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Fengyuan Che, Xiaoli Xie, Long Wang, Quanping Su, Feiyu Jia, Yufu Ye, Lanlan Zang, Jing Wang, Hongyan Li, Yanchun Quan, Cuiping You, Jiawei Yin, Zhiqiang Wang, Gen Li, Yifeng Du, Lijuan Wang
Although great progress has been made in treatment regimens, gliomas are still incurable and the 5-year survival remains poor. Studies focusing on molecules that regulate tumorigenesis or tumor immunity may provide potential therapeutic strategies for patients with glioma. B7-H6 is selectively expressed in tumor cells and plays vital roles in host immune responses. In this study, we demonstrated that B7-H6 was expressed in glioma cell lines, including CRT, U251, SHG-44, SF-295, TG-905 and U373, and tumor tissues isolated from glioma patients...
April 18, 2018: International Immunopharmacology
Xin Chen, Deheng Li, Yang Gao, Yiqun Cao, Bin Hao
Gliomas are the most common brain tumors of the central nervous system. In this study, we investigated the molecular mechanisms and biological function of SIRT6 in human gliomas. The expression levels of SIRT6 in glioma tissues and cells were analyzed by qRT-PCR and western blot analysis. CCK8 and clonogenicity assays were performed to detect the cell proliferation. Furthermore, the migration and invasion of glioma cells were examined by transwell assays. It was found that the expression of SIRT6 was significantly lower in human glioma tissues or cell lines compared with the normal brain tissue or NHA...
April 1, 2018: Acta Biochimica et Biophysica Sinica
Rui Fu, Yan Ding, Jie Luo, Kuan Ming Huang, Xiang Jun Tang, Dong Sheng Li, Shi Wen Guo
Ten-eleven translocation 1 catalyzes the conversion of 5-methylcytosine (5mC) to 5-hydroxymethylcytosine (5hmC), which plays an important role in epigenetics and is related to the malignant biological behavior of tumors. However, its regulatory role in glioma remains unclear. In this study, the levels of 5mC and 5hmC were detected using immunohistochemistry, dot-blot, hMeDIP-chip, and western blot in glioma tissues and normal brain tissues, whereas 5hmC differentially enriched genes were determined and further validated...
April 13, 2018: Neuroreport
Yaoqi Ge, Yuejiao Zhong, Guozhong Ji, Qianling Lu, Xinyu Dai, Zhirui Guo, Peng Zhang, Gang Peng, Kangzhen Zhang, Yuntao Li
OBJECTIVE: To study the characterization of Fe3O4@Au-C225 composite targeted MNPs. METHODS: Fe3O4@Au-C225 was prepared by the absorption method. The immunosorbent assay was used to evaluate its absorption efficiency at C225 Fc. ZETA SIZER3000 laser particle size analyzer, ultraviolet photometer and its characteristics were analyzed by VSM. the targeting effect of Fe3O4@Au-C225 composite targeted MNPs on U251 cells in vitro were detected by 7.0 Tesla Micro-MR; and subcutaneous transplanted human glioma in nude mice were performed the targeting effect in vivo after tail vein injection of Fe3O4@Au-C225 composite targeted MNPs by MRI...
2018: PloS One
Tereza Cristina Costa Silva, Noelio de Jesus Menezes-Filho, Giselle Pinto de Faria Lopes, Diego Madureira de Oliveira, Ezequiel Pereira, Bruno Penas Seara Pitanga, Eudes S Velozo, Songeli Menezes Freire, Jorge Clarencio de Souza Andrade, Helena Lobo Borges, Stevens Kastrup Rehen, Vivaldo Moura-Neto, Silvia Lima Costa
A glioblastoma is a primary CNS tumor that is more aggressive and lethal than other brain tumors. Its location, rapid proliferation, invasive growth, angiogenesis and immunosuppression are the main factors that limit its treatment, making it a major challenge to neuro-oncology. OBJECTIVE: This study investigated the in vitro effects of the alkaloid dihydrochelerythrine (DHC), which is extracted from Zanthoxylum stelligerum, on the viability, proliferation, cell death and b-catenin, NFkB, STAT3/pSTAT3 and interleukins roles...
