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dichloroacetate

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https://www.readbyqxmd.com/read/29784240/role-of-reactive-oxygen-species-on-the-activity-of-noble-metal-doped-tio-2-photocatalysts
#1
Paula Ribao, Juan Corredor, Maria J Rivero, Inmaculada Ortiz
Modified TiO2 catalysts are of interest in environmental water remediation since they can lead to efficient electron-hole separation and greatly enhance the photocatalytic properties of TiO2 . Reactive oxygen species (ROS), such as the superoxide radical (O2 - ), hydroxyl radical (OH), and positive valence band holes (h+ VB ), have been reported as the main oxidative species involved in photocatalytic degradation processes. In this work, the role of these species using TiO2 , TiO2 /Pt 0.5 wt%, and TiO2 /Ag 10 wt% has been examined in order to clarify the oxidation pathways...
May 15, 2018: Journal of Hazardous Materials
https://www.readbyqxmd.com/read/29781527/the-role-of-dichloroacetate-in-improving-acute-hypoxic-tolerance-and-cardiac-function-translation-to-failing-hearts
#2
Da Hye Kim, Shelly Chauhan
Cardiac metabolism depends on a high rate of ATP production to maintain its myocardial pump function. Under physiological conditions, more than 70% of ATP generated in the heart is derived from beta oxidation of fatty acids (FA) in the mitochondria. This article is protected by copyright. All rights reserved.
May 21, 2018: Journal of Physiology
https://www.readbyqxmd.com/read/29780561/triple-action-pt-iv-derivatives-of-cisplatin-a-new-class-of-potent-anticancer-agents-that-overcome-resistance
#3
Emanuele Petruzzella, Roman Sirota, Irene Solazzo, Valentina Gandin, Dan Gibson
A series of triple action Pt(iv) prodrugs was designed to test the hypothesis that multi-action compounds, where each bioactive moiety intervenes in several cellular processes, might be more effective than a single agent at killing cancer cells. In particular, "triple action" Pt(iv) derivatives of cisplatin, where the axial ligands are inhibitors of cyclooxygenase (COXi), histone deacetylase (HDACi) or pyruvate dehydrogenase kinase (PDKi) were developed. All compounds, ctc-[Pt(NH3 )2 (COXi)(PDKi)Cl2 ], ctc-[Pt(NH3 )2 (COXi)(HDACi)Cl2 ] and ctc-[Pt(NH3 )2 (HDACi)(PDKi)Cl2 ], where COXi = aspirin or ibuprofen, PDKi = dichloroacetate and HDACi = valproate or phenylbutyrate, were significantly more cytotoxic than cisplatin against all cell lines of an in-house panel of human cancer cells...
May 14, 2018: Chemical Science
https://www.readbyqxmd.com/read/29779193/functional-role-of-tyr12-in-the-catalytic-activity-of-novel-zeta-like-glutathione-s-transferase-from-acidovorax-sp-kks102
#4
Dayyabu Shehu, Zazali Alias
Glutathione S-transferases (GSTs) are a family of enzymes that function in the detoxification of variety of electrophilic substrates. In the present work, we report a novel zeta-like GST (designated as KKSG9) from the biphenyl/polychlorobiphenyl degrading organism Acidovorax sp. KKS102. KKSG9 possessed low sequence similarity but similar biochemical properties to zeta class GSTs. Functional analysis showed that the enzyme exhibits wider substrate specificity compared to most zeta class GSTs by reacting with 1-chloro-2,4-dinitrobenzene (CDNB), p-nitrobenzyl chloride (NBC), ethacrynic acid (EA), hydrogen peroxide, and cumene hydroperoxide...
May 19, 2018: Protein Journal
https://www.readbyqxmd.com/read/29775761/the-bone-anabolic-effects-of-irisin-are-through-preferential-stimulation-of-aerobic-glycolysis
#5
Dingdong Zhang, ChuHyun Bae, Junghak Lee, Jiho Lee, Zeyu Jin, Myeongmo Kang, Young Suk Cho, Jeong-Han Kim, Weontae Lee, Sung-Kil Lim
Irisin, a recently identified hormone secreted by skeletal muscle in response to exercise, exhibits anabolic effects on the skeleton primarily through the stimulation of bone formation. However, the mechanism underlying the irisin-stimulated anabolic response remains largely unknown. To uncover the underlying mechanism, we biosynthesized recombinant irisin (r-irisin) using an Escherichia coli expression system and used it to treat several osteoblast cell types. Our synthesized r-irisin could promote proliferation and differentiation of osteoblasts as evidenced by enhanced expression of osteoblast-specific transcriptional factors, including Runt-related transcription factor-2 (Runx2), Oster (Osx), as well as early osteoblastic differentiation markers such as alkaline phosphatase (Alp) and collagen type I alpha 1 (Col1a1)...
