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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/27921229/an-extracellular-proteasome-releases-endostatin-from-human-collagen-xviii
#2
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
#3
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/27919961/effects-of-spiro-bisheterocycles-on-proliferation-and-apoptosis-in-human-breast-cancer-cell-lines
#4
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
#5
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
#6
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/27919264/acidic-tumor-microenvironment-abrogates-the-efficacy-of-mtorc1-inhibitors
#7
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
#8
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
#9
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/27918967/nanoencapsulation-an-efficient-and-promising-approach-to-maximize-wound-healing-efficacy-of-curcumin-a-review-of-new-trends-and-state-of-the-art
#10
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/27918490/activity-of-eribulin-in-a-primary-culture-of-well-differentiated-dedifferentiated-adipocytic-sarcoma
#11
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
#12
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
https://www.readbyqxmd.com/read/27918445/docetaxel-loaded-self-assembly-stearic-acid-modified-bletilla-striata-polysaccharide-micelles-and-their-anticancer-effect-preparation-characterization-cellular-uptake-and-in-vitro-evaluation
#13
Qingxiang Guan, Dandan Sun, Guangyuan Zhang, Cheng Sun, Miao Wang, Danyang Ji, Wei Yang
Poorly soluble drugs have low bioavailability after oral administration, thereby hindering effective drug delivery. A novel drug-delivery system of docetaxel (DTX)-based stearic acid (SA)-modified Bletilla striata polysaccharides (BSPs) copolymers was successfully developed. Particle size, zeta potential, encapsulation efficiency (EE), and loading capacity (LC) were determined. The DTX release percentage in vitro was determined using high performance liquid chromatography (HPLC). The hemolysis and in vitro anticancer activity were studied...
December 2, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27917873/dose-biomarker-response-modeling-of-the-anticancer-effect-of-ethaselen-in-a-human-non-small-cell-lung-cancer-xenograft-mouse-model
#14
Suo-Fu Ye, Jian Li, Shuang-Min Ji, Hui-Hui Zeng, Wei Lu
Thioredoxin reductase (TrxR) is a component of several redox-sensitive signaling cascades that mediate important biological processes such as cell survival, maturation, growth, migration and inhibition of apoptosis. The expression levels of TrxR1 in some human carcinoma cell lines are nearly 10 times higher than those in normal cells. Ethaselen is a novel antitumor candidate that exerts potent inhibition on non-small cell lung cancer (NSCLC) by targeting TrxR. In this study we explored the relationship between the ethaselen dose and TrxR activity level and the relationship between TrxR degradation and tumor apoptosis in a human lung carcinoma A549 xenograft model...
December 5, 2016: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/27917872/advances-in-the-study-of-berberine-and-its-derivatives-a-focus-on-anti-inflammatory-and-anti-tumor-effects-in-the-digestive-system
#15
REVIEW
Kun Zou, Zhao Li, Yong Zhang, Hao-Yue Zhang, Bo Li, Wei-Liang Zhu, Ji-Ye Shi, Qi Jia, Yi-Ming Li
It has been widely recognized that inflammation, particularly chronic inflammation, can increase the risk of cancer and that the simultaneous treatment of inflammation and cancer may produce excellent therapeutic effects. Berberine, an alkaloid isolated from Rhizoma coptidis, has broad applications, particularly as an antibacterial agent in the clinic with a long history. Over the past decade, many reports have demonstrated that this natural product and its derivatives have high activity against both cancer and inflammation...
December 5, 2016: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/27917784/suppression-of-bromodomain-containing-protein-4-by-shrna-a-new-approach-for-cancer-treatment
#16
Turan Kaya, Berke Kahraman, Nurgeldi Bazarov, Alperen S Toker, Ayse Celik, Sadik Cigdem, Esra Gunduz
PURPOSE: MYC is a transcription factor coding gene that is believed to control 15% of the genes in the entire human genome. The central role of c-MYC in cancer pathogenesis makes it a major therapeutic target in field of anticancer agent development. METHODS: We targeted the acetyl-lysine binding modules or bromodomains, which are associated with c-MYC transcriptional activation. RESULTS: Sequence specific inhibition of BET bromodomains with small hairpin RNAs (shRNAs) resulted in cessation of cellular proliferation in different cancer cell lines...
