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https://www.readbyqxmd.com/read/28102941/synthesis-of-primaquine-glyco-conjugates-as-potential-tissue-schizontocidal-antimalarial-agents
#1
Chandra S Azad, Mridula Saxena, Arif J Siddiqui, Jyoti Bhardwaj, Sunil K Puri, Guru P Dutta, Nity Anand, Anil K Saxena
Primaquine (PQ) is the only drug used to prevent relapse of malaria due to P. vivax and P. ovale, by eradicating the dormant liver form of the parasite (hypnozoites). The side effects associated with PQ limits is uses in treatment of malaria. To overcome the premature oxidative deamination and to increase the life span of drug in the biological system the novel glyco-conjugates of PQ were synthesized by coupling of primaquine with hexoses in phosphate buffer. The saccharide part of the hybrid molecules thought to be direct the drug to the liver, where hypnozoites resides...
January 19, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28102734/fibroblast-like-synoviocytes-dependent-effector-molecules-as-a-critical-mediator-for-rheumatoid-arthritis-current-status-and-future-directions
#2
Ramamoorthi Ganesan, Mahaboobkhan Rasool
Rheumatoid arthritis (RA) is a systemic-autoimmune-mediated disease characterized by synovial hyperplasia and progressive destruction of joint. Currently available biological agents and inhibitor therapy that specifically target tumor necrosis factor-α, interleukin 1β (IL-1β), IL-6, T cells, B cells, and subcellular molecules (p38 mitogen-activated protein kinase and janus kinase) cannot facilitate complete remission in all patients and are unable to cure the disease. Therefore, further potent therapeutic targets need to be identified for effective treatment and successful clinical outcomes in patients with RA...
January 19, 2017: International Reviews of Immunology
https://www.readbyqxmd.com/read/28102676/novel-antitumor-platinum-ii-conjugates-containing-the-nonsteroidal-anti-inflammatory-agent-diclofenac-synthesis-and-dual-mechanisms-of-antiproliferative-effects
#3
Francesco Paolo Intini, Juraj Zajac, Vojtech Novohradsky, Teresa Saltarella, Concetta Pacifico, Viktor Brabec, Giovanni Natile, Jana Kasparkova
One concept how to improve anticancer effects of conventional metallodrugs consists in conjugation of these compounds with other biologically (antitumor) active agents, acting by a different mechanism. Here, we present synthesis, biological effects, and mechanisms of action of new Pt(II) derivatives containing one or two nonsteroidal anti-inflammatory diclofenac (DCF) ligands also known for their antitumor effects. The antiproliferative properties of these metallic conjugates show that these compounds are potent and cancer cell selective cytotoxic agents exhibiting activity in cisplatin resistant and the COX-2 positive tumor cell lines...
January 19, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28102575/bcl-2-family-in-non-small-cell-lung-cancer-its-prognostic-and-therapeutic-implications
#4
Ping-Li Sun, Hironobu Sasano, Hongwen Gao
Non-small cell lung cancer (NSCLC) accounts for approximately 85% of all lung cancers. Despite significant advances in its research of tumor biology and therapy, the prognosis for this neoplasm has still remained poor. The great majority of anticancer agents, regardless of their mechanisms of action, exert their lethal actions on cancer cells by inducing apoptosis following drug-induced cellular damage. Many reported studies have evaluated the prognostic and therapeutic implications of apoptosis in lung cancer, but their exact clinical value has remained unclear...
January 19, 2017: Pathology International
https://www.readbyqxmd.com/read/28101823/biological-activities-of-asteraceae-achillea-millefolium-and-calendula-officinalis-and-lamiaceae-melissa-officinalis-and-origanum-majorana-plant-extracts
#5
Mónica R García-Risco, Lamia Mouhid, Lilia Salas-Pérez, Alexis López-Padilla, Susana Santoyo, Laura Jaime, Ana Ramírez de Molina, Guillermo Reglero, Tiziana Fornari
Asteraceae (Achillea millefolium and Calendula officinalis) and Lamiaceae (Melissa officinalis and Origanum majorana) extracts were obtained by applying two sequential extraction processes: supercritical fluid extraction with carbon dioxide, followed by ultrasonic assisted extraction using green solvents (ethanol and ethanol:water 50:50). The extracts were analyzed in terms of the total content of phenolic compounds and the content of flavonoids; the volatile oil composition of supercritical extracts was analyzed by gas chromatography and the antioxidant capacity and cell toxicity was determined...
