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https://www.readbyqxmd.com/read/28338292/rational-drug-design-of-indazole-based-diarylurea-derivatives-as-anticancer-agents
#1
Yan-Yan Chu, He-Juan Cheng, Zhenhua Tian, Jian-Chun Zhao, Gang Li, Yang-Yang Chu, Chang-Jun Sun, Wen-Bao Li
A series of novel indazole-based diarylurea derivatives targeting c-kit were designed by structure-based drug design. The derivatives were prepared and their antiproliferative activities were evaluated against human colon cancer HCT-116 cell line and hepatocellular carcinoma PLC/PRF/5 cell line. The antiproliferative activities demonstrated that six out of nine compounds exhibited comparable activities with Sorafenib against HCT-116. The structure-activity relationship (SAR) analysis indicated that the indazole ring part tolerated different kinds of substituents, the N position of the central pyridine ring played key roles in antiproliferative activity...
March 24, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28337333/efficient-semisynthesis-of-pseudoirroratin-a-from-flexicaulin-a-and-assessment-of-their-antitumor-activities
#2
Lei Guo, Siu Wai Tsang, Tong-Xin Zhang, Kang-Lun Liu, Yi-Fu Guan, Bo Wang, Han-Dong Sun, Hong-Jie Zhang, Man Shing Wong
Accumulating evidence indicates that natural ent-kaurane diterpenoids show great potential for medical treatment of different pathological conditions including cytotoxicity, antibacterial, and anti-inflammatory activity. Among a variety of diterpenoids tested, (-)-pseudoirroratin A displayed a promising antitumor property in vitro and in vivo. However, this diterpenoid could merely be isolated in a limited amount from a rare source of Isodon pseudoirrorata. To overcome such scanty source, we developed a novel, facile, and efficient semisynthetic strategy to prepare (-)-pseudoirroratin A from natural (-)-flexicaulin A, which can be expediently obtained from I...
March 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28335470/design-of-new-benzo-h-chromene-derivatives-antitumor-activities-and-structure-activity-relationships-of-the-2-3-positions-and-fused-rings-at-the-2-3-positions
#3
Rawda M Okasha, Fawzia F Alblewi, Tarek H Afifi, Arshi Naqvi, Ahmed M Fouda, Al-Anood M Al-Dies, Ahmed M El-Agrody
A series of novel 4H-benzo[h]chromenes 4, 6-11, 13, 14; 7H-benzo[h]chromeno[2,3-d]pyrimidines 15-18, 20, and 14H-benzo[h]chromeno[3,2-e][1,2,4]triazolo[1,5-c]pyrimidine derivatives 19a-e, 24 was prepared. The structures of the synthesized compounds were characterized on the basis of their spectral data. Some of the target compounds were examined for their antiproliferative activity against three cell lines; breast carcinoma (MCF-7), human colon carcinoma (HCT-116) and hepatocellular carcinoma (HepG-2). The cytotoxic behavior has been tested using MTT assay and the inhibitory activity was referenced to three standard anticancer drugs: vinblastine, colchicine and doxorubicin...
March 18, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28334277/in-bone-metastasis-mir-34a-5p-absence-inversely-correlates-with-met-expression-while-met-oncogene-is-unaffected-by-mir-34a-5p-in-non-metastatic-and-metastatic-breast-carcinomas
#4
Paola Maroni, Rossella Puglisi, Gianfranco Mattia, Alessandra Carè, Emanuela Matteucci, Paola Bendinelli, Maria Alfonsina Desiderio
The highlight of the molecular basis and therapeutic targets of the bone-metastatic process requires the identification of biomarkers of metastasis colonization. Here, we studied miR-34a-5p expression, and Met-receptor expression and localization in bone metastases from ductal breast carcinomas, and in ductal carcinomas without history of metastasis (20 cases). miR-34a-5p was elevated in non-metastatic breast carcinoma, intermediate in the adjacent tissue and practically absent in bone metastases, opposite to pair-matched carcinoma...
March 16, 2017: Carcinogenesis
https://www.readbyqxmd.com/read/28333601/simultaneous-occurrence-of-varicella-zoster-virus-induced-pancreatitis-and-hepatitis-in-a-renal-transplant-recipient-a-case-report-and-review-of-literature
#5
Puneet Chhabra, Priyadarshi Ranjan, Deepak K Bhasin
INTRODUCTION: Gastrointestinal complications are common after renal transplantation, including oral lesions, esophagitis, gastritis, diarrhea, and colon carcinoma. The differential diagnosis is difficult in this scenario because multiple factors such as drugs, infections, and preexisting gastrointestinal disease come into play. CASE PRESENTATION: We report a case of varicella zoster virus-induced pancreatitis and hepatitis in a renal transplant recipient. The patient underwent renal transplantation 3 years earlier and now presented with severe pain in the epigastrium radiating to his back and had raised serum lipase levels and skin lesions characteristic of varicella...
