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https://www.readbyqxmd.com/read/28742387/vitamin-d-loaded-nanostructured-lipid-carrier-nlc-a-new-strategy-for-enhancing-efficacy-of-doxorubicin-in-breast-cancer-treatment
#1
Mehdi Sabzichi, Jamal Mohammadian, Maryam Mohammadi, Farhad Jahanfar, Ali Akbar Movassagh Pour, Hamed Hamishehkar, Alireza Ostad-Rahimi
The dangerous dose-dependent side effects of anticancer agents triggered the finding of new approaches for elevated chemotherapy efficacy. This study investigated the potential application of nanostructured lipid careers (NLCs) in increasing vitamin D3 (VitD) effectiveness in breast cancer cell (MCF-7) in concurrent administration with doxorubicin (Dox). VitD-loaded NLCs were characterized by particle size, zeta potential, Fourier transform infrared spectroscopy, and scanning electron microscope. Cytotoxicity and molecular effects of formulation were evaluated by MTT, DAPI staining, flow cytometry, and real-time quantitative PCR assays...
July 25, 2017: Nutrition and Cancer
https://www.readbyqxmd.com/read/28742327/amphiphilic-peptide-nanorods-based-on-oligo-phenylalanine-as-a-biocompatible-drug-carrier
#2
Su Jeong Song, Seulgi Lee, Kyoung-Seok Ryu, Joon Sig Choi
Peptide nanostructure has been widely explored for drug delivery systems in recent studies. Peptides possess comparatively lower cytotoxicity and are more efficient than polymeric carriers. Here, we propose a peptide nanorod system, composed of an amphiphilic oligo-peptide RH3F8 (Arg-His3-Phe8) as a drug delivery carrier. Arginine is an essential amino acid in typical cell penetration peptides, and histidine induces endo/lysosomal escape because of its proton sponge effect. Phenylalanine is introduced to provide rich hydrophobicity for stable self-assembly and drug encapsulation...
July 25, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28741926/redesigned-spider-peptide-with-improved-antimicrobial-and-anticancer-properties
#3
Sonia Troeira Henriques, Nicole Lawrence, Stephanie Chaousis, Anjaneya S Ravipati, Olivier Cheneval, Aurélie H Benfield, Alysha G Elliott, Angela Maria Kavanagh, Matthew A Cooper, Lai Yue Chan, Yen-Hua Huang, David J Craik
Gomesin, a disulfide-rich antimicrobial peptide produced by the Brazilian spider Acanthoscurria gomesiana, has been shown to be potent against Gram-negative bacteria and to possess selective anticancer properties against melanoma cells. In a recent study, a backbone cyclized analogue of gomesin was shown to be as active but more stable than its native form. In the current study, we were interested in improving the antimicrobial properties of the cyclic gomesin, understanding its selectivity towards melanoma cells and elucidating its antimicrobial and anticancer mode of action...
July 25, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28741878/anticancer-gold-n-heterocyclic-carbene-complexes-a-comparative-in-vitro-and-ex-vivo-study
#4
Angela Casini, Natalia Estrada-Ortiz, Chiara Gabbiani, Federica Guarra, Geny Groothuis, Inge de Graaf, Marina de Jager, Lorella Marchetti
A series of organometallic Au(I) N-heterocyclic carbene (NHC) complexes was synthesized and characterized on anticancer activity in four human cancer cell lines. The compounds' toxicity in healthy tissue was determined using precision cut kidney slices (PCKS) as a tool to determine the potential selectivity of the Au complexes ex vivo. All evaluated compounds presented cytotoxic activity towards the cancer cells in the nano- or low micromolar range. The mixed Au(I) NHC complex - (ter-butylethynyl)-1,3-bis-(2,6-diisopropylphenyl)-imidazol-2-ylidene gold(I), bearing an alkynyl moiety as ancillary ligand, showed high cytotoxicity in cancer cells in vitro, while being barely toxic in healthy rat kidney tissues...
