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Francesca Citossi, Thomas Smith, Jong Bong Lee, Joel Segal, Pavel Gershkovich, Michael John Stocks, Tracey D Bradshaw, Barrie Kellam, Maria Marlow
Low molecular weight gelators (LMWGs) of chemotherapeutic drugs represent a valid alternative to the existing poly-mer-based formulations used for targeted delivery of anticancer drugs. Herein we report the design and development of novel self-assembling gelators of the antitumour benzothiazole 5F 203 (1). Two different types of derivatives of 1 were synthesized, formed by an amide (2) and a carbamate (3a-3d) linker, respectively, which showed potent in vitro anti-tumour activity against MCF-7 mammary and IGROV-1 ovarian carcinoma cells...
March 5, 2018: Molecular Pharmaceutics
Song-Ming Ding, Ai-Li Lu, Wu Zhang, Lin Zhou, Hai-Yang Xie, Shu-Sen Zheng, Qi-Yong Li
Background: Our previous study showed that cancer-associated fibroblast MRC-5 promoted hepatocellular carcinoma progression by enhancing migration and invasion capability. However, few studies have explored the role of MRC-5 in pancreatic cancer (PC). In this study, we examined the exact role and associated mechanisms of MRC-5. Methods: The conditioned media for MRC-5 was used to culture PC cell lines SW1990 and PANC-1. Cell proliferation was compared based on colony formation assays of PC cells in normal media and of PC cells cultured with conditioned media of MRC-5...
2018: Journal of Cancer
Susan Oliver, Eugene Yee, Maria Kavallaris, Orazio Vittorio, Cyrille Boyer
Quercetin, a naturally occurring potent antioxidant, is limited in therapeutic use, owing to its poor water solubility and stability. Herein, a method of conjugating quercetin to an aldehyde functionalized dextran via an HCl catalyzed condensation reaction to yield a water soluble quercetin functionalized polymer is reported. The prepared conjugate is characterized by 1 H and 1 H-13 C heteronuclear single quantum correlation (HSQC) NMR, which demonstrate that conjugation occurs via both the A- and B-rings of quercetin...
February 7, 2018: Macromolecular Bioscience
Ines A Barbosa, Ignacio Vega-Naredo, Rute Loureiro, Ana F Branco, Rita Garcia, Patricia M Scott, Paulo J Oliveira
BACKGROUND: Expression of TRAP1, a member of the HSP90 chaperone family, has been implicated in tumor protective effects, based on differential mitochondrial localization and function. DESIGN: This work was designed to provide new insights on the pathways involved in TRAP1-provided cytoprotection on NSCLC. For this, TRAP1-depleted A549 human NSCLC cells and MRC-5 normal lung fibroblasts were produced using a siRNA approach and main cellular quality control mechanisms were investigated...
January 31, 2018: European Journal of Clinical Investigation
A Kyzioł, A Cierniak, J Gubernator, A Markowski, M Jeżowska-Bojczuk, U K Komarnicka
The cytotoxic effect of iodide or thiocyanate copper(i) complexes (1-PSf, 2-PSf, 3-PSf, 4-PSf) with phosphine derived from sparfloxacin (HSf) and 2,9-dimethyl-1,10-phenanthroline (dmp) or 2,2'-biquinoline (bq) as diimine auxiliary ligands was proved in vitro on somatic (MRC-5) and neoplastic (MCF7) human cell lines. Differences in mode of action were investigated in-depth for the selected dmp and bq complexes (1-PSf, 3-PSf, respectively) by elucidation of the following: (i) the efficiency to produce reactive oxygen species (ROS) in biological systems (cyclic voltammetry); (ii) their impact on mitochondrial membrane potential; (iii) potency for the activation of caspases 3 and 9; (iv) influence on the degree of DNA degradation (comet assay)...
January 18, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
Hitesh Kumar Dewangan, Tarun Pandey, Lakshmi Maurya, Sanjay Singh
The present work is focused on the development and evaluation of single dose sustained-release Hepatitis B surface antigen (HBsAg) loaded nanovaccine for Hepatitis B. The conventional treatment suffers from repeated administration and hence requires a booster dose. Therefore, polymeric nanovaccine of HBsAg was developed by double emulsion solvent evaporation technique, utilizing central composite design for formulation optimization. The effects of independent variables (like polymer amount, stabilizer concentration, aqueous/organic phase ratio and homogenizer speed) were also studied on critical quality attributes like particle size and entrapment efficiency...
