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https://www.readbyqxmd.com/read/28343085/guava-fruit-extract-and-its-triterpene-constituents-have-osteoanabolic-effect-stimulation-of-osteoblast-differentiation-by-activation-of-mitochondrial-respiration-via-the-wnt-%C3%AE-catenin-signaling
#1
Konica Porwal, Subhashis Pal, Kapil Dev, Shyamsundar Pal China, Yogesh Kumar, Chandan Singh, Tarun Barbhuyan, Neeraj Sinha, Sabyasachi Sanyal, Arun Kumar Trivedi, Rakesh Maurya, Naibedya Chattopadhyay
The aim of this study was to evaluate the skeletal effect of guava triterpene-enriched extract (GE) in rats and identify osteogenic compounds thereof, and determine their modes of action. In growing female rats, GE at 250 mg/kg dose increased parameters of peak bone mass including femur length, bone mineral density (BMD) and biomechanical strength, suggesting that GE promoted modeling-directed bone growth. GE also stimulated bone regeneration at the site of bone injury. In adult osteopenic rats (osteopenia induced by ovariectomy, OVX) GE completely restored the lost bones at both axial and appendicular sites, suggesting a strong osteoanabolic effect...
March 8, 2017: Journal of Nutritional Biochemistry
https://www.readbyqxmd.com/read/28342290/verapamil-treatment-induces-cytoprotective-autophagy-by-modulating-cellular-metabolism
#2
Elzbieta Kania, Beata Pajak, Jim O'Prey, Pablo Sierra Gonzalez, Anna Litwiniuk, Kaja Urbańska, Kevin M Ryan, Arkadiusz Orzechowski
Verapamil, an L-type calcium channel blocker, has been used successfully to treat cardiovascular diseases. Interestingly, we have recently shown that treatment of cancer cells with Verapamil causes an effect on autophagy. As autophagy is known to modulate chemotherapy responses, this prompted us to explore the impact of Verapamil on autophagy and cell viability in greater detail. We report here that Verapamil causes an induction of autophagic flux in a number or tumor cells and immortalized normal cells. Moreover, we found that inhibition of autophagy in COLO 205 cells, via treatment with the chloroquine or by CRISPR/Cas9-mediated disruption of the autophagy genes Atg7 and Atg5, causes an upregulation of apoptotic markers in response to Verapamil...
March 25, 2017: FEBS Journal
https://www.readbyqxmd.com/read/28341536/the-role-of-cpla2-in-methylglyoxal-induced-cell-apoptosis-of-huvecs
#3
Jie Yuan, Chao Zhu, Yali Hong, Zongxing Sun, Xianjun Fang, Biao Wu, Shengnan Li
Methylglyoxal (MGO), a highly reactive dicarbonyl compound, is mainly formed as a byproduct of glycolysis. Elevated MGO level is known to induce apoptosis of vascular endothelial cells, which is implicated with progression of atherosclerosis and diabetic complications. However, the underlying mechanisms have not been exhaustively investigated yet. Here, we further characterized the mechanisms how MGO induced apoptosis in human umbilical vein endothelial cells (HUVECs). Our data revealed that cytosolic phospholipase A2 (cPLA2) played an important role in MGO-induced cell apoptosis...
March 21, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28339028/2-methoxyestradiol-enhances-radiosensitivity-in-radioresistant-melanoma-mda-mb-435r-cells-by-regulating-glycolysis-via-hif-1%C3%AE-pdk1-axis
#4
Hong Zhao, Huangang Jiang, Zheng Li, Yafei Zhuang, Yinyin Liu, Shuliang Zhou, Youde Xiao, Conghua Xie, Fuxiang Zhou, Yunfeng Zhou
HIF-1α overexpression is associated with radio-resistance of various cancers. A radioresistant human melanoma cell model MDA-MB-435R (435R) was established by us previously. Compared with the parental cells MDA-MB‑435 (435S), an elevated level of HIF-1α expression in 435R cells was demonstrated in our recent experiments. Therefore, in the current study, we sought to determine whether selective HIF-1α inhibitors could radiosensitize the 435R cells to X-ray, and to identify the potential mechanisms. Our data demonstrated that inhibition of HIF-1α with 2-methoxyestradiol (2-MeOE2) significantly enhanced radiosensitivity of 435R cells...
