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Drug compounding

Alekxander Popov, Zinaida K Blinnikova, Maria P Tsyurupa, Vadim A Davankov
New restricted access materials based on microporous hypercrosslinked polystyrene have been developed. The materials are aimed at the use as packings for solid-phase extraction cartridges to isolate low-molecular-weight analytes from biological fluids (for instance, blood plasma or serum). Two features distinguish these polymers from all known restricted access materials. The first one consists in that the microporous hypercrosslinked polystyrene not only exclude proteins from the sorbent phase but also do not adsorb them on the bead outer surface and so they do not cause coagulation of blood protein components...
June 21, 2018: Journal of Separation Science
Jiayin Diao, Can Xu, Huiting Zheng, Siyi He, Shumei Wang
Viticis Fructus is a traditional Chinese herbal drug processed by various methods to achieve different clinical purposes. Thermal treatment potentially alters chemical composition, which may impact on effectiveness and toxicity. In order to interpret the constituent discrepancies of raw versus processed (stir-fried) Viticis Fructus, a multivariate detection method (NIR, HPLC, and UPLC-MS) based on metabonomics and chemometrics was developed. Firstly, synergy interval partial least squares and partial least squares-discriminant analysis were employed to screen the distinctive wavebands (4319 - 5459 cm-1 ) based on preprocessed near-infrared spectra...
June 21, 2018: Planta Medica
Juliana Bazzan Arsand, Rodrigo Barcellos Hoff, Louise Jank, Lucas N Meirelles, M Silvia Díaz-Cruz, Tânia Mara Pizzolato, Damià Barceló
Antibiotics are widely used in human medicine and veterinary production. Residues of these compounds reach the water sources through waste or direct application (e.g. aquaculture). The constant input of the parent drugs and their transformation products into the environment leads these pharmaceuticals to be considered as emerging pollutants. For some molecules, the pathway of degradation and formation in products is less known. To assess the impact of these substances in the environment and in the human health, it is necessary to elucidate the transformation products and their kinetic of degradation to evaluate the possible risks...
June 18, 2018: Science of the Total Environment
Upendra K Sharma, Dinesh Mohanakrishnan, Nandini Sharma, Danish Equbal, Dinkar Sahal, Arun K Sinha
The inherent affinity of natural compounds for biological receptors has been comprehensively exploited with great success for the development of many drugs, including antimalarials. Here the natural flavoring compound vanillin has been used as an economical precursor for the synthesis of a series of novel bischalcones whose in vitro antiplasmodial activities have been evaluated against erythrocytic stages of Plasmodium falciparum. Bischalcones 9, 11 and 13 showed promising antiplasmodial activity {Chloroquine (CQ) sensitive Pf3D7 IC50 (μM): 2...
June 15, 2018: European Journal of Medicinal Chemistry
Gina N Tageldin, Salwa M Fahmy, Hayam M Ashour, Mounir A Khalil, Rasha A Nassra, Ibrahim M Labouta
Two new series of pyrazolo[3,4-d]pyrimidine bearing thiazolidinone moiety were designed and synthesized. The newly synthesized compounds were evaluated for their in vitro (COX-1 and COX-2) inhibitory assay. Compounds that showed promising COX-2 selectivity were further subjected to in vivo anti-inflammatory screening applying formalin induced paw edema (acute model) and cotton-pellet induced granuloma (chronic model) assays using celecoxib and diclofenac sodium as reference drugs. The histopathological and ulcerogenic potential were also determined...
June 5, 2018: Bioorganic Chemistry
Dennis A Smith, Robert A B van Waterschoot, Neil J Parrott, Andrés Olivares-Morales, Thierry Lavé, Malcolm Rowland
Target concentration is typically not considered in drug discovery. However, if targets are expressed at relatively high concentrations and compounds have high affinity, such that most of the drug is bound to its target, in vitro screens can give unreliable information on compound affinity. In vivo, a similar situation will generate pharmacokinetic (PK) profiles that deviate greatly from those normally expected, owing to target binding affecting drug distribution and clearance. Such target-mediated drug disposition (TMDD) effects on small molecules have received little attention and might only become apparent during clinical trials, with the potential for data misinterpretation...
June 18, 2018: Drug Discovery Today
S Jiang, J Zeng, X Zhou, Y Li
Growing evidence suggests the existence of new antibiotic resistance mechanisms. Recent studies have revealed that quorum-quenching enzymes, such as MacQ, are involved in both antibiotic resistance and cell-cell communication. Furthermore, some small bacterial regulatory RNAs, classified into RNA attenuators and small RNAs, modulate the expression of resistance genes. For example, small RNA sprX, can shape bacterial resistance to glycopeptide antibiotics via specific downregulation of protein SpoVG. Moreover, some bacterial lipocalins capture antibiotics in the extracellular space, contributing to severe multidrug resistance...
