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https://www.readbyqxmd.com/read/29223099/nontoxic-combretafuranone-analogues-with-high-in%C3%A2-vitro-antibacterial-activity
#1
P Horký, M Voráčová, K Konečná, D Sedlák, P Bartůněk, J Vacek, J Kuneš, M Pour
A library of thirty two 3,4-diphenylfuranones related to both combretastatin A-4 and antifungal 5-(acyloxymethyl)-3-(halophenyl)-2,5-dihydrofuran-2-ones was prepared. Cytotoxic effects on a panel of cancer and normal cell lines and antiinfective activity were evaluated, and the data were complemented with tests for the activation of caspase 3 and 7. High cytotoxicity was observed in some of the halogenated analogues, eg. 3-(3,4-dichlorophenyl)-4-(4-methylphenyl)-2,5-dihydrofuran-2-one with IC50 0.12-0.23 μM, but the compounds were also highly toxic against non-malignant control cells...
November 29, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29222028/sodium-butyrate-enhanced-physical-barrier-function-referring-to-nrf2-jnk-and-mlck-signaling-pathways-in-the-intestine-of-young-grass-carp-ctenopharyngodon-idella
#2
Pei Wu, Li Tian, Xiao-Qiu Zhou, Wei-Dan Jiang, Yang Liu, Jun Jiang, Fei Xie, Sheng-Yao Kuang, Ling Tang, Wu-Neng Tang, Juan Yang, Yong-An Zhang, He-Qun Shi, Lin Feng
This study evaluated the effect of dietary sodium butyrate (SB) supplementation on the intestinal physical barrier function of young grass carp (Ctenopharyngodon idella). The fish were fed one powdery sodium butyrate (PSB) diet (1000.0 mg kg-1 diet) and five graded levels of microencapsulated sodium butyrate (MSB) diets: 0.0 (control), 500.0, 1000.0, 1500.0 and 2000.0 mg kg-1 diet for 60 days. Subsequently, a challenge test was conducted by injection of Aeromonas hydrophila to explore the effect of SB supplementation on intestinal physical barrier function and the potential mechanisms in fish...
December 5, 2017: Fish & Shellfish Immunology
https://www.readbyqxmd.com/read/29221199/long-non-coding-rna-uca1-indicates-an-unfavorable-prognosis-and-promotes-tumorigenesis-via-regulating-akt-gsk-3%C3%AE-signaling-pathway-in-cholangiocarcinoma
#3
Yi Xu, Yue Yao, Kaiming Leng, Zhenglong Li, Wei Qin, Xiangyu Zhong, Pengcheng Kang, Ming Wan, Xingming Jiang, Yunfu Cui
Long non-coding RNAs (lncRNAs) have been documented to play key roles in a wide range of pathophysiological processes, including cancer initiation and progression. Recently, the aberrant expression of urothelial carcinoma associated 1 (UCA1) was observed in many types of cancers. However, its clinical relevance and exact effects in cholangiocarcinoma (CCA) remains unknown. In the present study, we aimed to investigate the clinical significance of UCA1 and evaluate its prognostic value in patients with CCA. Besides, the functional roles of UCA1 were detected both in vitro and in vivo...
November 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/29221182/differential-modulation-of-bax-bcl-2-ratio-and-onset-of-caspase-3-7-activation-induced-by-derivatives-of-justicidin-b-in-human-melanoma-cells-a375
#4
Aljawharah Al-Qathama, Simon Gibbons, Jose M Prieto
Diphyllin and its derivatives are well known cytotoxic natural products structurally related to the anti-cancer drug podophyllotoxin. We here study their structure-activity relationship upon human melanoma cells for first time. To this end, human melanoma A375 cells were incubated with Justicidin B and its 4-methoxylated or 4-glycosylated derivatives to evaluate their selective cytotoxicity and study their effects on cell cycle distribution, caspase activation, apoptosis induction using Annexin V-FITC/PI staining, cell morphology and western blot analysis...