July 25, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28741710/il-33-expanded-human-v%C3%AE-9v%C3%AE-2-t-cells-have-anti-lymphoma-effect-in-a-mouse-tumor-model
#5
Caroline Duault, Delphine Betous, Christine Bezombes, Stéphane Roga, Corinne Cayrol, Jean-Philippe Girard, Jean-Jacques Fournié, Mary Poupot
From several years, the anticancer effects of Vγ9 T lymphocytes make these cells good candidates for cancer immunotherapies. However, the proved efficacy of γδ Τ cell-based cancer immunotherapies in some clinical trials was minimized due to the inherent toxicity of IL-2, which is essential for the combination therapy with Phosphoantigen (PAg). Recently, we showed that IL-33, a γ chain receptor-independent cytokine, was able to induce the in vitro proliferation of PAg-activated Vγ9 T cells, which were fully functional expressing IFN-γ and TNF-α and showing in vitro anti-tumor cytotoxicity...
July 25, 2017: European Journal of Immunology
https://www.readbyqxmd.com/read/28741634/mitochondria-targeting-near-infrared-light-triggered-thermosensitive-liposomes-for-localized-photothermal-and-photodynamic-ablation-of-tumors-combined-with-chemotherapy
#6
Caixia Yue, Yuming Yang, Jie Song, Gabriel Alfranca, Chunlei Zhang, Qian Zhang, Ting Yin, Fei Pan, Jesús M de la Fuente, Daxiang Cui
Lonidamine, an anticancer drug that acts on mitochondria, has poor water solubility. Mitochondria are the primary source of cellular reactive oxygen species (ROS), which are necessary for photodynamic therapy. Hence, a mitochondria-targeting drug delivery system loaded with Lonidamine and a ROS-produced photosensitizer could improve the bioavailability of Lonidamine and maximize photodynamic therapeutic efficiency. Here we report, for the first time, new IR-780 and Lonidamine encapsulated mitochondria-targeting thermosensitive liposomes (IL-TTSL)...
July 25, 2017: Nanoscale
https://www.readbyqxmd.com/read/28741618/the-immune-contexture-in-cancer-prognosis-and-treatment
#7
REVIEW
Wolf H Fridman, Laurence Zitvogel, Catherine Sautès-Fridman, Guido Kroemer
Immunotherapy is currently the most rapidly advancing area of clinical oncology, and provides the unprecedented opportunity to effectively treat, and even cure, several previously untreatable malignancies. A growing awareness exists of the fact that the success of chemotherapy and radiotherapy, in which the patient's disease can be stabilized well beyond discontinuation of treatment (and occasionally is cured), also relies on the induction of a durable anticancer immune response. Indeed, the local immune infiltrate undergoes dynamic changes that accompany a shift from a pre-existing immune response to a therapy-induced immune response...
July 25, 2017: Nature Reviews. Clinical Oncology
https://www.readbyqxmd.com/read/28741521/hypoxia-inducible-factors-master-regulators-of-cancer-progression
#8
REVIEW
Luana Schito, Gregg L Semenza
Intratumoral hypoxia (reduced O2 availability) is a common finding in human cancer and leads to increased activity of hypoxia-inducible factors (HIFs), which regulate the expression of genes that contribute to angiogenesis, metabolic reprogramming, extracellular matrix remodeling, epithelial-mesenchymal transition, motility, invasion, metastasis, cancer stem cell maintenance, immune evasion, and resistance to chemotherapy and radiation therapy. Conventional anticancer therapies target well-oxygenated and proliferating cancer cells, whereas there are no approved therapies that target hypoxic cancer cells, despite growing clinical and experimental evidence indicating that intratumoral hypoxia is a critical microenvironmental factor driving cancer progression...