March 22, 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28332584/akt-targeting-as-a-strategy-to-boost-chemotherapy-efficacy-in-non-small-cell-lung-cancer-through-metabolism-suppression
#5
Marion Le Grand, Raphael Berges, Eddy Pasquier, Marie-Pierre Montero, Laurence Borge, Alice Carrier, Sophie Vasseur, Veronique Bourgarel, Duje Buric, Nicolas André, Diane Braguer, Manon Carré
Metabolic reprogramming is a hallmark of cancer development, mediated by genetic and epigenetic alterations that may be pharmacologically targeted. Among oncogenes, the kinase Akt is commonly overexpressed in tumors and favors glycolysis, providing a rationale for using Akt inhibitors. Here, we addressed the question of whether and how inhibiting Akt activity could improve therapy of non-small cell lung cancer (NSCLC) that represents more than 80% of all lung cancer cases. First, we demonstrated that Akt inhibitors interacted synergistically with Microtubule-Targeting Agents (MTAs) and specifically in cancer cell lines, including those resistant to chemotherapy agents and anti-EGFR targeted therapies...
March 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28325912/lysosomal-activity-maintains-glycolysis-and-cyclin-e1-expression-by-mediating-ad4bp-sf-1-stability-for-proper-steroidogenic-cell-growth
#6
Jhih-Siang Syu, Takashi Baba, Jyun-Yuan Huang, Hidesato Ogawa, Chi-Han Hsieh, Jin-Xian Hu, Ting-Yu Chen, Tzu-Chien Lin, Megumi Tsuchiya, Ken-Ichirou Morohashi, Bu-Miin Huang, Fu-L Lu, Chia-Yih Wang
The development and differentiation of steroidogenic organs are controlled by Ad4BP/SF-1 (adrenal 4 binding protein/steroidogenic factor 1). Besides, lysosomal activity is required for steroidogenesis and also enables adrenocortical cell to survive during stress. However, the role of lysosomal activity on steroidogenic cell growth is as yet unknown. Here, we showed that lysosomal activity maintained Ad4BP/SF-1 protein stability for proper steroidogenic cell growth. Treatment of cells with lysosomal inhibitors reduced steroidogenic cell growth in vitro...
March 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28319810/inhibitors-of-glut-slc2a-enhance-the-action-of-bcnu-and-temozolomide-against-high-grade-gliomas
#7
Alberto Azzalin, Giulia Nato, Elena Parmigiani, Francesca Garello, Annalisa Buffo, Lorenzo Magrassi
Glucose transport across glioblastoma membranes plays a crucial role in maintaining the enhanced glycolysis typical of high-grade gliomas and glioblastoma. We tested the ability of two inhibitors of the glucose transporters GLUT/SLC2A superfamily, indinavir (IDV) and ritonavir (RTV), and of one inhibitor of the Na/glucose antiporter type 2 (SGLT2/SLC5A2) superfamily, phlorizin (PHZ), in decreasing glucose consumption and cell proliferation of human and murine glioblastoma cells. We found in vitro that RTV, active on at least three different GLUT/SLC2A transporters, was more effective than IDV, a specific inhibitor of GLUT4/SLC2A4, both in decreasing glucose consumption and lactate production and in inhibiting growth of U87MG and Hu197 human glioblastoma cell lines and primary cultures of human glioblastoma...
March 17, 2017: Neoplasia: An International Journal for Oncology Research
https://www.readbyqxmd.com/read/28319066/nucleus-accumbens-associated-protein-1-promotes-glycolysis-and-survival-of-hypoxic-tumor-cells-via-the-hdac4-hif-1%C3%AE-axis
#8
Y Zhang, Y-J Ren, L-C Guo, C Ji, J Hu, H-H Zhang, Q-H Xu, W-D Zhu, Z-J Ming, Y-S Yuan, X Ren, J Song, J-M Yang
Nucleus accumbens-associated protein-1 (NAC1), a nuclear factor of the BTB/POZ gene family, has emerging roles in cancer. In this study, we identified the NAC1-HDAC4-HIF-1α axis as an important pathway in regulating glycolysis and hypoxic adaptation in tumor cells. We show that nuclear NAC1 binds to histone deacetylase type 4 (HDAC4), hindering phosphorylation of HDAC4 at Ser(246) and preventing its nuclear export that leads to cytoplasmic degradation of the deacetylase. Accumulation of HDAC4 in the nuclei results in an attenuation of HIF-1α acetylation, enhancing the stabilization and transcriptional activity of HIF-1α and strengthening adaptive response of cells to hypoxia...