November 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/29221122/checkpoint-kinase-1-inhibition-sensitises-transformed-cells-to-dihydroorotate-dehydrogenase-inhibition
#5
Stéphanie Arnould, Geneviève Rodier, Gisèle Matar, Charles Vincent, Nelly Pirot, Yoann Delorme, Charlène Berthet, Yoan Buscail, Jean Yohan Noël, Simon Lachambre, Marta Jarlier, Florence Bernex, Hélène Delpech, Pierre Olivier Vidalain, Yves L Janin, Charles Theillet, Claude Sardet
Reduction in nucleotide pools through the inhibition of mitochondrial enzyme dihydroorotate dehydrogenase (DHODH) has been demonstrated to effectively reduce cancer cell proliferation and tumour growth. The current study sought to investigate whether this antiproliferative effect could be enhanced by combining Chk1 kinase inhibition. The pharmacological activity of DHODH inhibitor teriflunomide was more selective towards transformed mouse embryonic fibroblasts than their primary or immortalised counterparts, and this effect was amplified when cells were subsequently exposed to PF477736 Chk1 inhibitor...
November 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/29220411/hexahydrocurcumin-protects-against-cerebral-ischemia-reperfusion-injury-attenuates-inflammation-and-improves-antioxidant-defenses-in-a-rat-stroke-model
#6
Piyawadee Wicha, Jiraporn Tocharus, Adchara Janyou, Jinatta Jittiwat, Chatchawan Changtam, Apichart Suksamrarn, Chainarong Tocharus
The purpose of the present experiment was to investigate whether hexahydrocurcumin (HHC) attenuates brain damage and improves functional outcome via the activation of antioxidative activities, anti-inflammation, and anti-apoptosis following cerebral ischemia/reperfusion (I/R). In this study, rats with cerebral I/R injury were induced by a transient middle cerebral artery occlusion (MCAO) for 2 h, followed by reperfusion. The male Wistar rats were randomly divided into five groups, including the sham-operated, vehicle-treated, 10 mg/kg HHC-treated, 20 mg/kg HHC-treated, and 40 mg/kg HHC-treated I/R groups...
2017: PloS One
https://www.readbyqxmd.com/read/29220397/desethylamiodarone-a-metabolite-of-amiodarone-induces-apoptosis-on-t24-human-bladder-cancer-cells-via-multiple-pathways
#7
Zita Bognar, Katalin Fekete, Csenge Antus, Eniko Hocsak, Rita Bognar, Antal Tapodi, Arpad Boronkai, Nelli Farkas, Ferenc Gallyas, Balazs Sumegi, Arpad Szanto
Bladder cancer (BC) is a common malignancy of the urinary tract that has a higher frequency in men than in women. Cytostatic resistance and metastasis formation are significant risk factors in BC therapy; therefore, there is great interest in overcoming drug resistance and in initiating research for novel chemotherapeutic approaches. Here, we suggest that desethylamiodarone (DEA)-a metabolite of amiodarone-may have cytostatic potential. DEA activates the collapse of mitochondrial membrane potential (detected by JC-1 fluorescence), and induces cell death in T24 human transitional-cell bladder carcinoma cell line at physiologically achievable concentrations...
2017: PloS One
https://www.readbyqxmd.com/read/29218943/-effect-of-germacrone-in-alleviating-huvecs-damaged-by-h2o2-induced-oxidative-stress
#8
Qiong-Fang Chen, Gang Wang, Li-Qing Tang, Xian-Wen Yu, Zhao-Fei Li, Xiu-Fen Yang
This study focuses on the protective effect of germacrone on human umbilical vein endothelial cells(HUVECs) damaged by H2O2-induced oxidative stress and its possible mechanisms. The oxidative damage model was established by using 500 μmol•L⁻¹ H2O2 to treat HUVECs for 3 hours, and then protected with different concentrations of germacrone for 24 hours. The effect of germacrone on cell viability of HUVECs damaged by H2O2 was detected by MTT. The contents of PGI2, TXB2, ET-1, t-PA, PAI-1, TNF-α and IL-6 were detected by ELISA...
