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https://www.readbyqxmd.com/read/29779163/discovering-simple-phenylboronic-acid-and-benzoxaborole-derivatives-for-experimental-oncology-phase-cycle-specific-inducers-of-apoptosis-in-a2780-ovarian-cancer-cells
#1
Mateusz Psurski, Agnieszka Łupicka-Słowik, Agnieszka Adamczyk-Woźniak, Joanna Wietrzyk, Andrzej Sporzyński
Objective The aim of the study was to evaluate the antiproliferative potential of simple phenylboronic acid and benzoxaborole derivatives as well as to provide preliminary insight into their mode of action in cancer cells in vitro. Methods The antiproliferative activity was assessed in five diverse cancer cell lines via the SRB method (sulforhodamine B) or MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) method after 72 h of treatment. Further studies of the mechanism of action consisted of the influence of the compounds on cell cycle progression and apoptosis induction, which was assessed by flow cytometry, caspase-3 enzymatic activity, fluorescence microscopy and western blot analysis...
May 19, 2018: Investigational New Drugs
https://www.readbyqxmd.com/read/29778902/perspectives-on-the-past-present-and-future-of-cancer-nanomedicine
#2
Yu Seok Youn, You Han Bae
The justification of cancer nanomedicine relies on enhanced permeation (EP) and retention (R) effect and the capability of intracellular targeting due primarily to size after internalization (endocytosis) into the individual target cells. The EPR effect implies improved efficacy. Affinity targeting for solid tumors only occur after delivery to individual cells, which help internalization and/or retention. The design principles have been supported by animal results in numerous publications, but hardly translated...
May 17, 2018: Advanced Drug Delivery Reviews
https://www.readbyqxmd.com/read/29778892/structure-based-design-of-novel-quinoxaline-2-carboxylic-acids-and-analogues-as-pim-1-inhibitors
#3
Bruno Oyallon, Marie Brachet-Botineau, Cédric Logé, Pascal Bonnet, Mohamed Souab, Thomas Robert, Sandrine Ruchaud, Stéphane Bach, Pascal Berthelot, Fabrice Gouilleux, Marie-Claude Viaud-Massuard, Caroline Denevault-Sabourin
We identified a new series of quinoxaline-2-carboxylic acid derivatives, targeting the human proviral integration site for Moloney murine leukemia virus-1 (HsPim-1) kinase. Seventeen analogues were synthesized providing useful insight into structure-activity relationships studied. Docking studies realized in the ATP pocket of HsPim-1 are consistent with an unclassical binding mode of these inhibitors. The lead compound 1 was able to block HsPim-1 enzymatic activity at nanomolar concentrations (IC50 of 74 nM), with a good selectivity profile against a panel of mammalian protein kinases...
May 11, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29778887/biological-potential-of-oxo-vanadium-salicylediene-amino-acid-complexes-as-cytotoxic-antimicrobial-antioxidant-and-dna-interaction
#4
Mohamed Shaker S Adam, Hany Elsawy
New series of oxo-vanadium N-salicyledieneamino acid Schiff base complexes are synthesized and characterized. They are synthesized from the reaction of sodium salicylaldehyde-5-sulfonate, some amino acids, alanine (VOHL1), leucine (VOHL2) or glycine (VOHL3) in an aqueous media, and leucine (VOHLpy1) or tryptophan (VOHLpy2) in pyridine with vanadyl acetylacetonate. The complexes are characterized by EA, TGA, IR, UV-Visible and mass spectra, conductivity and magnetic measurements. The biological activity of the VO-complexes shows that VOHL1, VOHL2 and VOHL3 exhibit anti-proliferative effect and may be used as anticancer drugs...
May 4, 2018: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/29778718/nimbolide-epigenetically-regulates-autophagy-and-apoptosis-in-breast-cancer
#5
Venkatesh Pooladanda, Soumya Bandi, Sandhya Rani Mondi, Krishna Mohan Gottumukkala, Chandraiah Godugu
Autophagy is a critical regulator of cellular homeostasis and its dysregulation often results in various disease manifestations, including cancer. Nimbolide, an active chemical constituent of neem (Azadirachta indica) exhibits potent anticancer effects. Although, nimbolide mediated apoptosis activation in breast cancer cells is well known. Nevertheless, its role in autophagy induction mechanism and epigenetic alteration is not explored previously. Our current study intended to bridge the gaps in the existing research by exploring the potential of nimbolide in inducing autophagy, which could counter regulate the transformations in breast cancer...