December 2016: Trends in Cancer
https://www.readbyqxmd.com/read/28741121/interaction-of-newly-platinum-ii-with-tris-2-carboxyethyl-phosphine-complex-with-dna-and-model-lipid-membrane
#9
Hanna Pruchnik, Teresa Kral, Martin Hof
Structural properties of plasmid DNA and model lipid membrane treated with newly synthesized platinum(II) complex cis-[PtCl2{P(CH2CH2COOH)3}2] (cis-DTCEP for short) were studied and compared with effects of anticancer drug cisplatin, cis-[Pt(NH3)2Cl2] (cis-DDP for short). Time Correlated Single Photon Counting Fluorescence Correlation Spectroscopy (TCSPC-FCS) was employed to study interactions between those platinum complexes and DNA. The TCSPC-FCS results suggest that bonding of cis-DTCEP derivative to DNA leads to plasmid strain realignment towards much more compact structure than in the case of cis-DDP...
July 25, 2017: Journal of Membrane Biology
https://www.readbyqxmd.com/read/28740727/structure-modeling-of-human-tyrosyl-dna-phosphodiesterase-1-and-screening-for-its-inhibitors
#10
I V Gushchina, D K Nilov, A L Zakharenko, O I Lavrik, V K Švedas
The DNA repair enzyme tyrosyl-DNA phosphodiesterase 1 (Tdp1) represents a potential molecular target for anticancer therapy. A human Tdp1 model has been constructed using the methods of quantum and molecular mechanics, taking into account the ionization states of the amino acid residues in the active site and their interactions with the substrate and competitive inhibitors. The oligonucleotide- and phosphotyrosine-binding cavities important for the inhibitor design have been identified in the enzyme's active site...
April 2017: Acta Naturae
https://www.readbyqxmd.com/read/28740549/targeted-delivery-to-tumor-associated-pericytes-via-an-affibody-with-high-affinity-for-pdgfr%C3%AE-enhances-the-in-vivo-antitumor-effects-of-human-trail
#11
Ze Tao, Hao Yang, Qiuxiao Shi, Qing Fan, Lin Wan, Xiaofeng Lu
Human tumor necrosis factor-related apoptosis-inducing ligand (hTRAIL) has exhibited superior in vitro cytotoxicity in a variety of tumor cells. However, hTRAIL showed a disappointing anticancer effect in clinical trials, although hTRAIL-based regimens were well tolerated. One important reason might be that hTRAIL was largely trapped by its decoy receptors, which are ubiquitously expressed on normal cells. Tumor-targeted delivery might improve the tumor uptake and thus enhance the antitumor effect of hTRAIL...
2017: Theranostics
https://www.readbyqxmd.com/read/28739745/reduced-expression-of-metastasis-suppressor-1-mtss1-accelerates-progression-of-human-bladder-uroepithelium-cell-carcinoma
#12
Peng DU, Shuo Wang, Xingxing Tang, Chao An, Yong Yang, Wen G Jiang
BACKGROUND: Metastasis suppressor 1 (MTSS1) is a multi-functional cytoskeletal protein. Recent research showed that MTSS1 is a potential tumor suppressor in many types of cancer cells, including kidney and bladder cancer cells. However, the clinical implication of MTSS1 in human bladder uroepithelium cell carcinoma (BUCC) and its potential in suppressing BUCC tumorigenesis remains undetermined. In the present study, the expression of MTSS1 in human BUCC tissue samples, and correlations between MTSS1 and pathological grade and stage of the tumors were examined in BUCC specimens...
August 2017: Anticancer Research
https://www.readbyqxmd.com/read/28739690/nicotine-exposure-augments-renal-toxicity-of-5-aza-cytidine-through-p66shc-prevention-by-resveratrol
#13
Istvan Arany, Samuel Hall, Amir Faisal, Mehul Dixit
BACKGROUND/AIM: We have shown that either chronic nicotine (NIC) exposure or 5-aza-cytidine (AZA) augments oxidative stress-dependent injury through stimulating p66shc in renal cells. Hence, NIC could exacerbate adverse effects of AZA while antioxidants such as resveratrol (RES) could prevent it. MATERIALS AND METHODS: Renal proximal tubule cells (NRK52E) were treated with 20 μM RES prior to 200 μM NIC plus 100 nM AZA and cell injury (LDH release) was determined...
