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https://www.readbyqxmd.com/read/29777989/synthesis-antiproliferative-activity-and-mechanism-of-gallium-iii-thiosemicarbazone-complexes-as-potential-anti-breast-cancer-agents
#1
Jinxu Qi, Qian Yao, Kun Qian, Liang Tian, Zhen Cheng, Dongmei Yang, Yihong Wang
Five thiosemicarbazone ligands were synthesized and characterized by condensation with different aldehydes or ketones by 4-phenylthiosemicarbazone. The representative dichlorido[2-(Di-2-pyridinylmethylene)-Nphenylhydrazinecarbothioamide-N,N,S]-gallium(III) (Ga4) was characterized by X-ray single crystal diffraction, which was 1:1 ligand/Ga(III) complexes. The structure-activity relationship of these ligands and Ga (III) complexes have been investigated, and the results demonstrate that the formation of Ga (III) complexes have significant antiproliferative activity over the corresponding ligands...
May 14, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29777637/thymol-inhibits-oral-squamous-cell-carcinoma-growth-via-mitochondria-mediated-apoptosis
#2
Jorge J De La Chapa, Prajjal Kanti Singha, Debbie R Lee, Cara B Gonzales
BACKGROUND: Thymol is a Transient Receptor Potential Ankyrin Subtype 1 channel, (TRPA1) agonist found in thyme and oregano. Thymol has antioxidant, anti-inflammatory, and antimicrobial properties; thus thymol is added to many commercially available products including Listerine mouthwash. Thymol is also cytotoxic to HL-60 (acute promyelotic leukemia) cells in vitro. Therefore, we evaluated the effects of thymol against oral squamous cell carcinoma (OSCC) and its anticancer mechanism-of-action...
May 19, 2018: Journal of Oral Pathology & Medicine
https://www.readbyqxmd.com/read/29777444/comparison-of-lawsone-contents-among-lawsonia-inermis-plant-parts-and-neurite-outgrowth-accelerators-from-branches
#3
Yoshimi Oda, Souichi Nakashima, Erina Kondo, Seikou Nakamura, Mamiko Yano, Chisa Kubota, Yusuke Masumoto, Minami Hirao, Yuki Ogawa, Hisashi Matsuda
Lawsonia inermis L. (Lythraceae) is cultivated in many countries, including Japan, China, India and Egypt. Its leaves are well known as hair dye and exhibit antibacterial, anticancer, antifungal and anticonvulsant activities. However, there are few reports on its branches. 2-Hydroxy-1,4-naphthoquinone (lawsone) is a characteristic compound in its leaves. However, it remains to be clarified whether lawsone is present in other plant parts or not. In this study, we measured lawsone contents in the extracts of L...
May 17, 2018: Journal of Natural Medicines
https://www.readbyqxmd.com/read/29776741/a-small-diversity-library-of-%C3%AE-methyl-amide-analogs-of-sulindac-for-probing-anticancer-structure-activity-relationships
#4
Bini Mathew, Timothy S Snowden, Michele C Connelly, R Kiplin Guy, Robert C Reynolds
Non-steroidal anti-inflammatory drugs (NSAIDs) have a variety of potential indications that include management of pain and inflammation as well as chemoprevention and/or treatment of cancer. Furthermore, a specific form of ibuprofen, dexibuprofen or the S-(+) form, shows interesting neurological activities and has been proposed for the treatment of Alzheimer's disease. In a continuation of our work probing the anticancer activity of small sulindac libraries, we have prepared and screened a small diversity library of α-methyl substituted sulindac amides in the profen class...
May 10, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29774202/loss-of-the-cyclin-dependent-kinase-inhibitor-1-in-the-context-of-brachyury-mediated-phenotypic-plasticity-drives-tumor-resistance-to-immune-attack
#5
Duane H Hamilton, Kristen K McCampbell, Claudia Palena
The acquisition of mesenchymal features by carcinoma cells is now recognized as a driver of metastasis and tumor resistance to a range of anticancer therapeutics, including chemotherapy, radiation, and certain small-molecule targeted therapies. With the recent successful implementation of immunotherapies for the treatment of various types of cancer, there is growing interest in understanding whether an immunological approach could be effective at eradicating carcinoma cells bearing mesenchymal features. Recent studies, however, demonstrated that carcinoma cells that have acquired mesenchymal features may also exhibit decreased susceptibility to lysis mediated by immune effector cells, including antigen-specific CD8+ T cells, innate natural killer (NK), and lymphokine-activated killer (LAK) cells...
