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https://www.readbyqxmd.com/read/28239957/activating-transcription-factor-3-promotes-malignance-of-lung-cancer-cells-in-vitro
#1
Xuebing Li, Xuexia Zhou, Yongwen Li, Lingling Zu, Hongli Pan, Boning Liu, Wang Shen, Yaguang Fan, Qinghua Zhou
BACKGROUND: Lung cancer remains the most common cause of cancer-related death, with high rates of recurrence and poor outcomes. An abnormally high expression of activating transcription factor 3 (ATF3) in various cancers suggests an oncogenic role; however, its function in lung cancer is largely unknown. METHODS: Sixty-four pairs of lung cancer tissues were collected for ATF3 expression analysis by quantitative real-time PCR, immunoblotting, and immunohistochemistry staining...
February 27, 2017: Thoracic Cancer
https://www.readbyqxmd.com/read/28238782/vaccination-efficacy-with-marrow-mesenchymal-stem-cell-against-cancer-was-enhanced-under-simulated-microgravity
#2
Jing Li, Jun Chen, Xiuyu Li, Yanfang Qian
Stem cell vaccination can induce consistent and strong anti-tumor immunity against cancer in mice model. The antigenic similarity between tumors and embryos has been appreciated for many years and reflects the expression of embryonic gene products by cancer cells and/or cancer-initiating stem cells. Taking advantage of this similarity, we have tested a prophylactic lung cancer vaccine composed of allogeneic murine MSCs. Based on this conception, we first compared their tumor vaccines intervention effects of adult MSCs and MSCs under simulated microgravity (MSC/SMG)...
February 24, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28238614/synthesis-and-in-vitro-biological-evaluation-of-novel-quinazoline-derivatives
#3
Yaling Zhang, Ying Zhang, Juan Liu, Li Chen, Lijun Zhao, Baolin Li, Wei Wang
A series of novel 4-arylamino-6-(5-substituted furan-2-yl)quinazoline derivatives were designed, synthesized and evaluated on biological activities in vitro. Compound 2a, 3a and 3c exhibited highly anti-proliferation activities on all tested tumor cell lines including SW480, A549, A431 and NCI-H1975 cells. Especially, compound 2a not only exhibited strong anti-proliferation activities against the tumor cell lines which expressed wild type or mutant EGFR(L858R/T790M), but also showed the most potent inhibitory activity toward wild type EGFR (IC50=5...
February 16, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28237794/combination-of-amino-acid-dipeptide-with-ligustrazine-betulinic-acid-as-antitumor-agents
#4
Bing Xu, Wen-Qiang Yan, Xin Xu, Gao-Rong Wu, Chen-Ze Zhang, Yao-Tian Han, Fu-Hao Chu, Rui Zhao, Peng-Long Wang, Hai-Min Lei
The lead compound TBA, 3β-Hydroxy-lup-20(29)-ene-28-oic acid-3, 5, 6-trimethylpyrazin-2-methyl ester, which exhibited promising antitumor activity and induced tumor cell apoptosis in various cancer cell lines, had previously been reported. Moreover, reports have revealed that the introduction of amino acid to betulinic acid could improve selective cytotoxicity as well as water solubility. Thus, a series of novel TBA amino acid and dipeptide derivatives were designed, synthesized and screened for selective cytotoxic activity against five cancer cell lines (HepG2, HT-29, Hela, BCG-823 and A549) and the not malignant cell line MDCK by standard MTT assay...
February 17, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28237792/facile-and-efficient-access-to-androsten-17-1-3-4-pyrazoles-and-androst-17%C3%AE-1-3-4-pyrazoles-via-vilsmeier-reagents-and-their-antiproliferative-activity-evaluation-in%C3%A2-vitro
#5
Jian Li, Haibo Huo, Rui Guo, Biao Liu, Longbo Li, Wenjia Dan, Xinmin Xiao, Jiwen Zhang, Baojun Shi
In this work, twenty-seven novel steroidal pyrazole derivatives were designed and effectively synthesized with two different commercially available staring material, Isopregnanolone 1 and 5,16-Pregnadienolone 7, via the key intermediates, 17β-(4'-formyl)pyrazolylandrost-3β-yl formate and 17-(4'-formyl)pyrazolylandrost- 5,16-dienes-3β-yl formate, which were obtained from the cyclization of steroidal phenylhydrazone with Vilsmeier reagent catalyzed by phosphorous oxychloride followed by hydrolysis, then Borch reduction to afford the target derivatives under mild conditions...