March 20, 2017: Oncogene
https://www.readbyqxmd.com/read/28315323/increased-serotonin-signaling-contributes-to-the-warburg-effect-in-pancreatic-tumor-cells-under-metabolic-stress-and-promotes-growth-of-pancreatic-tumors-in-mice
#9
Shu-Heng Jiang, Jun Li, Fang-Yuan Dong, Jian-Yu Yang, De-Jun Liu, Xiao-Mei Yang, Ya-Hui Wang, Min-Wei Yang, Xue-Liang Fu, Xiao-Xin Zhang, Qing Li, Xiu-Feng Pang, Yan-Miao Huo, Jiao Li, Jun-Feng Zhang, Ho-Young Lee, Su-Jae Lee, Wen-Xin Qin, Jian-Ren Gu, Yong-Wei Sun, Zhi-Gang Zhang
BACKGROUND & AIMS: The desmoplasia and poor vascularity cause severe metabolic stress in pancreatic ductal adenocarcinomas (PDACs). Serotonin (5-HT) is a neuromodulator with neurotransmitter and neuroendocrine functions that contributes to tumorigenesis. We investigated the role of 5-HT signaling in the growth of pancreatic tumors. METHODS: We measured the levels of proteins that regulate 5-HT synthesis, packaging, and degradation in pancreata from Kras(G12D/+); Trp53(R172H/+); Pdx1-Cre; (KPC) mice, which develop pancreatic tumors, as well as in PDAC cell lines and a tissue microarray containing 81 human PDAC samples...
March 14, 2017: Gastroenterology
https://www.readbyqxmd.com/read/28300544/pre-analytical-and-analytical-aspects-affecting-clinical-reliability-of-plasma-glucose-results
#10
REVIEW
Sara Pasqualetti, Federica Braga, Mauro Panteghini
The measurement of plasma glucose (PG) plays a central role in recognizing disturbances in carbohydrate metabolism, with established decision limits that are globally accepted. This requires that PG results are reliable and unequivocally valid no matter where they are obtained. To control the pre-analytical variability of PG and prevent in vitro glycolysis, the use of citrate as rapidly effective glycolysis inhibitor has been proposed. However, the commercial availability of several tubes with studies showing different performance has created confusion among users...
March 11, 2017: Clinical Biochemistry
https://www.readbyqxmd.com/read/28298645/role-for-the-atpase-inhibitory-factor-1-in-the-environmental-carcinogen-induced-warburg-phenotype
#11
Kévin Hardonnière, Morgane Fernier, Isabelle Gallais, Baharia Mograbi, Normand Podechard, Eric Le Ferrec, Nathalie Grova, Brice Appenzeller, Agnès Burel, Martine Chevanne, Odile Sergent, Laurence Huc, Sylvie Bortoli, Dominique Lagadic-Gossmann
Most tumors undergo metabolic reprogramming towards glycolysis, the so-called Warburg effect, to support growth and survival. Overexpression of IF1, the physiological inhibitor of the F0F1ATPase, has been related to this phenomenon and appears to be a relevant marker in cancer. Environmental contributions to cancer development are now widely accepted but little is known about the underlying intracellular mechanisms. Among the environmental pollutants humans are commonly exposed to, benzo[a]pyrene (B[a]P), the prototype molecule of polycyclic aromatic hydrocarbons (PAHs), is a well-known human carcinogen...
March 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28285917/examining-the-structure-activity-relationship-of-benzopyran-based-inhibitors-of-the-hypoxia-inducible-factor-1-pathway
#12
Jalisa Ferguson, Zeus De Los Santos, Narra Devi, Erwin Van Meir, Sarah Zingales, Binghe Wang
Many forms of solid tumor have a characteristic feature known as hypoxia, which describes a low or non-existent presence of oxygen in the cellular microenvironment. This decrease in oxygen causes activation of the hypoxia inducible factor (HIF) pathway, which activates the transcription of many genes that cause cell proliferation, metastasis, increased glycolysis and angiogenesis. Increased HIF expression has been linked with poor patient prognosis, increased malignancy, and therapeutic resistance. Previous work in our lab has identified 1 and 2 as inhibitors of the HIF pathway, specifically as disrupters of the p300-HIF-1α complex formation...
