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https://www.readbyqxmd.com/read/28340411/synthesis-and-biological-evaluation-of-novel-chalcone-derivatives-as-a-new-class-of-microtubule-destabilizing-agents
#1
Xiaochao Huang, Rizhen Huang, Lingxue Li, Shaohua Gou, Hengshan Wang
A series of novel chalcone derivatives were designed and synthesized as potential antitumor agents. Structures of target molecules were confirmed by (1)H NMR, (13)C NMR and HR-MS, and evaluated for their in vitro anti-proliferative activities using MTT assay. Among them, compound 12k displayed potent activity against the test tumor cell lines including multidrug resistant human cancer lines, with the IC50 values ranged from 3.75 to 8.42 μM. In addition, compound 12k was found to induce apoptosis in NCI-H460 cells via the mitochondrial pathway, including an increase of the ROS level, loss of mitochondrial membrane potential, release of cytochrome c, down-regulation of Bcl-2, up-regulation of Bax, activation of caspase-9 and caspase-3, respectively...
March 18, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28339853/prosurvival-effect-of-cumulus-prostaglandin-g-h-synthase-2-prostaglandin2-signaling-on-bovine-blastocyst-impact-on-in-vivo-posthatching-development%C3%A2
#2
Fabienne Nuttinck, Alice Jouneau, Gilles Charpigny, Isabelle Hue, Christophe Richard, Pierre Adenot, Sylvie Ruffini, Ludivine Laffont, Martine Chebrout, Véronique Duranthon, Brigitte Marquant-Le Guienne
Apoptotic activity is a common physiological process which culminates at the blastocyst stage in the preimplantation embryo of many mammals. The degree of embryonic cell death can be influenced by the oocyte microenvironment. However, the prognostic significance of the incidence of apoptosis remains undefined. Prostaglandin E2 (PGE2) derived from prostaglandin G/H synthase-2 (PTGS2) activity is a well-known prosurvival factor that is mainly studied in oncology. PGE2 is the predominant PTGS2-derived prostaglandin present in the oocyte microenvironment during the periconceptional period...
March 7, 2017: Biology of Reproduction
https://www.readbyqxmd.com/read/28338203/mir-155-regulates-oral-squamous-cell-carcinoma-tca8113-cell-proliferation-cycle-and-apoptosis-via-regulating-p27kip1
#3
S Fu, H-H Chen, P Cheng, C-B Zhang, Y Wu
OBJECTIVE: P27Kip1 is the one of the negative regulators of the cell cycle that plays an important role in regulating cell cycle and inhibiting cell proliferation by restraining cell in G1 phase. P27Kip1 downregulation maybe related to the occurrence of oral squamous cell carcinoma (OSCC). It was found that miR-155 significantly upregulated in OSCC tissue. Bioinformatics analysis revealed that miR-155 may bind with the 3'-UTR of p27Kip1. This study investigated the role of miR-155 in regulating p27Kip1 and affecting Tca8113 cell proliferation, cycle, and apoptosis...
March 2017: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/28337703/umi-77-primes-glioma-cells-for-trail-induced-apoptosis-by-unsequestering-bim-and-bak-from-mcl-1
#4
Ji-Wei Liu, Zhi-Chuan Zhu, Kui Li, Hong-Tao Wang, Zhi-Qi Xiong, Jing Zheng
Malignant glioma is the most common and aggressive form of brain tumor with poor prognosis of survival. Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) is a promising anticancer agent but is insufficient of inducing apoptosis in some types of gliomas. In this study, we showed that the small-molecule Mcl-1 inhibitor UMI-77 sensitized glioma cells to TRAIL treatment, as evidenced by cell viability assay, Annexin V staining and JC-1 staining. Combination of UMI-77 and TRAIL in glioma cells led to the activation of caspase-8 and Bid, cleavage of caspase-3 and poly-ADP ribose polymerase (PARP), accumulation of tBid in the mitochondria and release of cytochrome c into the cytosol...
March 23, 2017: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/28337253/hepatoprotective-effects-of-antrodia-cinnamomea-the-modulation-of-oxidative-stress-signaling-in-a-mouse-model-of-alcohol-induced-acute-liver-injury
#5
Yange Liu, Juan Wang, Lanzhou Li, Wenji Hu, Yidi Qu, Yipei Ding, Lina Meng, Lirong Teng, Di Wang
In the present study, the components of A. cinnamomea (AC) mycelia were systematically analyzed. Subsequently, its hepatoprotective effects and the underlying mechanisms were explored using a mouse model of acute alcohol-induced liver injury. AC contained 25 types of fatty acid, 16 types of amino acid, 3 types of nucleotide, and 8 types of mineral. The hepatoprotective effects were observed after 2 weeks of AC treatment at doses of 75 mg/kg, 225 mg/kg, and 675 mg/kg in the mouse model. These effects were indicated by the changes in the levels of aspartate aminotransferase, alanine aminotransferase, several oxidation-related factors, and inflammatory cytokines in serum and/or liver samples...