January 18, 2017: Plant Foods for Human Nutrition
https://www.readbyqxmd.com/read/28101682/synthesis-spectral-and-extended-spectrum-beta-lactamase-studies-of-transition-metal-tetraaza-macrocyclic-complexes
#6
Dinesh Kumar, Nutan Sharma, Manjula Nair
Urinary tract infections commonly occur in humans due to microbial pathogens invading the urinary tract, which can bring about a range of clinical symptoms and potentially fatal sequelae. The present study is aimed at addressing the development of a new antimicrobial agent against extended spectrum beta lactamase (ESBL) producing E. coli bacteria. We have synthesised some biologically potent (NNNN) donor macrocycles (L 1  = dibenzo[f,n]dipyrido[3,4-b:4',3'-j][1,4,9,12]tetraazacyclohexadecine-6,11,18,23(5H,12H, 7H, 24H)-tetraone, and L 2  = 6,12,19,25-tetraoxo-4,6,11,12,16,18,23,24-octahydrotetrabenzo [b,g,k,p][1,5,10,14]tetra azacyclooctadecine-2,13-dicarboxylic acid) and their Ti and Zr metal complexes in alcoholic media using microwave protocol...
January 18, 2017: Journal of Biological Inorganic Chemistry: JBIC
https://www.readbyqxmd.com/read/28101576/multiple-effects-of-ellagic-acid-on-human-colorectal-carcinoma-cells-identified-by-gene-expression-profile-analysis
#7
Jinlu Zhao, Guodong Li, Wanlan Bo, Yuhui Zhou, Shuwei Dang, Jiufeng Wei, Xinglong Li, Ming Liu
Colorectal carcinoma (CRC) is the third most commonly diagnosed cancer in the world. Phytochemicals have become a research hotspot in recent years as cancer prevention and treatment agents due to their low toxicity and limited side-effects. Ellagic acid (EA), a natural phenolic constituent, displays various biological activities, including anticancer effects. However, the detailed anticancer mechanisms of EA remain unclear. In the present study, we found that EA inhibited the growth of HCT-116 colon cancer cells...
February 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28101535/the-case-for-adopting-the-species-complex-nomenclature-for-the-etiologic-agents-of-cryptococcosis
#8
Kyung J Kwon-Chung, John E Bennett, Brian L Wickes, Wieland Meyer, Christina A Cuomo, Kurt R Wollenburg, Tihana A Bicanic, Elizabeth Castañeda, Yun C Chang, Jianghan Chen, Massimo Cogliati, Françoise Dromer, David Ellis, Scott G Filler, Matthew C Fisher, Thomas S Harrison, Steven M Holland, Shigeru Kohno, James W Kronstad, Marcia Lazera, Stuart M Levitz, Michail S Lionakis, Robin C May, Popchai Ngamskulrongroj, Peter G Pappas, John R Perfect, Volker Rickerts, Tania C Sorrell, Thomas J Walsh, Peter R Williamson, Jianping Xu, Adrian M Zelazny, Arturo Casadevall
Cryptococcosis is a potentially lethal disease of humans/animals caused by Cryptococcus neoformans and Cryptococcus gattii. Distinction between the two species is based on phenotypic and genotypic characteristics. Recently, it was proposed that C. neoformans be divided into two species and C. gattii into five species based on a phylogenetic analysis of 115 isolates. While this proposal adds to the knowledge about the genetic diversity and population structure of cryptococcosis agents, the published genotypes of 2,606 strains have already revealed more genetic diversity than is encompassed by seven species...
January 2017: MSphere
https://www.readbyqxmd.com/read/28101472/the-effects-of-hypoxia-on-u937-cell-line-in-mesenchymal-stem-cells-co-culture-system
#9
Mostafa Ejtehadifar, Karim Shamsasenjan, Parvin Akbarzadehlaleh, Sarah Zahedi, Narjes Kazemi
Purpose: Mesenchymal Stem Cells (MSCs) are the most important members of Bone Marrow (BM) milieu. MSCs affect different kinds of cells, particularly malignant cells of hematologic malignancies, but the effects of MSCs are unclear exactly. Here we analyzed the effects of derived Umbilical Cord Blood-MSCs on proliferation, cell death and some surface markers of U937 cell line in a Co-culture system with MSCs. Methods: Here we designed Co-culture systems as a model of BM milieu. We cultured U937 cells on UCB-MSCs and MSCs Conditioned Medium (C...
