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https://www.readbyqxmd.com/read/28710964/design-synthesis-and-biological-studies-of-a-library-of-nk1-receptor-ligands-based-on-a-5-arylthiosubstituted-2-amino-4-6-diaryl-3-cyano-4h-pyran-core-switch-from-antagonist-to-agonist-effect-by-chemical-modification
#1
Rocío Recio, Empar Vengut-Climent, Bernard Mouillac, Hélène Orcel, Miguel López-Lázaro, José Manuel Calderón-Montaño, Eleuterio Álvarez, Noureddine Khiar, Inmaculada Fernández
A library of 5-arylthiosubstituted 2-amino-4,6-diaryl-3-cyano-4H-pyrans has been synthesized as a new family of non-peptide NK1 receptor ligands by a one-pot cascade process. Their biological effects via interaction with the NK1 receptor were experimentally determined as percentage of inhibition (for antagonists) and percentage of activation (for agonists), compared to the substance P (SP) effect, in IPone assay. A set of these amino compounds was found to inhibit the action of SP, and therefore can be considered as a new family of SP-antagonists...
June 28, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28710015/bactericidal-impact-of-ag-zno-and-mixed-agzno-colloidal-nanoparticles-on-h37rv-mycobacterium-tuberculosis-phagocytized-by-thp-1%C3%A2-cell-lines
#2
Alireza Jafari, Nader Mosavari, Farahnaz Movahedzadeh, Saeedeh Jafari Nodooshan, Roya Safarkar, Rossella Moro, Morteza Kamalzadeh, Ali Majidpour, Mina Boustanshenas, Tahereh Mosavi
The purpose of this research project was to infection of human macrophages (THP-1) cell lines by H37Rv strain of Mycobacterium tuberculosis (H37RvMTB) and find out the ratio/dilution of mixture silver (Ag NPs) and zinc oxide nanoparticles (ZnO NPs) whose ability to eliminate phagocytized bacteria compared to rifampicin. The colloidal Ag NPs and ZnO NPs were synthesized and their characteristics were evaluated. The THP-1 cell lines were infected with different concentration of H37RvMTB. Next, the infected cells were treated with different ratios/dilutions of Ag NPs, ZnO NPs and rifampicin...
July 11, 2017: Microbial Pathogenesis
https://www.readbyqxmd.com/read/28709826/synthesis-antioxidant-and-antiproliferative-activities-of-1-3-4-thiadiazoles-derived-from-phenolic-acids
#3
Katarina Jakovljević, Ivana Z Matić, Tatjana Stanojković, Ana Krivokuća, Violeta Marković, Milan D Joksović, Nevena Mihailović, Marija Nićiforović, Ljubinka Joksović
Two 2-amino-1,3,4-thiadiazoles containing phenolic hydroxyl groups were combined with different carboxylic acid chlorides giving sixteen amide derivatives with good antioxidant and antiproliferative potential. The compound 3'c with an adamantane ring displayed excellent DPPH radical scavenging activity and good cytotoxic activity against human acute promyelocytic leukemia HL-60 cells, while 1,3,4-thiadiazole 3'h with 4-chlorophenyl moiety was found to be the most effective in inhibition of survival of lung carcinoma A549 cells...
July 3, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28689097/design-synthesis-and-antitubercular-potency-of-4-hydroxyquinolin-2-1h-ones
#4
Maíra Bidart de Macedo, Roman Kimmel, Damijana Urankar, Martin Gazvoda, Antonio Peixoto, Freya Cools, Eveline Torfs, Luc Verschaeve, Emerson Silva Lima, Antonín Lyčka, David Milićević, Antonín Klásek, Paul Cos, Stanislav Kafka, Janez Košmrlj, Davie Cappoen
In this study, a 50-membered library of substituted 4-hydroxyquinolin-2(1H)-ones and two closely related analogues was designed, scored in-silico for drug likeness and subsequently synthesized. Thirteen derivatives, all sharing a common 3-phenyl substituent showed minimal inhibitory concentrations against Mycobacterium tuberculosis H37Ra below 10 μM and against Mycobacterium bovis AN5A below 15 μM but were inactive against faster growing mycobacterial species. None of these selected derivatives showed significant acute toxicity against MRC-5 cells or early signs of genotoxicity in the Vitotox™ assay at the active concentration range...