April 12, 2018: Anti-cancer Agents in Medicinal Chemistry
Halh Al-Serori, Franziska Ferk, Michael Kundi, Andrea Bileck, Christopher Gerner, Miroslav Mišík, Armen Nersesyan, Monika Waldherr, Manuel Murbach, Tamara T Lah, Christel Herold-Mende, Andrew R Collins, Siegfried Knasmüller
Some epidemiological studies indicate that the use of mobile phones causes cancer in humans (in particular glioblastomas). It is known that DNA damage plays a key role in malignant transformation; therefore, we investigated the impact of the UMTS signal which is widely used in mobile telecommunications, on DNA stability in ten different human cell lines (six brain derived cell lines, lymphocytes, fibroblasts, liver and buccal tissue derived cells) under conditions relevant for users (SAR 0.25 to 1.00 W/kg)...
2018: PloS One
Jun-Bo Gao, Xing-Jie Zhang, Rui-Han Zhang, Li-Li Zhu, De-Bing Pu, Xiao-Li Li, Hong-Lin Li, Min Xu, Wei-Lie Xiao
Four new dolabellane-type diterpene alkaloids, glandulamines A - D (1:  - 4: ), together with twelve known compounds (5:  - 16: ), were isolated from the seeds of Nigella glandulifera using repeated column chromatography and semipreparative HPLC. The structures of 1:  - 16: were elucidated based on NMR data analysis, HRMS experiments and other spectroscopic interpretations. The absolute configuration of 5: was determined by single-crystal X-ray diffraction data for the first time. Compounds 10: and 12: showed human dihydroorotate dehydrogenase inhibitory activity with IC50 values of 61...
April 5, 2018: Planta Medica
Viviana P Ribeiro, Joana Silva-Correia, Cristiana Gonçalves, Sandra Pina, Hajer Radhouani, Toni Montonen, Jari Hyttinen, Anirban Roy, Ana L Oliveira, Rui L Reis, Joaquim M Oliveira
Timely and spatially-regulated injectable hydrogels, able to suppress growing tumors in response to conformational transitions of proteins, are of great interest in cancer research and treatment. Herein, we report rapidly responsive silk fibroin (SF) hydrogels formed by a horseradish peroxidase (HRP) crosslinking reaction at physiological conditions, and demonstrate their use as an artificial biomimetic three-dimensional (3D) matrix. The proposed SF hydrogels presented a viscoelastic nature of injectable hydrogels and spontaneous conformational changes from random coil to β-sheet conformation under physiological conditions...
2018: PloS One
Sarfaraz Alam, Feroz Khan
Caged xanthones are bioactive compounds mainly derived from the Garcinia genus. In this study, a structure-activity relationship (SAR) of caged xanthones and their derivatives for anticancer activity against different cancer cell lines such as A549, HepG2 and U251 were developed through quantitative (Q)-SAR modeling approach. The regression coefficient (r2 ), internal cross-validation regression coefficient (q2 ) and external cross-validation regression coefficient (pred_r2 ) of derived QSAR models were 0.87, 0...
April 3, 2018: Scientific Reports
Nathalie Hinfray, Cleo Tebby, Benjamin Piccini, Gaelle Bourgine, Sélim Aït-Aïssa, Jean-Marc Porcher, Farzad Pakdel, François Brion
Comprehension of compound interactions in mixtures is of increasing interest to scientists, especially from a perspective of mixture risk assessment. However, most of conducted studies have been dedicated to the effects on gonads, while only few of them were. interested in the effects on the central nervous system which is a known target for estrogenic compounds. In the present study, the effects of estradiol (E2), a natural estrogen, and genistein (GEN), a phyto-estrogen, on the brain ER-regulated cyp19a1b gene in radial glial cells were investigated alone and in mixtures...
