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https://www.readbyqxmd.com/read/28437720/determination-of-a-novel-anticancer-ampk-activator-hernandezine-in-rat-plasma-and-tissues-with-a-validated-uhplc-ms-ms-method-application-to-pharmacokinetics-and-tissue-distribution-study
#1
Yang Song, Zhibin Wang, Baozhen Zhang, Yujia Zhang, Weipeng Zhang, Chunjuan Yang, Fanhao Meng, Xuesong Feng
Hernandezine, a novel anticancer AMPK activator, is a major active constituent of Thalictrum Ranunculaceae. A simple, specific and sensitive liquid chromatography tandem mass spectrometry (LC-MS/MS) method has been developed and validated for the quantification of hernandezine in rat plasma and tissues after intravenous administration. Sample preparation was carried out through a protein-precipitation extraction with acetonitrile using tetrandrine as internal standard (IS). The chromatographic separation was achieved by using an Agilent ZORBAX Eclipse Plus C18 column with a mobile phase of acetonitrile and water (containing 10mM ammonium acetate) in an isocratic elution way...
April 8, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28437090/improved-photodynamic-therapy-efficacy-of-protoporphyrin-ix-loaded-polymeric-micelles-using-erlotinib-pretreatment
#2
Lesan Yan, Joann Miller, Min Yuan, Jessica F Liu, Theresa M Busch, Andrew Tsourkas, Zhiliang Cheng
Photodynamic therapy (PDT) has attracted widespread attention in recent years as a non-invasive and highly selective approach for cancer treatment. We have previously reported a significant increase in the 90-day complete response rate when tumor-bearing mice are treated with the epidermal growth factor receptor (EGFR) inhibitor erlotinib prior to PDT with the photosensitizer benzoporphyrin-derivative monoacid ring A (BPD-MA) compared to treatment with PDT alone. To further explore this strategy for anticancer therapy and clinical practice, we tested whether pre-treatment with erlotinib also exhibited a synergistic therapeutic effect with a nanocarrier containing the clinically relevant photosensitizer protoporphyrin IX (PpIX)...
April 24, 2017: Biomacromolecules
https://www.readbyqxmd.com/read/28437008/effects-from-metal-ion-in-tumor-endothelial-marker-8-and-anthrax-protective-antigen-biolayer-interferometry-experiment-and-molecular-dynamics-simulation-study
#3
Zhe Jia, Christine Ackroyd, Tingting Han, Vibhor Agrawal, Yinling Liu, Kenneth Christensen, Brian Dominy
One of the anthrax receptors, tumor endothelial marker 8 (TEM8), is reported to be a potential anticancer target due to its over-expression during tumor angiogenesis. To extend our BioLayer Interferometry study in PA-TEM8 binding, we present a computational approach to reveal the role of an integral metal ion on receptor structure and binding thermodynamics. We estimated the interaction energy between PA and TEM8 using computer simulation. Consistent with experimental study, computational results indicate the metal ion in TEM8 contributes significantly to the binding affinity, and PA-TEM8 binding is more favorable in the presence of Mg(2+) than Ca(2+) ...