2017: Permanente Journal
https://www.readbyqxmd.com/read/28333202/risk-of-rectal-neoplasia-after-colectomy-and-ileorectal-anastomosis-for-ulcerative-colitis
#6
Mathieu Uzzan, Julien Kirchgesner, Nadia Oubaya, Aurélien Amiot, Jean-Marc Gornet, Philippe Seksik, Stéphane Nancey, Eddy Cotte, Matthieu Allez, Gilles Boschetti, David Laharie, Nicola de Angelis, Maria Nachury, Anne-Laure Pelletier, Vered Abitbol, Mathurin Fumery, Antoine Brouquet, Anthony Buisson, Romain Altwegg, Jacques Cosnes, Yves Panis, Xavier Treton
Introduction-: Colectomy can be required in the management of ulcerative colitis (UC). While ileal pouch anal-anastomosis (IPAA) is the recommended reconstruction technique, ileorectal anastomosis (IRA) is still performed and might present some advantages. However, the risk of rectal neoplasia might limit its indication. The aims of our study were to determine the incidence of rectal neoplasias following IRA for UC and to identify risk factors associated with rectal carcinomas. Methods-: We performed a multicenter retrospective study including patients who underwent IRA for UC from 1960 to 2014 in 13 centers...
February 21, 2017: Journal of Crohn's & Colitis
https://www.readbyqxmd.com/read/28332760/cytotoxic-essential-oils-from-eryngium-campestre-and-eryngium-amethystinum-apiaceae-growing-in-central-italy
#7
Kevin Cianfaglione, Evy E Blomme, Luana Quassinti, Massimo Bramucci, Giulio Lupidi, Stefano Dall'Acqua, Filippo Maggi
Eryngium campestre and E. amethystinum are thorny herbs belonging to the Apiaceae family and spontaneously growing in stony pastures and dry meadows, preferentially on calcareous substrates. In the Mediterranean countries, these plants have been used as a food or traditional remedies to treat various ailments. In the present work, we have analysed the chemical composition of the essential oils distilled from the aerial parts by GC-FID and GC-MS, and evaluated their cytotoxic effects on a panel of human cancer cells, namely A375 (human malignant melanoma), MDA-MB 231 cells (human breast adenocarcinoma) and HCT116 cells (human colon carcinoma), by the MTT assay...
March 23, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/28331349/antibiotic-resistance-among-helicobacter-pylori-clinical-isolates-in-lima-peru
#8
Kevin F Boehnke, Manuel Valdivieso, Alejandro Bussalleu, Rachael Sexton, Kathryn C Thompson, Soledad Osorio, Italo Novoa Reyes, John J Crowley, Laurence H Baker, Chuanwu Xi
OBJECTIVES: Gastric carcinoma is the most common cancer and cause of cancer mortality in Peru. Helicobacter pylori, a bacterium that colonizes the human stomach, is a Group 1 carcinogen due to its causal relationship to gastric carcinoma. While eradication of H. pylori can help prevent gastric cancer, characterizing regional antibiotic resistance patterns is necessary to determine targeted treatment for each region. Thus, we examined primary antibiotic resistance in clinical isolates of H...
2017: Infection and Drug Resistance
https://www.readbyqxmd.com/read/28331341/investigating-the-expression-effect-and-tumorigenic-pathway-of-padi2-in-tumors
#9
Wei Guo, Yabing Zheng, Bing Xu, Fang Ma, Chang Li, Xiaoqian Zhang, Yao Wang, Xiaotian Chang
BACKGROUND: Peptidylarginine deiminase (PAD) catalyzes the conversion of arginine residues to citrulline residues, termed citrullination. Recent studies have suggested that PAD isoform 2 (PADI2) plays an important role in tumors, although its tumorigenic effect and mechanism are largely unknown. MATERIALS AND METHODS: Immunohistochemistry and enzyme-linked immunosorbent assay (ELISA) were used to investigate the expression level of PADI2 in various tumor tissues and patient blood samples, respectively...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/28330602/the-pneumococcal-alpha-glycerophosphate-oxidase-enhances-nasopharyngeal-colonization-through-binding-to-host-glycoconjugates
#10
Layla K Mahdi, Melanie A Higgins, Christopher J Day, Joe Tiralongo, Lauren E Hartley-Tassell, Michael P Jennings, David L Gordon, Adrienne W Paton, James C Paton, Abiodun D Ogunniyi
Streptococcus pneumoniae (the pneumococcus) is a major human pathogen, causing a broad spectrum of diseases including otitis media, pneumonia, bacteraemia and meningitis. Here we examined the role of a potential pneumococcal meningitis vaccine antigen, alpha-glycerophosphate oxidase (SpGlpO), in nasopharyngeal colonization. We found that serotype 4 and serotype 6A strains deficient in SpGlpO have significantly reduced capacity to colonize the nasopharynx of mice, and were significantly defective in adherence to human nasopharyngeal carcinoma cells in vitro...