April 1, 2018: International Journal of Molecular Sciences
Xiaohong Zhang, Zhujun Liu, Zhichao Lou, Feng Chen, Shuquan Chang, Yuji Miao, Zhuo Zhou, Xiaodan Hu, Jundong Feng, Qi Ding, Peidang Liu, Ning Gu, Haiqian Zhang
Radiotherapy is one of the main therapeutic methods for cancers, but radiation resistance of cancer cells still remains a serious concern. Searching for radiosensitizers to overcome such resistance is therefore urgently required. The goal of this study is to evaluate and compare the radiosensitizing efficacy of Fe3 O4 -OA, Ag and Fe3 O4 @Ag nanoparticles on U251 cells. The results show that Fe3 O4 @Ag nanoparticles have the highest ability of radiosensitization among the three nanoparticles. The underlying mechanism of Fe3 O4 @Ag nanoparticles' radiosensitivity enhancement is through decrease of the cytoprotective autophagy at the early stage, and increase of the calcium-dependent apoptosis at the later stage...
April 3, 2018: Artificial Cells, Nanomedicine, and Biotechnology
Thomas Nittoli, Marcus P Kelly, Frank Delfino, John Rudge, Arthur Kunz, Thomas Markotan, Jan Spink, Zhaoyuan Chen, Jing Shan, Elizabeth Navarro, Michele Tait, Kathleen Provoncha, Jason Giurleo, Feng Zhao, Xiaobo Jiang, Donna Hylton, Sosina Makonnen, Carlos Hickey, Jessica R Kirshner, Gavin Thurston, Nicholas Papadopoulos
Natural products have been used for many medicinal purposes for centuries. Antibody drug conjugates (ADCs) have utilized this rich source of small molecule therapeutics to produce several clinically useful treatments. ADCs based on the natural product maytansine have been successful clinically. The authors further the utility of the anti-cancer natural product maytansine by developing efficacious payloads and linker-payloads for conjugating to antibodies. The success of our approach was realized in the EGFRvIII targeting ADC EGFRvIII-16...
February 21, 2018: Bioorganic & Medicinal Chemistry
Xiong Weng, Shun-Qin Zhu, Hong-Juan Cui
Glioblastoma is a common brain tumor and the overall survival rate of the patients is very low, so it is an effective way to develop the potential chemotherapy or adjuvant chemotherapy drugs in glioblastoma treatment. As a well-known antimalarial drug, artesunate(ARTs) has clear side effects, and recently it has been reported to have antitumor effects, but rarely reported in glioblastoma. Different concentrations of ARTs were used to treat the glioblastoma cells, and then the inhibitory effect of ARTs on glioblastoma proliferation was detected by MTT assay; Ki67 immunofluorescence assay was used to detect the proliferation of cells; Soft agar experiment was used to explain the clonal formation abilities in vitro ; Flow Cytometry was used to detect the cell cycle; and Western blot assay was used to determine the expression of key cell cycle protein...
February 2018: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Bing Yang, Xiaobo Li, Lu He, Yu Zhu
Despite the development of temozolomide (TMZ), a novel type of glioma therapeutic drug, malignant glioma remains to cause severe damage to human health. The present study aimed to utilize the molecular biological differences between tumor and normal cells to design TMZ derivatives with improved selectivity and targeting using computer-aided drug design (CADD). Taking alkylglycerone phosphate synthase (AGPS) as a target, a 3D structure-activity relationship model was built using CADD technology; molecular docking of isothiocyanate (ITC) and TMZ compounds was conducted; ITC-TMZ derivatives were designed; and predictions on the absorption, distribution, metabolism and excretion (ADME) processes and toxicity of the ITC-TMZ derivatives were established in order to obtain improved understanding of the structure-activity relationship of the candidate compounds...
March 2018: Biomedical Reports
Tao-Ran Li, Yan-Jie Jia, Chao Ma, Wen-Ying Qiu, Qun Wang, Xiao-Qiu Shao, Rui-Juan Lv
Increasing evidence indicates that neuroinflammation plays a crucial role in the pathogenesis of temporal lobe epilepsy (TLE). However, it is unclear how the perpetuate inflammation develops. Some recent studies have suggested the possible involvement of microRNA-146a (miR-146a) in the modulation of inflammatory signaling occurring in TLE. To understand how miR-146a modulates inflammatory signaling in TLE, we investigated the role of interleukin-1β (IL-1β), miR-146a and human complement factor H (CFH) in the perpetuate inflammation in rat models of chronic TLE and U251 cells...
