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Cheng-Ming Wei, Yi-Ji Su, Xiong Qin, Jia-Xin Ding, Qian Liu, Fang-Ming Song, Shao-Hui Zong, Jiake Xu, Bo Zhou, Jin-Min Zhao
BACKGROUND/AIMS: Extensive osteoclast formation plays a critical role in bone diseases, including rheumatoid arthritis, periodontitis and the aseptic loosening of orthopedic implants. Thus, identification of agents that can suppress osteoclast formation and bone resorption is important for the treatment of these diseases. Monocrotaline (Mon), the major bioactive component of crotalaria sessiliflora has been investigated for its anti-cancer activities. However, the effect of Mon on osteoclast formation and osteolysis is not known...
July 19, 2018: Cellular Physiology and Biochemistry
Levent Dizdar, Jasmin Drusenheimer, Thomas Artur Werner, Birte Möhlendick, Sina Christin Schütte, Irene Esposito, Timm Filler, Wolfram Trudo Knoefel, Andreas Krieg
<br>Background: Gastroenteropancreatic neuroendocrine carcinomas (GEP-NECs) are biologically aggressive tumors, associated with a very poor survival. Due to their rarity, our knowledge on GEP-NEC biology is very limited. The aim of this study was to establish a GEP-NEC cell line model that might contribute to a better understanding of this rare malignant disease to further develop novel therapeutic approaches in preclinical studies. METHODS: Small cell neuroendocrine cancer cell line NEC-DUE3 was derived from a lymph node metastasis of a neuroendocrine carcinoma (NEC) located at the anal canal...
July 19, 2018: Neuroendocrinology
Zhong-Ling Qiu, Wei-Jun Wei, Zhen-Kui Sun, Chen-Tian Shen, Hong-Jun Song, Xin-Yun Zhang, Guo-Qiang Zhang, Xiao-Yue Chen, Quan-Yong Luo
BACKGROUND/AIMS: As biomarkers, circulating tumor cells (CTCs) from solid tumors can predict metastases and prognoses, and help monitor treatment efficacy. However, conventional CellSearch methods have low sensitivity to differentiated thyroid cancer (DTC) CTCs. In this study, for the first time, we used negative enriching (NE) immunofluorescence-in situ hybridization (iFISH) of chromosome 8 to capture and identify CTCs in DTC patients; and investigated how CTCs correlate with clinicopathological factors and prognosis in DTC patients with distant metastases (DM)...
July 19, 2018: Cellular Physiology and Biochemistry
Azam Sargazi, Fereshteh Shiri, Sheida Keikha, Mostafa Heidari Majd
Hyaluronic acid (HA) is increasingly investigated for biomedical applications such as regenerative medicine, aesthetic medicine, and drug delivery. Accordingly, conjugation of HA to PEGylated MNPs could increase the active targeting ability of nano-drug carriers toward CD44 receptors and be useful in a clinical setting such as drug delivery. So, we chemically conjugated mitoxantrone (MTX) to HA-PEGylated MNPs to use concurrent advantages such as prolong the circulation time, decrease the side effects and delivery toward special tumor cells...
July 11, 2018: Colloids and Surfaces. B, Biointerfaces
Pham Thi Thu Phuong, Sungin Lee, Changkyu Lee, Bohyung Seo, Sanghyun Park, Kyung Taek Oh, Eun Seong Lee, Han-Gon Choi, Beom Soo Shin, Yu Seok Youn
Chlorin e6 (Ce6) has attracted considerable interest as a promising second-generation photosensitizer for photodynamic therapy (PDT). However, the in vivo availability of Ce6 is significantly restricted by its low water solubility and poor ability to target tumors. We sought to overcome the limitations of Ce6 by using albumin nanoparticles with nab™ (nanoparticle albumin-bound) technology. The fabricated albumin nanoparticles consisted of bovine serum albumin (BSA), Ce6-BSA, and beta-carotene as a carrier, photosensitizing agent, and cross-linker, respectively...