February 20, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28237662/the-derivatives-of-pulsatilla-saponin-a-a-bioactive-compound-from-pulsatilla-chinensis-their-synthesis-cytotoxicity-haemolytic-toxicity-and-mechanism-of-action
#6
Xiaohang Tong, Li Han, Huaqing Duan, Yaru Cui, Yulin Feng, Yongming Zhu, Zhong Chen, Shilin Yang
The strong haemolytic toxicity of Pulsatilla saponin A (PSA) has hampered its clinical development as an injectable anticancer agent. To circumvent this challenge, twenty PSA derivatives with C ring or C-28 or C-3 modifications were synthesized and evaluated for cytotoxicity against seven selected human tumor lines, as well as for haemolytic toxicity. Structure-activity relationship (SAR) and structure-toxicity relationship (STR) correlations were also elucidated. Compared with PSA, compound 22 showed a better balance between haemolytic toxicity (HD50 > 500 μM) and cytotoxicity toward lung cancer cells A549 (IC50 = 4...
February 15, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28236246/rgd-and-ngr-modified-trail-protein-exhibited-potent-anti-metastasis-effects-on-trail-insensitive-cancer-cells-in-vitro-and-in-vivo
#7
Xiaofei Wang, Xinran Qiao, Yue Shang, Shenghua Zhang, Yi Li, Hongwei He, Shu-Zhen Chen
The tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) has been considered to be a promising anti-tumor agent since the discovery of TRAIL-mediated apoptosis specifically on cancer cells. However, TRAIL resistance of tumor cells and patients remains to be an insurmountable obstacle for its clinical application. Here, we expressed TRAIL-related recombinant protein RGD-TRAIL, TRAIL-NGR, and RGD-TRAIL-NGR by fusing tumor targeting peptides RGD and (or) NGR at the N-terminus and C-terminus, respectively, to not only induce apoptosis of cancer cells but also inhibit metastasis...
February 24, 2017: Amino Acids
https://www.readbyqxmd.com/read/28235701/design-synthesis-and-biological-evaluation-of-imidazo-1-2-b-pyridazine-derivatives-as-mtor-inhibitors
#8
Beibei Mao, Shanyun Gao, Yiran Weng, Liangren Zhang, Lihe Zhang
ATP-competitive mTOR inhibitors have been studied as potential antitumor agents. Based on the structure-activity relationship of known mTOR inhibitors, a series of novel imidazo[1,2-b]pyridazine derivatives were synthesized and characterized. The anti-proliferative activities of these compounds were evaluated by SRB assay against six human cancer cell lines. Imidazo[1,2-b]pyridazine diaryl urea derivatives A15-A24 exhibited significant anti-proliferative activity especially against non-small cell lung cancer A549 and H460 with IC50 values ranging from 0...
February 9, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28235607/the-preparation-of-three-selenium-containing-cordyceps-militaris-polysaccharides-characterization-and-anti-tumor-activities
#9
Fei Liu, Zhen-Yuan Zhu, Xiaoli Sun, Hui Gao, Yong-Min Zhang
In the present work, three fractions of selenized Cordyceps militaris polysaccharides (SeCPS) named SeCPS-I, SeCPS-II and SeCPS-III were isolated and purified by ultra-filtration. Their selenium content were measured as 541.3, 863.7 and 623.3μg/g respectively by a graphite furnace atomic absorption spectroscopy. The monosaccharide comformation analysis showed that they were mainly consisted of D-Mannose, D-Glucose, and D-Galactose in mole ratios of 1:7.63:0.83, 1:1.34:0.31 and 1:3.77:0.41 respectively. Their structure characteristics were compared by IFR and NMR spectroscopy...
February 21, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28231533/synthesis-characterization-and-dna-binding-cleavage-protein-binding-and-cytotoxicity-studies-of-co-ii-ni-ii-cu-ii-and-zn-ii-complexes-of-aminonaphthoquinone
#10
A Kosiha, C Parthiban, Kuppanagounder P Elango
The Co(II), Ni(II), Cu(II) and Zn(II) complexes of an aminonaphthoquinone ligand (L) have been prepared and characterized using analytical and spectral techniques. The structures of L and its Zn(II) complex are confirmed by single crystal X-ray diffraction study. The results indicate that Co(II), Ni(II) and Zn(II) complexes possess tetrahedral geometry while Cu(II) complex exhibits square planar structure. The interaction of L and its complexes with CT-DNA reveal that they could interact with CT-DNA through intercalation...