September 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29218509/protective-effect-of-cadmium-induced-autophagy-in-rat-renal-mesangial-cells
#9
Hitomi Fujishiro, Ying Liu, Bilal Ahmadi, Douglas M Templeton
Cadmium damages renal cells, and in particular may cause mesangial cell death by necrosis or apoptosis, depending on exposure conditions in cultured cells. However, there is an uncertainty as to whether Cd2+-induced autophagy can protect mesangial cells against these other mechanisms of cell death. We have used autophagy-incompetent mouse embryonic fibroblast (MEF) cells lacking the Atg16 gene, as well as cultured rat mesangial cells (RMC) in which Atg16 has been silenced, to examine this issue. Measuring the processing of LC3-I to LC3-II and expression of sequestosome-1 (p62), we define conditions under which RMC can be induced to undergo autophagy in response to 0-20 µM CdCl2...
December 7, 2017: Archives of Toxicology
https://www.readbyqxmd.com/read/29218434/inhibition-of-gsk-3beta-signaling-pathway-rescues-ketamine-induced-neurotoxicity-in-neural-stem-cell-derived-neurons
#10
Jingjing Zhang, Changlei Cui, Yanhui Li, Haiyang Xu
Clinical application of anesthetic reagent, ketamine (Keta), may induce irreversible neurotoxicity in central nervous system. In this work, we utilized an in vitro model of neural stem cells-derived neurons (nSCNs) to evaluate the role of GSK-3 signaling pathway in Keta-induced neurotoxicity. Embryonic mouse-brain neural stem cells were differentiated into neurons in vitro. Keta (50 μM)-induced neurotoxicity in cultured nSCNs was monitored by apoptosis, immunohistochemical and western blot assays, respectively...
December 7, 2017: Neuromolecular Medicine
https://www.readbyqxmd.com/read/29218106/extracorporeal-shock-wave-therapy-effectively-protects-brain-against-chronic-cerebral-hypo-perfusion-induced-neuropathological-changes
#11
Han-Tan Chai, Kuan-Hung Chen, Christopher Glenn Wallace, Chih-Hung Chen, Pei-Hsun Sung, Yung-Lung Chen, Chun-Man Yuen, Pei-Lin Shao, Cheuk-Kwan Sun, Hsueh-Wen Chang, Ching-Jen Wang, Mel S Lee, Hon-Kan Yip, Sheung-Fat Ko
This study tested the hypothesis that extracorporeal shock wave (ECSW) therapy could protect mouse brain from chronic cerebral hypoperfusion (CHP)-induced neuropathological changes in a bilateral carotid arterial stenosis (CAS) model. Adult-male C57BL/6 (B6) mice (n=36) were randomized into group 1 (sham-control), group 2 (CHP) and group 3 [CHP+ECSW (100 impulses at 0.15 mJ/mm2) on day 5, 10 and 15 after CHP induction]. By day 60 after CHP induction, the white matter lesion, protein expressions of inflammatory (TNF-α/NF-κB/iNOS), oxidative-stress (NOX-1/NOX-2/NOX-4/nitrotyrosine), angiogenesis (eNOS/CD31), apoptotic (Bax/caspase-3/PARP), fibrotic (Smad3/TGF-ß) and mitochondrial-damaged (cytosolic cytochrome-C) biomarkers were significantly higher in group 2 than in groups 1 and 3, and significantly higher in group 3 than in group 1, whereas the protein expressions of anti-apoptotic (Bcl-2), anti-fibrotic (BMP-2/Smad1/5), and mitochondrial-integrity (mitochondrial cytochrome-C) biomarkers showed an opposite pattern to inflammation among the three groups (all P<0...
