta-blockers-in-the-rat-events-in-tissues-and-plasma-following-an-intravenous-bolus-dose
#6
S Y A Cheung, T Rodgers, L Aarons, I Gueorguieva, G L Dickinson, S Murby, C Brown, B Collins, M Rowland
BACKGROUND AND PURPOSE: Whole body physiologically based pharmacokinetic (PBPK) models have been increasingly applied in drug development to describe kinetic events of therapeutic agents in animals and human. The advantage of such modelling is the ability to incorporate vast amounts of physiological information, such as organ blood flow and volume, to ensure that the model is as close to reality as possible. EXPERIMENTAL APPROACH: Prior PBPK model development of enantiomers of a series of seven racemic betablockers, namely acebutolol, betaxolol, bisoprolol, metoprolol, oxprenolol, pindolol and propranolol, together with S-timolol in rat was based on tissue and blood concentration data at steady state...
October 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29052925/structural-insights-into-natural-compounds-as-inhibitors-of-fasciola-gigantica-thioredoxin-glutathione-reductase
#7
Rohit Shukla, Harish Shukla, Parismita Kalita, Timir Tripathi
Fascioliasis is caused by the helminth parasites of genus Fasciola. Thioredoxin glutathione reductase (TGR) is an important enzyme in parasitic helminths and plays an indispensable role in its redox biology. In the present study, we conducted a structure-based virtual screening of natural compounds against the Fasciola gigantica TGR (FgTGR). The compounds were docked against FgTGR in four sequential docking modes. The screened ligands were further assessed for Lipinski and ADMET prediction so as to evaluate drug proficiency and likeness property...
October 20, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/29052740/short-term-effects-of-the-anti-sea-lice-therapeutant-emamectin-benzoate-on-clam-worms-nereis-virens
#8
G J McBriarty, K A Kidd, L E Burridge
The polychaete Nereis virens occurs commonly in marine sediments, is widely distributed, and is a popular bait species, as well as a potential replacement for wild-caught fish in commercial fish feed preparations. It is being considered as a potential co-extractive species for culture in integrated multi-trophic aquaculture operations. However, it is not known whether pesticides or drugs used to treat sea lice on farmed salmon, such as emamectin benzoate (EB), would adversely affect cultured or wild worms, because these compounds may persist in the environment...
October 20, 2017: Archives of Environmental Contamination and Toxicology
https://www.readbyqxmd.com/read/29052423/streamlined-total-synthesis-of-trioxacarcins-and-its-application-to-the-design-synthesis-and-biological-evaluation-of-analogues-thereof-discovery-of-simpler-designed-and-potent-trioxacarcin-analogues
#9
K C Nicolaou, Pengxi Chen, Shugao Zhu, Quan Cai, Rohan D Erande, Ruofan Li, Hongbao Sun, Kiran Kumar Pulukuri, Stephan Rigol, Monette Aujay, Joseph Sandoval, Julia Gavrilyuk
A streamlined total synthesis of the naturally occurring antitumor agents trioxacarcins is described, along with its application to the construction of a series of designed analogues of these complex natural products. Biological evaluation of the synthesized compounds revealed a number of highly potent, and yet structurally simpler, compounds that are effective against certain cancer cell lines, including a drug-resistant line. A novel one-step synthesis of anthraquinones and chloro anthraquinones from simple ketone precursors and phenylselenyl chloride is also described...
October 20, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29052416/n-heterocycle-forming-amino-carboperfluoroalkylations-of-aminoalkenes-by-using-perfluoro-acid-anhydrides-mechanistic-studies-and-applications-directed-toward-perfluoroalkylated-compound-libraries
#10
Shintaro Kawamura, Kento Dosei, Elena Valverde, Kiminori Ushida, Mikiko Sodeoka
This work describes a practical and efficient method for synthesizing a diverse array of perfluoroalkylated amines, including N-heterocycles, to afford perfluoroalkylated chemical libraries as potential sources of drug candidates, agrochemicals, and probe molecules for chemical-biology research. Perfluoro acid anhydrides, which are commonly used in organic synthesis, were employed as a perfluoroalkyl source for intramolecular amino- and carbo-perfluoroalkylations of aminoalkenes, affording perfluoroalkylated N-heterocycles, including: aziridines, pyrrolidines, benzothiazinane dioxides, indolines, and hydroisoquinolinones...
