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https://www.readbyqxmd.com/read/28804952/evaluation-of-cytotoxicity-of-propofol-and-its-related-mechanism-in-glioblastoma-cells-and-astrocytes
#1
Shu-Shong Hsu, Chung-Ren Jan, Wei-Zhe Liang
Propofol (2,6-diisopropylphenol), one of the extensively and commonly used anesthetic agents, has been shown to affect the biological behavior of various models. Previous researches have shown that propofol-induced cytotoxicity might cause anticancer effect in different cells. However, the mechanisms underlying the effect of propofol on cytotoxicity is still elusive in human glioblastoma cells. The aims of this study were to evaluate effects of propofol on cytotoxicity, cell cycle distribution and ROS production, and establish the relationship between oxidative stress and cytotoxicity in GBM 8401 human glioblastoma cells and DI TNC1 rat astrocytes...
August 14, 2017: Environmental Toxicology
https://www.readbyqxmd.com/read/28804691/combination-of-celecoxib-celebrex-%C3%A2-and-cd19-car-redirected-ctl-immunotherapy-for-the-treatment-of-b-cell-non-hodgkin-s-lymphomas
#2
REVIEW
Tam Nm Dinh, Alexandra S Onea, Ali R Jazirehi
The nonsteroidal anti-inflammatory drug (NSAID) Celecoxib (Celebrex(®)) received Food and Drug Administration (FDA) approval in 1998 for treatment of osteoarthritis and rheumatoid arthritis, and in recent years, its use has been extended to various types of malignancies, such as breast, colon, and urinary cancers. To maintain the survival of malignant B cells, non-Hodgkin's Lymphoma (NHL) is highly dependent on inflammatory microenvironment, and is inhibited by celecoxib. Celecoxib hinders tumor growth interacting with various apoptotic genes, such as cyclooxygenase-2 (Cox-2), B-cell lymphoma 2 (Bcl-2) family, phosphor-inositide-3 kinase/serine-threonine-specific protein kinase (PI3K/Akt), and inhibitors of apoptosis proteins (IAP) family...
2017: American Journal of Clinical and Experimental Immunology
https://www.readbyqxmd.com/read/28804614/protective-effect-of-bioactive-compounds-from-echinophora-cinerea-against-cisplatin-induced-oxidative-stress-and-apoptosis-in-the-pc12-cell-line
#3
Yald Shokoohinia, Shekoufeh Khajouei, Farahnaz Ahmadi, Nastaran Ghiasvand, Leila Hosseinzadeh
OBJECTIVES: The present study aims to evaluate the protective effect of the compounds isolated from Echinophora cinerea (E. cinerea) against oxidative stress and apoptosis induced by cisplatin (CIS) in PC12 cells. MATERIALS AND METHODS: Six compounds were isolated as quercetrin-3-O-β-D-glucopyranoside (QUE), osthol (OST), verbenone-5-O-β-D-glycopyranoside (VER), Isoimperatorin (ISO), kaempferol-3-O-β-D-glucopyranoside (KAM), and echinophorin B (ECH). For this study, we used MTT reduction assay for detection of protective effects of isolated compounds on CIS-induced cytotoxicity in PC12 cells...
April 2017: Iranian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/28802125/novel-4-3-4-oxo-5-2-oxoindolin-3-ylidene-thiazolidin-2-ylidene-amino-benzenesulfonamides-synthesis-carbonic-anhydrase-inhibitory-activity-anticancer-activity-and-molecular-modelling-studies
#4
Wagdy M Eldehna, Mahmoud F Abo-Ashour, Alessio Nocentini, Paola Gratteri, Ibrahim H Eissa, Mohamed Fares, Omnia E Ismael, Hazem A Ghabbour, Mahmoud M Elaasser, Hatem A Abdel-Aziz, Claudiu T Supuran
Herein we report the synthesis of two series of novel 4/3-((4-oxo-5-(2-oxoindolin-3-ylidene)thiazolidin-2-ylidene)amino)benzenesulfonamides (4a-m and 7a-g). All the newly prepared sulfonamides were in vitro investigated as inhibitors of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1) isoforms hCA I, II, IV and IX, using a stopped-flow CO2 hydrase assay. In particular, hCA isoforms II and IX (tumor-associated) were more susceptible to inhibition by the synthesized derivatives, with KIs in the range of 2...