2017: American Journal of Translational Research
https://www.readbyqxmd.com/read/29218013/lung-oxidative-stress-dna-damage-apoptosis-and-fibrosis-in-adenine-induced-chronic-kidney-disease-in-mice
#12
Abderrahim Nemmar, Turan Karaca, Sumaya Beegam, Priya Yuvaraju, Javed Yasin, Badreldin H Ali
It is well-established that there is a crosstalk between the lung and the kidney, and several studies have reported association between chronic kidney disease (CKD) and pulmonary pathophysiological changes. Experimentally, CKD can be caused in mice by dietary intake of adenine. Nevertheless, the consequence of such intervention on the lung received only scant attention. Here, we assessed the pulmonary effects of adenine (0.2% w/w in feed for 4 weeks)-induced CKD in mice by assessing various physiological histological and biochemical endpoints...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/29217487/genistein-and-daidzein-treatments-differently-affect-uterine-homeostasis-in-the-ovary-intact-middle-aged-rats
#13
Ivana Jarić, Jasmina Živanović, Marko Miler, Vladimir Ajdžanović, Duško Blagojević, Nataša Ristić, Verica Milošević, Nataša Nestorović
This study aimed to investigate the effects of soy isoflavones, genistein (GEN) and daidzein, (DAI) on the uterine function in ovary-intact middle-aged rats. GEN and DAI (35mg/kg) were subcutaneously administrated to acyclic (12-month-old) Wistar females, daily, for 4weeks. Control group received either vehicle (olive oil and ethanol, 9:1) or remained intact. We found that GEN and DAI differently affect uterine morphophysiology. GEN significantly increased the uterine wet weight which was associated with hyperplastic changes, revealed by stereological and histomorphometrical analyses...
December 4, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29216948/-tea-polyphenols-down-regulate-jnk-phosphorylation-to-inhibit-neuron-apoptosis-in-rats-with-cardiac-arrest
#14
Yumei Liu, Thi Phuong Anh Nguyen, Menghua Chen, Lu Xie
OBJECTIVE: To study the effect of tea polyphenols (TP) on c-Jun N-terminal kinase 1/2 (JNK1/2) phosphorylation and cell apoptosis in brain tissues in rats with cardiac arrest (CA) following cardiopulmonary resuscitation (CPR). METHODS: Healthy male Sprague-Dawley (SD) rats were randomly divided into sham group (n = 6), CA group (n = 12), and TP group (n = 12). The rats in CA and TP groups were induced ventricular fibrillation (VF) via esophagus stimulation with alternating current...
December 2017: Zhonghua Wei Zhong Bing Ji Jiu Yi Xue
https://www.readbyqxmd.com/read/29216766/vanillin-mitigates-the-adverse-impact-of-cisplatin-and-methotrexate-on-rat-kidneys
#15
A A Fouad, W N Al-Melhim
The present study investigated the probable protective effect of vanillin (VLN) against kidney injury induced by cisplatin (CSN) and methotrexate (MTX) in rats. The rats received a single injection of either CSN (7.5 mg/kg, i.p.) or MTX (20 mg/kg, i.p.). VLN treatment (150 mg/kg/day, i.p.) was started 1 day before administration of the nephrotoxic agents and continued for 7 days. Both CSN and MTX significantly increased serum creatinine, cystatin C, and neutrophil gelatinase-associated lipocalin and kidney tissue renal malondialdehyde, inducible nitric oxide synthase, tumor necrosis factor-α, interleukin-18, nuclear factor-κB p65, cytosolic cytochrome C, and caspase-3 and significantly decreased renal total antioxidant capacity and Bcl-2/Bax ratio in rats...
January 1, 2017: Human & Experimental Toxicology
https://www.readbyqxmd.com/read/29216630/rapamycin-promotes-the-survival-and-adipogenesis-of-ischemia-challenged-adipose-derived-stem-cells-by-improving-autophagy
#16
Chichi Li, Lechi Ye, Li Yang, Xiaofang Yu, Yucang He, Zhuojie Chen, Liqun Li, Dan Zhang
BACKGROUND/AIMS: Ischemia is one of the main causes of the high rate of absorption of transplanted autologous fat. Autophagy allows cells to survive by providing energy under starvation. Rapamycin has been found to play a role in promoting autophagy. In this study, we investigated whether rapamycin participates in the survival and adipogenesis of ischemia-challenged adipose-derived stem cells (ADSCs) by regulating autophagy. METHODS: Before the cells were exposed to oxygen-glucose deprivation (OGD), a simulated ischemic microenvironment, the level of autophagy was reduced or increased by lentiviral transfection with short hairpin RNA targeting microtubule-associated protein 1-light chain 3 gene (shRNA-LC3) or treatment with rapamycin, respectively...