2018: Frontiers in Oncology
https://www.readbyqxmd.com/read/29774137/saudi-anti-human-cancer-plants-database-sacpd-a-collection-of-plants-with-anti-human-cancer-activities
#6
Ateeq Ahmed Al-Zahrani
Several anticancer drugs have been developed from natural products such as plants. Successful experiments in inhibiting the growth of human cancer cell lines using Saudi plants were published over the last three decades. Up to date, there is no Saudi anticancer plants database as a comprehensive source for the interesting data generated from these experiments. Therefore, there was a need for creating a database to collect, organize, search and retrieve such data. As a result, the current paper describes the generation of the Saudi anti-human cancer plants database (SACPD)...
January 30, 2018: Oncology Reviews
https://www.readbyqxmd.com/read/29774111/ceragenin-csa-13-as-free-molecules-and-attached-to-magnetic-nanoparticle-surfaces-induce-caspase-dependent-apoptosis-in-human-breast-cancer-cells-via-disruption-of-cell-oxidative-balance
#7
Ewelina Piktel, Izabela Prokop, Urszula Wnorowska, Grzegorz Król, Mateusz Cieśluk, Katarzyna Niemirowicz, Paul B Savage, Robert Bucki
Natural antimicrobial peptides and ceragenins, as non-peptide amphipathic mimics, have been proposed as anti-cancer agents. To date, it has been confirmed that cathelicidin LL-37 and ceragenin CSA-13, both in free form and immobilized on the surface of magnetic nanoparticles (MNP@LL-37, MNP@CSA-13) induce apoptosis in colon cancer cells. Nevertheless, the question remains whether ceragenins, as synthetic analogs of LL-37 peptide and mimicking a number of its properties, act as antineoplastic agents in breast cancer cells, where LL-37 peptide stimulates oncogenesis...
April 24, 2018: Oncotarget
https://www.readbyqxmd.com/read/29773987/celastrol-attenuates-the-invasion-and-migration-and-augments-the-anticancer-effects-of-bortezomib-in-a-xenograft-mouse-model-of-multiple-myeloma
#8
Muthu K Shanmugam, Kwang S Ahn, Jong H Lee, Radhamani Kannaiyan, Nurulhuda Mustafa, Kanjoormana A Manu, Kodappully S Siveen, Gautam Sethi, Wee J Chng, Alan P Kumar
Several lines of evidence have demonstrated that deregulated activation of NF-κB plays a pivotal role in the initiation and progression of a variety of cancers including multiple myeloma (MM). Therefore, novel molecules that can effectively suppress deregulated NF-κB upregulation can potentially reduce MM growth. In this study, the effect of celastrol (CSL) on patient derived CD138+ MM cell proliferation, apoptosis, cell invasion, and migration was investigated. In addition, we studied whether CSL can potentiate the apoptotic effect of bortezomib, a proteasome inhibitor in MM cells and in a xenograft mouse model...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29773887/varacin-1-a-novel-analog-of-varacin-c-induces-p53-independent-apoptosis-in-cancer-cells-through-ros-mediated-reduction-of-xiap
#9
Jing Zhou, Wen-Li Li, Zi-Xuan Wang, Nai-Yuan Chen, Yue Tang, Xiao-Xiao Hu, Jing-Huan Deng, Yixin Lu, Guo-Dong Lu
Varacin C is a promising anticancer agent and possesses acid-promoted and photo-induced DNA-damaging activities. In this study, we synthesized an analog varacin-1 (VCA-1) and examined its anticancer potentials. The results demonstrated that VCA-1 caused dose-dependent apoptotic cell death in cancer cells. Note that this action is independent of p53 status, because VCA-1 induced similar levels of apoptosis in two different panels of cell lines (HCT116 p53- wild-type vs. HCT116 p53-knockout colon cancer cells, and p53-expressing U2OS vs...
May 17, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29773403/synthesis-of-chitin-glucan-aldehyde-quercetin-conjugate-and-evaluation-of-anticancer-and-antioxidant-activities
#10
Anu Singh, P K Dutta, Hridyesh Kumar, Amit Kumar Kureel, Ambak Kumar Rai
In the present study, we have synthesized chitin-glucan-aldehyde-quercetin (chi-glu-ald-que) conjugate via condensation reaction. Synthesis of chitin-glucan-aldehyde (chi-glu-ald) complex was facilitated by the oxidation of chitin-glucan (chi-glu) complex. Formation of conjugate was confirmed by Proton nuclear magnetic resonance spectroscopy (1 H NMR) and Fourier-transform infrared spectroscopy (FT-IR). Morphological studies showed that after grafting of quercetin, several changes on surface were depicted and a more crystalline nature was observed...
