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https://www.readbyqxmd.com/read/28448872/curcumin-attenuates-lipopolysaccharide-d-galactosamine-induced-acute-liver-injury-by-activating-nrf2-nuclear-translocation-and-inhibiting-nf-kb-activation
#1
Yi-Lian Xie, Jin-Guo Chu, Xiao-Min Jian, Jin-Zhong Dong, Li-Ping Wang, Guo-Xiang Li, Nai-Bin Yang
Curcumin, a polyphenol in curry spice isolated from the rhizome of turmeric, has been reported to possess versatile biological properties including anti-inflammatory, anti-oxidant, antifibrotic, and anticancer activities. In this study, the hepatoprotective effect of curcumin was investigated in lipopolysaccharide (LPS)/d-galactosamine (d-GalN)-induced acute liver injury (ALI) in rats. Experimental ALI was induced with an intraperitoneal (ip) injection of sterile 0.9% sodium chloride (NaCl) solution containing 8μg LPS and 800mg/kg d-GalN...
April 24, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28448438/antiplatelet-activity-of-a-newly-synthesized-novel-ruthenium-ii-a-potential-role-for-akt-jnk-signaling
#2
Themmila Khamrang, Kuo-Chen Hung, Chih-Hsuan Hsia, Cheng-Ying Hsieh, Marappan Velusamy, Thanasekaran Jayakumar, Joen-Rong Sheu
In oncotherapy, ruthenium complexes are considered as potential alternatives for platinum compounds, and have been proved as promising anticancer drugs with high efficacy and lesser side effects. Platelet activation plays a major role in cancer metastasis and progression. Hence, this study explored the effect of a newly synthesized ruthenium complex, [Ru(η⁶-cymene)(L)Cl]BF₄(TQ5), where L = 4-phenyl-2-pyridin-2-yl-quinazoline), on human platelet activation. TQ5 (3-5 µM) inhibited concentration-dependent collagen-induced platelet aggregation in washed human platelets...
April 27, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28447740/calyptranthes-grandifolia-o-berg-myrtaceae-ethanolic-extract-inhibits-tnf-%C3%AE-gene-expression-and-cytokine-release-in%C3%A2-vitro
#3
Geórgia Muccillo Dexheimer, Luciana Knabben de Oliveira Becker Delving, Henrique Sulzbach de Oliveira, Vanderlei Biolchi, Márcia Inês Goettert, Adriane Pozzobon
Anti-tumor therapies based on anti-inflammatory effects have been considered in cancer treatment. Survival, proliferation and, resultantly, invasion and metastasis of tumor cells are regulated by local inflammatory mediators. Primary inflammatory cytokines, such as tumor necrosis factor (TNF), are targets for anticancer therapy. Several anti‑inflammatory agents isolated from natural products are becoming important chemopreventive and therapeutic agents for cancer. The present study aimed to investigate the expression of TNF‑α, nuclear factor‑κΒ (NF‑κΒ) and p38α mitogen-activated protein kinase (p38α) genes, associated with proliferation and inflammation in the Caco‑2 cell line treated with ethanolic and hexanic extracts of Calyptranthes grandifolia O...
March 14, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28447739/neural-precursor-cell-expressed-developmentally-downregulated-8%C3%A2-activating-enzyme-inhibitor-mln4924-sensitizes-colorectal-cancer-cells-to-oxaliplatin-by-inducing-dna-damage-g2-cell-cycle-arrest-and-apoptosis
#4
Wanwei Zheng, Zhongguang Luo, Jun Zhang, Pei Min, Wenshuai Li, Diannan Xu, Ziqiang Zhang, Panpan Xiong, Hong Liang, Jie Liu
Oxaliplatin-based chemotherapy is a primary treatment for patients with metastatic colorectal cancer (CRC); however, its efficacy is limited. Therefore, novel therapeutic agents are urgently required. MLN4924 is a first‑in‑class inhibitor of neural precursor cell expressed, developmentally downregulated 8 (NEDD8)‑activating enzyme E1, and has entered various phase‑I/II clinical trials for cancer therapy due to its significant anticancer efficacy. The aim of the present study was to examine the synergistic effect and underlying mechanisms of MLN4924 and oxaliplatin combined treatment for CRC...
March 9, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28447548/preparation-of-wormlike-polymeric-nanoparticles-coated-with-silica-for-delivery-of-methotrexate-and-evaluation-of-anticancer-activity-against-mcf7-cells
#5
Farhad Gharebaghi, Naser Dalali, Ebrahim Ahmadi, Hossein Danafar
Methotrexate is one of the most effective drugs that is commonly used in the treatment of cancer. However, its application is limited due to low solubility, high toxicity and rapid metabolism. Therefore, in the present study, worm-like polymeric nanoparticles as carrier of methotrexate were prepared using biodegradable copolymers (mPEG-PCL). The impact of nanoparticles' geometry on the loading, delivery and drug's anti-cancer activity was investigated. The di-block copolymer mPEG-PCL was being synthesized by a ring opening polymerization of ɛ-caprolactone in the presence of mPEG as the initiator and Sn(oct)2 as the catalyst...