December 6, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29215373/mangiferin-prevents-the-growth-of-gastric-carcinoma-by-blocking-the-pi3k-akt-signalling-pathway
#17
Min Du, Gang Wen, Juan Jin, Yuanguang Chen, Jun Cao, Aman Xu
The aim of the present study was to investigate the effects of mangiferin on gastric carcinoma cells and to determine the possible mechanisms underlying such effects. The MTT assay was performed to evaluate the antiproliferative effect of mangiferin. Following treatment, apoptosis rates of SGC-7901 were established by flow cytometry and laser confocal microscopy, and western blot analysis was used to detect the expression of apoptosis-related proteins. The MTT assay showed that mangiferin inhibited the proliferation of SGC-7901 and BCG-823 cells in a dose-dependent and time-dependent manner...
December 5, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29214688/nootkatone-confers-hepatoprotective-and-anti-fibrotic-actions-in-a-murine-model-of-liver-fibrosis-by-suppressing-oxidative-stress-inflammation-and-apoptosis
#18
Amani Kurdi, Kamal Hassan, Balaji Venkataraman, Mohanraj Rajesh
In this study, the hepatoprotective and anti-fibrotic actions of nootkatone (NTK) were investigated using carbon tetrachloride (CCl4 )-induced liver fibrosis in mice. CCl4 administration elevated serum aspartate and alanine transaminases levels, respectively. In addition, CCl4 produced hepatic oxidative and nitrative stress, characterized by diminished hemeoxygenase-1 expression, antioxidant defenses, and accumulation of 4-hydroxynonenal and 3-nitrotyrosine. Furthermore, CCl4 administration evoked profound expression of pro-inflammatory cytokine expressions such as tumor necrosis factor-α, monocyte chemoattractant protein-1, and interleukin-1β in hepatic tissues, which corroborated with nuclear factor κB activation...
December 7, 2017: Journal of Biochemical and Molecular Toxicology
https://www.readbyqxmd.com/read/29214600/apoptosis-induction-by-alantolactone-in-breast-cancer-mda-mb-231-cells-through-reactive-oxygen-species-mediated-mitochondrion-dependent-pathway
#19
Li Cui, Weiquan Bu, Jie Song, Liang Feng, Tingting Xu, Dan Liu, Wenbo Ding, Jianhua Wang, Changyang Li, Binge Ma, Yi Luo, Ziyu Jiang, Chengcheng Wang, Juan Chen, Jian Hou, Hongmei Yan, Lei Yang, Xiaobin Jia
Alantolactone is a sesquiterpene lactone isolated from Inula helenium L. Although alantolactone possesses anti-inflammation and apoptosis-induction activities, the underlying mechanism of anti-cancer effect on human breast cancer cells remains largely unknown. In this study, we explored the possibility of alantolactone as an apoptosis-inducing cytotoxic agent using MDA-MB-231 cells as in vitro model. Alantolactone significantly induced its apoptosis, demonstrated by cell cycle analysis, annexin V-APC/7-AAD double staining and dUTP nick end labeling...
December 6, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29210665/synthesis-and-evaluation-of-a-new-series-of-arylidene-indanones-as-potential-anticancer-agents
#20
Ahmet Ozdemir, Sevtem Gokbulut, Belgin Sever, Gulsen Akalın Ciftci, Mehlika Dilek Altıntop
BACKGROUND: Arylidene indanones have attracted a great deal of interest due to their outstanding therapeutic applications. In particular, considerable research has pointed out the importance of arylidene indanones in the field of cancer research. OBJECTIVE: The aim of the current work was to design and synthesize arylidene indanone-based anticancer agents. METHOD: New arylidene indanones were obtained via the Claisen-Schmidt condensation of 5-chloro-6-methoxy-2,3-dihydro-1H-inden-1-one with p-substituted benzaldehyde derivatives...
December 5, 2017: Anti-cancer Agents in Medicinal Chemistry
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