March 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28280275/high-mtorc1-activity-drives-glycolysis-addiction-and-sensitivity-to-g6pd-inhibition-in-acute-myeloid-leukemia-cells
#13
L Poulain, P Sujobert, F Zylbersztejn, S Barreau, L Stuani, M Lambert, T L Palama, V Chesnais, R Birsen, F Vergez, T Farge, C Chenevier-Gobeaux, M Fraisse, F Bouillaud, C Debeissat, O Herault, C Récher, C Lacombe, M Fontenay, P Mayeux, T T Maciel, J-C Portais, J-E Sarry, J Tamburini, D Bouscary, N Chapuis
Alterations in metabolic activities are cancer hallmarks that offer a wide range of new therapeutic opportunities. Here, we decipher the interplay between mTORC1 activity and glucose metabolism in acute myeloid leukemia (AML). We show that mTORC1 signaling which is constantly overactivated in AML cells promotes glycolysis and leads to glucose addiction. The level of mTORC1 activity determines the sensitivity of AML cells to glycolysis inhibition as switch-off mTORC1 activity leads to glucose-independent cell survival that is sustained by an increase in mitochondrial oxidative phosphorylation...
March 10, 2017: Leukemia: Official Journal of the Leukemia Society of America, Leukemia Research Fund, U.K
https://www.readbyqxmd.com/read/28275929/in-silico-and-in-vitro-investigation-on-the-phenylalanine-metabolites-interactions-with-hexokinase-of-rat-s-brain-mitochondria
#14
Nasrin Ziamajidi, Shirin Jamshidi, Abdolvahab Ehsani-Zonouz
Hexokinase (HK) is the first enzyme of glycolysis pathway. In brain, most dominant form of HK, HK-I, binds reversibly to the outer mitochondria membrane. Those metabolites that affect binding or releasing of the enzyme from the mitochondria have regulatory effect on glucose consumption of the cell. In this study destructive effect of phenylalanine and its metabolites in relation to glucose metabolism in brain have been studied. The results show that phenylpyruvic acid decreases the activity of enzyme in the presence and absence of glucose-6-phosphate (G6P) and increases the release of the enzyme from mitochondria, whereas phenylalanine and phenyllactic acid have no such effects...
March 8, 2017: Journal of Bioenergetics and Biomembranes
https://www.readbyqxmd.com/read/28275189/glycolysis-glutaminolysis-and-fatty-acid-synthesis-are-required-for-distinct-stages-of-kshv-lytic-replication
#15
Erica L Sanchez, Thomas H Pulliam, Terri A Dimaio, Angel B Thalhofer, Tracie Delgado, Michael Lagunoff
Kaposi's Sarcoma-associated Herpesvirus (KSHV) is the etiologic agent of Kaposi's Sarcoma (KS). KSHV infection induces and requires multiple metabolic pathways, including glycolysis, glutaminolysis and fatty acid synthesis (FAS) for the survival of latently infected endothelial cells. To determine the metabolic requirements for productive KSHV infection, we induced lytic replication in the presence of inhibitors of different metabolic pathways. We found that glycolysis, glutaminolysis and FAS are all required for maximal KSHV virus production and that these pathways appear to participate in virus production at different stages of the viral life cycle...
March 8, 2017: Journal of Virology
https://www.readbyqxmd.com/read/28273955/lack-of-xpc-leads-to-a-shift-between-respiratory-complexes-i-and-ii-but-sensitizes-cells-to-mitochondrial-stress
#16
Mateus P Mori, Rute A P Costa, Daniela T Soltys, Thiago de S Freire, Franco A Rossato, Ignácio Amigo, Alicia J Kowaltowski, Aníbal E Vercesi, Nadja C de Souza-Pinto
Genomic instability drives tumorigenesis and DNA repair defects are associated with elevated cancer. Metabolic alterations are also observed during tumorigenesis, although a causal relationship between these has not been clearly established. Xeroderma pigmentosum (XP) is a DNA repair disease characterized by early cancer. Cells with reduced expression of the XPC protein display a metabolic shift from OXPHOS to glycolysis, which was linked to accumulation of nuclear DNA damage and oxidants generation via NOX-1...