June 1, 2018: Journal of Dental Research
Katharina Hammerbacher, Katharina Görtemaker, Christine Knies, Eugenia Bender, Gabriel A Bonaterra, Helmut Rosemeyer, Ralf Kinscherf
Two series of nucleolipids, (i) O-2',3'-heptanylidene- as well as O-2',3'-undecanylidene ketals of 6 ß-D-ribonucleosides (type A) and partly N-farnesyl derivatives thereof (type B) were prepared in a combinatorial manner. All novel compounds were characterized by elemental analysis and/or ESI mass spectrometry and by UV-, 1 H-, and 13 C-NMR spectroscopy. Conformational parameters of the nucleosides and nucleolipids were calculated from various 3 J(H,H), 3 J(1 H,13 C) and 5 J(F,H) coupling constants. For a drug profiling the parent nucleosides and their lipophilic derivatives were studied with respect to their distribution (log P) between water and n-octanol as well as water and cyclohexane...
June 21, 2018: Chemistry & Biodiversity
Harald Schwalbe, Alix Tröster, Stephanie Heinzlmeir, Benedict-Tilman Berger, Santosh L Gande, Krishna Saxena, Sridhar Sreeramulu, Verena Linhard, Amir H Nasiri, Michael Bolte, Susanne Müller, Bernhard Kuster, Guillaume Médard, Denis Kudlinzki
EPH receptors are transmembrane receptor tyrosine kinases. Their extracellular domains bind specifically to ephrin A/B ligands, and this binding modulates the intracellular kinase activity. EPHs are key players in bidirectional intercellular signaling, controlling cell morphology, adhesion and migration. They are increasingly recognized as cancer drug targets. We analyzed the binding of the Novartis inhibitor NVP-BHG712 (NVP) to EPHA2 and EPHB4. Unexpectedly, all tested commercially available NVP samples turned out to be a regioisomer (NVPiso) of the inhibitor, initially described in a Novartis patent application...
June 21, 2018: ChemMedChem
Mohammad Rafienia, Ashkan Bigham, Seyed Ali Hassanzadeh-Tabrizi
At present, solvothermal fabrication method has widely been applied in the synthesis of spinel ferrite nanoparticles (SFNs), which is mainly because of its great advantages such as precise control over size, shape distribution, and high crystallinity that do not require postannealing treatment. Among various SFNs, Fe3 O4 nanoparticles have attracted tremendous attention because of their favorable physical and structural properties which are advantageous, especially in biomedical applications, among which the vast application of these materials as targeted drug delivery systems, hyperthermia, and imaging agents in cancer therapy can be mentioned...
April 2018: Journal of Medical Signals and Sensors
Parisa Zargar, Esmaeel Ghani, Farideh Jalali Mashayekhi, Amin Ramezani, Ebrahim Eftekhar
5-Fluorouracil (5-FU)-based chemotherapy improves the overall survival rates of patients with colorectal cancer (CRC). However, only a small proportion of patients respond to 5-FU when used as a single agent. The aim of the present study was to investigate whether the anticancer property of 5-FU is potentiated by combination treatment with acriflavine (ACF) in CRC cells. Additionally, the potential underlying molecular mechanisms of the cytotoxic effect of ACF were determined. The cytotoxic effects of ACF, 5-FU and irinotecan on different CRC cell lines with different p53 status were investigated using an MTT assay...
June 2018: Oncology Letters
Kristiina Nygren, Mukesh Dubey, Antonio Zapparata, Mudassir Iqbal, Georgios D Tzelepis, Mikael Brandström Durling, Dan Funck Jensen, Magnus Karlsson
Clonostachys rosea is a necrotrophic mycoparasitic fungus, used for biological control of plant pathogenic fungi. A better understanding of the underlying mechanisms resulting in successful biocontrol is important for knowledge-based improvements of the application and use of biocontrol in agricultural production systems. Transcriptomic analyses revealed that C. rosea responded with both common and specific gene expression during interactions with the fungal prey species Botrytis cinerea and Fusarium graminearum ...
July 2018: Evolutionary Applications
Evan Kesinger, Jianing Liu, Aaron Jensen, Catherine P Chia, Andrew Demers, Hideaki Moriyama
BACKGROUND: A new type of influenza virus, known as type D, has recently been identified in cattle and pigs. Influenza D virus infection in cattle is typically asymptomatic; however, its infection in swine can result in clinical disease. Swine can also be infected with all other types of influenza viruses, namely A, B, and C. Consequently, swine can serve as a "mixing vessel" for highly pathogenic influenza viruses, including those with zoonotic potential. Currently, the only antiviral drug available targets influenza M2 protein ion channel is not completely effective...