January 14, 2018: International Journal of Biological Macromolecules
Xiao-Yu Wan, Li-Yun Xu, Bing Li, Qiu-Hong Sun, Qiu-Liang Ji, Dong-Dong Huang, Lan Zhao, Yong-Tao Xiao
It has been previously reported that human embryonic fibroblasts and mouse embryonic fibroblasts can be converted into neuronal cells using chemical agents, along with forced expression specific transcriptional factors. However, the materials required for reprogramming in these approaches presents major technical difficulties and safety concerns. The current study investigated whether a cocktail of small molecules can convert human lung fibroblast cells into neurons. The small molecules valproic acid, CHIR99021, DMH1, Repsox, forskolin, Y‑27632 and SP600125 (VCHRFYS) were used to induce MRC‑5 cells into neuronal cells in vitro...
January 10, 2018: International Journal of Molecular Medicine
Efres Belmonte-Reche, Marta Martínez-García, Aurore Guédin, Michela Zuffo, Matilde Arévalo-Ruiz, Filippo Doria, Jenny Campos-Salinas, Marjorie Maynadier, Jose-Juan Lopez-Rubio, Mauro Freccero, Jean-Louis Mergny, Jose María Perez-Victoria, Juan Carlos Morales
G-quadruplexes (G4) are DNA secondary structures which take part in the regulation of gene expression. Putative G4 forming sequences (PQS) have been reported in mammals, yeast, bacteria and viruses. Here, we present PQS searches on the genomes of T. brucei, L. major and P. falciparum. We found telomeric sequences and new PQS motifs. Biophysical experiments showed that EBR1, a 29 nucleotide long highly repeated PQS in T. brucei, forms a stable G4 structure. G4 ligands based on carbohydrate conjugated naphthalene diimides (carb-NDIs) which bind G4's including hTel, could bind EBR1 with selectivity versus dsDNA...
January 11, 2018: Journal of Medicinal Chemistry
Lin Wu, Liping Sun, Yongqiang Hua, Chunyang Yang, Yu Teng
BACKGROUND: Acute lung injury is a life-threatening inflammatory lung condition. Studies have explored the role of lncRNA H19 in several diseases, including cancers. In this study, We aimed to explore the role of H19 in lipopolysaccharide (LPS)-induced lung injury and to elucidate the underlying molecular mechanism. METHODS: MRC-5 cells (lung fibroblast cells) were used in the experiment. Cell viability, proliferation, and apoptosis were measured by specific assays...
January 8, 2018: Journal of Cellular Biochemistry
Giovanna Gomes Lara, Marcelo Fernandes Cipreste, Gracielle Ferreira Andrade, Wellington Marcos da Silva, Edésia Martins Barros de Sousa
Recently, flufenamic acid (FFA) was discovered among fenamates as a free radical scavenger and gap junction blocker; however, its effects have only been studied in cancer cells. Normal cells in the surroundings of a tumor also respond to radiation, although they are not hit by it directly. This phenomenon is known as the bystander effect, where response molecules pass from tumor cells to normal ones, through communication channels called gap junctions. The use of the enhanced permeability and retention effect, through which drug-loaded nanoparticles smaller than 200 nm may accumulate around a tumor, can prevent the local side effect upon controlled release of the drug...
January 9, 2018: Bioengineering
M Abastabar, A Akbari, J Akhtari, M T Hedayati, T Shokohi, H Mehrad-Majd, H Ghalehnoei, S Ghasemi
Background and Purpose: Patulin is a mycotoxin produced by some molds, especially Aspergillus and Penicilium, and is responsible for mycotoxicosis in animals and humans.There is still not very detailed data about the anti-cancer potency of patulin, but some reports demonstrated that it induces cellular apoptosis and toxicity. Materials and Methods: To determine the efficacy of patulin as a therapeutic strategy for cervical and colorectal cancers, we investigated its effects on HeLa,SW-48, and MRC-5 cell lines...
