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https://www.readbyqxmd.com/read/29154868/naphthoquinones-from-the-leaves-of-rhinacanthus-nasutus-having-acetylcholinesterase-inhibitory-and-cytotoxic-activities
#1
Sirada Boonyaketgoson, Vatcharin Rukachaisirikul, Souwalak Phongpaichit, Kongkiat Trisuwan
Four new naphthoquinones (1-4), named rhinacanthins S (1), T (2), U (3) and V (4), together with 13 known naphthoquinones were isolated from the leaf extract of Rhinacanthus nasutus. The structures of isolated compounds were elucidated by spectroscopic methods, especially 1D and 2D NMR spectroscopy and mass spectrometry. Rhinacanthin S (1) exhibited acetylcholinesterase inhibition activity with a % inhibition value of 48.04±3.25. The known rhinacanthin A (5) showed cytotoxicity against a MCF-7 cell line with an IC50 value of 8...
November 14, 2017: Fitoterapia
https://www.readbyqxmd.com/read/29152075/a-novel-multikinase-inhibitor-r8-exhibits-potent-inhibition-on-cancer-cells-through-both-apoptosis-and-autophagic-cell-death
#2
Yuqiong Xie, Chunchun Li, Yali Huang, Zhenyu Jia, Jiang Cao
Chemotherapy is an important treatment for cancer patients, especially for those with unresectable lesions. Targeted therapy of cancer by specific inhibition of aberrant tyrosine kinase activities in cancer cells with chemically synthesized tyrosine kinase inhibitors (TKIs), shows better responses while less side effects than traditional chemotherapeutic drugs. It is common that cancer cells often exhibit deregulation of several tyrosine kinases simultaneously, multikinase TKIs (MKIs) therefore have greater advantages over single-target TKIs...
October 20, 2017: Oncotarget
https://www.readbyqxmd.com/read/29151985/synthesis-and-anticancer-evaluation-of-some-new-3-benzyl-4-8-dimethylbenzopyrone-derivatives
#3
Sohair L El-Ansary, Doaa E Abdel Rahman, Lina M A Abdel Ghany
Introduction: New benzopyrone derivatives such as Schiff's like compounds, acetohydrazides or substituted with oxadiazole or pyrazole heterocycles were synthesized from parent acid hydrazide compound 3. Methods and Materials: Structures of the synthesized compounds were elucidated using IR, NMR and mass spectroscopy. All the synthesized derivatives were selected by National Cancer Institute (NCI), Bethesda, and evaluated for their in vitro anticancer activity in the full NCI 60 cell lines panel assay...
2017: Open Medicinal Chemistry Journal
https://www.readbyqxmd.com/read/29151951/potential-synergistic-effect-of-phosphodiesterase-inhibitors-with-chemotherapy-in-lung-cancer
#4
Kalliopi Domvri, Konstantinos Zarogoulidis, Nikolaos Zogas, Paul Zarogoulidis, Savvas Petanidis, Konstantinos Porpodis, Efrosini Kioseoglou, Wolfgang Hohenforst-Schmidt
Purpose: Lung cancer remains the leading cause of cancer-related deaths worldwide and novel therapeutic approaches targeting crucial pathways are urgently needed to improve its treatment. Differentiation-based therapeutics (Methylxanthines) and phosphodiesterase inhibitors (type 4 and 5), have been implicated in cancer treatment. Our objectives were to capture any potential anti-tumor effect of these drug combinations with chemotherapeutic agents in vitro. Methods: Theophylline as Methylxanthines, Roflumilast as phosphodiesterase type 4 (PDE4) inhibitor and Sildenafil as phosphodiesterase type 5 (PDE5) inhibitor are the drugs that we combined with the chemotherapeutic agents (Docetaxel, Cisplatin and Carboplatin) in vitro...