2017: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/28337252/small-interfering-rna-targeting-mitochondrial-calcium-uniporter-improves-cardiomyocyte-cell-viability-in-hypoxia-reoxygenation-injury-by-reducing-calcium-overload
#6
Yuriana Oropeza-Almazán, Eduardo Vázquez-Garza, Héctor Chapoy-Villanueva, Guillermo Torre-Amione, Gerardo García-Rivas
Intracellular Ca(2+) mishandling is an underlying mechanism in hypoxia/reoxygenation (H/R) injury that results in mitochondrial dysfunction and cardiomyocytes death. These events are mediated by mitochondrial Ca(2+) (mCa(2+)) overload that is facilitated by the mitochondrial calcium uniporter (MCU) channel. Along this line, we evaluated the effect of siRNA-targeting MCU in cardiomyocytes subjected to H/R injury. First, cardiomyocytes treated with siRNA demonstrated a reduction of MCU expression by 67%, which resulted in significant decrease in mitochondrial Ca(2+) transport...
2017: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/28335888/second-and-third-generation-drugs-for-immuno-oncology-treatment-the-more-the-better
#7
REVIEW
Wolfram C M Dempke, Klaus Fenchel, Peter Uciechowski, Stephen P Dale
Recent success in cancer immunotherapy (anti-CTLA-4, anti-PD1/PD-L1) has confirmed the hypothesis that the immune system can control many cancers across various histologies, in some cases producing durable responses in a way not seen with many small-molecule drugs. However, only less than 25% of all patients do respond to immuno-oncology drugs and several resistance mechanisms have been identified (e.g. T-cell exhaustion, overexpression of caspase-8 and β-catenin, PD-1/PD-L1 gene amplification, MHC-I/II mutations)...
March 2017: European Journal of Cancer
https://www.readbyqxmd.com/read/28331100/microrna-434-3p-regulates-age-related-apoptosis-through-eif5a1-in-the-skeletal-muscle
#8
Patricia S Pardo, Ameena Hajira, Aladin M Boriek, Junaith S Mohamed
Sarcopenia is caused by increased activation of catabolic pathways, including apoptosis. However, the mechanism underlying sarcopenia is not well understood. We report that aging alters miRNA expression profile as evidenced by miRNA microarray and real-time PCR. Our data show that miR-434-3p is highly downregulated miRNA in skeletal muscles of the aging mouse and provided the first evidence that miR-434 is a novel regulator of apoptosis. Myocytes transfected with miR-434-3p mimic prevents apoptosis induced by various apoptotic stimuli, and that inhibitory role of miR-434-3p was abolished by its antagomir, suggesting a role for miR-434-3p in apoptosis...
March 22, 2017: Aging
https://www.readbyqxmd.com/read/28327651/inhibition-of-cathepsin-s-confers-sensitivity-to-methyl-protodioscin-in-oral-cancer-cells-via-activation-of-p38-mapk-jnk-signaling-pathways
#9
Ming-Ju Hsieh, Chiao-Wen Lin, Mu-Kuan Chen, Su-Yu Chien, Yu-Sheng Lo, Yi-Ching Chuang, Yi-Ting Hsi, Chia-Chieh Lin, Jui-Chieh Chen, Shun-Fa Yang
Oral cancer is one of the most common cancers in the world. Approximately 90% of oral cancers are subtyped to oral squamous cell carcinoma (OSCC). Despite advances in diagnostic techniques and improvement in treatment modalities, the prognosis remains poor. Therefore, an effective chemotherapy mechanism that enhances tumor sensitivity to chemotherapeutics is urgently needed. Methyl protodioscin (MP) is a furostanol bisglycoside with a wide range of beneficial effects, including anti-inflammatory and anti-cancer properties...
March 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28327595/x-linked-inhibitor-of-apoptosis-inhibits-apoptosis-and-preserves-the-blood-brain-barrier-after-experimental-subarachnoid-hemorrhage
#10
Cheng Gao, Hongwei Yu, Cong Yan, Wenyang Zhao, Yao Liu, Dongdong Zhang, Jingwei Li, Nan Liu
Early brain injury following subarachnoid hemorrhage (SAH) strongly determines the prognosis of patients suffering from an aneurysm rupture, and apoptosis is associated with early brain injury after SAH. This study was designed to explore the role of X-linked inhibitor of apoptosis (XIAP) in early brain injury following SAH. The expression of XIAP was detected using western blotting and real-time RT-PCR in an autologous blood injection model of SAH. We also studied the role of XIAP in early brain injury and detected apoptosis-related proteins...