March 3, 2017: EBioMedicine
https://www.readbyqxmd.com/read/28329636/correlation-between-cancer-incidences-and-google-searches-in-the-united-states
#11
Mackenzie R Wehner, Kevin T Nead, Eleni Linos
IntroductionDespite being highly prevalent, keratinocyte carcinomas (basal cell and squamous cell carcinomas lack nationwide registries. Internet search data has emerged as a new method to evaluate previously difficult to quantify public health outcomes and may be useful in keratinocyte carcinoma research.ObjectiveWe aimed to evaluate whether Google search density correlated with known incidences of common cancers in the United States.MethodsWe used the Center for Disease Control's National Program of Cancer Registries ageTadjusted cancer incidences (2008T2012 ...
September 15, 2016: Dermatology Online Journal
https://www.readbyqxmd.com/read/28328969/oral-tegafur-uracil-as-metronomic-therapy-following-intravenous-folfox-for-stage-iii-colon-cancer
#12
Wen-Yen Huang, Ching-Liang Ho, Chia-Cheng Lee, Cheng-Wen Hsiao, Chang-Chieh Wu, Shu-Wen Jao, Jen-Fu Yang, Cheng-Hsiang Lo, Jia-Hong Chen
The purpose of this study was to estimate the impact of metronomic therapy with oral tegafur-uracil (UFUR) following an intravenous FOLFOX regimen as surgical adjuvant chemotherapy on the overall survival (OS) and disease-free survival (DFS) of stage III colon cancer patients. From the retrospective database of patients who underwent a surgical resection for colorectal cancer at the Tri-Service General Hospital from October 2008 through December 2014, stage III colon carcinomas treated with radical R0 resection were reviewed...
2017: PloS One
https://www.readbyqxmd.com/read/28327550/significant-role-of-collagen-xvii-and-integrin-%C3%AE-4-in-migration-and-invasion-of-the-less-aggressive-squamous-cell-carcinoma-cells
#13
Jyri M Moilanen, Stefanie Löffek, Nina Kokkonen, Sirpa Salo, Juha P Väyrynen, Tiina Hurskainen, Aki Manninen, Pilvi Riihilä, Ritva Heljasvaara, Claus-Werner Franzke, Veli-Matti Kähäri, Tuula Salo, Markus J Mäkinen, Kaisa Tasanen
Collagen XVII and integrin α6β4 have well-established roles as epithelial adhesion molecules. Their binding partner laminin 332 as well as integrin α6β4 are largely recognized to promote invasion and metastasis in various cancers, and collagen XVII is essential for the survival of colon and lung cancer stem cells. We have studied the expression of laminin γ2, collagen XVII and integrin β4 in tissue microarray samples of squamous cell carcinoma (SCC) and its precursors, actinic keratosis and Bowen's disease...
March 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28327343/astilbin-from-engelhardtia-chrysolepis-enhances-intestinal-barrier-functions-in-caco-2-cell-monolayers
#14
Tatsuo Nakahara, Yosuke Nishitani, Shin Nishiumi, Masaru Yoshida, Takeshi Azuma
Astilbin, which is one of polyphenolic compounds isolated from the leaves of Engelhardtia chrysolepis HANCE (Chinese name, huang-qui), is available as the effective component in food and cosmetics because of its anti-oxidant and anti-inflammatory effects. The tight junction (TJ) proteins, which protect the body from foreign substances, are related to adhesion between a cell and a cell. Previously, the enhancement of TJ's functions induced by aglycones of flavonoids has been demonstrated, but the effects of the glycosides such as astilbin have not been observed yet...
March 18, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28327179/pterostilbene-prevents-akt-erk-axis-mediated-polymerization-of-surface-fibronectin-on-suspended-lung-cancer-cells-independently-of-apoptosis-and-suppresses-metastasis
#15
Ying-Jan Wang, Jing-Fang Lin, Li-Hsin Cheng, Wen-Tsan Chang, Ying-Hsien Kao, Ming-Min Chang, Bour-Jr Wang, Hung-Chi Cheng
BACKGROUND: Polymeric fibronectin (polyFN) assembled on suspended breast cancer cells is required for metastasis. Conceivably, drugs that target such polyFN may fight against cancer metastasis. While stilbene analogs trigger pro-apoptotic effect on attached cancer cells, whether they prevent polyFN assembly and metastasis of suspended cancer cells via an apoptosis-independent manner remains unexplored. METHODS: We depleted suspended Lewis lung carcinoma (LLC) cells of polyFN by silencing the endogenous FN expression or pterostilbene (PS) to examine whether metastasis of lung cancer cells could thus be suppressed...
