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https://www.readbyqxmd.com/read/27922057/antiproliferative-activities-of-amaryllidaceae-alkaloids-from-lycoris-radiata-targeting-dna-topoisomerase-i
#1
Gui-Lin Chen, Yong-Qiang Tian, Jian-Lin Wu, Na Li, Ming-Quan Guo
Crude Amaryllidaceae alkaloids (AAs) extracted from Lycoris radiata are reported to exhibit significant anti-cancer activity. However, the specific alkaloids responsible for the pharmacodynamic activity and their targets still remain elusive. In this context, we strived to combine affinity ultrafiltration with topoisomerase I (Top I) as a target enzyme aiming to fish out specific bioactive AAs from Lycoris radiata. 11 AAs from Lycoris radiata were thus screened out, among which hippeastrine (peak 5) with the highest Enrichment factor (EF) against Top I exhibited good dose-dependent inhibition with IC50 at 7...
December 6, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27921283/choices-have-consequences-the-nexus-between-dna-repair-pathways-and-genomic-instability-in-cancer
#2
REVIEW
Sonali Bhattacharjee, Saikat Nandi
BACKGROUND: The genome is under constant assault from a multitude of sources that can lead to the formation of DNA double-stand breaks (DSBs). DSBs are cytotoxic lesions, which if left unrepaired could lead to genomic instability, cancer and even cell death. However, erroneous repair of DSBs can lead to chromosomal rearrangements and loss of heterozygosity, which in turn can also cause cancer and cell death. Hence, although the repair of DSBs is crucial for the maintenance of genome integrity the process of repair need to be well regulated and closely monitored...
December 2016: Clinical and Translational Medicine
https://www.readbyqxmd.com/read/27921229/an-extracellular-proteasome-releases-endostatin-from-human-collagen-xviii
#3
Maria L V Reiss-Pistilli, Detlef Schuppan, Madalena M S Barroso, Iranaia Assunção-Miranda, Shirley Farias, Letícia Lery, Michael Bauer, Luiz Juliano, Maria A Juliano, Tatiana Coelho-Sampaio
Endostatin is a potent anti-angiogenic and anti-tumor protein capable of regressing tumors without inducing acquired resistance. Since it is a fragment of the parental molecule, collagen XVIII, its endogenous production depends on the activity of a specific proteolytic enzyme. While such an enzyme has been described in mice, a human counterpart has not been identified so far. Here, we searched for this enzyme by using a fluorescence resonance energy transfer peptide containing the cleavage site of human collagen XVIII...
December 5, 2016: Angiogenesis
https://www.readbyqxmd.com/read/27920817/pharmacological-characterization-of-liquiritigenin-a-chiral-flavonoid-in-licorice
#4
Samaa Alrushaid, Neal M Davies, Stephanie E Martinez, Casey L Sayre
Liquiritigenin is a chiral flavonoid present in plant based food, nutraceuticals, and traditional medicines. It is also an important ingredient present in licorice. The purpose of this study is to explore the pharmacological activity of racemic liquiritigenin utilizing several in vitro assays with relevant roles in colon cancer and diabetes. Where possible, the pure enantiomers were tested to identify the stereospecific contribution to the activity. In vitro antioxidant, anticancer, anti-inflammatory activities (cyclooxygenase inhibition), antidiabetic activities (alpha-amylase and alpha-glucosidase inhibition) as well as cytochrome P450 (CYP450) inhibitory activities were assessed...
October 2016: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27920704/autoimmune-hemolytic-anemia-as-a-complication-of-nivolumab-therapy
#5
Amruth R Palla, Devin Kennedy, Hossain Mosharraf, Donald Doll
Recently, immunotherapeutic drugs, including PD-1 inhibitors (nivolumab, pembrolizumab), PD-L1 inhibitors (atezolizumab, avelumab), and CTLA4 inhibitors (ipiliumumab), have emerged as important additions to the armamentarium against certain malignancies and have been incorporated into therapeutic protocols for first-, second-, or third-line agents for these metastatic cancers. Immune checkpoint inhibitor nivolumab is currently FDA approved for the treatment of patients with metastatic malignant melanoma [Redman et al...