June 29, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28682604/extending-the-excitation-wavelength-of-potential-photosensitizers-via-appendage-of-a-kinetically-stable-terbium-iii-macrocyclic-complex-for-applications-in-photodynamic-therapy
#5
Phuc Ung, Michèle Clerc, Huaiyi Huang, Kangqiang Qiu, Hui Chao, Michael Seitz, Ben Boyd, Bim Graham, Gilles Gasser
The development of viable photodynamic therapy protocols is often hindered by photosensitizers that require high-energy UV irradiation that has limited potential for clinical use due to its low tissue penetration. Herein, we report a strategy for extending the excitation wavelength of potential photosensitizers via the covalent attachment of a terbium(III)-1,4,7,10-tetraazacyclododecane-1,4,7-triacetate complex (DO3A-Tb). The method was systematically demonstrated with a series of polycyclic aromatic hydrocarbons (naphthalene, phenanthrene, anthracene, pyrene, and fluoranthene) to prepare six new complexes (Tb1-Tb6) with bathochromic shifts that extended into the visible region...
July 17, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28675952/a-novel-fine-tuning-scheme-of-mir-200c-in-modulating-lung-cell-redox-homeostasis
#6
Yi-Hsuan Wu, Hsin-Ru Lin, Ying-Hsuan Lee, Pin-Hao Huang, Huei-Chung Wei, Arnold Stern, Daniel Tsun-Yee Chiu
Oxidative stress induces miR-200c, the predominant microRNA (miRNA) in lung tissues; however, the antioxidant role and biochemistry of such induction have not been clearly defined. Therefore, a lung adenocarcinoma cell line (A549) and a normal lung fibroblast (MRC-5) were used as models to determine the effects of miR-200c expression on lung antioxidant response. Hydrogen peroxide (H2O2) upregulated miR-200c, whose overexpression exacerbated the decrease in cell proliferation, retarded the progression of cells in the G2/M-phase, and increased oxidative stress upon H2O2 stimulation...
July 4, 2017: Free Radical Research
https://www.readbyqxmd.com/read/28673683/single-walled-carbon-nanotubes-swcnts-inhibit-heat-shock-protein-90-hsp90-signaling-in-human-lung-fibroblasts-and-keratinocytes
#7
Li-Chu Ong, Yuen-Fen Tan, Boon Shing Tan, Felicia Fei-Lei Chung, Soon-Keng Cheong, Chee-Onn Leong
Single-walled carbon nanotubes (SWCNTs) are carbon-based nanomaterials that possess immense industrial potential. Despite accumulating evidence that exposure to SWCNTs might be toxic to humans, our understanding of the mechanisms for cellular toxicity of SWCNTs remain limited. Here, we demonstrated that acute exposure of short (1-3μm) and regular-length (5-30μm) pristine, carboxylated or hydroxylated SWCNTs inhibited cell proliferation in human somatic and human stem cells in a cell type-dependent manner...