June 5, 2017: Journal of Computational Chemistry
https://www.readbyqxmd.com/read/28436718/design-of-a-novel-curcumin-soybean-phosphatidylcholine-complex-based-targeted-drug-delivery-systems
#4
Jiajiang Xie, Yanxiu Li, Liang Song, Zhou Pan, Shefang Ye, Zhenqing Hou
Recently, the global trend in the field of nanomedicine has been toward the design of combination of nature active constituents and phospholipid (PC) to form a therapeutic drug-phospholipid complex. As a particular amphiphilic molecular complex, it can be a unique bridge of traditional dosage-form and novel drug delivery system. In thisarticle, on the basis of drug-phospholipid complex technique and self-assembly technique, we chose a pharmacologically safe and low toxic drug curcumin (CUR) to increase drug-loading ability, achieve controlled/sustained drug release and improve anticancer activity...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28436311/role-of-6-mercaptopurine-in-the-potential-therapeutic-targets-dna-base-pairs-and-g-quadruplex-dna-insights-from-quantum-chemical-and-molecular-dynamics-simulations
#5
R Radhika, R Shankar, S Vijayakumar, P Kolandaivel
The theoretical studies on DNA with the anticancer drug 6-Mercaptopurine (6-MP) are investigated using theoretical methods to shed light on drug designing. Among the DNA base pairs considered, 6-MP is stacked with GC with the highest interaction energy of -46.19 kcal/mol. Structural parameters revealed that structure of the DNA base pairs is deviated from the planarity of the equilibrium position due to the formation of hydrogen bonds and stacking interactions with 6-MP. These deviations are verified through the systematic comparison between X-H bond contraction and elongation and the associated blue shift and red shift values by both NBO analysis and vibrational analysis...
April 24, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28436164/synthesis-and-sar-study-of-novel-anticancer-protoflavone-derivatives-investigation-of-cytotoxicity-and-interaction-with-the-abcb1-and-abcg2-multidrug-efflux-transporters
#6
Balázs Dankó, Szilárd Tóth, Ana Martins, Vágvölgyi Máté, Norbert Kúsz, Joseph Molnár, Fang-Rong Chang, Yang-Chang Wu, Gergely Szakács, Attila Hunyadi
There is a constant need for new therapies against multidrug resistant (MDR) cancer. Natural compounds represent a promising class of novel anticancer agents. Recently, we have shown that protoflavones display activity in multidrug resistant cancer cell lines overexpressing the drug efflux pump P-glycoprotein. In the present study, 52 protoflavones, including 22 new derivatives were synthesized and tested against a panel of sensitive parental cells and their MDR derivatives obtained by transfection with the human ABCB1 or ABCG2 genes, or by adaptation to chemotherapeutics...
April 23, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28435453/sirna-delivery-with-pegylated-graphene-oxide-nanosheets-for-combined-photothermal-and-genetherapy-for-pancreatic-cancer
#7
Feng Yin, Kuan Hu, Yangzi Chen, Mengying Yu, Dongyuan Wang, Qianqian Wang, Ken-Tye Yong, Fei Lu, Yongye Liang, Zigang Li
Since the successful exfoliation of graphene from graphite in 2004, graphene and graphene oxide (GO) have been considered the most promising two-dimensional (2D) nanomaterials with distinguished physical and chemical characteristics and have attracted great attention in many different fields. Graphene oxide is well-known for its distinct physiochemical properties and shows only minimal cytotoxicity compared to carbon nanotubes. Until now, only limited efforts have been invested in utilizing GO for gene therapy in pancreatic cancer treatments...
2017: Theranostics
https://www.readbyqxmd.com/read/28435434/study-of-the-cytotoxic-effects-of-2-5-diaziridinyl-3-6-dimethyl-1-4-benzoquinone-medzq-in-mouse-hepatoma-cells
#8
Rasa Jarasiene-Burinskaja, Milda Alksne, Violeta Bartuskiene, Violeta Voisniene, Jaroslav Burinskij, Narimantas Cenas, Virginija Bukelskiene
A number of quinones have been shown to be efficient anticancer agents. However, some mechanisms of their action, in particular cell signaling are not well understood. The aim of this study was to partly fill this gap by characterizing the mode of cytotoxicity of 2,5-diaziridinyl-3,6-dimethyl-1,4-benzoquinone (MeDZQ) in malignant mouse hepatoma cells (MH-22A) with regard to the expression and activation of main molecules in MAPK cell signaling pathway. The study revealed unequal roles of MAP kinases in MeDZQ-induced cell death: the compound did not induce significant changes in ERK expression or its phosphorylation; JNK appeared to be responsible for cell survival, however, p38 kinase was shown to be involved in cell death...