August 1, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28799432/targeted-therapies-in-acute-myeloid-leukemia-a-focus-on-flt-3-inhibitors-and-abt199
#5
Kiran Naqvi, Marina Konopleva, Farhad Ravandi
Acute myeloid leukemia (AML) remains a therapeutic challenge. Despite ongoing research, the standard therapy for AML has not changed significantly in the past four decades. With the identification of cytogenetic and molecular abnormalities, several promising therapeutic agents are currently being investigated. FLT3 mutation is a well-recognized target seen in 30% of the cytogenetically normal AML. More recently, the BCL2 family of anti-apoptotic proteins have also generated great interest as a therapeutic target...
August 11, 2017: Expert Review of Hematology
https://www.readbyqxmd.com/read/28794469/targeting-the-pi3k-akt-mtor-signalling-pathway-in-cystic-fibrosis
#6
R Reilly, M S Mroz, E Dempsey, K Wynne, S J Keely, E F McKone, C Hiebel, C Behl, J A Coppinger
Deletion of phenylalanine 508 of the cystic fibrosis transmembrane conductance regulator (ΔF508 CFTR) is a major cause of cystic fibrosis (CF), one of the most common inherited childhood diseases. ΔF508 CFTR is a trafficking mutant that is retained in the endoplasmic reticulum (ER) and unable to reach the plasma membrane. Efforts to enhance exit of ΔF508 CFTR from the ER and improve its trafficking are of utmost importance for the development of treatment strategies. Using protein interaction profiling and global bioinformatics analysis we revealed mammalian target of rapamycin (mTOR) signalling components to be associated with ∆F508 CFTR...
August 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28793831/deciphering-the-crucial-molecular-properties-of-a-series-of-benzothiazole-hydrazone-inhibitors-that-targets-anti-apoptotic-bcl-xl-protein
#7
Parthiban Marimuthu, Pavithra K Balasubramanian, Kalaimathy Singaravelu
The Bcl-2 family proteins are the central regulators of apoptosis. Due to its predominant role in cancer progression, the Bcl-2 family proteins act as attractive therapeutic targets. Recently,molecular series of BenzothiazoleHydrazone(BH) inhibitorsthat exhibits drug-likenesscharacteristics,whichselectivelytargets Bcl-xLhave been reported.In the present study,dockingwas used toexplore the plausible binding mode of the highly active BH inhibitorwith Bcl-xL;and Molecular Dynamics(MD) simulation wasapplied toinvestigate the stability of predicted conformationover time...
August 10, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28790887/mir-16-and-fluoxetine-both-reverse-autophagic-and-apoptotic-change-in-chronic-unpredictable-mild-stress-model-rats
#8
Yang Yang, Zhiying Hu, Xiaoxue Du, Henry Davies, Xue Huo, Marong Fang
In the clinic selective serotonin reuptake inhibitors (SSRIs), like Fluoxetine, remain the primary treatment for major depression. It has been suggested that miR-16 regulates serotonin transporters (SERT) via raphe nuclei and hippocampal responses to antidepressants. However, the underlying mechanism and regulatory pathways are still obtuse. Here, a chronic unpredicted mild stress (CUMS) depression model in rats was established, and then raphe nuclei miR-16 and intragastric Fluoxetine injections were administered for a duration of 3 weeks...