July 1, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28672143/synthesis-characterization-and-crystal-structures-of-two-pentagonal-bipyramidal-fe-iii-complexes-with-dihydrazone-of-2-6-diacetylpyridine-and-girard-s-t-reagent-anticancer-properties-of-various-metal-complexes-of-the-same-ligand
#8
Katarina Anđelković, Milica R Milenković, Andrej Pevec, Iztok Turel, Ivana Z Matić, Miroslava Vujčić, Dušan Sladić, Dušanka Radanović, Gabrijela Brađan, Svetlana Belošević, Božidar Čobeljić
In this work synthesis, characterization and crystal structures of two isothiocyanato Fe(III) complexes with 2,2'-[2,6-pyridinediylbis(ethylidyne-1-hydrazinyl-2-ylidene)]bis[N,N,N-trimethyl-2-oxoethanaminium] dichloride (H2LCl2) ligand, with composition [FeL(NCS)2]SCN·2H2O and [FeL(NCS)2]2[Fe(H2O)(NCS)5]·4H2O, has been reported. Both iron(III) complexes possess the same pentagonal-bipyramidal complex cation, while the nature of their anions depends on mole ratio of NH4SCN and FeCl3·6H2O used in reaction...
September 2017: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/28664293/targeting-autophagy-to-modulate-cell-survival-a-comparative-analysis-in-cancer-normal-and-embryonic-cells
#9
Aleksandra Divac Rankov, Mila Ljujić, Marija Petrić, Dragica Radojković, Milica Pešić, Jelena Dinić
Autophagy is linked to multiple cancer-related signaling pathways, and represents a defense mechanism for cancer cells under therapeutic stress. The crosstalk between apoptosis and autophagy is essential for both tumorigenesis and embryonic development. We studied the influence of autophagy on cell survival in pro-apoptotic conditions induced by anticancer drugs in three model systems: human cancer cells (NCI-H460, COR-L23 and U87), human normal cells (HaCaT and MRC-5) and zebrafish embryos (Danio rerio). Autophagy induction with AZD2014 and tamoxifen antagonized the pro-apoptotic effect of chemotherapeutics doxorubicin and cisplatin in cell lines, while autophagy inhibition by wortmannin and chloroquine synergized the action of both anticancer agents...
June 29, 2017: Histochemistry and Cell Biology
https://www.readbyqxmd.com/read/28654117/synthesis-and-biological-evaluation-of-novel-acyclic-and-cyclic-glyoxamide-based-derivatives-as-bacterial-quorum-sensing-and-biofilm-inhibitors
#10
Shashidhar Nizalapur, Onder Kimyon, Eugene Yee, Mohan M Bhadbhade, Mike Manefield, Mark Willcox, David StC Black, Naresh Kumar
Bacteria regulate the expression of various virulence factors and processes such as biofilm formation through a chemically-mediated communication mechanism called quorum sensing. Bacterial biofilms contribute to antimicrobial resistance as they can protect bacteria embedded in their matrix from the effects of antibiotics. Thus, developing novel quorum sensing inhibitors, which can inhibit biofilm formation, is a viable strategy to combat antimicrobial resistance. We report herein the synthesis of novel acyclic and cyclic glyoxamide derivatives via ring-opening reactions of N-acylisatins...
June 27, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28653252/sil-24-peptide-a-human-interleukin-24-isoform-induces-mitochondrial-mediated-apoptosis-in-human-cancer-cells
#11
Samira Valiyari, Mona Salami, Reza Mahdian, Mohammad Ali Shokrgozar, Mana Oloomi, Azadeh Mohammadi Farsani, Saeid Bouzari
PURPOSE: Interleukin-24 (IL-24) is a unique cytokine in the IL-10 family that reveals tumor-suppressive activity against a broad range of cancers. Alternative splicing of human IL-24 generates several isoforms with different pro-apoptotic activities. In the current study, we aimed to investigate the cytotoxic properties of a recombinant smallest isoform of IL-24 (sIL-24) and the underlying molecular mechanisms in PC-3, A549, U937, and Raji cancer cells as well as normal cell line MRC-5...