2017: EXCLI journal
https://www.readbyqxmd.com/read/28435351/in-vitro-antifungal-activity-of-1-n-2-methoxybenzyl-1-10-phenanthrolinium-bromide-against-candida-albicans-and-its-effects-on-membrane-integrity
#9
Setiawati Setiawati, Titik Nuryastuti, Ngatidjan Ngatidjan, Mustofa Mustofa, Jumina Jumina, Dhina Fitriastuti
Metal-based drugs, such as 1,10-phenanthroline, have demonstrated anticancer, antifungal and antiplasmodium activities. One of the 1,10-phenanthroline derivatives compounds (1)-N-2-methoxybenzyl-1,10-phenanthrolinium bromide (FEN), which has been demonstrated an inhibitory effect on the growth of Candida spp. This study aimed to explore the in vitro antifungal activity of FEN and its effect on the membrane integrity of Candida albicans. The minimum inhibitory concentration (MIC) and the minimum fungicidal concentration (MFC) of FEN against planktonic C...
March 2017: Mycobiology
https://www.readbyqxmd.com/read/28435333/new-insights-into-therapeutic-activity-and-anticancer-properties-of-curcumin
#10
REVIEW
Abir Kumar Panda, Dwaipayan Chakraborty, Irene Sarkar, Tila Khan, Gaurisankar Sa
Natural compounds obtained from plants are capable of garnering considerable attention from the scientific community, primarily due to their ability to check and prevent the onset and progress of cancer. These natural compounds are primarily used due to their nontoxic nature and the fewer side effects they cause compared to chemotherapeutic drugs. Furthermore, such natural products perform even better when given as an adjuvant along with traditional chemotherapeutic drugs, thereby enhancing the potential of chemotherapeutics and simultaneously reducing their undesired side effects...
2017: Journal of Experimental Pharmacology
https://www.readbyqxmd.com/read/28435256/doxorubicin-loaded-cell-derived-nanovesicles-an-alternative-targeted-approach-for-anti-tumor-therapy
#11
Wei Jiang Goh, Choon Keong Lee, Shui Zou, Esther Cy Woon, Bertrand Czarny, Giorgia Pastorin
Cell-derived nanovesicles (CDNs) are an emerging class of biological drug delivery systems (DDS) that retain the characteristics of the cells they were derived from, without the need for further surface functionalization. CDNs are also biocompatible, being derived from natural sources and also take advantage of the enhanced permeability and retention effect due to their nanodimensions. Furthermore, CDNs derived from monocytes were shown to have an in vivo targeting effect, accumulating at the tumor site in a previous study conducted in a mouse tumor model...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28435252/polyphenol-nanoformulations-for-cancer-therapy-experimental-evidence-and-clinical-perspective
#12
REVIEW
Yasamin Davatgaran-Taghipour, Salar Masoomzadeh, Mohammad Hosein Farzaei, Roodabeh Bahramsoltani, Zahra Karimi-Soureh, Roja Rahimi, Mohammad Abdollahi
Cancer is defined as the abnormal cell growth that can cause life-threatening malignancies with high financial costs for patients as well as the health care system. Natural polyphenols have long been used for the prevention and treatment of several disorders due to their antioxidant, anti-inflammatory, cytotoxic, antineoplastic, and immunomodulatory effects discussed in the literature; thus, these phytochemicals are potentially able to act as chemopreventive and chemotherapeutic agents in different types of cancer...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28435247/delivery-of-curcumin-by-directed-self-assembled-micelles-enhances-therapeutic-treatment-of-non-small-cell-lung-cancer
#13
Wen-Ting Zhu, Sheng-Yao Liu, Lei Wu, Hua-Li Xu, Jun Wang, Guo-Xin Ni, Qing-Bing Zeng
BACKGROUND: It has been widely reported that curcumin (CUR) exhibits anticancer activity and triggers the apoptosis of human A549 non-small-cell lung cancer (NSCLC) cells. However, its application is limited owing to its poor solubility and bioavailability. Therefore, there is an urgent need to develop a new CUR formulation with higher water solubility and better biocompatibility for clinical application in the future. MATERIALS AND METHODS: In this study, CUR-loaded methoxy polyethylene glycol-polylactide (CUR/mPEG-PLA) polymeric micelles were prepared by a thin-film hydration method...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28435038/a-convergent-synthesis-of-novel-alkyne-azide-cycloaddition-congeners-of-betulinic-acid-as-potent-cytotoxic-agent
#14
Nisar A Dangroo, Jasvinder Singh, Santosh K Rath, Nidhi Gupta, Arem Qayum, Shashank Singh, Payare L Sangwan
In an endeavour to develop potent anti-tumor agents from betulinic acid (BA), a series of C-28 derived 1,2,3-triazolyl derivatives were designed and synthesized by employing Cu(I) catalyzed Huisgen 1,3-dipolar cycloaddition reaction. All the derivatives were evaluated for cytotoxic activity by MTT assay against five different human cancer cell lines: lung (A549), colon (HCT116), prostate (PC3), pancreatic (MIA PaCa-2) and breast (T47D). The data revealed that compounds 11c, 11d, 11g, 11h and 13a possess most promising cytotoxic potential...