March 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28325143/synthesis-and-characterization-of-a-new-benzo-indole-derivative-with-apoptotic-activity-against-colon-cancer-cells
#11
Fatemeh Hajiaghaalipou, Fadhil Lafta Faraj, Elham Bagheri, Hamid Khaledi, Hapipah Mohd Ali, Nazia Abdul Majid, Mahmood Ameen Abdulla
BACKGROUND: Colorectal cancer is the third most common form of cancer in both men and women around the world. The chemistry and biological study of heterocyclic compounds have been an interesting area for a long time in pharmaceutical and medicinal chemistry. METHODS: A new synthetic compound, 2-(1,1-Dimethyl-1,3-dihydro-benzo[e]indol-2-ylidene)-3-(2-hydroxy-phenylimino)-propionaldehyde, abbreviated as DBID has been synthesized by reaction of 2-(1,1-Dimethyl-1,3-dihydro-benzo[e]indol-2-ylidene)-malonaldehyde with 2-aminophenol...
March 20, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28323918/elucidating-the-role-of-the-desmosome-protein-p53-apoptosis-effector-related-to-pmp-22-perp-in-growth-hormone-tumors
#12
Katja Kiseljak-Vassiliades, Taylor S Mills, Yu Zhang, Mei Xu, Kevin O Lillehei, B K Kleinschmidt-DeMasters, Margaret E Wierman
Purpose: Densely granulated (DG) and sparsely granulated (SG) growth hormone (GH) pituitary adenomas differ in biological behavior which may be correlated with their known differences in cytoplasmic keratin distribution and E-cadherin expression. We desired to explore candidate genes which might further explain this behavior. Methods: Exon expression microarray was performed on 21 GH tumors (10 SG and 11 DG) and 20 normal control pituitaries from autopsy. Results: Bioinformatic analyses confirmed a differential molecular signature between normal pituitary and GH tumors as well as between the GH tumor subtypes...
February 9, 2017: Endocrinology
https://www.readbyqxmd.com/read/28316571/anti-cancerous-potential-of-polysaccharide-fractions-extracted-from-peony-seed-dreg-on-various-human-cancer-cell-lines-via-cell-cycle-arrest-and-apoptosis
#13
Fang Zhang, Jun-Jun Shi, Kiran Thakur, Fei Hu, Jian-Guo Zhang, Zhao-Jun Wei
In this study, four homo/heterogenous polysaccharides (HBSS, CHSS, DASS, and CASS) extracted from peony seed dreg with respective molecular weights of 3467, 4677, 229, and 56 kDa were evaluated for anti-cancerous attributes in prostate cancer cells (Pc-3), colon cancer cells (HCT-116), human breast cancer cells (MCF-7), cervical cancer (Hela cells) and human embryonic kidney 293 (HEK 293) cells as control. Among them, CASS and DASS extracted by alkali, consisted of 34.43% Gal, 26.39% Ara, 21.80% Glc and 35...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28315687/-10-gingerol-a-major-phenolic-constituent-of-ginger-root-induces-cell-cycle-arrest-and-apoptosis-in-triple-negative-breast-cancer-cells
#14
Megan M Bernard, Jason R McConnery, David W Hoskin
The ginger rhizome is rich in bioactive compounds, including [6]-gingerol, [8]-gingerol, and [10]-gingerol; however, to date, most research on the anti-cancer activities of gingerols have focused on [6]-gingerol. In this study, we compared [10]-gingerol with [8]-gingerol and [6]-gingerol in terms of their ability to inhibit the growth of human and mouse mammary carcinoma cells. A colorimetric assay based on the enzymatic reduction of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide revealed that [10]-gingerol was more potent than [6]-gingerol and at least as potent as [8]-gingerol for the inhibition of triple-negative human (MDA-MB-231, MDA-MB-468) and mouse (4T1, E0771) mammary carcinoma cell growth...
March 16, 2017: Experimental and Molecular Pathology
https://www.readbyqxmd.com/read/28315432/splicing-factors-of-sr-and-hnrnp-families-as-regulators-of-apoptosis-in-cancer
#15
Hanna Kędzierska, Agnieszka Piekiełko-Witkowska
SR and hnRNP proteins were initially discovered as regulators of alternative splicing: the process of controlled removal of introns and selective joining of exons through which multiple transcripts and, subsequently, proteins can be expressed from a single gene. Alternative splicing affects genes involved in all crucial cellular processes, including apoptosis. During cancerogenesis impaired apoptotic control facilitates survival of cells bearing molecular aberrations, contributing to their unrestricted proliferation and chemoresistance...