April 2017: Journal of Biomaterials Applications
https://www.readbyqxmd.com/read/28447479/autotaxin-inhibitors-a-patent-review-2012-2016
#6
Aikaterini Nikolaou, Maroula G Kokotou, Dimitris Limnios, Anastasia Psarra, George Kokotos
Autotaxin (ATX) is a secreted enzyme that hydrolyzes lysophosphatidylcholine to lysophosphatidic acid (LPA) and choline. The ATX/LPA axis has received increasing interest in recent years because both the enzyme ATX and the bioactive lipid LPA are involved in various pathological conditions such as tumor progression and metastasis, fibrotic diseases, autoimmune diseases, arthritis, chronic hepatitis, obesity and impaired glucose homeostasis. Thus, a great effort has been devoted in developing synthetic ATX inhibitors as new agents to treat various diseases including cancer and fibrotic diseases...
April 27, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28447182/co-ii-complexes-of4-3-ethoxy-2-hydroxybenzylidene-amino-n-thiazol-2-yl-benzenesulphonamide-and-4-pyridin-2-ylmethylene-amino-n-thiazol-2-tl-benzenesulfonamide-synthesis-fluorescence-properties-and-anticancer-activity
#7
Gomathi Vellaiswamy, Selvameena Ramaswamy
Two new Co(II) complexes of 4-((3-ethoxy-2-hydroxybenzylidene)amino)-N-(thiazol-2-yl)benzenesulphonamide and 4-((pyridin-2-ylmethylene)amino)-N-(thiazol-2-yl)benzene sulfonamide were synthesised. The structure of the complexes was identified by elemental analysis, FT-IR, electronic, EI mass, Powder XRD spectra and magnetic moment. The TG and DTA patterns of the complexes were supported the structures. The fluorescence quenching of these complexes with alizarin dye were premeditated and the free energy change (∆Get) for electron transfer process was designed by Rehm-Weller equation...
April 26, 2017: Journal of Fluorescence
https://www.readbyqxmd.com/read/28446463/the-national-cancer-institute-almanac-a-comprehensive-screening-resource-for-the-detection-of-anticancer-drug-pairs-with-enhanced-therapeutic-activity
#8
Susan L Holbeck, Richard Camalier, James A Crowell, Jeevan Prasaad Govindharajulu, Melinda G Hollingshead, Lawrence W Anderson, Eric C Polley, Larry Rubinstein, Apurva K Srivastava, Deborah F Wilsker, Jerry M Collins, James H Doroshow
To date, over 100 small molecule oncology drugs have been approved by the US Food and Drug Administration.  Due to the inherent heterogeneity of tumors, these small molecules are often administered in combination to prevent emergence of resistant cell subpopulations.  Therefore, new combination strategies to overcome drug resistance in patients with advanced cancer are needed.  In this study, we performed a systematic evaluation of the therapeutic activity of over 5,000 pairs of FDA-approved cancer drugs against a panel of 60 well-characterized human tumor cell lines (NCI-60) to uncover combinations with greater than additive growth-inhibitory activity...
April 26, 2017: Cancer Research
https://www.readbyqxmd.com/read/28445526/biosynthesis-of-the-oxygenated-diterpene-nezukol-in-the-medicinal-plant-isodon-rubescens-is-catalyzed-by-a-pair-of-diterpene-synthases
#9
Kyle A Pelot, David M Hagelthorn, J Bennett Addison, Philipp Zerbe
Plants produce an immense diversity of natural products (i.e. secondary or specialized metabolites) that offer a rich source of known and potentially new pharmaceuticals and other desirable bioproducts. The Traditional Chinese Medicinal plant Isodon rubescens (Lamiaceae) contains an array of bioactive labdane-related diterpenoid natural products. Of these, the ent-kauranoid oridonin is the most prominent specialized metabolite that has been extensively studied for its potent antimicrobial and anticancer efficacy...
2017: PloS One
https://www.readbyqxmd.com/read/28445391/telomerase-inhibitory-effects-of-red-pigment-rubropunctatin-and-statin-monacolin-l-isolated-from-red-yeast-rice
#10
Baojun Xu, Qijun Wang, Changkeun Sung
In addition to the cholesterol-lowering activity of red yeast rice (RYR), its anticancer activities have been frequently reported. However, the mechanism of action of the anticancer activity of RYR is not yet fully understood. The objective of the current study was to elucidate anticancer compositions and anticancer mechanism of actions of RYR. The isolated compounds from RYR were subjected to anti-proliferation assay, apoptosis assay via flow cytometry, and telomerase inhibitory assay via telomeric repeat amplification protocol-PCR (TRAP-PCR) assay, and Western blotting assay in an in vitro cell culture system...