July 10, 2018: Colloids and Surfaces. B, Biointerfaces
Islam Zaki, Mohammed K Abdelhameid, Ibrahim M El-Deen, Abdel Hady A Abdel Wahab, Abeer M Ashmawy, Khaled O Mohamed
Some triazinone derivatives are designed and synthesized as potential antitumor agents. Triazinone derivatives 4c, 5e and 7c show potent anticancer activity over MCF-7 breast cancer cells higher than podophyllotoxin (podo) by approximate 6-fold. DNA flow cytometry analysis for the compounds 3c, 4c, 5e, 6c and 7c show a potent inhibitory activity of cell proliferation and cell cycle arrest at G2 /M phase. Compounds 4c, 5e and 7c exhibit low to moderate β-tubulin polymerization inhibition percentage. Meanwhile, compound 6c displayed excellent β-tubulin percentage of polymerization inhibition equivalent to that exhibited by podo...
July 7, 2018: European Journal of Medicinal Chemistry
Dora C S Costa, Gabriella Silva de Almeida, Vitor Won-Held Rabelo, Lucio Mendes Cabral, Plínio Cunha Sathler, Paula Alvarez Abreu, Vitor Francisco Ferreira, Luiz Cláudio Rodrigues Pereira da Silva, Fernando de C da Silva
Naphthoquinones and 1,2,3-triazoles are structural pharmacophore that is known to impart several cancer cells. This work shows a synthetic methodology to obtain hybrid molecules involving naphthoquinone and triazol scaffold as multiple ligands. A simple and efficient synthetic route was used to prepare a series of sixteen compounds being eight 2-(1-aryl-1H-1,2,3-triazol-4-yl)-2,3-dihydronaphtho[1,2 b]furan-4,5-diones and eight 2-(1-aryl-1H-1,2,3-triazol-4-yl)-2,3-dihydronaphtho[2,3-b]furan-4,9-diones. These compounds were tested in MDA-MB231, Caco-2 and Calu-3 human cancer cells, and among them 7a was the most selective compound on Caco-2 cells, the most sensitized cell line in this study...
July 9, 2018: European Journal of Medicinal Chemistry
Michał Antoszczak, Alicja Urbaniak, Magdalena Delgado, Ewa Maj, Björn Borgström, Joanna Wietrzyk, Adam Huczyński, Youzhong Yuan, Timothy C Chambers, Daniel Strand
The polyether ionophore salinomycin has recently captured much interest due to its potent activity against multi-drug resistant cancer cells and cancer stem cells. Previous studies have shown that either acylation of the C20 position or esterification/amidation of the C1 carboxylate moiety is beneficial in terms of biological properties. In this paper, we present the first analogs combining such modifications. Evaluation of the anti-proliferative activity against a series of cancer cell lines showed that acylation of the C20 hydroxyl group improves the activity of salinomycin C1 amides but not of the corresponding C1 esters...
July 10, 2018: European Journal of Medicinal Chemistry
Jie Quan Wang, Xiaobin Wang, Yang Wang, Wen Jian Tang, Jing Bo Shi, Xin Hua Liu
In this study, twenty curcumin analogue hybrids as potential anticancer agents through regulation protein of TrxR were designed and synthesized. Results of anticancer activity showed that 5,7-dimethoxy-3-(3-(2-((1E, 4E)-3-oxo-5-(pyridin-2-yl)penta-1,4-dien-1- yl)phenoxy)propoxy)-2-(3,4,5-trimethoxyphenyl)-4H-chromen-4-one (compound 7d) could induce gastric cancer cells apoptosis by arresting cell cycle, break mitochondria function and inhibit TrxR activity. Meanwhile, western blot revealed that this compound could dramatically up expression of Bax/Bcl-2 ratio and high expression of TrxR oxidation...