May 15, 2018: Bone
https://www.readbyqxmd.com/read/29766157/dual-acting-antitumor-pt-iv-prodrugs-of-kiteplatin-with-dichloroacetate-axial-ligands
#6
Salvatore Savino, Valentina Gandin, James D Hoeschele, Cristina Marzano, Giovanni Natile, Nicola Margiotta
With the aim to obtain dual acting drugs able to target both nuclear DNA and mitochondria, Pt(iv) kiteplatin derivatives having dichloroacetate (DCA) ligands in axial positions have been synthesized. The rather fast hydrolysis (t1/2 of ca. 1 h) and reduction (by ascorbic acid) of these Pt(iv) derivatives did not impede a potent pharmacological effect on tumor cells. Moreover, similarly to kiteplatin, also the Pt(iv)-DCA compounds proved to be capable of overcoming oxaliplatin-resistance, which is particularly important in view of the fact that metastatic colorectal cancer is the third most common cancer in males and the second in females...
May 16, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/29739849/a-novel-inhibitor-of-pyruvate-dehydrogenase-kinase-stimulates-myocardial-carbohydrate-oxidation-in-diet-induced-obesity
#7
Cheng-Yang Wu, Santhosh Satapati, Wenjun Gui, Richard M Wynn, Gaurav Sharma, Mingliang Lou, Xiangbing Qi, Shawn C Burgess, Craig Malloy, Chalermchai Khemtong, A Dean Sherry, David Chuang, Matthew E Merritt
The pyruvate dehydrogenase complex (PDC) is a key control point of energy metabolism and is subject to regulation by multiple mechanisms, including post-translational phosphorylation by pyruvate dehydrogenase kinase (PDK). Pharmacological modulation of PDC activity could provide a new treatment for diabetic cardiomyopathy, as dysregulated substrate selection is concomitant with decreased heart function. Dichloroacetate (DCA), a classic PDK inhibitor, has been used to treat diabetic cardiomyopathy, but the lack of specificity and side effects of DCA indicate a more specific inhibitor of PDK is needed...
May 8, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29704441/improving-culture-performance-and-antibody-production-in-cho-cell-culture-processes-by-reducing-the-warburg-effect
#8
Maria Buchsteiner, Lake-Ee Quek, Peter Gray, Lars K Nielsen
Lactate is one of the key waste metabolites of mammalian cell culture. High lactate levels are caused by high aerobic glycolysis, also known as the Warburg effect, and are usually associated with adverse culture performance. Therefore, reducing lactate accumulation has been an ongoing challenge in cell culture development in order to improve growth, productivity and process robustness. The pyruvate dehydrogenase complex (PDC) plays a crucial role for the fate of pyruvate, as it converts pyruvate to acetyl-CoA...
April 28, 2018: Biotechnology and Bioengineering
https://www.readbyqxmd.com/read/29653124/doxorubicin-triggers-bioenergetic-failure-and-p53-activation-in-mouse-stem-cell-derived-cardiomyocytes
#9
Teresa Cunha-Oliveira, Luciana L Ferreira, Ana Raquel Coelho, Cláudia M Deus, Paulo J Oliveira
Doxorubicin (DOX) is a widely used anticancer drug that could be even more effective if its clinical dosage was not limited because of delayed cardiotoxicity. Beating stem cell-derived cardiomyocytes are a preferred in vitro model to further uncover the mechanisms of DOX-induced cardiotoxicity. Our objective was to use cultured induced-pluripotent stem cell(iPSC)-derived mouse cardiomyocytes (Cor.At) to investigate the effects of DOX on cell and mitochondrial metabolism, as well as on stress responses. Non-proliferating and beating Cor...