March 14, 2017: Cancer Letters
https://www.readbyqxmd.com/read/28315386/card9-mediated-ambient-pm2-5-induced-pulmonary-injury-is-associated-with-th17-cell
#16
Shuo Jiang, Liang Bo, Xihao Du, Jie Liu, Xuejiao Zeng, Guanglong He, Qinghua Sun, Haidong Kan, Weimin Song, Yuquan Xie, Jinzhuo Zhao
Inflammation and oxidative stress are important risk factors in PM2.5-induced injury. The current study attempted to study the role of caspase recruitment domain (CARD) 9 in ambient PM2.5-induced pulmonary injury in mice. The CARD9(-/-) and C57BL/6 mice were exposed to 3.6, 7.8 and 15.6mg/kg.bw of PM2.5 or saline by intratracheal instillation. After the last PM2.5 exposure, the spleen, bronchoalveolar lavage fluid (BALF) and pulmonary tissue were collected and examined. The results showed that PM2.5 exposure induced inflammatory cell infiltration and alveolar septal thickening in the lung...
March 14, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28315173/ricolinostat-a-selective-hdac6-inhibitor-shows-anti-lymphoma-cell-activity-alone-and-in-combination-with-bendamustine
#17
Maria Cosenza, Monica Civallero, Luigi Marcheselli, Stefano Sacchi, Samantha Pozzi
Histone deacetylase inhibitors (HDACis) have emerged as a new class of anticancer agents, targeting the biological process including cell cycle and apoptosis. We investigated and explained the anticancer effects of an HDAC6 inhibitor, ricolinostat alone and in combination with bendamustine in lymphoma cell lines. Cell viability was measured by MTT assay. Apoptosis, reactive oxygen species (ROS) generation, Bcl-2 protein expression, cell cycle progression and tubuline expression were determined by flow cytometry...
March 17, 2017: Apoptosis: An International Journal on Programmed Cell Death
https://www.readbyqxmd.com/read/28314430/calf-spleen-extractive-injection-csei-a-small-peptides-enriched-extraction-induces-human-hepatocellular-carcinoma-cell-apoptosis-via-ros-mapks-dependent-mitochondrial-pathway
#18
Dongxu Jia, Wenqian Lu, Xinrui Zhang, Guangsheng Cai, Lirong Teng, Xinyu Wang, Minghai Zhang, Yan Zeng, Chunhua Liang, Di Wang
Calf Spleen Extractive Injection (CSEI), a small peptides enriched extraction, performs immunomodulatory activity on cancer patients suffering from radiotherapy or chemotherapy. The present study aims to investigate the anti-hepatocellular carcinoma effects of CSEI in cells and tumor-xenografted mouse models. In HepG2 and SMMC-7721 cells, CSEI reduced cell viability, enhanced apoptosis rate, caused reactive oxygen species (ROS) accumulation, inhibited migration ability, and induced caspases cascade and mitochondrial membrane potential dissipation...
October 2016: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28306139/the-tir-bb-loop-mimetic-as-1-prevents-nonalcoholic-steatohepatitis-and-hepatic-insulin-resistance-by-inhibiting-nlrp3-asc-inflammasome-activation
#19
Xiaolu Wang, Yun Gao, Juan Song, Chao Tang, Man Wang, Linli Que, Li Liu, Guoqing Zhu, Qi Chen, Yong Yao, Yong Xu, Jiantao Li, Yuehua Li
BACKGROUND AND PURPOSE: Non-alcoholic steatohepatitis (NASH) is characterized by excessive intracellular lipid accumulation, inflammation and hepatic insulin resistance. Considering the rising prevalence of NASH worldwide, it is urgent to find novel interventional approaches. The pro-inflammatory cytokine IL-1β, generated and released from the Kupffer cells, is considered to be an initiating event in NASH. AS-1, a synthetic low-molecule mimetic to myeloid differentiation primary response gene 88 (MyD88), has been reported to disrupt the IL-1R-MyD88 interaction...
March 17, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28303974/antifibrotic-effect-of-pirfenidone-in-a-mouse-model-of-human-nonalcoholic-steatohepatitis
#20
Chikara Komiya, Miyako Tanaka, Kyoichiro Tsuchiya, Noriko Shimazu, Kentaro Mori, Shunsaku Furuke, Yasutaka Miyachi, Kumiko Shiba, Shinobu Yamaguchi, Kenji Ikeda, Kozue Ochi, Kazuhiko Nakabayashi, Ken-Ichiro Hata, Michiko Itoh, Takayoshi Suganami, Yoshihiro Ogawa
Non-alcoholic steatohepatitis (NASH) is characterized by steatosis with lobular inflammation and hepatocyte injury. Pirfenidone (PFD) is an orally bioavailable pyridone derivative that has been clinically used for the treatment of idiopathic pulmonary fibrosis. However, it remains unknown whether PFD improves liver fibrosis in a mouse model with human NASH-like phenotypes. In this study, we employed melanocortin 4 receptor-deficient (MC4R-KO) mice as a mouse model with human NASH-like phenotypes to elucidate the effect and action mechanisms of PFD on the development of NASH...
March 17, 2017: Scientific Reports
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