September 2016: Case Reports in Oncology
https://www.readbyqxmd.com/read/27919961/effects-of-spiro-bisheterocycles-on-proliferation-and-apoptosis-in-human-breast-cancer-cell-lines
#6
Lamia Hamdan Ramdani, Oualid Talhi, Nadia Taibi, Laetitia Delort, Caroline Decombat, Artur Silva, Khaldoun Bachari, Marie-Paule Vasson, Florence Caldefie-Chezet
Breast cancer is the leading cause of cancer-related death in women worldwide and a critical public health concern. Here we investigated the anticancer potential and effects of low-molecular-weight bridgehead oxygen and nitrogen-containing spiro-bisheterocycles on proliferation and apoptosis of the human breast cancer cell lines MCF-7 and MDA-MB-231. The compounds feature a hydantoin moiety attached to either diazole, isoxazole, diazepine, oxazepine or benzodiazepine via the privileged tetrahedral spiro-linkage...
December 2016: Anticancer Research
https://www.readbyqxmd.com/read/27919953/bishydroquinone-renieramycin-m-induces-apoptosis-of-human-lung-cancer-cells-through-a-mitochondria-dependent-pathway
#7
Tatchakorn Pinkhien, Arnatchai Maiuthed, Supakarn Chamni, Khanit Suwanborirux, Naoki Saito, Pithi Chanvorachote
BACKGROUND: Renieranycin M (RM), a bistetrahydro-isoquinolinequinone isolated from the Thai blue sponge, Xestospongia sp. was reported to be a potent anti-lung cancer agent. Modification at quinone ring enhanced apoptosis over necrosis. Thus, bishydroquinone renieramycin M (HQ-RM) was prepared and evaluated for apoptosis induction in lung cancer cells. METHODS: HQ-RM was examined for cytotoxicity and apoptosis induction in human lung cancer H292 cells by 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyltetrazoliumbromide and Hoechst/propidium iodide staining, respectively...
December 2016: Anticancer Research
https://www.readbyqxmd.com/read/27919940/vitamin-d-and-myofibroblasts-in-fibrosis-and-cancer-at-cross-purposes-with-tgf-%C3%AE-smad-signaling
#8
REVIEW
Shraga Shany, Ina Sigal-Batikoff, Sergio Lamprecht
The multifaceted involvement of the active vitamin D metabolite 1,25-dihydroxyvitamin D3 (henceforth referred to by the synonyms 1,25(OH)2D3, calcitriol or vitamin D) in blunting the growth of cancer cells is amply recognized. In this review we focused our attention on the cross-talk between 1,25 (OH)2D3 and the tumor microenvironment (TME), signaling out stromal cancer-associated fibroblasts (CAFs), the most abundant TME population, as a target for calcitriol anticancer action. In view of the commonality of the phenotypic signature in myofibroblasts, resident in the cancer stroma and in non-neoplastic fibrotic loci, we examined modes of action of vitamin D in non-neoplastic chronic diseases and in cancer to assess mechanistic similarities and divergences...
December 2016: Anticancer Research
https://www.readbyqxmd.com/read/27919789/unravelling-a-p73-regulated-network-the-role-of-a-novel-p73-dependent-target-mir3158-in-cancer-cell-migration-and-invasiveness
#9
Sotiris Galtsidis, Stella Logotheti, Athanasia Pavlopoulou, Christos P Zampetidis, Georgia Papachristopoulou, Andreas Scorilas, Borek Vojtesek, Vassilis Gorgoulis, Vassilis Zoumpourlis
The transcription factor p73 is homologous to the well-known tumor-suppressor p53. The p73-regulated networks are of significant clinical interest, because they may substitute for impaired p53-regulated networks which are commonly perturbed in cancer. Herein, we aimed to characterize a p73-regulated network that mediates cell migration and restores anti-oncogenic responses in p53-mutant cancer cells. In this study, we demonstrate that p73 regulates a network underlying cell migration, which consists of MIR34A/MIR3158/vimentin/β-catenin/lef1...
December 2, 2016: Cancer Letters
https://www.readbyqxmd.com/read/27919613/cellular-uptake-of-glucoheptoamidated-poly-amidoamine-pamam-g3-dendrimer-with-amide-conjugated-biotin-a-potential-carrier-of-anticancer-drugs
#10
Łukasz Uram, Magdalena Szuster, Aleksandra Filipowicz, Magdalena Zaręba, Elżbieta Wałajtys-Rode, Stanisław Wołowiec
In search for soluble derivatives of PAMAM dendrimers as potential carriers for hydrophobic drugs, the conjugates of PAMAM G3 with biotin, further converted into glycodendrimer with d-glucoheptono-1,4-lactone, were prepared. Polyamidoamine dendrimer (PAMAM) of third generation, G3 was functionalized with four biotin equivalents covalently attached to terminal amine nitrogens via amide bond G3(4B). The remaining 28 amine groups were blocked by glucoheptoamide substituents (gh) to give G3(4B28gh) or with one fluorescein equivalent (attached by reaction of G3(4B) with fluorescein isothiocyanate, FITC) via thiourea bond as FITC followed by exhaustive glucoheptoamidation to get G3(4B27gh1F)...