May 17, 2018: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/29778097/hyperprolactinemia-inducing-antipsychotics-increase-breast-cancer-risk-by-activating-jak-stat5-in-precancerous-lesions
#6
A N Johnston, W Bu, S Hein, S Garcia, L Camacho, L Xue, L Qin, C Nagi, S G Hilsenbeck, J Kapali, K Podsypanina, J Nangia, Y Li
BACKGROUND: Psychiatric medications are widely prescribed in the USA. Many antipsychotics cause serum hyperprolactinemia as an adverse side effect; prolactin-Janus kinase 2 (JAK2)-signal transducer and activator of transcription 5 (STAT5) signaling both induces cell differentiation and suppresses apoptosis. It is controversial whether these antipsychotics increase breast cancer risk. METHODS: We investigated the impact of several antipsychotics on mammary tumorigenesis initiated by retrovirus-mediated delivery of either ErbB2 or HRas or by transgenic expression of Wnt-1...
May 19, 2018: Breast Cancer Research: BCR
https://www.readbyqxmd.com/read/29777989/synthesis-antiproliferative-activity-and-mechanism-of-gallium-iii-thiosemicarbazone-complexes-as-potential-anti-breast-cancer-agents
#7
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/29777913/the-tp53-induced-glycolysis-and-apoptosis-regulator-mediates-cooperation-between-htlv-1-p30-ii-and-the-retroviral-oncoproteins-tax-and-hbz-and-is-highly-expressed-in-an-in-vivo-xenograft-model-of-htlv-1-induced-lymphoma
#8
Tetiana Hutchison, Aditi Malu, Laçin Yapindi, Rachel Bergeson, Kendra Peck, Megan Romeo, Carolyn Harrod, Jordan Pope, Louisa Smitherman, Wesleigh Gwinn, Lee Ratner, Courtney Yates, Robert Harrod
The human T-cell leukemia virus type-1 (HTLV-1) is an oncoretrovirus that infects and transforms CD4+ T-cells and causes adult T-cell leukemia/lymphoma (ATLL) -an aggressive lymphoproliferative disease that is highly refractive to most anticancer therapies. The HTLV-1 proviral genome encodes several regulatory products within a conserved 3' nucleotide sequence, known as pX; however, it remains unclear how these factors might cooperate or dynamically interact in virus-infected cells. Here we demonstrate that the HTLV-1 latency-maintenance factor p30II induces the TP53-induced glycolysis and apoptosis regulator (TIGAR) and counters the oxidative stress, mitochondrial damage, and cytotoxicity caused by the viral oncoproteins Tax and HBZ...
May 16, 2018: Virology
https://www.readbyqxmd.com/read/29777637/thymol-inhibits-oral-squamous-cell-carcinoma-growth-via-mitochondria-mediated-apoptosis
#9
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
#10
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
#11
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/29775731/targeted-and-controlled-drug-delivery-by-multifunctional-mesoporous-silica-nanoparticles-with-internal-fluorescent-conjugates-and-external-polydopamine-and-graphene-oxide-layers
#12
Anh-Vy Tran, KyuHwan Shim, Thu-Thao Vo Thi, Jeong-Keun Kook, Seong Soo A An, Sang-Wha Lee
This study demonstrated the targeted delivery and controlled release of cisplatin drug molecules from doubly decorated mesoporous silica nanoparticles (MSNs), which were internally grafted with fluorescent conjugates and externally coated with polydopamine (PDA) and graphene oxide (GO) layers. The brush-like internal conjugates conferred fluorescent functionality and high capacity of cisplatin loading into MSNs, as well as contributing to a sustained release of the cisplatin through a porous channel with the assistance of external PDA layer...
May 15, 2018: Acta Biomaterialia
https://www.readbyqxmd.com/read/29775625/reduction-sensitive-polymeric-nanomedicines-an-emerging-multifunctional-platform-for-targeted-cancer-therapy
#13
Huanli Sun, Yifan Zhang, Zhiyuan Zhong
The development of smart delivery systems that are robust in circulation and quickly release drugs following selective internalization into target cancer cells is a key to precision cancer therapy. Interestingly, reduction-sensitive polymeric nanomedicines showing high plasma stability and triggered cytoplasmic drug release behavior have recently emerged as one of the most exciting platforms for targeted delivery of various anticancer drugs including small chemical drugs, proteins, and nucleic acids. In vivo studies in varying tumor models reveal that these reduction-sensitive multifunctional nanomedicines outperform the currently used clinical formulations and reduction-insensitive counterparts, bringing about not only significantly enhanced tumor selectivity, accumulation and inhibition efficacy but also markedly reduced systemic toxicity and improved therapeutic index...