2018: PloS One
Ying Wang, Qiuyun Liu, Haojie Chen, Jun You, Bin Peng, Fanfan Cao, Xue Zhang, Qing Chen, Georges Uzan, Limin Xu, Denghai Zhang
The development of resistance to therapy continues to be a serious clinical problem in lung cancer management. Epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) is one of the most common chemotherapy drugs to treat non-small-cell lung cancer. However, almost all treatments fail after ∼1 year of treatment because of drug tolerance, probably occurring from the threonine 790 mutation (T790M) of the EGFR, resulting in overactivation of the EGFR. Celastrol is a natural compound that exhibits antiproliferative activity...
June 20, 2018: Anti-cancer Drugs
Matthew L Danielson, Geri A Sawada, Thomas J Raub, Prashant V Desai
The organic anion-transporting polypeptide 1B1 transporter belongs to the solute carrier superfamily and is highly expressed at the basolateral membrane of hepatocytes. Several clinical studies showed drug-drug interactions involving OATP1B1 thereby prompting the International Transporter Consortium to label OATP1B1 as a critical transporter that can influence a compound's disposition. To examine OATP1B1 inhibition early in the drug discovery process, we established a medium-throughput concentration-dependent OATP1B1 assay...
June 21, 2018: Molecular Pharmaceutics
Maria Julia Mora, R Onnainty, Gladys Ester Granero
Biopharmaceutics classification systems based on properties of solubility and permeability or extension of metabolism are very important tools in the early stages of development and regulatory stages of new products. However, until now there is no clear understanding between the interplay among these classification systems. Therefore, the main objective of this work was to make a comparison of concepts of BCS and BDDCS to understand what are the key factors that allowing the integration of these biopharmaceutics classification systems...
June 21, 2018: Molecular Pharmaceutics
Monika Raab, Mourad Sanhaji, Larissa Pietsch, Isabelle Béquignon, Amanda K Herbrand, Evelyn Süß, Santosh L Gande, Birgit Caspar, Denis Kudlinzki, Krishna Saxena, Sridhar Sreeramulu, Harald Schwalbe, Klaus Strebhardt, Ricardo M Biondi
The Polo-like kinases (Plks) are an evolutionary conserved family of Ser/Thr protein kinases that possess, in addition to the classical kinase domain at the N-terminus, a C-terminal polo-box domain (PBD) that binds to phosphorylated proteins, modulates the kinase activity and its localization. Plk1, which regulates the formation of the mitotic spindle, has emerged as a validated drug target for the treatment of cancer, because it is required for numerous types of cancer cells but not for the cell division in non-cancer cells...
June 21, 2018: ACS Chemical Biology
Srinivasa Reddy Bonam, Seng Wu Yuan, Lakshmi Tunki, Ranjithkumar Chellian, Sampath Kumar Halmuthur M, Sylviane Muller, Vijayapandi Pandy
Several modern treatment strategies have been adopted to combat cancer with the aim of minimizing toxicity. Medicinal plant-based compounds with the potential to treat cancer have been widely studied in preclinical research and have elicited many innovative ways of leading-edge clinical research. In parallel, researchers have eagerly tried to reduce the toxicity of current chemotherapeutic agents either by combining them with herbals or in using herbals alone. The focus of this article is to present an update of medicinal plants and their bioactive compounds, or mere changes in the bioactive compounds, and herbal edibles, which display efficacy against diverse cancer cells and in anticancer therapy...
June 21, 2018: ChemMedChem
Hao-Fei Yu, Xu-Jie Qin, Cai-Feng Ding, Xin Wei, Jing Yang, Jie-Rong Luo, Lu Liu, Afsar Khan, Lan-Chun Zhang, Cheng-Feng Xia, Xiao-Dong Luo
Two monoterpenoid indole alkaloid erchinines A (1) and B (2), possessing unique 1,4-diazepine fused with oxazolidine architecture and three hemiaminals, were isolated from Ervatamia chinensis. Their structures were elucidated on the basis of intensive spectroscopic analysis, and a plausible biosynthetic pathway from ibogaine was proposed. Both compounds exhibited significant antimicrobial activity against Trichophyton rubrum and Bacillus subtilis, and their activities were comparable to the first line antifungal drug griseofulvin and antibiotic cefotaxime...
June 21, 2018: Organic Letters
Kathrin Tan, Christian Jäger, Dagmar Schlenzig, Stephan Schilling, Mirko Buchholz, Daniel Ramsbeck
Metalloproteinases of the astacin family are more and more drawing attention as potential drug targets. However, the knowledge about inhibitors thereof is limited in most cases. Crucial for the development of metalloprotease inhibitors is a high selectivity to avoid side effects through the inhibition of off-target proteases and the interference with physiological pathways. Here we aimed at the design of novel selective inhibitors for the astacin proteinase meprin α. Based on a recently identified tertiary amine scaffold, a series of compounds was synthesized and evaluated...
June 21, 2018: ChemMedChem
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