February 16, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28230989/development-of-the-first-generation-of-disulfide-based-subtype-selective-and-potent-covalent-pyruvate-dehydrogenase-kinase-1-pdk1-inhibitors
#11
Yifu Liu, Zuoquan Xie, Dan Zhao, Jin Zhu, Fei Mao, Shuai Tang, Hui Xu, Cheng Luo, Mei-Yu Geng, Min Huang, Jian Li
Pyruvate dehydrogenase kinases (PDKs) are overexpressed in most cancer cells and are responsible for aberrant glucose metabolism. We previously described Bis(4-morpholinyl thiocarbonyl)-disulfide (JX06, 16) as the first covalent inhibitor of PDK1. Here, based on the scaffold of 16, we identify two novel types of disulfide-based PDK1 inhibitors. The most potent analog, 3a, effectively inhibits PDK1 both at the molecular (kinact/Ki = 4.17×103M-1s-1) and the cellular level (down to 0.1 μM). In contrast to 16, 3a is a potent and subtype-selective inhibitor of PDK1 with >40-fold selectivity for PDK2-4...
February 23, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28230863/oncogenic-role-of-rab-escort-protein-1-through-egfr-and-stat3-pathway
#12
Un-Jung Yun, Jee Young Sung, Seog-Yun Park, Sang-Kyu Ye, Jaegal Shim, Jae-Seon Lee, Masahiko Hibi, Young-Ki Bae, Yong-Nyun Kim
Rab escort protein-1 (REP1) is linked to choroideremia (CHM), an X-linked degenerative disorder caused by mutations of the gene encoding REP1 (CHM). REP1 mutant zebrafish showed excessive cell death throughout the body, including the eyes, indicating that REP1 is critical for cell survival, a hallmark of cancer. In the present study, we found that REP1 is overexpressed in human tumor tissues from cervical, lung, and colorectal cancer patients, whereas it is expressed at relatively low levels in the normal tissue counterparts...
February 23, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28230093/pentabromophenol-suppresses-tgf-%C3%AE-signaling-by-accelerating-degradation-of-type-ii-tgf-%C3%AE-receptors-via-caveolae-mediated-endocytosis
#13
Chun-Lin Chen, Pei-Hua Yang, Yu-Chen Kao, Pei-Yu Chen, Chih-Ling Chung, Shih-Wei Wang
Pentabromophenol (PBP), a brominated flame retardant (BFR), is widely used in various consumer products. BFRs exert adverse health effects such as neurotoxic and endocrine-disrupting effects. In this study, we found that PBP suppressed TGF-β response by accelerating the turnover rate of TGF-β receptors. PBP suppressed TGF-β-mediated cell migration, PAI-1 promoter-driven reporter gene activation, and Smad2/3 phosphorylation in various cell types. Furthermore, PBP abolished TGF-β-mediated repression of E-cadherin expression, in addition to the induction of vimentin expression and N-cadherin and fibronectin upregulation, thus blocking TGF-β-induced epithelial-mesenchymal transition in A549 and NMuMG cells...
February 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28229971/breviscapine-suppresses-the-growth-of-non-small-cell-lung-cancer-by-enhancing-microrna-7-expression
#14
Jian Zeng, Shunv Cai
Breviscapine (BVP) has previously been shown to inhibit the proliferation of hepatocellular carcinoma cells. However, little is known about the effects of BVP on non-small cell lung cancer (NSCLC) growth. Here, we aimed to study the effects of BVP on human NSCLC growth. We employed A549, NCL-H460 and A549 cells transfected with microRNA-7 (miR-7) mimic and inhibitor to investigate the effect of BVP on cell proliferation, apoptosis and apoptosis-associated molecules. The results showed that BVP significantly reduced the growth of A549 and NCLH460 cells in a concentration-dependent and time-dependent manner, accompanied by a significant elevation of apoptosis...
March 2017: Journal of Biosciences
https://www.readbyqxmd.com/read/28229930/atrial-natriuretic-peptide-a-novel-mediator-for-tgf-%C3%AE-1-induced-epithelial-mesenchymal-transition-in-16hbe-14o-and-a549-cells
#15
Shuyuan Chu, Xiufeng Zhang, Yabing Sun, Yuanyuan Yu, Yaxi Liang, Ming Jiang, Jianwei Huang, Libing Ma
Atrial natriuretic peptide (ANP) is increasingly expressed on airway and inhibits pulmonary arterial remodeling. However, the role of ANP in remodeling of respiratory system is still unclear. The role of ANP on airway remodeling and the possible mechanism was explored in this study. Both human bronchial epithelial 16HBE-14o cells and alveolar epithelial A549 cells were stimulated by TGF-β1, ANP, cGMP inhibitor, PKG inhibitor, and cGMP analogue. The expressions of epithelial markers, mesenchymal markers, and Smad3 were assessed by quantitative real-time PCR and western blotting...