May 15, 2018: Advanced Drug Delivery Reviews
https://www.readbyqxmd.com/read/29775573/indole-3-carbinol-i3c-enhances-the-sensitivity-of-murine-breast-adenocarcinoma-cells-to-doxorubicin-dox-through-inhibition-of-nf-%C3%AE%C2%BA%C3%AE-blocking-angiogenesis-and-regulation-of-mitochondrial-apoptotic-pathway
#14
Subhadip Hajra, Arup Ranjan Patra, Abhishek Basu, Prosenjit Saha, Sudin Bhattacharya
Various epidemiological and preclinical studies have already established the cancer chemopreventive potential of naturally occurring glucosinolate breakdown product Indole-3-Carbinol (I3C) as well as its abilities to induce selective cell death towards malignant cell. Therefore, the objective of the present study is to improve the therapeutic efficacy and prevention of doxorubicin (DOX)-induced toxicity, by the concurrent use of Indole-3-Carbinol (I3C). In this study, I3C was administered (20 mg/kg b.w., p...
May 15, 2018: Chemico-biological Interactions
https://www.readbyqxmd.com/read/29774995/-study-on-the-relationship-between-mct-1-and-p53-in-laryngeal-squamous-cell-carcinoma
#15
Y B Wang, O Xu, R J Zhang, C G Shan
Objective: The aim of this study is to investigate the expression and clinical significance of monocarboxylate transporter 1 (MCT-1) and p53 in laryngeal squamous cell carcinoma (LSCC). Method: Immunohistochemical staining of MCT-1 and p53 was carried out in 41 cases of laryngeal squamous cell carcinoma embedded in paraffin, and the relationship between positive expression and clinicopathological data was evaluated. All data were analyzed by SPSS software (Windows version 21.0). Result: In normal mucosa p53 expression was absent; while, the basal "stem cell" layer is highly enriched in MCT-1...
June 5, 2017: Journal of Clinical Otorhinolaryngology, Head, and Neck Surgery
https://www.readbyqxmd.com/read/29774985/microrna-1270-is-associated-with-poor-prognosis-and-its-inhibition-yielded-anticancer-mechanisms-in-human-osteosarcoma
#16
Lei Zhong, Changjun Zheng, Hongjuan Fang, Meng Xu, Bingpeng Chen, Chen Li
In this work, we explored the aberrant expression pattern, clinical association, and functional regulations of microRNA-1270 (miR-1270) in osteosarcoma. Among in vitro osteosarcoma cell lines and in situ tissues of osteosarcoma patients, quantitative real time-PCR was used to examine their endogenous miR-1270 expression. Clinical correlation between endogenous miR-1270 expression and clinicopathological features of osteosarcoma patients, as well as cancer patients' overall survival, was statistically examined...
May 18, 2018: IUBMB Life
https://www.readbyqxmd.com/read/29774752/effects-of-ethanol-on-the-anticancer-function-of-doxorubicin-in-jj012-cells
#17
Hui Huang, Yanze Li, Mingjuan Wu, Jing Luo, Junhui Nie, Baoyu Hou, Qi He, Yan Diao, Lin Qi, Yuanyuan Zhao, Ying Liu, Dan Yang, Lingyun Zhou
AIM: Chondrosarcoma is difficult to treat because of resistance to conventional chemotherapy and radiotherapy. This study evaluated the effects of ethanol in combination with doxorubicin in chondrosarcoma cells. MATERIALS & METHODS: JJ012, was treated with doxorubicin alone or in combination with ethanol. Effects on cellular proliferation, migration, invasion, apoptosis, and the cell cycle were evaluated. RESULTS: Treatment of JJ012 cells with 100 mM ethanol and doxorubicin resulted in reduced cell growth, invasion, and migration...
May 18, 2018: Future Oncology
https://www.readbyqxmd.com/read/29774603/programmed-nanoparticle-loaded-nanoparticles-for-deep-penetrating-3d-cancer-therapy
#18
Jinhwan Kim, Changshin Jo, Won-Gwang Lim, Sungjin Jung, Yeong Mi Lee, Jun Lim, Haeshin Lee, Jinwoo Lee, Won Jong Kim
Tumors are 3D, composed of cellular agglomerations and blood vessels. Therapies involving nanoparticles utilize specific accumulations due to the leaky vascular structures. However, systemically injected nanoparticles are mostly uptaken by cells located on the surfaces of cancer tissues, lacking deep penetration into the core cancer regions. Herein, an unprecedented strategy, described as injecting "nanoparticle-loaded nanoparticles" to address the long-lasting problem is reported for effective surface-to-core drug delivery in entire 3D tumors...
May 18, 2018: Advanced Materials
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
#19
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
#20
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
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