2017: Journal of Cancer
https://www.readbyqxmd.com/read/29148081/synthesis-antitumor-activity-evaluation-and-dna-binding-study-of-coumarin-based-agents
#5
Kamilia M Amin, Aly M Taha, Riham F George, Nada M Mohamed, Fardous F Elsenduny
A novel series of coumarin-thiadiazole heterocycle derivatives was synthesized by the nucleophilic substitution reaction. The synthesized compounds were structurally verified by IR, (1) H NMR, (13) C NMR, mass spectra, and elemental analyses. The antitumor activity of the synthesized compounds was evaluated through DNA binding assays and the 60-cell line panel according to the US NCI-DTP protocol or a selection of human tumor cell lines: breast cancer (MCF-7), liver cancer (HepG-2), and colorectal cancer (HCT-116)...
November 17, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/29146185/biomarker-identification-for-statin-sensitivity-of-cancer-cell-lines
#6
Vineet K Raghu, Colin H Beckwitt, Katsuhiko Warita, Alan Wells, Panayiotis V Benos, Zoltán N Oltvai
Statins are potent cholesterol reducing drugs that have been shown to reduce tumor cell proliferation in vitro and tumor growth in animal models. Moreover, retrospective human cohort studies demonstrated decreased cancer-specific mortality in patients taking statins. We previously implicated membrane E-cadherin expression as both a marker and mechanism for resistance to atorvastatin-mediated growth suppression of cancer cells; however, a transcriptome-profile-based biomarker signature for statin sensitivity has not yet been reported...
November 13, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29143776/gastric-cancer-cell-glycosylation-as-a-modulator-of-the-erbb2-oncogenic-receptor
#7
Henrique O Duarte, Meritxell Balmaña, Stefan Mereiter, Hugo Osório, Joana Gomes, Celso A Reis
Aberrant expression and hyperactivation of the human epidermal growth factor receptor 2 (ErbB2) constitute crucial molecular events underpinning gastric neoplastic transformation. Despite ErbB2 extracellular domain being a well-known target for glycosylation, its glycosylation profile and the molecular mechanisms through which it actively tunes tumorigenesis in gastric cancer (GC) cells remain elusive. We aimed at disclosing relevant ErbB2 glycan signatures and their functional impact on receptor's biology in GC cells...
October 28, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29143041/joint-experimental-and-theoretical-studies-of-the-surprising-stability-of-the-aryl-pentazole-upon-noncovalent-binding-to-%C3%AE-cyclodextrin
#8
Yu-Zhang Yang, Xiao-Feng Liu, Ru-Bo Zhang, Si-Ping Pang
Herein, binding of the β-cyclodextrin (β-CD) host to the unstable aryl pentazole guest has been confirmed experimentally and theoretically. After the confinement of aryl pentazole, electron density reorganization was studied by M06-2X dispersion-corrected DFT and further reflected in the characteristic shift in the NMR spectra. Among the host-guest complexes, the inclusion complex is favored with the phenyl ring expectedly encapsulated within the cavity through noncovalent interactions such as hydrogen bonding, C-Hπ, and the special Csp(2)-HH-Csp(3) bonding discovered by the NBO, QTAIM, and NCI-RDG theories...
November 16, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/29140573/-99m-tc-labeled-rhuepo-for-imaging-of-the-erythropoietin-receptor-in-tumors
#9
Xiaoqing Zhuang, Dan Zhao, Pengfei Yang, Yingqin Jia, Rui Liang, Qian Zhao, Chunlei Han, Joseph M Kinsella, Ruilong Sheng, Juan Li
To analyze erythropoietin receptor (EpoR) status in tumors, recombinant human erythropoietin (rHuEpo) was labeled with (99m) Tc by (99m) Tc-centered one-pot synthesis, resulting in high radiochemical purity, stability and biological activity. Both in vitro cell culture experiments and biodistribution studies of normal rats demonstrated successful EpoR targeting. The biodistribution of labeled rHuEpo in a NCI-H1975 xenograft model showed tumor accumulation (tumor-to-muscle ratio: 4.27±1.77), confirming the expression of active EpoR in tumors...