August 2017: Anticancer Research
https://www.readbyqxmd.com/read/28739687/rational-design-of-a-potent-pan-pim-kinases-inhibitor-with-a-rhodanine-benzoimidazole-structure
#14
Yuichi Sawaguchi, Ryuta Yamazaki, Yukiko Nishiyama, Toshio Sasai, Masayuki Mae, Atsuhiro Abe, Takashi Yaegashi, Hiroyuki Nishiyama, Takeshi Matsuzaki
BACKGROUND/AIM: The serine/threonine Pim kinases are overexpressed in various types of solid carcinomas and hematological malignancies, and contribute to regulating cell-cycle progression and cell survival. The aim of this study was to discover a novel pan-Pim kinases inhibitor with potent anti-proliferative activities against cancer cell lines. MATERIALS AND METHODS: We screened a panel of small molecule compounds for their ability to inhibit Pim-1 kinase activity, and the hit compound was optimized using the docking analysis to Pim-1...
August 2017: Anticancer Research
https://www.readbyqxmd.com/read/28738876/enterolactone-has-stronger-effects-than-enterodiol-on-ovarian-cancer
#15
Huidi Liu, Jianrui Liu, Siwen Wang, Zheng Zeng, Ting Li, Yongfang Liu, Emilio Mastriani, Qing-Hai Li, Hong-Xia Bao, Yu-Jie Zhou, Xiaoyu Wang, Sijing Hu, Shan Gao, Yingying Qi, Zhihang Shen, Hongyue Wang, Miao Yu, Tingting Gao, Randal N Johnston, Shu-Lin Liu
BACKGROUND: Ovarian cancer is one of the three leading gynecological malignancies, characterized by insidious growth, highly frequent metastasis, and quick development of drug resistance. As a result, this disease has low 5-year survival rates. Estrogen receptor inhibitors were commonly used for the treatment, but only 7% to 18% of patients respond to anti-estrogen therapies. Therefore, more effective therapies to inhibit estrogen-related tumors are urgently needed. Recently, phytoestrogens, such as lignans with estrogen-like biological activities, have attracted attention for their potential effects in the prevention or treatment of estrogen-related diseases...
July 24, 2017: Journal of Ovarian Research
https://www.readbyqxmd.com/read/28738767/synthesis-and-anticancer-evaluation-of-thiazacridine-derivatives-reveals-new-selective-molecules-to-hematopoietic-neoplastic-cells
#16
Moacyr Jesus Barreto de Melo Rêgo, Wanessa Layssa Batista de Sena, Ricardo Olímpio de Moura, Iris Trindade Tenório Jacob, Thiago Ubiratan Lins E Lins, Michelly Cristiny Pereia, Maria do Carmo Alves de Lima, Marina Rocha Galdino-Pitta, Ivan da Rocha Pitta, Maira Galdino da Rocha Pitta
Cancer has become one of the leading causes of morbidity and mortality worldwide. Limitations associated with existing agents increase the need to develop more effective anticancer drugs to improve the therapeutic arsenal available. Here, we describe the synthesis, characterization, toxicity and selectivity in vitro of three novel thiazacridine derivatives (ATZD): (Z)-5-acridin-9-ylmethylene-3-(4-methyl-benzyl)-4-thioxo-thiazolidin-2-one (LPSF/AC-99), (Z)-5-acridin-9-ylmethylene-3-(4-chloro-benzyl)-4-thioxo-thiazolidin-2-one (LPSF/AC-119) and (Z)-5-acridin-9-ylmethylene-3-(3-chloro-benzyl)-4-thioxo-thiazolidin-2-one (LPSF/AC-129)...