November 25, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27919280/patient-derived-xenografts-a-relevant-preclinical-model-for-drug-development
#11
REVIEW
Luca Pompili, Manuela Porru, Carla Caruso, Annamaria Biroccio, Carlo Leonetti
Identifying appropriate preclinical cancer models remains a major challenge in increasing the efficiency of drug development. A potential strategy to improve patient outcomes could be selecting the 'right' treatment in preclinical studies performed in patient-derived xenografts (PDXs) obtained by direct implants of surgically resected tumours in mice. These models maintain morphological similarities and recapitulate molecular profiling of the original tumours, thus representing a useful tool in evaluating anticancer drug response...
December 5, 2016: Journal of Experimental & Clinical Cancer Research: CR
https://www.readbyqxmd.com/read/27919264/acidic-tumor-microenvironment-abrogates-the-efficacy-of-mtorc1-inhibitors
#12
Seraina Faes, Adrian P Duval, Anne Planche, Emilie Uldry, Tania Santoro, Catherine Pythoud, Jean-Christophe Stehle, Janine Horlbeck, Igor Letovanec, Nicolo Riggi, Nicolas Demartines, Olivier Dormond
BACKGROUND: Blocking the mechanistic target of rapamycin complex-1 (mTORC1) with chemical inhibitors such as rapamycin has shown limited clinical efficacy in cancer. The tumor microenvironment is characterized by an acidic pH which interferes with cancer therapies. The consequences of acidity on the anti-cancer efficacy of mTORC1 inhibitors have not been characterized and are thus the focus of our study. METHODS: Cancer cell lines were treated with rapamycin in acidic or physiological conditions and cell proliferation was investigated...
December 5, 2016: Molecular Cancer
https://www.readbyqxmd.com/read/27919108/biocatalytic-synthesis-of-flavonoid-esters-by-lipases-and-their-biological-benefits
#13
Maria Elisa M B de Araújo, Yollanda E M Franco, Marcia C F Messias, Giovanna B Longato, João A Pamphile, Patricia de O Carvalho
Several studies have described important biological activities of flavonoids such as coronary heart disease prevention, hepatoprotective, anti-inflammatory and anticancer activities, enzyme inhibition activity, and antibacterial, antifungal, and antiviral activities. Flavonoids show promising activity as natural plant-based antioxidants due to their antioxidant and free radical scavenging properties. However, their primary applications as antioxidants in the pharmaceutical, cosmetic, and food industries are limited because of their moderately hydrophilic nature...
December 5, 2016: Planta Medica
https://www.readbyqxmd.com/read/27919107/synthetic-modification-of-9%C3%AE-and-9%C3%AE-hydroxyparthenolide-by-heck-or-acylation-reactions-and-evaluation-of-cytotoxic-activities
#14
Abderrahman El Bouakher, Badr Jismy, Hassan Allouchi, Eric Duverger, Latifa Barkaoui, Ahmed El Hakmaoui, Richard Daniellou, Gérald Guillaumet, Mohamed Akssira
Motivated by the widely reported anticancer activity of parthenolides and their derivatives, a series of new substituted parthenolides was efficiently synthesized. Structural modifications were performed at the C-9 and C-13 positions of 9α- and 9β-hydroxyparthenolide, which were isolated from the aerial parts of Anvillea radiata. Twenty-one derivatives were synthesized and evaluated for their in vitro cytotoxic activity against HS-683, SK-MEL-28, A549, and MCF-7 human cancer cell lines using the MTT colorimetric assay...
December 5, 2016: Planta Medica
https://www.readbyqxmd.com/read/27918989/ph-responsive-polymeric-micelles-based-on-poly-ethyleneglycol-b-poly-2-diisopropylamino-ethyl-methacrylate-block-copolymer-for-enhanced-intracellular-release-of-anticancer-drugs
#15
Zhigang Xu, Peng Xue, Yong-E Gao, Shiying Liu, Xiaoxiao Shi, Meili Hou, Yuejun Kang
We present a pH-responsive poly(ethyleneglycol)-b-poly(2-(diisopropylamino) ethyl methacrylate) block copolymer (MPEG-PPDA) that can self-assemble into micelles at very low critical micelle concentration. The formed micelles exhibit superior stability in physiological environment and pH-triggered transforming capability between self-assembly and disassembly. Moreover, the resulting micelles can load hydrophobic anticancer drug molecules such as doxorubicin in the core of micelles. The pH-triggered drug release kinetics matches the classical hydrazone bond model...