December 2017: Scientific Reports
https://www.readbyqxmd.com/read/28272459/enoblock-a-unique-small-molecule-inhibitor-of-the-non-glycolytic-functions-of-enolase-alleviates-the-symptoms-of-type-2-diabetes
#17
Haaglim Cho, JungIn Um, Ji-Hyung Lee, Woong-Hee Kim, Wan Seok Kang, So Hun Kim, Hyung-Ho Ha, Yong-Chul Kim, Young-Keun Ahn, Da-Woon Jung, Darren R Williams
Type 2 diabetes mellitus (T2DM) significantly impacts on human health and patient numbers are predicted to rise. Discovering novel drugs and targets for treating T2DM is a research priority. In this study, we investigated targeting of the glycolysis enzyme, enolase, using the small molecule ENOblock, which binds enolase and modulates its non-glycolytic 'moonlighting' functions. In insulin-responsive cells ENOblock induced enolase nuclear translocation, where this enzyme acts as a transcriptional repressor. In a mammalian model of T2DM, ENOblock treatment reduced hyperglycemia and hyperlipidemia...
March 8, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28270414/targeting-mtor-signaling-can-prevent-the-progression-of-fsgs
#18
Stefan Zschiedrich, Tillmann Bork, Wei Liang, Nicola Wanner, Kristina Eulenbruch, Stefan Munder, Björn Hartleben, Oliver Kretz, Simon Gerber, Matias Simons, Amandine Viau, Martine Burtin, Changli Wei, Jochen Reiser, Nadja Herbach, Maria-Pia Rastaldi, Clemens D Cohen, Pierre-Louis Tharaux, Fabiola Terzi, Gerd Walz, Markus Gödel, Tobias B Huber
Mammalian target of rapamycin (mTOR) signaling is involved in a variety of kidney diseases. Clinical trials administering mTOR inhibitors to patients with FSGS, a prototypic podocyte disease, led to conflicting results, ranging from remission to deterioration of kidney function. Here, we combined complex genetic titration of mTOR complex 1 (mTORC1) levels in murine glomerular disease models, pharmacologic studies, and human studies to precisely delineate the role of mTOR in FSGS. mTORC1 target genes were significantly induced in microdissected glomeruli from both patients with FSGS and a murine FSGS model...
March 7, 2017: Journal of the American Society of Nephrology: JASN
https://www.readbyqxmd.com/read/28260082/cancer-associated-fibroblasts-enhance-pancreatic-cancer-cell-invasion-by-remodeling-the-metabolic-conversion-mechanism
#19
Tao Shan, Shuo Chen, Xi Chen, Wan Run Lin, Wei Li, Jiancang Ma, Tao Wu, Xijuan Cui, Hong Ji, Yiming Li, Ya'an Kang
We investigated the mechanism of cancer-associated fibroblasts (CAFs) in promoting the invasion and metastasis of pancreatic cancer cells in a non-vascular manner. We verified the original generation of isolated cultured CAFs and normal fibroblasts (NFs) based on the expression of α-SMA and vimentin, and we examined the cell glycolysis level through glucose consumption and lactate production experiments. The mRNA and protein expression of CAF glycolytic enzymes, lactate dehydrogenase and pyruvate kinase m2, were examined by RT-PCR and western blotting, respectively...
February 28, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28255362/her-family-receptors-are-important-theranostic-biomarkers-for-cervical-cancer-blocking-glucose-metabolism-enhances-the-therapeutic-effect-of-her-inhibitors
#20
Olga Martinho, Renato Silva-Oliveira, Fernanda P Cury, Ana Martins Barbosa, Sara Granja, Adriane Feijó Evangelista, Fábio Marques, Vera Miranda-Gonçalves, Diana Cardoso-Carneiro, Flávia E de Paula, Maicon Zanon, Cristovam Scapulatempo-Neto, Marise A R Moreira, Fátima Baltazar, Adhemar Longatto-Filho, Rui Manuel Reis
Persistent HPV infection alone is not sufficient for cervical cancer development, which requires additional molecular alterations for tumor progression and metastasis ultimately leading to a lethal disease. In this study, we performed a comprehensive analysis of HER family receptor alterations in cervical adenocarcinoma. We detected overexpression of HER protein, mainly HER2, which was an independent prognostic marker for these patients. By using in vitro and in vivo approaches, we provided evidence that HER inhibitors, allitinib and lapatinib, were effective in reducing cervical cancer aggressiveness...
2017: Theranostics
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