December 1, 2016: Clinical and Investigative Medicine. Médecine Clinique et Experimentale
https://www.readbyqxmd.com/read/27917474/germacrone-inhibits-adipogenesis-and-stimulates-lipolysis-via-the-amp-activated-protein-kinase-signalling-pathway-in-3t3-l1-preadipocytes
#17
Yuan-Ri Guo, Se-Young Choung
OBJECTIVES: In a previous study, we reported that Aster spathulifolius Maxim extract (ASE) inhibited lipid accumulation and adipocyte differentiation in 3T3-L1 cells. Of the components in ASE, germacrone (GM) was identified as a potent bioactive constituent. GM is known for its anticancer and antiviral activity. However, the effects of GM and the molecular mechanism by which GM regulates adipogenesis and lipolysis were not reported. Therefore, we investigated the effect of GM on adipogenesis and lipolysis and to elucidate its underlying molecular mechanism...
December 5, 2016: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/27917282/ginkgetin-induces-apoptosis-in-786-o-cell-line-via-suppression-of-jak2-stat3-pathway
#18
Yu Ren, Shuang-Shuang Huang, Xue Wang, Zhong-Guan Lou, Xu-Ping Yao, Guo-Bin Weng
OBJECTIVES: Renal cell carcinoma (RCC) is insensitive to conventional chemotherapy. Ginkgetin effectively treats several carcinoma cells. However, little is known about effects of Ginkgetin on RCC. In the present study, using 786-O cells, we evaluate whether Ginkgetin exerts anticancer effects against RCC. MATERIALS AND METHODS: 786-O cells suspended in the medium containing Ginkgetin were cultured for 24 hr to 72 hr, and then MTT assay was used to study cytotoxic effect of Ginkgetin...
November 2016: Iranian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/27917206/anticancer-and-antibacterial-secondary-metabolites-from-the-endophytic-fungus-penicillium-sp-cam64-against-multi-drug-resistant-gram-negative-bacteria
#19
Jean-Bosco Jouda, Jean-de-Dieu Tamokou, Céline Djama Mbazoa, Prodipta Sarkar, Prasanta Kumar Bag, Jean Wandji
BACKGROUND: The emergence of multiple-drug resistance bacteria has become a major threat and thus calls for an urgent need to search for new effective and safe anti-bacterial agents. OBJECTIVES: This study aims to evaluate the anticancer and antibacterial activities of secondary metabolites from Penicillium sp., an endophytic fungus associated with leaves of Garcinia nobilis. METHODS: The culture filtrate from the fermentation of Penicillium sp...
September 2016: African Health Sciences
https://www.readbyqxmd.com/read/27917100/synthesis-of-st7612aa1-a-novel-oral-hdac-inhibitor-via-radical-%C3%A2-thioacetic-acid-addition
#20
Gianfranco Battistuzzi, Giuseppe Giannini
ABSTRACT BACKGROUND: In the expanding field of anticancer drugs, HDAC inhibitors are playing an increasingly important role. To date, four/five HDAC inhibitors have been approved by FDA. All these compounds fit the widely accepted HDAC inhibitors pharmacophore model characterized by a cap group, a linker chain and a zinc binding group (ZBG), able to bind the Zn(2+) ion in a pocket of the HDAC active site. Romidepsin, a natural compound, is the only thiol derivative. We have selected a new class of synthetic HDAC inhibitors, the thio-ω(lactam-carboxamide) derivatives, with ST7612AA1 as drug candidate, pan-inhibitor active in the range of single- to two-digit nanomolar concentrations...
December 2016: Current Bioactive Compounds
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