April 20, 2017: Steroids
https://www.readbyqxmd.com/read/28433938/imaging-lysosomal-highly-reactive-oxygen-species-and-lighting-up-cancer-cells-and-tumors-enabled-by-a-si-rhodamine-based-near-infrared-fluorescent-probe
#15
Hongxing Zhang, Jing Liu, Chenlu Liu, Pengcheng Yu, Minjia Sun, Xiaohan Yan, Jian-Ping Guo, Wei Guo
Lysosomes have recently been regarded as the attractive pharmacological targets for selectively killing of cancer cells via lysosomal cell death (LCD) pathway that is closely associated with reactive oxygen species (ROS). However, the details on the ROS-induced LCD of cancer cells are still poorly understood, partially due to the absence of a lysosome-targetable, robust, and biocompatible imaging tool for ROS. In this work, we brought forward a Si-rhodamine-based fluorescent probe, named PSiR, which could selectively and sensitively image the pathologically more relavent highly reactive oxygen species (hROS: HClO, HO, and ONOO(-)) in lysosomes of cancer cells...
April 14, 2017: Biomaterials
https://www.readbyqxmd.com/read/28433834/antimicrobial-and-anticancer-photodynamic-activity-of-a-phthalocyanine-photosensitizer-with-n-methyl-morpholiniumethoxy-substituents-in-non-peripheral-positions
#16
Jolanta Dlugaszewska, Wojciech Szczolko, Tomasz Koczorowski, Paulina Skupin-Mrugalska, Anna Teubert, Krystyna Konopka, Malgorzata Kucinska, Marek Murias, Nejat Düzgüneş, Jadwiga Mielcarek, Tomasz Goslinski
Photodynamic therapy involves the use of a photosensitizer that is irradiated with visible light in the presence of oxygen, resulting in the formation of reactive oxygen species. A novel phthalocyanine derivative, the quaternary iodide salt of magnesium(II) phthalocyanine with N-methyl morpholiniumethoxy substituents, was synthesized, and characterized. The techniques used included mass spectrometry (MALDI TOF), UV-vis, NMR spectroscopy, and photocytotoxicity against bacteria, fungi and cancer cells. The phthalocyanine derivative possessed typical characteristics of compounds of the phthalocyanine family but the effect of quaternization was observed on the optical properties, especially in terms of absorption efficiency...
