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Silvana Russo, Walter Filgueira De Azevedo
BACKGROUND: Cannabinoid Receptor 1 (CB1) is a membrane protein prevalent in the central nervous system, whose crystallographic structure has recently been solved. Studies will be needed to investigate CB1 complexes with its ligands and its role in the development of new drugs. OBJECTIVE: Our goal here is to review the studies on CB1, starting with general aspects and focusing on the recent structural studies, with emphasis on the inverse agonists bound structures...
April 17, 2018: Current Medicinal Chemistry
Yue Zhao, Junwei Zhao, Chang Lu, Hui Zhang, Huan Qi, Shanwen Jiang, Xiaowei Guo, Jidong Wang, Wensheng Xiang
Two new spliceostatin derivatives, designed as spliceostatin H (1) and spliceostatin I (2), and one known compound FR901464 (3), were isolated from the strain Pseudomonas sp. HS-NF-1408. Their structures were determined by the comprehensive spectroscopic data, including 1D, 2D NMR, MS spectral analysis and comparison with data from the literature. Compound 1 exhibited potent cytotoxicity activity against A549 and HepG2 with IC50 values of 3.57 and 16.72 μg/ml, respectively.
April 17, 2018: Journal of Antibiotics
Mingyue Liu, Xiqing Li, Ke-Zheng Peng, Tianhui Gao, Yao Cui, Ning Ma, Yun Zhou, Guiqin Hou
Kruppel-like factor 4 (Klf4) was reported to have both tumor suppressive and oncogenic roles on tumorigenesis, which is depend on its subcellular localization. In this study, the expression and subcellular localization of Klf4 in non-small cell lung cancer (NSCLC) patients as well as its clinical significance were analyzed, and the expression and subcellular localization of Klf4 in A549 cells and A549/DDP cells were detected. The results showed that the expression of Klf4 in nucleus was related to the histological grade and clinical stage of NSCLC patients...
March 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Yang Zhao, Ke Wang, Deyong Chen, Beiyuan Fan, Ying Xu, Yifei Ye, Junbo Wang, Jian Chen, Chengjun Huang
This paper presents a new microfluidic impedance cytometry with crossing constriction microchannels, enabling the characterization of cellular electrical markers (e.g., specific membrane capacitance (Csm ) and cytoplasm conductivity (σcy )) in large cell populations (~ 100,000 cells) at a rate greater than 100 cells/s. Single cells were aspirated continuously through the major constriction channel with a proper sealing of the side constriction channel. An equivalent circuit model was developed and the measured impedance values were translated to Csm and σcy ...
April 7, 2018: Biosensors & Bioelectronics
Guang-Lei Ma, Juan Xiong, Ezzat E A Osman, Ting Huang, Guo-Xun Yang, Jin-Feng Hu
Two previously undescribed chimonanthine-type [sinodamines A and B] and five related known dimeric tryptamine-derived alkaloids were isolated and characterized from the leaves of the endangered ornamental plant Sinocalycanthus chinensis under the guidance of LC-MS detection and dereplication analyses, along with conventional isolation procedures. Their structures were established on the basis of spectroscopic methods and chemical transformations. Sinodamine A can be regarded as the naturally occurring N-oxide derivative of its pseudo-mesomer sinodamine B...
April 14, 2018: Phytochemistry
Michał Otręba, Leon Kośmider, Jakub Knysak, Jared D Warncke, Andrzej Sobczak
E-cigarettes are used by millions of people despite the fact that the harmful effect of aerosol emitted from these products to the human organism is still not clear. In this paper, toxicity of vapor generated using different solutions and battery output voltage on A549 cells viability is presented. The obtained EC50 values for commercially available propylene glycol/glycerol solution 1:1 e-liquids based on 3.2 V (0.127%), 4.0 V (0.112%) and 4.8 V (0.038%) were about 1.5-4.5 times higher than in tobacco smoke (0...
April 17, 2018: Journal of Applied Toxicology: JAT
Zhaoshuai He, Yajie Chou, Hanxin Zhou, Han Zhang, Tanyu Cheng, Guohua Liu
Nitroreductase and acidity are common features of a tumor, which is associated with serious disease with a high mortality rate. However, solo detection of nitroreductase or acidic environments may cause false-positive results. Thus, it is very meaningful to develop dual functional probes for detecting nitroreductase and acidity, as these could be used for accurate tumor imaging. Here we report on the first dual functional ratiometric fluorescent probe, NAFP, for acidity and nitroreductase detection. This probe enables the measurement of the acidic microenvironment and the concentration of nitroreductase at the same time and the same site...