November 15, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/29140488/us-national-cancer-institute-china-collaborative-studies-on-chinese-medicine-and-cancer
#10
Libin Jia, Hongsheng Lin, Joost Oppenheim, O M Zack Howard, Jie Li, Huiting Fan, Zhizheng Zhao, William Farrar, Ying Zhang, Nancy Colburn, Matthew R Young, Weidong Li, David Newman, Barry R O'Keefe, John Beutler, Jikai Liu, Xiaojiang Hao, Xiaosheng Yang, Tengfei Ji, Jeffrey D White
Since 2007, the US National Cancer Institute (NCI) Office of Cancer Complementary and Alternative Medicine (OCCAM), together with the Cancer Institute of the China Academy of Chinese Medical Sciences (CICACMS), institutes at China Academy of Sciences and Chinese Academy of Medical Sciences, have engaged in collaborations on Chinese medicine (CM) and cancer research. Through these collaborations, CM drugs and compounds have been studied at NCI labs. This paper summarizes the discoveries and progress on these research projects, exploring the aspects of cancer prevention, botanical drug mechanisms of action and component analysis/quality control (QC), and anticancer activity screening...
November 1, 2017: Journal of the National Cancer Institute. Monographs
https://www.readbyqxmd.com/read/29140486/the-national-cancer-institute-s-conference-on-acupuncture-for-symptom-management-in-oncology-state-of-the-science-evidence-and-research-gaps
#11
Farah Z Zia, Oluwadamilola Olaku, Ting Bao, Ann Berger, Gary Deng, Arthur Yin Fan, Mary K Garcia, Patricia M Herman, Ted J Kaptchuk, Elena J Ladas, Helene M Langevin, Lixing Lao, Weidong Lu, Vitaly Napadow, Richard C Niemtzow, Andrew J Vickers, Xin Shelley Wang, Claudia M Witt, Jun J Mao
The Division of Cancer Treatment and Diagnosis, Office of Cancer Complementary and Alternative Medicine, at the National Cancer Institute (NCI) held a symposium on "Acupuncture for Cancer Symptom Management" on June 16 and 17, 2016. Invited speakers included 19 scientists and scholars with expertise in acupuncture and cancer research from the United States, Europe, and China. The conference reviewed the NCI's grant funding on acupuncture, analyzed the needs of cancer patients, reviewed safety issues, and assessed both the current scientific evidence and research gaps of acupuncture in oncology care...
November 1, 2017: Journal of the National Cancer Institute. Monographs
https://www.readbyqxmd.com/read/29140485/growth-of-integrative-medicine-at-leading-cancer-centers-between-2009-and-2016-a-systematic-analysis-of-nci-designated-comprehensive-cancer-center-websites
#12
Hyeongjun Yun, Lingyun Sun, Jun J Mao
Background: Cancer centers have increasingly offered integrative medicine therapies in response to their patients' unmet needs. We evaluated the growth of integrative medicine in leading academic cancer centers in the United States as reflected by their public-facing websites. Methods: We performed a systematic review of 45 National Cancer Institute (NCI)-designated comprehensive cancer center websites. Two researchers independently evaluated whether the websites provided information regarding integrative medicine modalities and, if so, whether the services were provided in the same health system...
November 1, 2017: Journal of the National Cancer Institute. Monographs
https://www.readbyqxmd.com/read/29140484/state-of-the-science-cancer-complementary-and-alternative-medicine-therapeutics-research-nci-strategic-workshop-highlights-of-discussion-report
#13
Dan Xi, Ting Bao, Qi Chen, Sushing Chen, Yung-Chi Cheng, Joseph Cullen, David A Frank, Jonathan W Friedberg, Ian Kronish, Jeffrey E Lee, Mark Levine, Pingping Li, Shao Li, Weidong Lu, Jun J Mao, Stephen O'Keefe, Larry Rubinstein, Manish A Shah, Leanna Standish, Channing J Paller, Edward Chu
In May 2016, the Office of Cancer Complementary and Alternative Medicine, Division of Cancer Diagnosis and Treatment, of the National Cancer Institute convened a special workshop focused on the State of the Science: Cancer Complementary and Alternative Medicine Therapeutics Research. The current state of the science, gaps, and future opportunities were reviewed and discussed by a distinguished panel of experts in this field of research, and the highlights of this meeting are reported herein.