2017: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/28790012/mdivi-1-ameliorates-early-brain-injury-after-subarachnoid-hemorrhage-via-the-suppression-of-inflammation-related-blood-brain-barrier-disruption-and-endoplasmic-reticulum-stress-based-apoptosis
#9
Lin-Feng Fan, Ping-You He, Yu-Cong Peng, Qing-Hua Du, Yi-Jun Ma, Jian-Xiang Jin, Hang-Zhe Xu, Jian-Ru Li, Zhi-Jiang Wang, Sheng-Long Cao, Tao Li, Feng Yan, Chi Gu, Lin Wang, Gao Chen
Aberrant modulation of mitochondrial dynamic network, which shifts the balance of fusion and fission towards fission, is involved in brain damage of various neurodegenerative diseases including Parkinson's disease, Huntington's disease and Alzheimer's disease. A recent research has shown that the inhibition of mitochondrial fission alleviates early brain injury after experimental subarachnoid hemorrhage, however, the underlying molecular mechanisms have remained to be elucidated. This study was undertaken to characterize the effects of the inhibition of dynamin-related protein-1 (Drp1, a dominator of mitochondrial fission) on blood-brain barrier (BBB) disruption and neuronal apoptosis following SAH and the potential mechanisms...
August 5, 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28782841/microrna-184-inhibits-proliferation-and-promotes-apoptosis-of-human-colon-cancer-sw480-and-hct116-cells-by-downregulating-c-myc-and-bcl-2
#10
Yong-Bing Wang, Xiao-Hui Zhao, Gang Li, Jun-Hua Zheng, Wei Qiu
This study aimed to investigate the effects of microRNA-184 (miR-184) on the proliferation and apoptosis of human colon cancer cells through the regulation of C-MYC and BCL-2. Human colon cancer tissues were selected as case group, and adjacent normal tissues were as control group. Human colon cancer SW480 and HCT116 cells were allocated into blank, miR-184 mimic negative control (mimic-NC), miR-184 inhibitor NC (inhibitor-NC), miR-184 mimic and miR-184 inhibitor groups. Flow cytometry, Annexin V/PI and MTT assay were used to examine the cell cycle, apoptosis and viability...
August 7, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28779993/the-class-i-pi3k-inhibitor-s14161-induces-autophagy-in-malignant-blood-cells-by-modulating-the-beclin-1-vps34-complex
#11
Siyu Wang, Jie Li, Yanyun Du, Yujia Xu, Yali Wang, Zubin Zhang, Zhuan Xu, Yuanying Zeng, Xinliang Mao, Biyin Cao
S14161 is a pan-Class I PI3K inhibitor that induces blood cancer cell death, but its mechanism is largely unknown. In the present study, we evaluated the role of S14161 in autophagy, an emerging event in cell destination. Multiple myeloma cell lines RPMI-8226, OPM2, KMS11 and leukemia cell line K562 were treated with S14161. The results showed that S14161 induced autophagy as demonstrated by increased LC3-II and decreased p62, which were prevented by autophagy inhibitors including 3-methyladenine and bafilomycin A1...
July 19, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28777484/5-azacytidine-specifically-inhibits-the-nih-3t3-pcd-process-induced-by-tnf-alpha-and-cycloheximide-via-affecting-bcl-xl
#12
Qing Wang, Pu Wang, Hong Zhou, Yan Hu, Chengshen Xie, Fei Gao, Ningjie Ma, Haoli Hou, Hao Zhang, Lijia Li
DNA methylation plays a crucial role in lots of biological processes and cancer. 5-azacytidine (5-AC), a DNA methylation inhibitor, has been used as a potential chemotherapeutic agent for cancer. In this study, we used 5-AC treatment to investigate whether DNA methylation was involved in regulation of programmed cell death (PCD) in mouse embryo fibroblast NIH-3T3 cells which could undergo PCD after treatment with TNF-α and cycloheximide (CHX). The results showed that the genomic DNA of NIH-3T3 cells was hypermethylated during PCD induced by TNF-α and CHX, and 5-AC might prevent this PCD process...