April 17, 2018: Organic & Biomolecular Chemistry
Mangmang Sang, Zhongtao Zhang, Fulei Liu, Lejian Hu, Lingchao Li, Li Chen, Feng Feng, Wenyuan Liu, Wei Qu
A novel multifunctional hyaluronic acid-decorated redox-responsive magnetic complex micelle (HA/CSO-SS-Hex/Fe3O4/PTX) based on a reducible hexadecanol-modified chitosan oligosaccharide polymer micelle (CSO-SS-Hex) coated with hyaluronic acid (HA) and loaded with paclitaxel (PTX) Fe3O4 nanoparticles is developed. HA is coated onto the surface of micelles via electrostatic absorption and acts as a targeting ligand for CD44 over expression in many tumor cells. A CSO-SS-Hex polymer micelle was used for PTX incorporation and GSH-triggered intracellular release...
March 1, 2018: Journal of Biomedical Nanotechnology
Chongyu Su, Xu Cheng, Yunsong Li, Yi Han, Xiaoyun Song, Daping Yu, Xiaoqing Cao, Zhidong Liu
This study was aimed at the investigation of the effects of miR-21 on drug resistance, invasion, migration, and epithelial-mesenchymal transition (EMT) of lung adenocarcinoma cells and the related molecular mechanisms. Cell viability of A549 cell line was measured by MTT assay. Wound healing assay and transwell assay were, respectively, employed to examine cell migration and invasion abilities. The cells were transfected with miR-21 mimic or inhibitor using Lipofectamine 3000. The target relationship between miR-21 and HBP1 was confirmed by luciferase reporter gene assay...
April 16, 2018: Cancer Medicine
Ren Wang, Hui-Xing Dong, Jian Zeng, Jing Pan, Xiao-Yan Jin
Non-coding RNAs can exert significant roles various cancers, including NSCLC. Previously, we indicated that lncRNA DGCR5 can promote lung cancer progression through inhibiting hsa-mir-22-3p. In our current study, we investigated the role of DGCR5 in cancer stem cell-like properties of NSCLC. CSCs have been recognized as the frequent cause of tumor metastasis, tumor recurrence, and chemotherapy resistance. Here, lung cancer stem cells were successfully enriched from the parental NSCLC A549, H460, and H1299 cells by using tumor sphere formation assays and side population (SP) assays...
April 16, 2018: Journal of Cellular Physiology
Liang-Ting Lin, Shin-Yi Liu, Jyh-Der Leu, Chun-Yuan Chang, Shih-Hwa Chiou, Te-Chang Lee, Yi-Jang Lee
Arsenic trioxide (ATO) is a traditional Chinese medicine that can induce oxidative stress for treatment of cancer cells. However, ATO may generate anti-oxidative responses to compromise the cytotoxic effect, but the underlying mechanisms remain unclear. Here we found that ATO could inhibit miR-182-5p expression in patient-derived primary S1 glioblastoma (GBM) cells accompanied by up-regulation of Sestrin-2 ( SESN2 ) mRNA, a known anti-oxidant molecule. This phenomenon was also detected in a U87MG glioma cell line, human lung adenocarcinoma H1299 cell line and A549 cell line...
March 23, 2018: Oncotarget
Hussein H K Abbas, Kheloud M H Alhamoudi, Mark D Evans, George D D Jones, Steven S Foster
BACKGROUND: Targeted therapies are based on exploiting cancer-cell-specific genetic features or phenotypic traits to selectively kill cancer cells while leaving normal cells unaffected. Oxidative stress is a cancer hallmark phenotype. Given that free nucleotide pools are particularly vulnerable to oxidation, the nucleotide pool sanitising enzyme, MTH1, is potentially conditionally essential in cancer cells. However, findings from previous MTH1 studies have been contradictory, meaning the relevance of MTH1 in cancer is still to be determined...
April 16, 2018: BMC Cancer
Fatma F Ahmed, Amer Ali Abd El-Hafeez, Samar H Abbas, Dalia Abdelhamid, Mohamed Abdel-Aziz
A series of novel 1, 2, 4-triazole/chalcone hybrids was prepared and identified with different spectroscopic techniques. The prepared compounds showed remarkable cytotoxic activity against different cancer cell lines. Compounds 24, 25, 27, 41 and 47 had shown the highest cytotoxicity among the tested compounds against human lung adenocarcinoma A549 cells with IC50 ranging from 4.4 to 16.04 μM compared to cisplatin with IC50 of 15.3 μM. Flow cytometric analysis of the tested compounds showed an increase in the number of apoptotic cells in a dose-dependent manner...
March 27, 2018: European Journal of Medicinal Chemistry
Ziran Zhao, Jiagen Li, Fengwei Tan, Shugeng Gao, Jie He
Previously, BEX family members have been reported to participate in cancer development. However, little is known about the role of BEX4 in lung adenocarcinoma (LAC). Here, we found that BEX4 was over-expressed in LAC tissues compared with adjacent tissues. LAC tissues from metastatic patients exhibited higher expression of BEX4 comparing to those from non-metastatic ones. In vitro, BEX4 ectopic expression accelerated the proliferation of both A549 and H1975 cells. By contrast, knockdown of BEX4 suppressed the proliferation of A549 and H1975 cells...