August 1, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29773371/modification-of-native-fucoidan-from-fucus-evanescens-by-recombinant-fucoidanase-from-marine-bacteria-formosa-algae
#11
Artem S Silchenko, Anton B Rasin, Mikhail I Kusaykin, Olesya S Malyarenko, Natalie M Shevchenko, Anastasya O Zueva, Anatoly I Kalinovsky, Tatyana N Zvyagintseva, Svetlana P Ermakova
Enzymatic depolymerization of fucoidans attracts many researchers due to the opportunity of obtaining standardized fucoidan fragments. Fucoidanase catalyzes the cleavage of fucoidan from Fucus evanescens (FeF) to form low molecular weight products (LMP) and a polymeric fraction (HMP) with 50.8 kDa molecular weight and more than 50% yield. NMR spectroscopy shows that the HMP fraction has regular structure and consists of a repeating fragment [→3)-α-l-Fucp2,4OSO3 - -(1 → 4)-α-l-Fucp2,4OSO3 - -(1 → 4)-α-l-Fucp2OSO3 - -(1→]n ...
August 1, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29773172/seleno-l-methionine-and-l-ascorbic-acid-differentiate-the-biological-activity-of-doxorubicin-and-its-metal-complexes-as-a-new-anticancer-drugs-candidate
#12
Marzena Matejczyk, Grzegorz Świderski, Renata Świsłocka, Stanisław Józef Rosochacki, Włodzimierz Lewandowski
The most important problems of anti-cancer therapy include the toxicity of the drugs applied to healthy cells and the multi-drug cells resistance to chemotherapeutics. One of the most commonly used anticancer drugs is doxorubicin (DOX) used to treat certain leukemias and non-Hodgkin's lymphomas, as well as bladder, breast, stomach, lung, ovarian, thyroid, multiple myeloma and other cancers. Preliminary studies showed that metal complex with DOX improve its cytostatic activity with changes in their molecular structure and distribution of electrons, resulting in a substantial change of its biological activity (including antitumor activity)...
July 2018: Journal of Trace Elements in Medicine and Biology
https://www.readbyqxmd.com/read/29773008/antimicrobial-cytotoxic-anti-inflammatory-and-antioxidant-activity-of-culinary-processed-shiitake-medicinal-mushroom-lentinus-edodes-agaricomycetes-and-its-major-sulfur-sensory-active-compound-lenthionine
#13
Kristyna Kupcova, Iveta Stefanova, Zuzana Plavcova, Jan Hosek, Pavel Hrouzek, Roman Kubec
The antimicrobial, cytotoxic, anti-inflammatory, and antioxidant properties of aqueous extracts of raw and culinary processed shiitake mushrooms were evaluated and compared with those of lenthionine (1,2,3,5,6-penta-thiepane), the principal aroma-bearing substance of the shiitake medicinal mushroom (Lentinus edodes). Antimicrobial activity was tested using a panel of 4 strains of bacteria, 2 yeasts, and 2 fungi. Cytotoxic properties were evaluated against 3 cell lines (HepG2, HeLa, PaTu), whereas the anti-inflammatory activity of tested samples was assayed based on their ability to attenuate the secretion of the cytokine tumor necrosis factor-α...
2018: International Journal of Medicinal Mushrooms
https://www.readbyqxmd.com/read/29772746/design-synthesis-and-biological-evaluation-of-benzimidazole-derived-biocompatible-copper-ii-and-zinc-ii-complexes-as-anticancer-chemotherapeutics
#14
Mohamed F AlAjmi, Afzal Hussain, Md Tabish Rehman, Azmat Ali Khan, Perwez Alam Shaikh, Rais Ahmad Khan
Herein, we have synthesized and characterized a new benzimidazole-derived "BnI" ligand and its copper(II) complex, [Cu(BnI)₂], 1 , and zinc(II) complex, [Zn(BnI)₂], 2 , using elemental analysis and various spectroscopic techniques. Interaction of complexes 1 and 2 with the biomolecules viz. HSA (human serum albumin) and DNA were studied using absorption titration, fluorescence techniques, and in silico molecular docking studies. The results exhibited the significant binding propensity of both complexes 1 and 2 , but complex 1 showed more avid binding to HSA and DNA...
May 16, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29772699/synthesis-molecular-structure-anticancer-activity-and-qsar-study-of-n-aryl-heteroaryl-4-1-h-pyrrol-1-yl-benzenesulfonamide-derivatives
#15
Beata Żołnowska, Jarosław Sławiński, Zdzisław Brzozowski, Anna Kawiak, Mariusz Belka, Joanna Zielińska, Tomasz Bączek, Jarosław Chojnacki
A series of N -(aryl/heteroaryl)-4-(1 H -pyrrol-1-yl)benzenesulfonamides were synthesized from 4-amino- N -(aryl/heteroaryl)benzenesulfonamides and 2,5-dimethoxytetrahydrofuran. All the synthesized compounds were evaluated for their anticancer activity on HeLa, HCT-116, and MCF-7 human tumor cell lines. Compound 28 , bearing 8-quinolinyl moiety, exhibited the most potent anticancer activity against the HCT-116, MCF-7, and HeLa cell lines, with IC50 values of 3, 5, and 7 µM, respectively. The apoptotic potential of the most active compound ( 28 ) was analyzed through various assays: phosphatidylserine translocation, cell cycle distribution, and caspase activation...