November 1, 2017: Journal of the National Cancer Institute. Monographs
https://www.readbyqxmd.com/read/29140422/multidisciplinary-clinic-approach-improves-overall-survival-outcomes-of-patients-with-metastatic-germ-cell-tumors
#14
C Albany, N Adra, A C Snavely, C Cary, T A Masterson, R S Foster, K Kesler, T M Ulbright, L Cheng, M Chovanec, F Taza, K Ku, M J Brames, N H Hanna, L H Einhorn
Background: To report our experience utilizing a multidisciplinary clinic (MDC) at Indiana University (IU) since the publication of the International Germ Cell Cancer Collaborative Group (IGCCCG), and to compare our overall survival to that of the National Cancer Institute (NCI) Surveillance, Epidemiology, and End Results (SEER) Program. Patients and Methods: We conducted a retrospective analysis of all patients with metastatic germ cell tumor (GCT) seen at IU from 1998-2014...
November 10, 2017: Annals of Oncology: Official Journal of the European Society for Medical Oncology
https://www.readbyqxmd.com/read/29138807/role-of-lasp-1-a-novel-sox9-transcriptional-target-in-the-progression-of-lung-cancer
#15
Jianguang Shi, Jing Guo, Xinjian Li
Lung cancer accounts for most cancer-related deaths worldwide. However, the underlying mechanism by which it mediates the progression of lung cancer remains unclear. Expression of LASP-1 (LIM and SH3 protein 1) was evaluated in lung cancer tissues and tumor-adjacent normal tissues using immunohistochemistry and western blotting. Functional studies have shown that siRNA-mediated silencing of LASP-1 in human lung cancer cells and reduced cell proliferation, migration, and invasion. Flow cytometry and immunofluorescence staining also revealed that rate of cell apoptosis was increased after knockdown of expression of LASP-1, thereby suggesting that LASP-1 may function as an oncogene during lung cancer progression...
November 10, 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/29138344/targeting-the-mycn-parp-dna-damage-response-pathway-inneuroendocrine-prostate-cancer
#16
Wei Zhang, Bo Liu, Wenhui Wu, Likun Li, Bradley M Broom, Spyridon M Basourakos, Dimitrios Korentzelos, Yang Luan, Jianxiang Wang, Guang Yang, Sanghee Park, Abul K Azad, Xuhong Cao, Jeri Kim, Paul Corn, Christopher Logothetis, Ana M Aparicio, Arul M Chinnayan, Nora M Navone, Patricia Troncoso, Timothy C Thompson
PURPOSE: We investigated MYCN-regulated molecular pathways in castration-resistant prostate cancer (CRPC) classified by morphological criteria as adenocarcinoma or neuroendocrine to extend the molecular phenotype, establish driver pathways, and identify novel approaches to combination therapy for NEPC. RESULTS: Using comparative bioinformatics analyses of CRPC-Adeno and CRPC-Neuro RNA sequence data from public datasets and a panel of 28 PDX models we identified a MYCN-PARP-DNA damage response (DDR) pathway that is enriched in CRPC with neuroendocrine differentiation (NED) and CRPC-Neuro...