March 2017: Advances in Medical Mycology (Iran)
Stoimir Kolarević, Dragana Milovanović, Margareta Kračun-Kolarević, Jovana Kostić, Karolina Sunjog, Rajko Martinović, Jelena Đorđević, Irena Novaković, Dušan Sladić, Branka Vuković-Gačić
In this study, mutagenic and genotoxic potential of anti-tumor compounds avarol, avarone, and its derivatives 3'-methoxyavarone, 4'-(methylamino)avarone and 3'-(methylamino)avarone was evaluated and compared to cytostatics commonly used in chemotherapy (5-fluorouracil, etoposid, and cisplatin). Mutagenic potential of selected hydroquinone and quinones was assessed in prokaryotic model by the SOS/umuC assay in Salmonella typhimurium TA1535/pSK1002. Genotoxic potential was also assessed in eukaryotic models using comet assay in human fetal lung cell line (MRC-5), human adenocarcinoma epithelial cell line (A549), and in human peripheral blood cells (HPBC)...
January 4, 2018: Drug and Chemical Toxicology
Jingwen Zhang, Anaïs Pitto-Barry, Lijun Shang, Nicolas P E Barry
We report an evaluation of the cytotoxicity of a series of electron-deficient (16-electron) half-sandwich precious metal complexes of ruthenium, osmium and iridium ([Os/Ru(η6-p-cymene)(1,2-dicarba-closo-dodecarborane-1,2-dithiolato)] (1/2), [Ir(η5-pentamethylcyclopentadiene)(1,2-dicarba-closo-dodecarborane-1,2-dithiolato)] (3), [Os/Ru(η6-p-cymene)(benzene-1,2-dithiolato)] (4/5) and [Ir(η5-pentamethylcyclopentadiene)(benzene-1,2-dithiolato)] (6)) towards RAW 264.7 murine macrophages and MRC-5 fibroblast cells...
November 2017: Royal Society Open Science
Agnieszka Szymanska-Michalak, Dariusz Wawrzyniak, Grzegorz Framski, Jacek Stawinski, Jan Barciszewski, Adam Kraszewski
We have designed and synthesized new 5-fluoro-2'-deoxyuridine 5'-phosphate pronucleotides which can function as potential agents against the glioblastoma multiforme tumor. Their anti-malignant potency has been tested against T98G, U-118 MG, U-87 MG gliomas, HeLa, and Caco-2 cancer cell lines, using MRC-5 healthy cells as a reference. Five of the sixteen compounds (4c, 4f-i) exhibited significant anticancer potency and high selectivity indices (SI 12-66). It is likely that these zwitterionic pronucleotides may function in a similar manner to zwitterionic phospholipids, by inducing cell membrane charge disorder, making the cell permeable to bioactive agents...
December 21, 2017: European Journal of Medicinal Chemistry
Bojana Vasilijević, Jelena Knežević-Vukčević, Dragana Mitić-Ćulafić, Dejan Orčić, Marina Francišković, Tatjana Srdic-Rajic, Marina Jovanović, Biljana Nikolić
Chemical composition and antioxidative, genotoxic and cytotoxic potential of essential oil (EO) and post-distillation waste (PDW) of Serbian Juniperus communis L. var. saxatilis Pall. was studied in human lung carcinoma (A549) and normal lung fibroblast (MRC-5) cells. GC-MS analysis identified 93.95% of total EO content and determined α-pinen as a dominant component (23.61%). LC-MS/MS analysis of PDW pointed at rutin (12.2 mg g-1) and quinic acid (11.1 mg g-1) as the most abundant. Antioxidativity of PDW was strong in DPPH (IC50 was 5...