May 16, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29772685/the-emergence-of-endophytic-microbes-and-their-biological-promise
#16
Gary Strobel
As is true with animal species, plants also have an associated microflora including endophytes as well as microbes associated with the phyllosphere and rhizosphere (plant surfaces) and this is considered the plant microbiome. However, those organisms within virtually all tissues and organs of the plant are known as endophytes. Most often fungi are the most frequently recovered endophytes from plant tissues, but bacterial forms generally occur in greater numbers, but not in species varieties. The exact biological/biochemical role of the endophyte in the plant and how it interacts with the plant and other endophytes and plant associated organisms has not been intensely and carefully examined...
May 16, 2018: Journal of Fungi (Basel, Switzerland)
https://www.readbyqxmd.com/read/29772645/anticancer-activity-of-euplotin-c-isolated-from-the-marine-ciliate-euplotes-crassus-against-human-melanoma-cells
#17
Sara Carpi, Beatrice Polini, Giulio Poli, Gabriela Alcantara Barata, Stefano Fogli, Antonella Romanini, Tiziano Tuccinardi, Graziano Guella, Francesco Paolo Frontini, Paola Nieri, Graziano Di Giuseppe
Cutaneous melanoma is the most serious type of skin cancer, so new cytotoxic weapons against novel targets in melanoma are of great interest. Euplotin C (EC), a cytotoxic secondary metabolite of the marine ciliate Euplotes crassus , was evaluated in the present study on human cutaneous melanoma cells to explore its anti-melanoma activity and to gain more insight into its mechanism of action. EC exerted a marked cytotoxic effect against three different human melanoma cell lines (A375, 501Mel and MeWo) with a potency about 30-fold higher than that observed in non-cancer cells (HDFa cells)...
May 16, 2018: Marine Drugs
https://www.readbyqxmd.com/read/29772538/targeting-fibroblast-activation-protein-in-cancer-prospects-and-caveats
#18
Petr Busek, Rosana Mateu, Michal Zubal, Lenka Kotackova, Aleksi Sedo
Fibroblast activation protein (FAP, seprase) is a serine protease with post-proline dipeptidyl peptidase and endopeptidase enzymatic activity. FAP is upregulated in several tumor types, while its expression in healthy adult tissues is scarce. FAP molecule itself and FAP+ stromal cells play an important although probably context-dependent and tumor type-specific pathogenetic role in tumor progression. We provide an overview of FAP expression under both physiological and pathological conditions with focus on human malignancies...
June 1, 2018: Frontiers in Bioscience (Landmark Edition)
https://www.readbyqxmd.com/read/29772529/microbial-bio-fuels-a-solution-to-carbon-emissions-and-energy-crisis
#19
Arun Kumar, Sumit Kaushal, Shubhini A Saraf, Jay Shankar Singh
Increasing energy demand, limited fossil fuel resources and climate change have prompted development of alternative sustainable and economical fuel resources such as crop-based bio-ethanol and bio-diesel. However, there is concern over use of arable land that is used for food agriculture for creation of biofuel. Thus, there is a renewed interest in the use of microbes particularly microalgae for bio-fuel production. Microbes such as micro-algae and cyanobacteria that are used for biofuel production also produce other bioactive compounds under stressed conditions...
June 1, 2018: Frontiers in Bioscience (Landmark Edition)
https://www.readbyqxmd.com/read/29772274/pharmacodynamic-and-pharmacokinetic-characteristics-of-ymr-65-a-tubulin-inhibitor-in-tumor-bearing-mice
#20
Ali Fan, Jiali Wei, Mengru Yang, Qing Zhang, Yaliang Zhang, Qingwang Liu, Ning Li, Di Zhao, Yang Lu, Junxiu Li, Jie Zhao, Shuhua Deng, Bingjie Zhang, Hailiang Zhu, Xijing Chen
YMR-65, 5-(5-bromo-1-methyl-1H-indol-3-yl)-3-(3-methoxyphenyl)-4, 5-dihydro-1H-pyrazole-1-carboxamide, is a potential tubulin inhibitor exhibiting good anticancer activity. In our study, we illustrated the biological activities in HepG2 cells and the pharmacodynamic and pharmacokinetic profiles were evaluated in murine H22 hepatoma-bearing mice. Molecular docking assay and colchicine competition assay indicated that YMR-65 could bind tightly to the colchicine binding site of tubulin. Further investigation demonstrated that YMR-65 arrested cells in the G2/M phase of cell cycle and induced apoptosis in HepG2 cells...
May 14, 2018: European Journal of Pharmaceutical Sciences
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