March 21, 2017: Journal of Hematology & Oncology
https://www.readbyqxmd.com/read/28327152/trim8-restores-p53-tumour-suppressor-function-by-blunting-n-myc-activity-in-chemo-resistant-tumours
#16
Francesca Mastropasqua, Flaviana Marzano, Alessio Valletti, Italia Aiello, Giuseppe Di Tullio, Annalisa Morgano, Sabino Liuni, Elena Ranieri, Luisa Guerrini, Giuseppe Gasparre, Elisabetta Sbisà, Graziano Pesole, Antonio Moschetta, Mariano Francesco Caratozzolo, Apollonia Tullo
BACKGROUND: TRIM8 plays a key role in controlling the p53 molecular switch that sustains the transcriptional activation of cell cycle arrest genes and response to chemotherapeutic drugs. The mechanisms that regulate TRIM8, especially in cancers like clear cell Renal Cell Carcinoma (ccRCC) and colorectal cancer (CRC) where it is low expressed, are still unknown. However, recent studies suggest the potential involvement of some microRNAs belonging to miR-17-92 and its paralogous clusters, which could include TRIM8 in a more complex pathway...
March 21, 2017: Molecular Cancer
https://www.readbyqxmd.com/read/28326211/early-onset-signet-ring-cell-adenocarcinoma-of-the-colon-a-case-report-and-review-of-the-literature
#17
Maliha Khan, Krittiya Korphaisarn, Aneeqa Saif, Wai C Foo, Scott Kopetz
Colorectal cancer (CRC) remains the second leading cause of cancer-related deaths in the United States. While a decline has been observed in the older population, the occurrence of CRC in the adolescent and young adult (AYA) population has increased over the past two decades. The histopathologic characteristics and clinical behavior of CRC in AYA patients have been shown to be distinct from those of CRC in older adults. The rarer subtypes of CRC such as mucinous adenocarcinoma and signet-ring cell carcinoma are associated with a poorer prognosis compared to the more common subtypes...
2017: Case Reports in Oncological Medicine
https://www.readbyqxmd.com/read/28325827/sessile-serrated-polyps-and-colon-cancer-prevention
#18
Shahrooz Rashtak, Rafaela Rego, Seth R Sweetser, Frank A Sinicrope
Evidence suggests that up to one fifth of colorectal carcinomas (CRC) develop from serrated polyps, named for their pattern of colonic crypts, and include the sessile serrated adenoma/polyp (SSA/P) that has malignant potential. SSA/Ps are typically located in the proximal colon and have molecular features of hypermethylation of CpG islands in gene promoters and activating point mutations (V600E) in the BRAF oncogene. Both of these features are seen in sporadic CRCs with microsatellite instability (MSI) which is potentially consistent with an origin of these cancers from precursor SSA/Ps...
March 21, 2017: Cancer Prevention Research
https://www.readbyqxmd.com/read/28325058/-mixed-adenoneuroendocrine-carcinoma-manec-of-the-gastrointestinal-tract
#19
R Šefr, L Němec, P Fabian, L Fiala
Mixed adenoneuroendocrine carcinoma (MANEC) is a rare tumour of the gastrointestinal tract composed of adenocarcinoma and neuroendocrine carcinoma. This pathologic diagnosis was recently defined by the WHO in 2010. The tumour may appear in various levels of the digestive tract including the oesophagus, stomach, colon and appendix. Biological behaviour of MANEC seems to be quite unpredictable and the prognosis uncertain. The disease may also mimic "simple" carcinoma. Only several tens of cases have been reported so far...
2017: Rozhledy V Chirurgii: Měsíčník Československé Chirurgické Společnosti
https://www.readbyqxmd.com/read/28325052/-colorectal-cancer-the-importance-of-primary-tumor-location
#20
M Ryska, J Bauer
Retrospective evaluations of the relevance of primary colorectal cancer (CRC) location consistently indicate that right-sided tumors, arising in the cecum, ascending colon, hepatic bend, transverse colon and splenic flexure, are clinically, biologically and genetically different from left-sided tumors - those located in the descending colon, sigmoid colon or rectum. Location in the right-sided colon represents a negative prognostic indicator, particularly for stage III and IV carcinomas. Irrespective of treatment, the rightward location is associated with a significantly increased risk of death when compared to the left side...
2017: Rozhledy V Chirurgii: Měsíčník Československé Chirurgické Společnosti
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