July 10, 2018: European Journal of Medicinal Chemistry
Yiming Xu, Lichuan Wu, Haroon Ur Rashid, Dewang Jing, Xiaole Liang, Haodong Wang, Xu Liu, Jun Jiang, Lisheng Wang, Peng Xie
Based on the mechanism of action, novel scaffolds as Topo I inhibitors bearing indole and sophoridinine were designed. Preliminary docking study revealed that some molecules among the designed series possessed promising Topo I inhibitor properties. Subsequently, thirty new compounds were synthesized and characterized by 1 H NMR, 13 C NMR, and Mass spectral analyses. The compounds were then screened for their antiproliferative and enzymatic inhibitory activities. The results affirmed the consistency between docking and activities and the rationality of the design strategy...
July 16, 2018: European Journal of Medicinal Chemistry
Nada M Ghanem, Faten Farouk, Riham F George, Safinaz E S Abbas, Ossama M El-Badry
New imidazo[4,5-b]pyridine derivatives were designed, synthesized and screened for their anticancer activity against breast (MCF-7) and colon (HCT116) cancer cell lines. Nine compounds (I, II, IIIa, IIIb, IV, VI, VIIa, VIII, IX) showed significant activity against MCF-7, while six compounds (I, VIIc, VIIe, VIIf, VIII, IX) elicited a remarkable activity against HCT116. Compounds showing significant anticancer activity revealed remarkable CDK9 inhibitory potential (IC50  = 0.63-1.32 μM) relative to sorafenib (IC50  = 0...
July 6, 2018: Bioorganic Chemistry
Dominique Belpomme, Lennart Hardell, Igor Belyaev, Ernesto Burgio, David O Carpenter
Exposure to low frequency and radiofrequency electromagnetic fields at low intensities poses a significant health hazard that has not been adequately addressed by national and international organizations such as the World Health Organization. There is strong evidence that excessive exposure to mobile phone-frequencies over long periods of time increases the risk of brain cancer both in humans and animals. The mechanism(s) responsible include induction of reactive oxygen species, gene expression alteration and DNA damage through both epigenetic and genetic processes...
July 6, 2018: Environmental Pollution
Maia Thrift-Perry, Anna Cabanes, Fatima Cardoso, Katherine Moose Hunt, Tauane Araújo Cruz, Kyra Faircloth
Metastatic breast cancer (mBC) is an area with high unmet need across the world. Despite significant progress to meet patient need, current breast cancer (BC) policies fail to recognize the unique challenges of patients who are further along the cancer patient journey. This analysis aims to understand BC/mBC policy development at a global level and identify opportunities for further development. A comprehensive analysis of National Cancer Control Plans (NCCPs) policies and programs was conducted across 16 countries, which represent a diverse range of healthcare systems, economies and geographic regions...
June 18, 2018: Breast: Official Journal of the European Society of Mastology
Samira Yadamani, Ali Neamati, Masoud Homayouni-Tabrizi, S Ali Beyramabadi, Soheyla Yadamani, Azar Gharib, Ali Morsali, Maryam Khashi
The breast cancer is the most common type of cancer in women. In this project, the breast cancer was transplanted in vivo with the TUBO cells. Then, the cancerous mice were treated by radiation of low frequency electromagnetic fields and injection of the Mn(II) complex of the N,N'-dipyridoxyl(1,2-diaminobenzene) Schiff base. Three different concentrations of the Mn(II) complex were used. Cytotoxicity and morphological alterations caused by the Mn(II) complex in the TUBO breast cancer cell line have been evaluated...
July 11, 2018: Breast: Official Journal of the European Society of Mastology
Friederike Erdmann, Tengfei Li, George Luta, Brenda M Giddings, Guillermo Torres Alvarado, Eva Steliarova-Foucher, Joachim Schüz, Ana M Mora
BACKGROUND: Estimating childhood cancer incidence globally is hampered by a lack of reliable data from low- and middle-income countries. Costa Rica is one of the few middle-income countries (MIC) with a long-term high quality nationwide population-based cancer registry. METHODS: Data on incident cancers in children aged under 15 years reported to the Costa Rica National Cancer Registry between 2000 and 2014 were analyzed by diagnostic group, age, sex, and geographical region and compared with incidence data for Hispanic and Non-Hispanic White (NHW) children in California, USA...