June 26, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28613963/cytotoxic-and-antimicrobial-activities-of-cantharellus-cibarius-fr-cantarellaceae
#12
Marina Kolundžić, Tatjana Stanojković, Jelena Radović, Ana Tačić, Margarita Dodevska, Marina Milenković, Francesca Sisto, Carla Masia, Giampietro Farronato, Vesna Nikolić, Tatjana Kundaković
Antibacterial and cytotoxic activities of cyclohexane, dichloromethane, methanol, and aqueous extracts of Cantharellus cibarius were tested. Broth microdilution assay was performed against 10 bacterial strains (Staphylococcus aureus, S. epidermidis, Micrococcus luteus, Bacillus subtilis, Enterococcus feacalis, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Salmonella abony), with emphasis on Helicobacter pylori. Methanol extract was the most active against H. pylori strains with minimal inhibitory concentration values between 4 and 32 μg/mL...
June 14, 2017: Journal of Medicinal Food
https://www.readbyqxmd.com/read/28607618/catechin-and-epicatechin-reduce-mitochondrial-dysfunction-and-oxidative-stress-induced-by-amiodarone-in-human-lung-fibroblasts
#13
Luciana Fernandes Silva Santos, Adriana Stolfo, Caroline Calloni, Mirian Salvador
BACKGROUND: Amiodarone (AMD) and its metabolite N-desethylamiodarone can cause some adverse effects, which include pulmonary toxicity. Some studies suggest that mitochondrial dysfunction and oxidative stress may play a role in these adverse effects. Catechin and epicatechin are recognized as important phenolic compounds with the ability to decrease oxidative stress. Therefore, the aim of this study was to evaluate the potential of catechin and epicatechin to modulate mitochondrial dysfunction and oxidative damage caused by AMD in human lung fibroblast cells (MRC-5)...
June 2017: Journal of Arrhythmia
https://www.readbyqxmd.com/read/28601597/in-vitro-studies-on-cytotoxicity-of-delaminated-ti3c2-mxene
#14
A M Jastrzębska, A Szuplewska, T Wojciechowski, M Chudy, W Ziemkowska, L Chlubny, A Rozmysłowska, A Olszyna
MXenes are a novel family of 2D materials, the biological activity of which has been largely unexplored. The present study, for the first time, shows some aspects of the in vitro toxicity of 2D sheets of Ti3C2 MXene. The Ti3AlC2 MAX phase was used in an expansion and delamination process to obtain Ti3C2 material in the form of 2D sheets. The obtained 2D material was characterized using SEM, TEM, DLS, XPS, and zeta potential. The biological activity of the MXene was determined on two normal (MRC-5 and HaCaT) and two cancerous (A549 and A375) cell lines...
June 6, 2017: Journal of Hazardous Materials
https://www.readbyqxmd.com/read/28601070/sox9-protects-against-human-lung-fibroblast-cell-apoptosis-induced-by-lps-through-activation-of-the-akt-gsk3%C3%AE-pathway
#15
Zhankun Zhu, Jinhua Dai, Yufeng Liao, Tao Wang
Sex-determining region Y-box 9 (Sox9) is an important transcription factor that has been identified as a key regulator of several types of diseases. In this study, we explored the correlation of Sox9 with cell proliferation, apoptosis, inflammatory factor expression, and the possible signaling pathway in human lung fibroblast cell line to investigate the possible mechanism of neonatal pneumonia. Therefore, in the present study, pc-Sox9 and si-Sox9 were transfected into MRC-5 (human fetal lung fibroblast cell line) to promote or inhibit expression of Sox-9...
May 2017: Biochemistry. Biokhimii︠a︡
https://www.readbyqxmd.com/read/28589873/human-cytomegalovirus-micrornas-are-carried-by-virions-and-dense-bodies-and-are-delivered-to-target-cells
#16
Abdul-Aleem Mohammad, Helena Costa, Natalia Landázuri, Weng-Onn Lui, Kjell Hultenby, Afsar Rahbar, Koon-Chu Yaiw, Cecilia Söderberg-Nauclér
Human cytomegalovirus (HCMV) infection results in the production of virions, dense bodies (DBs) and non-infectious enveloped particles, all of which incorporate proteins and RNAs that can be transferred to host cells. Here, we investigated whether virions and DBs also carry microRNAs (miRNAs) and assessed their delivery and functionality in cells. Human lung fibroblasts (MRC-5) were infected with the HCMV strain AD169, and conditioned cell culture medium was collected and centrifuged. The pellets were treated with RNase-ONE, and the virions and DBs were purified with a potassium tartrate-glycerol gradient and dialysed...