February 13, 2017: Peptides
https://www.readbyqxmd.com/read/28229436/purification-and-characterization-of-a-novel-ubiquitin-like-antitumour-protein-with-hemagglutinating-and-deoxyribonuclease-activities-from-the-edible-mushroom-ramaria-botrytis
#16
Rong Zhou, Ya-Jie Han, Min-Hui Zhang, Ke-Ren Zhang, Tzi Bun Ng, Fang Liu
A novel ubiquitin-like antitumour protein (RBUP) was isolated from fruiting bodies of the edible mushroom Ramaria botrytis. The protein was isolated with a purification protocol involving ion exchange chromatography on DEAE-Sepharose fast flow and gel filtration on Sephadex G-75. SDS-PAGE, Native-PAGE and ultracentrifugation analysis disclosed that RBUP was a monomeric protein with a molecular weight of 18.5 kDa. ESI-MS/MS demonstrated that it shared 69% amino acid sequence similarity with Coprinellus congregates ubiquitin (gi|136667)...
December 2017: AMB Express
https://www.readbyqxmd.com/read/28225114/the-new-supramolecular-nano-aggregate-curcumin-cucurbit-7-uril-synthesis-photophysical-properties-and-biocompatibility-evaluation
#17
Leandro Araújo de Azevedo, Leonis Lourenço da Luz, Jamylle Nunes de Souza Ferro, Emiliano Barreto, Ricardo Oliveira Silva, Severino Alves, Iane Bezerra Vasconcelos Alves
The supramolecular nano-aggregate CUR-CB[7] (CUR = curcumin and CB[7] = cucurbit[7]uril) was efficiently prepared by mixing CUR and CB[7] at a molar ratio of 1 : 1 in ethanol at room temperature. The supramolecular aggregate formation was evidenced by mainly FTIR, (1)H NMR, DOSY and spectroscopy experiments. The supramolecular arrangement promotes the increase in the solubility and stability of CUR without affecting the biological properties of the A549 cells. The luminescence properties of CUR and CUR-CB[7] show anti-Kasha's rule fluorescence, and their remarkable NIR emission enables this material to be used as a luminescent probe and marker for in vivo tracking and structural integrity monitoring of the supramolecular complex...
February 22, 2017: Photochemical & Photobiological Sciences
https://www.readbyqxmd.com/read/28224118/heparin-binding-hemagglutinin-of-mycobacterium-tuberculosis-is-an-inhibitor-of-autophagy
#18
Qing Zheng, Zhi Li, Shan Zhou, Qian Zhang, Lei Zhou, Xiaorui Fu, Liu Yang, Yueyun Ma, Xiaoke Hao
Airway epithelial cell is often the initial site of attack by pathogens, and cell death is commonly caused by internalization of Mycobacterium tuberculosis (Mtb). However, the mechanism of interaction between epithelial cells and Mtb is not well understood. In this study, we investigated the role of the heparin-binding hemagglutinin (HBHA) protein of Mtb in the function of epithelial cells. In particular, the autophagy of A549 cells was determined based on microtubule-associated protein 1 light chain 3 alpha (LC3) activity...
2017: Frontiers in Cellular and Infection Microbiology
https://www.readbyqxmd.com/read/28223352/cross-talk-between-the-glucocorticoid-receptor-and-myod-family-inhibitor-domain-containing-protein-provides-a-new-mechanism-for-generating-tissue-specific-responses-to-glucocorticoids
#19
Robert H Oakley, John M Busillo, John A Cidlowski
Glucocorticoids are primary stress hormones that regulate many physiological processes, and synthetic derivatives of these molecules are widely used in the clinic. The molecular factors that govern tissue specificity of glucocorticoids, however, are poorly understood. The actions of glucocorticoids are mediated by the glucocorticoid receptor (GR). To discover new proteins that interact with GR and modulate its function, we performed a yeast 2-hybrid assay. The MyoD family inhibitor domain containing (MDFIC) protein was identified as a binding partner for GR...
February 21, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28223119/neferine-augments-therapeutic-efficacy-of-cisplatin-through-ros-mediated-non-canonical-autophagy-in-human-lung-adenocarcinoma-a549%C3%A2-cells
#20
Sivalingam Kalai Selvi, Amirthalingam Vinoth, Thiyagarajan Varadharajan, Ching Feng Weng, Viswanadha Vijaya Padma
Combination of dietary components with chemotherapy drugs is an emerging new strategy for cancer therapy to increase antitumor responses. Neferine, major bisbenzylisoquinoline alkaloid isolated from the seed embryo of Nelumbo nucifera (Lotus). In the present study, we investigated the efficacy of the combinatorial regimen of neferine and cisplatin compared to cisplatin high dose in human lung adenocarcinoma (A549) cells. Co-treatment with neferine enhanced cisplatin-induced autophagy in A549 cells was accompanied by Acidic vesicular accumulation (AVO), enhanced generation of reactive oxygen species (ROS) and depletion of intracellular glutathione (GSH), down regulation of PI3K/AKT/mTOR pathway, conversion of LC3B-I to LC3B-II...
February 18, 2017: Food and Chemical Toxicology
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