November 27, 2016: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/27918967/nanoencapsulation-an-efficient-and-promising-approach-to-maximize-wound-healing-efficacy-of-curcumin-a-review-of-new-trends-and-state-of-the-art
#16
REVIEW
Zahid Hussain, Hnin Ei Thu, Shiow-Fern Ng, Shahzeb Khan, Haliza Katas
Wound healing is a multifarious and vibrant process of replacing devitalized and damaged cellular structures, leading to restoration of the skin's barrier function, re-establishment of tissue integrity, and maintenance of the internal homeostasis. Curcumin (CUR) and its analogs have gained widespread recognition due to their remarkable anti-inflammatory, anti-infective, anticancer, immunomodulatory, antioxidant, and wound healing activities. However, their pharmaceutical significance is limited due to inherent hydrophobic nature, poor water solubility, low bioavailability, chemical instability, rapid metabolism and short half-life...
November 30, 2016: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/27918645/redox-and-ph-dual-responsive-polymer-based-nanoparticles-for-in-vivo-drug-delivery
#17
Chung Yen Ang, Si Yu Tan, Cathleen Teh, Jia Min Lee, Mun Fei Eddy Wong, Qiuyu Qu, Li Qing Poh, Menghuan Li, Yuanyuan Zhang, Vladimir Korzh, Yanli Zhao
Responsive nanomaterials have emerged as promising candidates as drug delivery vehicles in order to address biomedical diseases such as cancer. In this work, polymer-based responsive nanoparticles prepared by a supramolecular approach are loaded with doxorubicin (DOX) for the cancer therapy. The nanoparticles contain disulfide bonds within the polymer network, allowing the release of the DOX payload in a reducing environment within the endoplasm of cancer cells. In addition, the loaded drug can also be released under acidic environment...
December 5, 2016: Small
https://www.readbyqxmd.com/read/27918644/self-assembled-supramolecular-nanogels-as-a-safe-and-effective-drug-delivery-vector-for-cancer-therapy
#18
Chih-Chia Cheng, Mei-Chih Liang, Zhi-Sheng Liao, Jyun-Jie Huang, Duu-Jong Lee
Simple construction and manipulation of low-molecular-weight supramolecular nanogels, based on the introduction of multiple hydrogen bonding interactions, with the desired physical properties to achieve effective and safe delivery of drugs for cancer therapy remain highly challenging. Herein, a novel supramolecular oligomer cytosine (Cy)-polypropylene glycol containing self-complementary multiple hydrogen-bonded Cy moieties is developed, which undergoes spontaneous self-assembly to form nanosized particles in an aqueous environment...
December 5, 2016: Macromolecular Bioscience
https://www.readbyqxmd.com/read/27918490/activity-of-eribulin-in-a-primary-culture-of-well-differentiated-dedifferentiated-adipocytic-sarcoma
#19
Alessandro De Vita, Giacomo Miserocchi, Federica Recine, Laura Mercatali, Federica Pieri, Laura Medri, Alberto Bongiovanni, Davide Cavaliere, Chiara Liverani, Chiara Spadazzi, Dino Amadori, Toni Ibrahim
Eribulin mesylate is a novel, non-taxane, synthetic microtubule inhibitor showing antitumor activity in a wide range of tumors including soft tissue sarcomas (STS). Eribulin has been recently approved for the treatment of metastatic liposarcoma (LPS) patients previously treated with anthracyclines. This work investigated the mechanism of action of this innovative antitubulin agent in well-differentiated/dedifferentiated LPS (ALT/DDLPS) which represents one of the most common adipocytic sarcoma histotypes. A primary culture of ALT/DDLPS from a 54-year-old patient was established...
December 3, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27918447/enhanced-antimicrobial-and-anticancer-activity-of-silver-and-gold-nanoparticles-synthesised-using-sargassum-incisifolium-aqueous-extracts
#20
Mokone Mmola, Marilize Le Roes-Hill, Kim Durrell, John J Bolton, Nicole Sibuyi, Mervin E Meyer, Denzil R Beukes, Edith Antunes
A detailed, methodical approach was used to synthesise silver and gold nanoparticles using two differently prepared aqueous extracts of the brown algae Sargassum incisifolium. The efficiency of the extracts in producing nanoparticles were compared to commercially available brown algal fucoidans, a major constituent of brown algal aqueous extracts. The nanoparticles were characterised using TEM, XRD and UV/Vis spectroscopy and zeta potential measurements. The rate of nanoparticle formation was assessed using UV/Vis spectroscopy and related to the size, shape and morphology of the nanoparticles as revealed by TEM...
December 2, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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