December 2016: Advanced Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28101253/2-chromon-3-yl-imidazole-derivatives-as-potential-antimicrobial-agents-synthesis-biological-evaluation-and-molecular-docking-studies
#10
Shweta Sharma, Vishal Sharma, Gurpreet Singh, Harpreet Kaur, Shubham Srivastava, Mohan Paul S Ishar
A series of novel 2-(chromon-3-yl)-4,5-diphenyl-1H-imidazoles (4a-h) were synthesized by one pot condensation of substituted 3-formylchromones (1a-h), benzil (2) and ammonium acetate (3) in refluxing acetic acid at 110 °C under N2 atmosphere. Allylation of compounds 4a-h with allyl bromide in the presence of fused K2CO3 furnished N-allyl-2-(chromon-3-yl)-4,5-diphenyl-1H-imidazoles (6a-h). The synthesized compounds were characterized spectroscopically and evaluated for in vitro antimicrobial activity against various pathogenic bacterial and fungal strains by disc diffusion method...
January 2017: Journal of Chemical Biology
https://www.readbyqxmd.com/read/28100748/independent-neural-computation-of-value-from-other-people-s-confidence
#11
Daniel Campbell-Meiklejohn, Arndis Simonsen, Chris D Frith, Nathaniel D Daw
: Expectation of reward can be shaped by the observation of actions and expressions of other people in one's environment. A person's apparent confidence in the likely reward of an action, for instance, makes qualities of their evidence, not observed directly, socially accessible. This strategy is computationally distinguished from associative learning methods that rely on direct observation, by its use of inference from indirect evidence. In twenty-three healthy human subjects, we isolated effects of first-hand experience, other people's choices, and the mediating effect of their confidence, on decision-making and neural correlates of value within ventromedial prefrontal cortex (vmPFC)...
January 18, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28100395/replication-study-coadministration-of-a-tumor-penetrating-peptide-enhances-the-efficacy-of-cancer-drugs
#12
Christine Mantis, Irawati Kandela, Fraser Aird
In 2015, as part of the Reproducibility Project: Cancer Biology, we published a Registered Report (Kandela et al., 2015) that described how we intended to replicate selected experiments from the paper "Coadministration of a tumor-penetrating peptide enhances the efficacy of cancer drugs" (Sugahara et al., 2010). Here we report the results of those experiments. We found that coadministration with iRGD peptide did not have an impact on permeability of the chemotherapeutic agent doxorubicin (DOX) in a xenograft model of prostate cancer, whereas the original study reported that it increased the penetrance of this cancer drug (Figure 2B; Sugahara et al...
January 19, 2017: ELife
https://www.readbyqxmd.com/read/28099816/new-treatment-options-and-emerging-drugs-for-axial-spondyloarthritis-biological-and-targeted-synthetic-agents
#13
Eric Toussirot
Ankylosing spondylitis (AS) and axial spondyloarthritis (ax SpA) are chronic inflammatory diseases mainly involving the axial skeleton. Pharmacological treatments for AS and ax SpA usually include local glucocorticoid injections, NSAIDs and anti-TNFa agents. Since around 30% to 40% of patients are non responders or intolerant to anti-TNFa agents, we need new therapeutic options for AS and ax SpA. Areas covered: This review describes the new biological agents that can be used or are in development for AS or ax SpA as well as emerging synthetic targeted drugs...
January 18, 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28098883/developmental-expression-of-toll%C3%A2-like-receptors-in-the-guinea-pig-lung
#14
Lingjie Ma, Jiali Yang, Li Yang, Juan Shi, Jing Xue, Yong Li, Xiaoming Liu
The guinea pig is a useful model for investigating infectious and non‑infectious lung diseases due to the sensitivity of its respiratory system and susceptibility to infectious agents. Toll‑like receptors (TLRs) are important components of the innate immune response and are critical for lung immune function. In the present study, the differentiation of epithelial cells in the guinea pig lung was examined during gestation by studying anatomic morphology and the major epithelial cell types using cell type‑specific markers...
January 17, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28098865/endophytic-fungi-from-mangrove-inhibit-lung-cancer-cell-growth-and-angiogenesis-in-vitro
#15
Xin Liu, Xin Wu, Yuefan Ma, Wenzhang Zhang, Liang Hu, Xiaowei Feng, Xiangyong Li, Xudong Tang
The secondary metabolites of mangrove-derived endophytic fungi contain multiple substances with novel structures and biological activities. In the present study, three types of mangrove plants, namely Kandelia candel, Rhizophora stylosa and Rhizophoraceae from Zhanjiang region including the leaves, roots and stems were collected, and endophytic fungi were isolated, purified and identified from these mangrove plants. MTT assay was used to observe the effects of the isolated endophytic fungi on the growth of A549 and NCI-H460 lung cancer cells...