May 2017: Journal of General Virology
https://www.readbyqxmd.com/read/28554995/curcuma-mangga-mediated-synthesis-of-gold-nanoparticles-characterization-stability-cytotoxicity-and-blood-compatibility
#17
Yiing Yee Foo, Vengadesh Periasamy, Lik Voon Kiew, G Gnana Kumar, Sri Nurestri Abd Malek
The utilization of toxic chemicals as reducing and stabilizing agents in the preparation of gold nanoparticles (AuNPs) has increased in vivo toxicity and thus limited its application in clinical settings. Herein, we propose an alternative method of preparing highly stable AuNPs, where non-toxic Curcuma mangga (CM) extract was used as a single reducing and stabilizing agent to overcome the aforementioned constraints. The morphological images enunciated that the homogeneously dispersed AuNPs exhibited spherical morphology with an average particle diameter of 15...
May 27, 2017: Nanomaterials
https://www.readbyqxmd.com/read/28553231/hydroxysafflor-yellow-a-suppresses-mrc-5-cell-activation-induced-by-tgf-%C3%AE-1-by-blocking-tgf-%C3%AE-1-binding-to-t%C3%AE-rii
#18
Ruiyan Pan, Yadan Zhang, Meng Zheng, Baoxia Zang, Ming Jin
Hydroxysafflor yellow A (HSYA) is an active ingredient of Carthamus tinctorius L.. This study aimed to evaluate the effects of HSYA on transforming growth factor-β1 (TGF-β1)-induced changes in proliferation, migration, differentiation, and extracellular matrix accumulation and degradation in human fetal lung fibroblasts (MRC-5), to explore the mechanisms whereby HSYA may alleviate pulmonary fibrosis. MRC-5 cells were incubated with various doses of HSYA and/or the TGF-β receptor type I kinase inhibitor SB431542 and then stimulated with TGF-β1...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28548957/involvement-of-p38-%C3%AE-trcp-tristetraprolin-tnf%C3%AE-axis-in-radiation-pneumonitis
#19
Pranathi Meda Krishnamurthy, Shirish Shukla, Paramita Ray, Rohit Mehra, Mukesh K Nyati, Theodore S Lawrence, Dipankar Ray
Early release of tumor necrosis factor-alpha (TNF-α) during radiotherapy of thoracic cancers plays an important role in radiation pneumonitis, whose inhibition may provide lung radioprotection. We previously reported radiation inactivates Tristetraprolin (TTP), a negative regulator of TNF-α synthesis, which correlated with increased TNF-α release. However, the molecular events involved in radiation-induced TTP inactivation remain unclear. To determine if eliminating Ttp in mice resulted in a phenotypic response to radiation, Ttp-null mice lungs were exposed to a single dose of 15 Gy, and TNF-α release and lung inflammation were analyzed at different time points post-irradiation...
May 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/28521385/-ziziphus-oxyphylla-ethnobotanical-ethnopharmacological-and-phytochemical-review
#20
REVIEW
Rizwan Ahmad, Niyaz Ahmad, Atta Abbas Naqvi
ETHNOPHARMACOLOGICAL RELEVANCE: Ziziphus oxyphylla (ZO) is distributed mainly in tropic and warm temperate regions in the world. Pakistan owns six (06) indigenous species of genus Ziziphus out of which ZO is widely used for traditional treatment of different ailments such as diabetes, jaundice and liver diseases. AIM OF THE STUDY: The present review aims to provide in-depth and comprehensive literature overview, regarding botanical, chemical and biological characteristics of the plant alongwith phytochemical isolation and mechanistic studies to support its folklore and traditional uses...
July 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
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