August 4, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28774732/downregulation-of-tigar-sensitizes-the-antitumor-effect-of-physapubenolide-through-increasing-intracellular-ros-levels-to-trigger-apoptosis-and-autophagosome-formation-in-human-breast-carcinoma-cells
#13
Ting Ma, Yi Zhang, Chao Zhang, Jian-Guang Luo, Ling-Yi Kong
Physapubenolide (PB) is a cytotoxic withanolide isolated from Physalis angulate that was used as a traditional Chinese medicine. In this study, we investigated the role of TIGAR and ROS in PB-induced apoptosis and autophagosome formation in human breast carcinoma MDA-MB-231 and MCF-7 cells. PB induced apoptosis by decreasing mitochondrial membrane potential and elevating the Bax/Bcl-2 protein expression ratio in MDA-MB-231 and MCF-7 cells. Caspase inhibitor Z-VAD-FMK treatment partly blocked PB induced cytotoxicity, suggesting that apoptosis serves as an important role in the anti-proliferative effect of PB...
July 31, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28772212/mir-144-may-regulate-the-proliferation-migration-and-invasion-of-trophoblastic-cells-through-targeting-pten-in-preeclampsia
#14
Jianping Xiao, Tao Tao, Yongxiang Yin, Li Zhao, Lan Yang, Lingqing Hu
Previous studies indicated that microRNAs (miRNAs) were aberrantly expressed in the placentas of patients with Preeclampsia (PE); however, the underlying mechanism still requires further investigation. The aim of this study is to investigate the roles of miR-144 in preeclampsia and the related mechanism. The expression of miR-144 and PTEN in 30 placentas of patients with PE and 30 normal placentas was compared; next, HTR8/SVneo cells were transfected with miR-144 mimics and miR-144 inhibitors and cultured for 48h, and the proliferation and apoptosis, cell migration and invasion of the cells were examined; furthermore, the expression PTEN, Caspase-3 and Bcl-2 was examined; next, dual luciferase reporter assay has been performed to confirm that PTEN is a direct target of miR-144; finally, HTR-8/SVneo cells were transfected with either PTEN overexpression plasmid or PTEN RNAi to determine whether knockdown or overexpression of PTEN can mimic the effect of miR-144 We have observed that the expression of miR-144 was significantly decreased and the expression of PTEN was markedly increased in placentas of patients with PE compared with normal placentas; moreover, transfection of miR-144 mimics in trophoblastic cells induced significant increase in cell proliferation, migration, invasion, and decrease in cell apoptosis, and also affected the cell cycles; on the other hand, transfection of miR-144 inhibitors has shown the opposite effects; furthermore, transient overexpression of miR-144 induced marked decrease in the expression of PTEN, Caspase-3 and increase in expression of Bcl-2 (P<0...
July 31, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28770967/suppression-of-adriamycin-resistance-in-osteosarcoma-by-blocking-wnt-%C3%AE-catenin-signal-pathway
#15
B-Q Wu, Y Cao, Z-G Bi
OBJECTIVE: Wnt/β-catenin signal pathway plays a role in regulating cell proliferation and apoptosis, and is correlated with tumor onset, progression and drug resistance. B-cell lymphoma 2 (Bcl-2) is an anti-apoptotic factor inducing tumor cell drug resistance. Wnt/β-catenin signal pathway can modulate Bcl-2 expression. This study established a cell model of drug resistance using adriamycin (ADM) treatment. Wnt/β-catenin signal pathway was intervened to discuss its role in drug resistance of osteosarcoma cells...
July 2017: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/28769027/synergistic-effect-of-notch-3-specific-inhibition-and-paclitaxel-in-non-small-cell-lung-cancer-nsclc-cells-via-activation-of-the-intrinsic-apoptosis-pathway
#16
Fenglian He, Ting Du, Qian Jiang, Yanbei Zhang
BACKGROUND Lung cancers are resistant to conventional chemotherapeutic interventions such as paclitaxel. Notch signaling is crucial in the chemoresistance of lung cancer cells. The Notch inhibitor gamma-secretase inhibitor (GSI) inhibits the Notch signaling pathway. MATERIAL AND METHODS Here, we evaluated how Notch-3 inhibition by GSI can enhance the sensitivity of lung cancer cells to paclitaxel. To study how Notch-3-specific inhibition affects non-small cell lung cancer (NSCLC), we compared the cell viability, apoptosis, and colony formation of A549 and H1299 cells treated with Notch-3 siRNA and GSI...