November 14, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/29138027/imidazo-1-2-a-pyridines-linked-with-thiazoles-thiophene-motif-through-keto-spacer-as-potential-cytotoxic-agents-and-nf-%C3%AE%C2%BAb-inhibitors
#17
Kamala K Vasu, Chander Singh Digwal, Amit N Pandya, Dhaivat H Pandya, Jayesh A Sharma, Sneha Patel, Milee Agarwal
A series of new imidazo[1,2-a]pyridine linked with thiazole/thiophene motif through a keto spacer were synthesized and tested for their cytotoxic potential against three human cancer cell lines including A549, HeLa and U87-MG using MTT assay. Compounds A2, A3, A4, C1 and C2 showed cytotoxicity against all the three cell lines. The selectivity index for compound A4 for A549 and HeLa cells was comparable to that of doxorubicin. Among the synthesized compounds, B5 showed the maximum inhibition of NF-κB activity as ascertained by NF-κB reporter assay (IC50 = 6...
November 11, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29137939/in-silico-identification-and-in-vivo-characterization-of-small-molecule-therapeutic-hypothermia-mimetics
#18
Claire Coderch, María Díaz de Cerio, Jose María Zapico, Rafael Peláez, Ignacio M Larrayoz, Ana Ramos, Alfredo Martínez, Beatriz de Pascual-Teresa
Hypothermia has been proved to have a beneficial effect on several pathologies. CIRBP is one of the so termed cold-shock proteins involved in this process. In this work, we have detected small molecules capable of modulating the activity of CIRBP in the absence of a cold stimulus, by High Throughput Virtual Screening (HTVS) of the Diversity Set IV of the NCI and 15 compounds of our in-house data base. Fifteen compounds were selected from the HTVS to carry out a second screening through a cell-based Western blot assay...
October 31, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29137450/moving-forward-with-actionable-therapeutic-targets-and-opportunities-in-endometrial-cancer-nci-clinical-trials-planning-meeting-report-on-identifying-key-genes-and-molecular-pathways-for-targeted-endometrial-cancer-trials
#19
REVIEW
Helen J MacKay, Douglas A Levine, Victoria L Bae-Jump, Daphne W Bell, Jessica N McAlpine, Alessandro Santin, Gini F Fleming, David G Mutch, Kenneth P Nephew, Nicolas Wentzensen, Paul J Goodfellow, Oliver Dorigo, Hans W Nijman, Russell Broaddus, Elise C Kohn
The incidence and mortality rates from endometrial cancer are increasing. There have been no new drugs approved for the treatment of endometrial cancer in decades. The National Cancer Institute, Gynecologic Cancer Steering Committee identified the integration of molecular and/or histologic stratification into endometrial cancer management as a top strategic priority. Based on this, they convened a group of experts to review the molecular data in this disease. Here we report on the actionable opportunities and therapeutic directions identified for incorporation into future clinical trials...
October 13, 2017: Oncotarget
https://www.readbyqxmd.com/read/29136763/amorphous-solid-dispersions-of-hecogenin-acetate-using-different-polymers-for-enhancement-of-solubility-and-improvement-of-anti-hyperalgesic-effect-in-neuropathic-pain-model-in-mice
#20
Carlos Demócedes Luís de França Almeida Moreira, Jonas Gabriel de Oliveira Pinheiro, Walter Ferreira da Silva-Júnior, Euzébio Guimarães Barbosa, Zênia Maria Maciel Lavra, Erick Willyame Menezes Pereira, Marília Matos Resende, Eduardo Pereira de Azevedo, Lucindo José Quintans-Júnior, Adriano Antunes de Souza Araújo, Jullyana de Souza Siqueira Quintans, Ádley Antonini Neves de Lima
Hecogenin acetate (HA) is an acetylated sapogenin that has shown potential antihyperalgesic activity, inhibiting descending pain and acting in opioid receptors. However, HA exhibits poor aqueous solubility, which may limit its application. This study aims to develop amorphous solid dispersions (ASD) using five hydrophilic polymers, to characterize them and to evaluate their antihyperalgesic activity. Physicochemical characterization was performed by X-Ray Diffraction (XRD), Scanning Electron Microscopy (SEM) and Fourier Transformed Infrared (FTIR) spectroscopy...
November 6, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
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