October 20, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29052384/-research-progress-of-serum-pharmacochemistry-of-traditional-chinese-medicine
#11
REVIEW
Fei-Xiang Ma, Pei-Feng Xue, Yuan-Yuan Wang, Yi-Nuo Wang, Shu-Yuan Xue
Serum pharmacochemistry of traditional Chinese medicine(TCM) is an effective method to rapidly screen the effective substances and reveal the compatibility law of compound by identification and analysis of constituents migrating to blood after oral administration. In the last two decades, it has been universally accepted and widely applied in the field. With the cross-fusion with other disciplines, such as serum pharmacology, pharmacokinetics, metabolomics, network pharmacology and systems biology, serum pharmacochemistry shows comprehensive superiority in explaining drug changes in vivo and in vitro, interactions between drugs, interactions between drug and body, which coincides with the complexity of TCM compatibility, multi-components, multi-targets and multi-mechanisms...
April 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29052380/-action-mechanism-of-total-flavonoids-of-hippophae-rhamnoides-in-treatment-of-myocardial-ischemia-based-on-network-pharmacology
#12
Zhi-Cheng Wei, Dong Tong, Juan Yang, Ke-Hui Zhao, Xian-Li Meng, Yi Zhang
In this study, a network pharmacological screening method was adopted to further study the active ingredients and action mechanism of total flavonoids of Hippophae rhamnoides(TFH) for the treatment of myocardial ischemia. Firstly TCMSP database and PubChem database were searched, and then the data were combined with oral bioavailability and drug analysis to screen flavonoids of H.rhamnoides compounds. Then predictive analysis was conducted for the 7 screened compounds by ChemMapper server.The obtained potential targets were imported into MAS 3...
April 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29052376/-the-present-situation-and-countermeasures-of-uighur-medicine-compound
#13
Jiang He, Hong Wang, Lun-Li Zhang, Xiao-Jun Yang, Xuan-Chen Zhang, Wei-Jun Yang
Uighur medicine compound, which created and used by Uighur nationality, is under the guidance of the Uighur medical theory system of herbal formula and dialectical use of minority nationality conventional medicines. In recent years, Uighur medicine attracted more and more attention of people which have used and were using it. Combining the history of Uighur medicine, this article summarizes the Uighur resources, medicinal materials, drugs preparation, ancient documents, and the establishment of the clinical evaluation system and so on, and then analyzes the status quo and the existing problems in Uighur medicine compound research and industry...
April 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29051536/feasibility-and-physiological-relevance-of-designing-highly-potent-aminopeptidase-sparing-leukotriene-a4-hydrolase-inhibitors
#14
Shin Numao, Franziska Hasler, Claire Laguerre, Honnappa Srinivas, Nathalie Wack, Petra Jäger, Andres Schmid, Arnaud Osmont, Patrik Röthlisberger, Jeremy Houguenade, Christian Bergsdorf, Janet Dawson, Nathalie Carte, Andreas Hofmann, Christian Markert, Liz Hardaker, Andreas Billich, Romain M Wolf, Carlos A Penno, Birgit Bollbuck, Wolfgang Miltz, Till A Röhn
Leukotriene A4 Hydrolase (LTA4H) is a bifunctional zinc metalloenzyme that comprises both epoxide hydrolase and aminopeptidase activity, exerted by two overlapping catalytic sites. The epoxide hydrolase function of the enzyme catalyzes the biosynthesis of the pro-inflammatory lipid mediator leukotriene (LT) B4. Recent literature suggests that the aminopeptidase function of LTA4H is responsible for degradation of the tripeptide Pro-Gly-Pro (PGP) for which neutrophil chemotactic activity has been postulated. It has been speculated that the design of epoxide hydrolase selective LTA4H inhibitors that spare the aminopeptidase pocket may therefore lead to more efficacious anti-inflammatory drugs...
October 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29051318/evaluation-of-the-selectivity-and-cysteine-dependence-of-inhibitors-across-the-regulator-of-g-protein-signaling-family
#15
Michael P Hayes, Christopher R Bodle, David L Roman
Since their discovery over 20 years ago, Regulators of G Protein Signaling (RGS) proteins have received considerable attention as potential drug targets due to their ability to modulate G α activity. Efforts to identify small molecules capable of inhibiting the protein-protein interaction between activated G α subunits and RGS proteins have yielded a substantial number of inhibitors, especially towards the well-studied RGS4. These efforts also identified that many of these small molecules inhibit the protein- protein interaction through covalent modification of Cysteine residues within the RGS domain that are located distal to the G α -binding interface...