July 16, 2018: Cancer Epidemiology
Carl Kilander, Jesper Lagergren, Rickard Ljung, Omid Sadr-Azodi
BACKGROUND: The incidence trends of biliary tract cancer need to be established. This study investigated the incidence and mortality of biliary tract cancer in Sweden in 1970-2010. METHODS: Sex-specific biliary tract cancer incidence and mortality rates were evaluated using data from the Swedish Cancer Register, Patient Register and Causes of Death Register. Case registration was separate for each register. Gallbladder cancer and cancers of the extra-hepatic bile ducts were analyzed separately...
July 16, 2018: Cancer Epidemiology
Raghav Sundar, Terri McVeigh, David Dolling, Ann Petruckevitch, Nikolaos Diamantis, Joo Ern Ang, Maxime Chenard-Poiriér, Dearbhaile Collins, Joline Lim, Malaka Ameratunga, Khurum Khan, Stan B Kaye, Udai Banerji, Juanita Lopez, Angela J George, Johann S de Bono, Winette T van der Graaf
BACKGROUND: Adolescent and young adult (AYA) patients with advanced solid tumours are often considered for phase I clinical trials with novel agents. The outcome of AYAs in these trials have not been described before. AIM: To study the outcome of AYA patients in phase I clinical trials. METHODS: Clinical trial data of AYAs (defined as aged 15-39 years at diagnosis) treated at the Drug Development Unit, Royal Marsden Hospital, between 2002 and 2016, were analysed...
July 16, 2018: European Journal of Cancer
Federica Alessandrini, Laura Pezzè, Daniel Menendez, Michael A Resnick, Yari Ciribilli
Breast cancer treatment often includes Doxorubicin as adjuvant as well as neoadjuvant chemotherapy. Despite its cytotoxicity, cells can develop drug resistance to Doxorubicin. Uncovering pathways and mechanisms involved in drug resistance is an urgent and critical aim for breast cancer research oriented to improve treatment efficacy. Here we show that Doxorubicin and other chemotherapeutic drugs induce the expression of ETV7, a transcriptional repressor member of ETS family of transcription factors. The ETV7 expression led to DNAJC15 down-regulation, a co-chaperone protein whose low expression was previously associated with drug resistance in breast and ovarian cancer...
July 16, 2018: Neoplasia: An International Journal for Oncology Research
Thanigaimalai Pillaiyar, Ewelina Gorska, Gregor Schnakenburg, Christa E Müller
Diindolylmethane (DIM) and its derivatives have recently been in the focus of interest due to their significant biological activities, specifically in cancer prevention and therapy. Molecular targets of DIM have been identified, e.g., the immuno-stimulatory G protein-coupled receptor GPR84. However, most of the reported and investigated DIM derivatives are symmetrical because general methods for obtaining unsymmetrical DIMs have been lacking. To optimize the interaction of DIM derivatives with their protein targets, unsymmetrical substitution is required...
July 19, 2018: Journal of Organic Chemistry
Song Xue, Xiaolei Gu, Jian Zhang, Huanli Sun, Chao Deng, Zhiyuan Zhong
Polypeptide micelles though having been proved to be an appealing nanoplatform for cancer chemotherapy are met with issues like inefficient drug encapsulation, gradual drug release, and/or low tumor cell selectivity and uptake. Here, we report on cRGD-decorated, small-sized, robust and reduction-responsive polytyrosine micelles (cRGD-rPTM) based on poly(ethylene glycol)-b-poly(L-tyrosine)-lipoic acid (PEG-b-PTyr-LA) conjugate for high loading and targeted delivery of doxorubicin (Dox). Notably, cRGD-rPTM exhibited efficient loading of Dox, giving cRGD-rPTM-Dox with a drug loading content (DLC) of 18...
July 19, 2018: Biomacromolecules
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