April 8, 2017: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/28433679/part-i-design-synthesis-and-biological-evaluation-of-novel-pyrazole-benzimidazole-conjugates-as-checkpoint-kinase-2-chk2-inhibitors-with-studying-their-activities-alone-and-in-combination-with-genotoxic-drugs
#17
Shadia A Galal, Ahmed S Abdelsamie, Samia A Shouman, Yasmin M Attia, Hamed I Ali, Ashraf Tabll, Reem El-Shenawy, Yasmine S El Abd, Mamdouh M Ali, Abeer E Mahmoud, Abeer H Abdel-Halim, Amal A Fyiad, Adel S Girgis, Hoda I El-Diwani
Activated checkpoint kinase 2 (Chk2) is a tumor suppressor as one of the main enzymes that affect the cell cycle. 2-Biarylbenzimidazoles are potent selective class of Chk2 inhibitors; the structure-based design was applied to synthesize a new series of this class with replacing the lateral aryl group by substituted pyrazoles. Ten pyrazole-benzimidazole conjugates from the best fifty candidates according to docking programs have been subjected to chemical synthesis in this study. The activities of the conjugates 5-14 as checkpoint kinase inhibitors and as antitumor alone and in combination with genotoxic drugs were evaluated...
April 14, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28433634/dual-sphingosine-kinase-inhibitor-ski-ii-enhances-sensitivity-to-5-fluorouracil-in-hepatocellular-carcinoma-cells-via-suppression-of-osteopontin-and-fak-igf-1r-signalling
#18
Petra Grbčić, Ivana Tomljanović, Marko Klobučar, Sandra Kraljević Pavelić, Ksenija Lučin, Mirela Sedić
Hepatocellular carcinoma (HCC) represents the third leading cause of cancer-related deaths globally. Although 5-Fluorouracil (5-FU) is used as the first choice treatment for advanced HCC, it exerts poor efficacy and is associated with acquired and intrinsic resistance. Sphingosine kinases (Sphk) 1 and 2 play tumour-promoting roles in different cancer types including HCC and thus represent promising pharmacological targets. In the present study, we have investigated for the first time the anticancer efficacy and underlying molecular mechanisms of combined administration of 5-FU and dual Sphk1/Sphk2 inhibitor SKI-II (4-[[4-(4-chlorophenyl)-1,3-thiazol-2-yl]amino]phenol) in HepG2 hepatocellular carcinoma cells...
April 19, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28433158/characterization-of-a-sulfated-galactoglucan-from-antrodia-cinnamomea-and-its-anticancer-mechanism-via-tgf%C3%AE-fak-slug-axis-suppression
#19
Mei-Kuang Lu, Tung-Yi Lin, Chun-Hao Hu, Chi-Hsein Chao, Chia-Chuan Chang, Hsien-Yeh Hsu
A sulfated 1,4-β-d-galactoglucan (B86-III) with 1,6-branches was isolated and identified from Antrodia cinnamomea. The repeating unit of B86-III was proposed based on one-dimensional 1D ((1)H, (13)C and DEPT-135) and 2D (DQF-COSY, TOCSY, HSQC and HMBC) NMR spectra. The conformation of the sugars was hypothesized to be a rare boat form instead of a (4)C1 chair form. The sulfate substitutions were suggested to be on the C-2 and C-3 positions, resulting in the following structure: B86-III inhibited the viability of H1975 lung cancer cells via cell apoptosis, including the activation of caspase 3 and PARP...
July 1, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28433142/enhanced-degradation-of-chitosan-by-applying-plasma-treatment-in-combination-with-oxidizing-agents-for-potential-use-as-an-anticancer-agent
#20
Chayanaphat Chokradjaroen, Ratana Rujiravanit, Anyarat Watthanaphanit, Sewan Theeramunkong, Nagahiro Saito, Kazuko Yamashita, Ryuichi Arakawa
Solution plasma (SP) treatment in combination with oxidizing agents, i.e., hydrogen peroxide (H2O2), potassium persulfate (K2S2O8) and sodium nitrite (NaNO2) were adopted to chitosan degradation in order to achieve fast degradation rate, low chemicals used and high yield of low-molecular-weight chitosan and chitooligosaccharide (COS). Among the studied oxidizing agents, H2O2 was found to be the best choice in terms of appreciable molecular weight reduction without major change in chemical structure of the degraded products of chitosan...
July 1, 2017: Carbohydrate Polymers
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