August 3, 2017: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/28768804/synergistic-action-of-the-mcl-1-inhibitor-s63845-with-current-therapies-in-preclinical-models-of-triple-negative-and-her2-amplified-breast-cancer
#17
Delphine Merino, James R Whittle, François Vaillant, Antonin Serrano, Jia-Nan Gong, Goknur Giner, Ana Leticia Maragno, Maïa Chanrion, Emilie Schneider, Bhupinder Pal, Xiang Li, Grant Dewson, Julius Gräsel, Kevin Liu, Najoua Lalaoui, David Segal, Marco J Herold, David C S Huang, Gordon K Smyth, Olivier Geneste, Guillaume Lessene, Jane E Visvader, Geoffrey J Lindeman
The development of BH3 mimetics, which antagonize prosurvival proteins of the BCL-2 family, represents a potential breakthrough in cancer therapy. Targeting the prosurvival member MCL-1 has been an area of intense interest because it is frequently deregulated in cancer. In breast cancer, MCL-1 is often amplified, and high expression predicts poor patient outcome. We tested the MCL-1 inhibitor S63845 in breast cancer cell lines and patient-derived xenografts with high expression of MCL-1. S63845 displayed synergistic activity with docetaxel in triple-negative breast cancer and with trastuzumab or lapatinib in HER2-amplified breast cancer...
August 2, 2017: Science Translational Medicine
https://www.readbyqxmd.com/read/28767232/rna-polymerase-tags-to-monitor-multidimensional-protein-protein-interactions-reveal-pharmacological-engagement-of-bcl-2-proteins
#18
Jinyue Pu, Jeffrey Dewey, Abbas Hadji, James L LaBelle, Bryan C Dickinson
We report the development of a new technology for monitoring multidimensional protein-protein interactions (PPIs) inside live mammalian cells using split RNA polymerase (RNAP) tags. In this new system, a protein-of-interest is tagged with an N-terminal split RNAP (RNAPN) and multiple potential binding partners are each fused to orthogonal C-terminal RNAPs (RNAPC). Assembly of RNAPN with each RNAPC is highly dependent on interactions between the tagged proteins. Each PPI-mediated RNAPN-RNAPC assembly transcribes from a separate promoter on a supplied DNA substrate, thereby generating a unique RNA output signal for each PPI...
August 2, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28767174/inactivation-of-beclin-1-dependent-autophagy-promotes-ursolic-acid-induced-apoptosis-in-hypertrophic-scar-fibroblasts
#19
Chuan Cao, Wenping Wang, Lele Lu, Liang Wang, XiaoSong Chen, Rui Guo, Shirong Li, Junzi Jiang
A hypertrophic scar (HS) is caused by abnormal proliferation of dermal fibroblasts. Thus, promoting hypertrophic scar fibroblast (HSFB) apoptosis is an effective strategy for HS therapy. Ursolic acid (UA) has been widely used as an inducer of apoptosis in diverse cancers. However, whether UA plays an inhibitory role in HS formation is still unknown. In our study, UA was used to treat HSFBs and the cell viability, apoptosis, and collagen synthesis were determined by a Cell Counting Kit 8 (CCK8) assay, flow cytometry, and an H(3) -proline incorporation assay, respectively...
August 2, 2017: Experimental Dermatology
https://www.readbyqxmd.com/read/28766941/a-computational-investigation-of-small-molecule-engagement-of-hot-spots-at-protein-protein-interaction-interfaces
#20
David Xu, Yubing Si, Samy O Meroueh
The binding affinity of a protein-protein interaction is concentrated at amino acids known as hot spots. It has been suggested that small molecules disrupt protein-protein interactions by either (i) engaging receptor protein hot spots; or (ii) mimicking hot spots of the protein ligand. Yet, to date, no systematic studies have been done to explore how effectively existing small-molecule protein-protein interaction inhibitors mimic or engage hot spots at protein interfaces. Here, we employ explicit-solvent molecular dynamics simulations and end-point MM-GBSA free energy calculations to explore this question...
August 2, 2017: Journal of Chemical Information and Modeling
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