July 24, 2017: Combinatorial Chemistry & High Throughput Screening
https://www.readbyqxmd.com/read/28738705/new-sulfurated-derivatives-of-cinnamic-acids-and-rosmaricine-as-inhibitors-of-stat3-and-nf-%C3%AE%C2%BAb-transcription-factors
#17
Elena Gabriele, Dario Brambilla, Chiara Ricci, Luca Regazzoni, Kyoko Taguchi, Nicola Ferri, Akira Asai, Anna Sparatore
A set of new sulfurated drug hybrids, mainly derived from caffeic and ferulic acids and rosmaricine, has been synthesized and their ability to inhibit both STAT3 and NF-κB transcription factors have been evaluated. Results showed that most of the new hybrid compounds were able to strongly and selectively bind to STAT3, whereas the parent drugs were devoid of this ability at the tested concentrations. Some of them were also able to inhibit the NF-κB transcriptional activity in HCT-116 cell line and inhibited HCT-116 cell proliferation in vitro with IC50 in micromolar range, thus suggesting a potential anticancer activity...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28738522/combination-of-nrp1-mediated-irgd-with-5-fluorouracil-suppresses-proliferation-migration-and-invasion-of-gastric-cancer-cells
#18
Li Zhang, Yanfeng Xing, Qi Gao, Xuejun Sun, Di Zhang, Gang Cao
Gastric cancer is one of the most of common cancers in the world. 5-Fluorouracil (5-FU) has been identified as one of the standard first-line chemotherapy drugs for locally advanced or metastatic gastric cancer. However, poor tumor penetration, bad selectivity and toxic side effects are the major limitations for the application of chemotherapy drugs in anticancer therapy. Recently, plenty of studies demonstrate that the novel tumor-homing peptide iRGD could promote the tumor-penetrating capability of chemotherapy drugs in multiple cancers, and neuropilin-1 (NRP1) protein is the critical mediator for iRGD...
July 19, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28737925/lipid-bilayer-gated-mesoporous-silica-nanocarriers-for-tumor-targeted-delivery-of-zoledronic-acid-in-vivo
#19
Diti Desai, Jixi Zhang, Jouko Sandholm, Jaakko Lehtimäki, Tove Grönroos, Johanna Tuomela, Jessica M Rosenholm
Zoledronic acid (ZOL) is a nitrogen-containing bisphosphonate used for the treatment of bone diseases and calcium metabolism. Anticancer activity of ZOL has been established, but its extraskeletal effects are limited due to its rapid uptake and accumulation to bone hydroxyapatite. In this work, we report on the development of tethered lipid bilayer-gated mesoporous silica nanocarriers (MSNs) for the incorporation, retention and intracellular delivery of ZOL. The in vitro anticancer activity of ZOL-loaded nanocarriers was evaluated by cell viability assay and live-cell imaging...
July 24, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28737900/accumulation-of-charantin-and-expression-of-triterpenoid-biosynthesis-genes-in-bitter-melon-momordica-charantia
#20
Do Manh Cuong, Jin Jeon, Abubaker M A Morgan, Changsoo Kim, Jae Kwang Kim, Sook Young Lee, Sang Un Park
Charantin, a natural cucurbitane type triterpenoid, has been reported to have beneficial pharmacological functions such as anticancer, antidiabetic, and antibacterial activities. However, accumulation of charantin in bitter melon has been little studied. Here, we performed a transcriptome analysis to identify genes involved in the triterpenoid biosynthesis pathway in bitter melon seedlings. Total of 88,703 transcripts with an average length of 898 bp were identified in bitter melon seedlings. Based on a functional annotation, we identified 15 candidate genes encoding enzymes related to triterpenoid biosynthesis and analyzed their expression in different organs of mature plants...
July 24, 2017: Journal of Agricultural and Food Chemistry
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