December 26, 2017: Food and Chemical Toxicology
Sameera R Samarakoon, Meran K Ediriweera, Chukwumaobim Daniel Uzochukwuwulu Nwokwu, Chamara Janaka Bandara, Kamani H Tennekoon, Poorna Piyathilaka, D Nedra Karunaratne, Veranja Karunaratne
Lung cancer is the major cause of cancer death among men. A number of natural compounds have proven to be useful in the treatmet of lung cancer. This study was aimed to determine cytotoxic and apoptotoic effects of a natural compound 3-O-α-L-arabinosyl oleanolic acid (3-O-L-AO) isolated from Schumacheria castaneifolia in non-small-cell lung cancer (NCI-H292) cells. Cytotoxic effects of 3-O-L-AO were determined by Sulforhodamine B (SRB) assay and apoptotic effects were tested by evaluating (a) apoptotsis related morphological changes, (b) caspase 3/7 activity, and (c) expression of Bax, p53, and survivin genes...
2017: BioMed Research International
Christin Müller, Falk W Schulte, Kerstin Lange-Grünweller, Wiebke Obermann, Ramakanth Madhugiri, Stephan Pleschka, John Ziebuhr, Roland K Hartmann, Arnold Grünweller
Coronaviruses (CoV) and picornaviruses are plus-strand RNA viruses that use 5' cap-dependent and cap-independent strategies, respectively, for viral mRNA translation initiation. Here, we analyzed the effects of the plant compound silvestrol, a specific inhibitor of the DEAD-box RNA helicase eIF4A, on viral translation using a dual luciferase assay and virus-infected primary cells. Silvestrol was recently shown to have potent antiviral activity in Ebola virus-infected human macrophages. We found that silvestrol is also a potent inhibitor of cap-dependent viral mRNA translation in CoV-infected human embryonic lung fibroblast (MRC-5) cells...
December 16, 2017: Antiviral Research
Marcela Šafratová, Anna Hošťálková, Daniela Hulcová, Kateřina Breiterová, Veronika Hrabcová, Marta Machado, Diana Fontinha, Miguel Prudêncio, Jiří Kuneš, Jakub Chlebek, Daniel Jun, Martina Hrabinová, Lucie Nováková, Radim Havelek, Martina Seifrtová, Lubomír Opletal, Lucie Cahlíková
Fifteen Amaryllidaceae alkaloids (1-15) of various structural types were isolated by standard chromatographic methods from fresh bulbs of Narcissus poeticus cv. Pink Parasol. The chemical structures were elucidated by MS, and 1D and 2D NMR spectroscopic analyses, and by comparison with literature data. Narcipavline (5) and narcikachnine (6) are reported here for the first time. In their structure are combined two basic structural types of Amaryllidaceae alkaloids (galanthamine- and galanthindole-structural types), which represent a new structural type of these compounds...
December 14, 2017: Archives of Pharmacal Research
Cheng Cui, Huijun Lu, Qi Hui, Shiying Lu, Yan Liu, Waqas Ahmad, Yang Wang, Pan Hu, Xilin Liu, Yan Cai, Lingjiu Liu, Xiang Zhang, Ke Zhao, Yansong Li, Honglin Ren, Ningyi Jin, Zengshan Liu
Benzylpenicilloic acid (BPNLA) is a major cleavage product of benzylpenicillin G (BP) generated after heating treatment. It is found in animal derived products from the unstable residual penicillin. Previous studies have only reported the allergic reaction caused by BPNLA, but not described its toxicity. In this study, the toxicity of BPNLA was evaluated to report the potential public health risk posed by animal derived products using in vivo and in vitro models, including the acute toxicity assays, cytotoxicity assays, apoptosis assays and cell cycle progression assay...
December 9, 2017: Food and Chemical Toxicology
Kine Ø Hansen, Johan Isaksson, Annette Bayer, Jostein A Johansen, Jeanette H Andersen, Espen Hansen
Bryozoans belonging to the Flustridae family have proven to be a rich source of structurally unique secondary metabolites. As part of our continuing search for bioactive secondary metabolites from Arctic marine invertebrates, the organic extract of Securiflustra securifrons was examined. This resulted in the isolation of three new halogenated, hexacyclic indole-imidazole alkaloids, securamines H-J (1-3), together with the previously reported compounds securamines C (4) and E (5). The structures of the new compounds were elucidated by spectroscopic methods including 1D and 2D NMR and analysis of HRMS data...
December 22, 2017: Journal of Natural Products
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