March 23, 2018: Disease Models & Mechanisms
Josipa Matić, Irena Nekola, Aleksandar Višnjevac, Renata Kobetić, Irena Martin-Kleiner, Marijeta Kralj, Biserka Žinić
A fast and efficient route for the introduction of a methylene bridged-amine (morpholinomethyl) functionality in the C5 position of the sulfonylated cytosine nucleobase has been developed. First, novel N1-sulfonylcytosine derivatives 3-6 were prepared by the condensation of silylated cytosine with selected sulfonyl chlorides. They were subsequently transformed to 5-morpholinomethyl-N1-sulfonylcytosine derivatives (8, 12-15) using microwave irradiation. As a result of cytosine ring opening in N1-tosylcytosine, depending on the reaction conditions, peculiar tosyl-urea derivative 9 has been isolated, which provided additional insight into the reaction pathway...
March 26, 2018: Organic & Biomolecular Chemistry
Jae-Uk Jeong, Tung Nguyen Thanh Uong, Woong-Ki Chung, Taek-Keun Nam, Sung-Ja Ahn, Ju-Young Song, Sang-Ki Kim, Dong-Jun Shin, Eugene Cho, Kyoung Won Kim, Duck Cho, Mee Sun Yoon
BACKGROUND AIMS: Irradiation enhances the adhesion between natural killer (NK) cells and target cells by up-regulating intercellular adhesion molecule-1 (ICAM-1) on target cells. Therefore, we investigated the effect of irradiation-induced ICAM-1 expression on human cancer cells on NK cell-mediated cytotoxicity. METHODS: Expression levels of ICAM-1 on the target cell surface before and after irradiation of six human cancer cell lines (HL60, SKBR-3, T47D, HCT-116, U937 and U251) were analyzed by flow cytometry...
March 20, 2018: Cytotherapy
Xin Zhang, Xuehai Wang, Ran Xu, Jianxiong Ji, Yangyang Xu, Mingzhi Han, Yuzhen Wei, Bin Huang, Anjing Chen, Qing Zhang, Wenjie Li, Jian Wang, Xingang Li, Chen Qiu
BACKGROUND: Radiotherapy constitutes a standard arm of therapy in the multimodal treatment of patients with glioblastoma (GBM). Ironically, studies have recently revealed that radiation can augment malignant progression, by promoting migration and invasion, which make the disease especially difficult to cure. Here, we investigated the anticancer effects of YM155, a purported radiosensitizer, in GBM cell lines. METHODS: GBM cell lines U251 and U87 were treated with YM155 to assess cytotoxicity and activity of the molecule in vitro...
March 23, 2018: Journal of Translational Medicine
Zhanhui Du, Xiuxiang Song, Fangfang Yan, Jingjing Wang, Yuxia Zhao, Shangming Liu
Bromodomain containing 4 (BRD4), a member of the bromodomain and extra-terminal family, has become a promising drug target for numerous types of cancer. BRD4 has been reported to be deregulated in gliomas; however, the precise molecular pathways regulated by BRD4 remained elusive. In the present study, BRD4 expression was silenced in the glioma cell line U251 and the results demonstrated that BRD4 knockdown attenuated cell proliferation and promoted cell apoptosis. A genome-wide analysis of BRD4-regulated transcripts in U251 cells was performed using microarray to reveal the possible molecular mechanism...
March 16, 2018: International Journal of Oncology
Wei Jia, Xingjun Jiang, Weidong Liu, Lei Wang, Bin Zhu, Hecheng Zhu, Xingdong Liu, Meizuo Zhong, Dan Xie, Wei Huang, Wenting Jia, Shasha Li, Xuxu Liu, Xiang Zuo, Damei Cheng, Jianwu Dai, Caiping Ren
Three-dimensional (3D) culture has been increasingly used to investigate tumor cell biology for improved simulation of the natural developing environment. However, the way in which 3D culture affects the gene expression and biological functions of glioma cells remains to be fully elucidated. In the present study, 3D culture environments were established using collagen scaffolds with different pore sizes, followed by the comparison of gene expression profiles and associated biological functions of glioma cells, including the U87, U251 and HS683 cell lines, in 3D collagen scaffolds with conventional two-dimensional (2D) cultured cells...
March 20, 2018: International Journal of Oncology
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