October 19, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/29051119/novel-dissolving-microneedles-for-enhanced-transdermal-delivery-of-levonorgestrel-in-vitro-and-in-vivo-characterization
#16
Gangtao Yao, Guilan Quan, Shiqi Lin, Tingting Peng, Qingqing Wang, Hao Ran, Hangping Chen, Qian Zhang, Lili Wang, Xin Pan, Chuanbin Wu
Dissolving microneedles (DMN) have been studied as a drug delivery system to enhance the transport of drug molecules across the skin with almost no pain. However, the poor dissolving ability of microneedles in the skin and low drug loading have limited their potential application. The aim of this study was to develop a novel dissolving microneedle system with improved dissolving ability for the delivery of poorly water soluble contraception drug, levonorgestrel (LNG). Chitosan and beta-sodium glycerophosphate (β-GP) were incorporated in the formulation of microneedles...
October 16, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29050968/discovery-and-electrophysiological-characterization-of-skf-32802-a-novel-herg-agonist-found-through-a-large-scale-structural-similarity-search
#17
Brian T Donovan, Deepak Bandyopadhyay, Chaya Duraiswami, Christopher J Nixon, Claire Y Townsend, Stan F Martens
Despite the importance of the hERG channel in drug discovery and the sizable number of antagonist molecules discovered, only a few hERG agonists have been discovered. Here we report a novel hERG agonist; SKF-32802 and a structural analog of the agonist NS3623, SB-335573. These were discovered through a similarity search of published hERG agonists. SKF-32802 incorporates an amide linker rather than NS3623's urea, resulting in a compound with a different mechanism of action. We find that both compounds decrease the time constant of open channel kinetics, increase the amplitude of the envelope of tails assay, mildly increased the amplitude of the IV curve, bind the hERG channel in either open or closed states, increase the plateau of the voltage dependence of activation and modulate the effects of the hERG antagonist, quinidine...
October 16, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29050919/anthelmintic-therapy-of-equine-cyathostomin-nematodes-larvicidal-efficacy-egg-reappearance-period-and-drug-resistance
#18
Jennifer L Bellaw, Kristen Krebs, Craig R Reinemeyer, Jamie K Norris, Jessica A Scare, Stefanie Pagano, Martin K Nielsen
Cyathostomins are ubiquitous in grazing horses across the world, and anthelmintic resistance has been reported with increasing levels over past decades. The aims of the present study were i) to investigate the efficacy against encysted larval stages of moxidectin (0.4 mg/kg) and fenbendazole (10 mg/kg daily for five consecutive days) and compare these regimens at 2 and 5 weeks post-treatment, ii) to investigate individual cyathostomin species associated with shortened egg reappearance periods (ERP), and iii) to document species exhibiting decreased susceptibility to the evaluated compounds...
October 16, 2017: International Journal for Parasitology
https://www.readbyqxmd.com/read/29050883/evaluation-of-antimicrobial-potential-of-successive-extracts-of-ulmus-wallichiana-planch
#19
Kundan Singh Bora, Akhilesh Kumar, Gajraj Bisht
BACKGROUND: The plant Ulmus wallichiana Planch. is found in hills of Uttarakhand, India. Bark of U. wallichiana is commonly used as traditional healer for bone fracture of animals as well as human beings and also used as wound healer remedy. OBJECTIVE: The present study was designed to evaluate antimicrobial potential of various extracts of U. wallichiana bark. MATERIALS AND METHODS: Soxhlet extraction method was used for preparation of different extracts viz...
October 16, 2017: Journal of Ayurveda and Integrative Medicine
https://www.readbyqxmd.com/read/29050757/ionophore-a23187-shows-anti-tuberculosis-activity-and-synergy-with-tebipenem
#20
Wei Huang, Julien Briffotaux, Xinwei Wang, Lili Liu, Pei Hao, Mena Cimino, Maria Virginia Buchieri, Amine Namouchi, Jose-Antonio Ainsa, Brigitte Gicquel
The objective of this study was to find molecules with anti-mycobacterial activity from a natural compounds library, investigate their mechanisms of resistance, and assess their synergy with antibiotics. We screened a library of 2582 natural compounds with Mycobacterium aurum with the aim of identifying molecules with anti-mycobacterial activity. The hits with the lowest MICs in M. aurum were also tested for their antimicrobial activity in other mycobacterial species including M. tuberculosis complex strains...
December 2017: Tuberculosis
keyword
keyword
30527
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"