April 26, 2017: Genes
https://www.readbyqxmd.com/read/28445005/proteomic-based-investigations-on-the-mode-of-action-of-the-marine-anticancer-compound-rhizochalinin
#11
Sergey A Dyshlovoy, Katharina Otte, Simone Venz, Jessica Hauschild, Heike Junker, Tatyana N Makarieva, Stefan Balabanov, Winfried H Alsdorf, Ramin Madanchi, Friedemann Honecker, Carsten Bokemeyer, Valentin A Stonik, Gunhild von Amsberg
Rhizochalinin (Rhiz) is a novel marine natural sphingolipid-like compound which shows promising in vitro and in vivo activity in human castration-resistant prostate cancer (CRPC). In the present study, a global proteome screening approach was applied to investigate molecular targets and biological processes affected by Rhiz in CRPC. Bioinformatical analysis of the data predicted an anti-migratory effect of Rhiz on cancer cells. Validation of proteins involved in the cancer-associated processes, including cell migration and invasion, revealed down-regulation of specific isoforms of stathmin and LASP1, as well as up-regulation of Grp75, keratin 81, and precursor IL-1β by Rhiz...
April 26, 2017: Proteomics
https://www.readbyqxmd.com/read/28444959/controlling-and-monitoring-intracellular-delivery-of-anticancer-polymer-nanomedicines
#12
REVIEW
Claudia Battistella, Harm-Anton Klok
Polymer nanomedicines are very attractive to improve the delivery of chemotherapeutics. Polymer conjugates and other polymer-based nanocarriers allow to increase plasma half-life and drug bioavailability and can also be guided toward tumors using passive and active targeting strategies. Since many chemotherapeutics act on targets that are located in well-defined subcellular compartments, other important factors that contribute to an efficient therapy include cellular internalization and subsequent intracellular trafficking of the polymer nanomedicines and/or its payload to the appropriate organelle in the cytoplasm...
April 26, 2017: Macromolecular Bioscience
https://www.readbyqxmd.com/read/28444898/an-isoquinolin-1-2h-imine-derivative-induces-cell-death-via-generation-of-reactive-oxygen-species-and-activation-of-jnk-in-human-a549-cancer-cells
#13
Jing Liu, Tongyang Liu, Hanchuan Mou, Shuting Jia, Chao Huang, Shengjiao Yan, Jun Lin, Ying Luo, Jihong Zhang
BACKGROUND: Compound11-benzoyl-10-chloro-7,9-difluoro-6-imino-2,3,4,6-tetrahydro-1H-pyrimido[1,2-b]isoquinoline-8-carbonitrile (HC6h) is a novel polyhalo 1,3-diazaheterocycle fused isoquinolin-1(2H)-imines derivative, which displays good anticancer activity and low toxicity in vivo. However, the underlying anticancer mechanisms have not previously been identified. METHODS: The proliferation of A549 was assessed by MTT assay. The reactive oxygen species (ROS) level was assessed in A549 with a H2 DCFDA probe...
April 26, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28444820/casticin-impairs-cell-migration-and-invasion-of-mouse-melanoma-b16f10-cells-via-pi3k-akt-and-nf-%C3%AE%C2%BAb-signaling-pathways
#14
Yung-Luen Shih, Hsiao-Min Chou, Hsiu-Chen Chou, Hsu-Feng Lu, Yung-Lin Chu, Hung-Sheng Shang, Jing-Gung Chung
Casticin, a polymethoxyflavone, is one of the major active components obtained from Fructus viticis, which have been shown to have anticancer activities including induce cell apoptosis in human cancer cells. The aim of this study was to investigate the molecular mechanisms by which casticin inhibits cell migration and invasion of mouse melanoma B16F10 cells. Cell viability was examined by MTT assay and the results indicated that casticin decreased the total percentages of viable cells in dose-dependent manners...
April 26, 2017: Environmental Toxicology
https://www.readbyqxmd.com/read/28444624/targeting-ntrk-fusion-in-non-small-cell-lung-cancer-rationale-and-clinical-evidence
#15
REVIEW
Biagio Ricciuti, Marta Brambilla, Giulio Metro, Sara Baglivo, Roberta Matocci, Matteo Pirro, Rita Chiari
In the era of personalized medicine, the identification of targetable genetic alterations represented a major step forward in anticancer therapy. NTRK rearrangements represent the molecular driver of a subset of solid tumors, including 3% of non-small-cell lung cancers (NSCLCs). Preliminary data indicate that molecularly selected NSCLC patients harboring NTRK fusions derive an unprecedented clinical benefit from Trk-directed targeted therapies. The aim of this review is to describe the molecular biology of NTRK signaling pathway and to summarize the preclinical data on novel Trk inhibitors, touching upon the clinical development of these inhibitors for the treatment of advanced NSCLC, which have already shown encouraging anticancer activity and acceptable safety profile in early phase I clinical trials...