January 16, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28098791/development-of-high-throughput-method-for-measurement-of-vascular-nitric-oxide-generation-in-microplate-reader
#16
Soad S Abd El-Hay, Christa L Colyer
BACKGROUND: Despite the importance of nitric oxide (NO) in vascular physiology and pathology, a high-throughput method for the quantification of its vascular generation is lacking. OBJECTIVE: By using the fluorescent probe 4-amino-5-methylamino-2',7'-difluorofluorescein (DAF-FM), we have optimized a simple method for the determination of the generation of endothelial nitric oxide in a microplate format. METHODS: A nitric oxide donor was used (3-morpholinosydnonimine hydrochloride, SIN-1)...
January 13, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28098761/pancreatic-neuroendocrine-neoplasms-basic-biology-current-treatment-strategies-and-prospects-for-the-future
#17
REVIEW
Akihiro Ohmoto, Hirofumi Rokutan, Shinichi Yachida
Pancreatic neuroendocrine neoplasms (pNENs) are rare tumors accounting for only 1%-2% of all pancreatic tumors. pNENs are pathologically heterogeneous and are categorized into three groups (neuroendocrine tumor: NET G1, NET G2; and neuroendocrine carcinoma: NEC) on the basis of the Ki-67 proliferation index and the mitotic count according to the 2010 World Health Organization (WHO) classification of gastroenteropancreatic NENs. NEC in this classification includes both histologically well-differentiated and poorly differentiated subtypes, and modification of the WHO 2010 classification is under discussion based on genetic and clinical data...
January 13, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28098463/absolute-configuration-of-native-oligomeric-proanthocyanidins-with-dentin-biomodification-potency
#18
Joo-Won Nam, Rasika S Phansalkar, David C Lankin, James B McAlpine, Ariene A Leme-Kraus, Cristina M P Vidal, Li-She Gan, Ana Bedran-Russo, Shao-Nong Chen, Guido F Pauli
The structurally complex oligomeric proanthocyanidins (OPACs) are promising biomimetic agents, capable of strengthening the macromolecular backbone of teeth via intermolecular and intermicrofibrillar cross-linking. This study establishes analytical methods capable of determining the absolute configuration of the catechin-type monomeric units of underivatized OPACs. This preserves the capacity of their biological evaluation, aimed at understanding the inevitably stereospecific interactions between the OPACs and dentin collagen...
January 18, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28097810/physicochemical-and-biological-evaluation-of-a-cinnamamide-derivative-r-s-2e-1-3-hydroxypiperidin-1-yl-3-phenylprop-2-en-1-one-km-608-for-nervous-system-disorders
#19
Agnieszka Gunia-Krzyżak, Ewa Żesławska, Florence Bareyre, Wojciech Nitek, Anna M Waszkielewicz, Henryk Marona
A cinnamamide scaffold has been successfully incorporated in several compounds possessing desirable pharmacological activities in central and peripheral nervous system such as anticonvulsant, antidepressant, neuroprotective, analgesic, anti-inflammatory, muscle relaxant, and sedative/hypnotic properties. R,S-(2E)-1-(3-hydroxypiperidin-1-yl)-3-phenylprop-2-en-1-one (KM-608), a cinnamamide derivative, was synthesized, its chemical structure was confirmed by means of spectroscopy and crystallography, additionally thermal analysis showed that it exists in one crystalline form...
January 18, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28096932/contemporary-agents-in-the-management-of-metastatic-castration-resistant-prostate-cancer
#20
REVIEW
Anil Kapoor, Christopher Wu, Bobby Shayegan, Adrian P Rybak
Docetaxel-based chemotherapy has been the standard of care for metastatic castration-resistant prostate cancer (mCRPC) since 2004. Over the past few years, there has been a significant paradigm shift in the treatment landscape of this disease. A deeper understanding of prostate cancer biology, along with the development of novel agents has created hope towards treating chemotherapy-naïve and resistant disease. Following the implementation of docetaxel as the first-line therapy for mCRPC, five novel therapies have demonstrated survival benefit in mCRPC...
November 2016: Canadian Urological Association Journal, Journal de L'Association des Urologues du Canada
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