April 13, 2018: Biochemical and Biophysical Research Communications
Sathish Kumar Boda, Vasantha Pishka, P V Anantha Lakshmi, Srinivas Chinde, Paramjit Grover
A series of novel ethyl 2,7-dimethyl-4-oxo-3-((1-phenyl-1H-1,2,3-triazol-4-yl)methyl)-4,5-dihydro-3H-pyrano[2,3-d]pyrimidine-6-carboxylate derivatives 7(a-m) were efficiently synthesized employing click chemistry approach and evaluated for in vitro anti cancer activity against four tumor cell lines: A549 (human lung adenocarcenoma cell line), HepG2 (Human hematoma), MCF-7 (Human breast adenocarcinoma), and SKOV3 (human ovarian carcinoma cell line). Among the compounds tested, the compounds 7a, 7b, 7f, 7l and 7m have shown potential and selective activity against human lung adenocarcenoma cell line (A549) with IC50 ranging from 0...
April 16, 2018: Chemistry & Biodiversity
Yuan Wang, Lei Lei, Yi-Wen Zheng, Li Zhang, Zhi-Han Li, Hao-Yue Shen, Gui-Yang Jiang, Xiu-Peng Zhang, En-Hua Wang, Hong-Tao Xu
The odd-skipped related 1 (OSR1) gene encodes a zinc-finger transcription factor. The expression and significance of OSR1 in human tumors remains unclear. We found that OSR1 was downregulated in lung cancers, and its expression correlated with poor differentiation. Overexpression of OSR1 by OSR1 gene transfection into H1299 cells (H1299-OSR1) inhibited the proliferation and invasion of lung cancer cells. Knockdown of OSR1 with small interfering (si)RNA against OSR1 in A549 cells (A549-siOSR1) enhanced the proliferation and invasion of lung cancer cells...
April 16, 2018: Cancer Science
Shuaiguang Li, Enze Yang, Lianghua Shen, Dewei Niu, Mason Breitzig, Lee Charles Tan, Xiaocong Wu, Meiyan Huang, Hanxiao Sun, Feng Wang
Growing evidences have demonstrated alternative splicing makes great contribution to tumor metastasis since multiple protein isoforms from a single gene that often display different functions in the cell. Human manganese superoxide dismutase (hMnSOD) was revealed dysregulation in progress of tumor metastasis, while the effect of hMnSOD isoforms on metastasis remained unclear. In this study, we showed a novel truncated hMnSOD isoform hMnSOD183, which lacked 39 amino acids compared with hMnSOD222. We expressed two hMnSOD protein isoforms in E...
April 16, 2018: Cell Biology International
Dayoung Kim, Eun Ju Lee, Jihye Lee, Alain S Leutou, Yern-Hyerk Shin, Bomi Choi, Ji Sun Hwang, Dongyup Hahn, Hyukjae Choi, Jungwook Chin, Sung Jin Cho, Yong Deog Hong, Jaeyoung Ko, Chi Nam Seong, Katherine N Maloney, Dong-Chan Oh, Inho Yang, Hayoung Hwang, Sang-Jip Nam
Antartin ( 1 ), a new zizaane-type sesquiterpene, was isolated from Streptomyces sp. SCO736. The chemical structure of 1 was assigned from the interpretation of 1D and 2D NMR in addition to mass spectrometric data. The relative stereochemistry of 1 was determined by analysis of NOE data, while the absolute stereochemistry was decided based on a comparison of experimental and calculated electronic circular dichroism (ECD) spectra. Antartin ( 1 ) showed cytotoxicity against A549, H1299, and U87 cancer cell lines by causing cell cycle arrest at the G1 phase...
April 16, 2018: Marine Drugs
Manami Sugimoto, Yoichi Kitagawa, Masumi Yamada, Yuya Yajima, Rie Utoh, Minoru Seki
Cell migration and invasion are of significant importance in physiological phenomena, including wound healing and cancer metastasis. Here we propose a new system for quantitatively evaluating cancer cell invasion in a three-dimensional (3D), in vivo tissue-like environment. This system uses composite hydrogel microfibers whose cross section has a relatively soft micropassage region and that were prepared using a multilayered microfluidic device; cancer cells are encapsulated in the core and fibroblasts are seeded in the shell regions surrounding the core...
April 16, 2018: Lab on a Chip
Likun Liu, Cuicui Han, Haitao Yu, Wenbin Zhu, Hongxia Cui, Lihong Zheng, Chunjing Zhang, Liling Yue
Chloroquine (CQ) has been revealed to exhibit antitumor activity in several human tumors including lung cancer as mono‑ or add‑on therapy. The antitumor effect of CQ appears to depend on the tumor type, stage and genetic context. Few studies have focused on the mechanism concerning the antitumor effect of CQ monotherapy and the cause and effect relationship among autophagy, apoptosis and CQ in human lung A549 cells. Therefore, the present study aimed to identify the antitumor effect of CQ monotherapy and analyze the possible mechanism...
April 12, 2018: Oncology Reports
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