June 2017: Medical Oncology
https://www.readbyqxmd.com/read/28443665/octakis-2-pyridyl-porphyrazine-and-its-neutral-metal-derivatives-uv-visible-spectral-electrochemical-and-photoactivity-studies
#16
Fabiola Sciscione, Lei Cong, Maria Pia Donzello, Elisa Viola, Claudio Ercolani, Karl M Kadish
Tetrapyrrolic porphyrazine macrocycles with externally appended 2-pyridyl rings were synthesized and characterized as to their spectroscopic, electrochemical, and photophysical properties. The investigated compounds are represented as [Py8PzH2], the unmetalated octakis(2-pyridyl)porphyrazine, and the metal complexes [Py8PzM], where M is Mg(II)(H2O), Cu(II), Zn(II), or Co(II). The spectroscopic properties and the electrochemical behavior of these compounds were examined in solution of polar (pyridine, dimethyl sulfoxide, and dimethylformamide) and nondonor solvents (CHCl3, CH2Cl2), and the data were compared with those obtained from earlier studies on the related tetrapyrazinoporphyrazines, [Py8TPyzPzM], and the tetraquinoxalinoporphyrazines, [Py8QxPzM], also bearing externally 2-pyridyl rings, and characterized by a more extended central π-conjugated macrocyclic framework...
April 26, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28443659/new-class-of-half-sandwich-ruthenium-ii-arene-complexes-bearing-the-water-soluble-cap-ligand-as-an-in-vitro-anticancer-agent
#17
Antonella Guerriero, Werner Oberhauser, Tina Riedel, Maurizio Peruzzini, Paul J Dyson, Luca Gonsalvi
Ruthenium(II) arene complexes of 1,4,7-triaza-9-phosphatricyclo[5.3.2.1]tridecane (CAP) were obtained. Cytotoxicity studies against cancer cell lines reveal higher activity than the corresponding PTA analogues and, in comparison to the effects on noncancerous cells, the complexes are endowed with a reasonable degree of cancer cell selectivity.
April 26, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28443521/synthesis-anticancer-screening-and-molecular-docking-studies-of-new-heterocycles-with-trimethoxyphenyl-scaffold-as-combretastatin-analogues
#18
Korany A Ali, Naglaa A Abdel Hafez, Mohamed A Elsayed, Manal M Elshahawi, Salwa M El-Hallouty, Abd El-Galil E Amr
In this study, synthesis, molecular docking and anticancer screening of new series of substituted heterocycles with trimethoxy phenyl scaffold as Combretastatin analogues were described. Substituted pyridines were synthesized via reaction of (E)-3-(dimethylamino)-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one (2)with active methylene reagents. Substituted pyrimidines were prepared by the reaction of the enaminone (2) with heterocyclic amines and 6-amino thiouracil. Furthermore, a series of pyrazoles substituted with trimethoxyphenyl scaffold were prepared by reaction of the enaminone 2, with selected examples of hydrazonoyl halides...
April 24, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28443517/1-3-4-oxadiazoles-as-telomerase-inhibitor-potential-anticancer-agents
#19
Shalini Bajaj, Partha Pratim Roy, Jagadish Singh
Cancer is a rapidly growing disease of current era which poses a major life threaten situation to human beings. Continuous research is going on in the direction to develop effective molecules for the treatment of the cancer. These efforts include searching of more active heterocyclic compounds possessing potential anti-cancer activity. The 1,3,4-Oxadiazole scaffold is a five member heterocyclic ring having versatile activities and created interest for synthetic organic and medicinal chemists for the designing of novel compounds having anti-cancer activity...
April 24, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28443507/synthesis-and-biological-activity-of-unnatural-enediynes
#20
Roberto Romeo, Salvatore V Giofrè, Maria A Chiacchio
The first reports of the natural enediyne anticancer antibiotics date back to the late 1980s; since then, a great deal of interest has been devoted to the chemistry, biology and potential medical applications of this family of compounds. The biological activity of enediynes is linked to the presence of a highly unsaturated hex-1-ene- 1,5-diyne system. The thermally induced transformation of this unit into a benzene  diradical (the Bergman cycloaromatization) is the key step of the antitumor properties of such compounds: 1,4-diaryl radicals are able to abstract H-atoms from the deoxyribose backbone of DNA, thus leading to DNA strand cleavage and ultimately cell death...
April 24, 2017: Current Medicinal Chemistry
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