April 10, 2018: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/29626439/regulation-of-dichloroacetate-biotransformation-in-rat-liver-and-extrahepatic-tissues-by-gstz1-expression-and-chloride-concentration
#10
Stephan C Jahn, Marci G Smeltz, Zhiwei Hu, Laura Rowland-Faux, Guo Zhong, Ryan J Lorenzo, Katherine V Cisneros, Peter W Stacpoole, Margaret O James
Biotransformation of dichloroacetate (DCA) to glyoxylate by hepatic glutathione transferase zeta 1 (GSTZ1) is considered the principal determinant of the rate of plasma clearance of the drug. However, several other organismal and subcellular factors are also known to influence DCA metabolism. We utilized a female rat model to study these poorly understood processes. Rats aged 4 weeks (young) and 42 to 52 weeks (adult) were used to model children and adults, respectively. Hepatic chloride concentrations, which influence the rate of GSTZ1 inactivation by DCA, were lower in rat than in human tissues and rats did not show the age dependence previously seen in humans...
April 4, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29602463/treating-patients-suffering-from-myalgic-encephalopathy-chronic-fatigue-syndrome-me-cfs-with-sodium-dichloroacetate-an-open-label-proof-of-principle-pilot-trial
#11
Frank Comhaire
Twenty-two consecutive patients suffering from refractory myalgic encephalitis/chronic fatigue syndrome (ME/CFS) were treated with an innovative nutriceutical containing sodium dichloroacetate in a proof-of-principle, pilot, open-label prospective cohort trial. Ten patients experienced significant improvement of their health condition with reduction to almost half of their score in the fatigue severity scale. In twelve patients treatment failed to exert any beneficial effect. In the latter patients several other diseases have commonly been revealed by extensive biological and imaging investigations...
May 2018: Medical Hypotheses
https://www.readbyqxmd.com/read/29593636/combined-treatment-with-dichloroacetic-acid-and-pyruvate-reduces-hippocampal-neuronal-death-after-transient-cerebral-ischemia
#12
Dae Ki Hong, A Ra Kho, Bo Young Choi, Song Hee Lee, Jeong Hyun Jeong, Sang Hwon Lee, Kyoung-Ha Park, Jae-Bong Park, Sang Won Suh
Transient cerebral ischemia (TCI) occurs when blood flow to the brain is ceased or dramatically reduced. TCI causes energy depletion and oxidative stress, which leads to neuronal death and cognitive impairment. Dichloroacetic acid (DCA) acts as an inhibitor of pyruvate dehydrogenase kinase (PDK). Additionally, DCA is known to increase mitochondrial pyruvate uptake and promotes glucose oxidation during glycolysis, thus enhancing pyruvate dehydrogenase (PDH) activity. In this study, we investigated whether the inhibition of PDK activity by DCA, which increases the rate of pyruvate conversion to adenosine triphosphate (ATP), prevents ischemia-induced neuronal death...
2018: Frontiers in Neurology
https://www.readbyqxmd.com/read/29563787/a-facile-doxorubicin-dichloroacetate-conjugate-nanomedicine-with-high-drug-loading-for-safe-drug-delivery
#13
Conglian Yang, Tingting Wu, Yuting Qin, Yan Qi, Yu Sun, Miao Kong, Xue Jiang, Xianya Qin, Yaqi Shen, Zhiping Zhang
Background: Doxorubicin (DOX) is an effective chemotherapeutic agent but severe side effects limit its clinical application. Nanoformulations can reduce the toxicity while still have various limitations, such as complexity, low drug loading capability and excipient related concerns. Methods: An amphiphilic conjugate, doxorubicin-dichloroacetate, was synthesized and the corresponding nanoparticles were prepared. The in vitro cytotoxicity and intracellular uptake, in vivo imaging, antitumor effects and systemic toxicities of nanoparticles were carried out to evaluate the therapeutic efficiency of tumor...
2018: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/29555557/monte-carlo-and-multi-exposure-assessment-for-the-derivation-of-criteria-for-disinfection-byproducts-and-volatile-organic-compounds-in-drinking-water-allocation-factors-and-liter-equivalents-per-day
#14
Megumi Akiyama, Yoshihiko Matsui, Junki Kido, Taku Matsushita, Nobutaka Shirasaki
The probability distributions of total potential doses of disinfection byproducts and volatile organic compounds via ingestion, inhalation, and dermal exposure were estimated with Monte Carlo simulations, after conducting physiologically based pharmacokinetic model simulations to takes into account the differences in availability between the three exposures. If the criterion that the 95th percentile estimate equals the TDI (tolerable daily intake) is regarded as protecting the majority of a population, the drinking water criteria would be 140 (trichloromethane), 66 (bromodichloromethane), 157 (dibromochloromethane), 203 (tribromomethane), 140 (dichloroacetic acid), 78 (trichloroacetic acid), 6...
June 2018: Regulatory Toxicology and Pharmacology: RTP
https://www.readbyqxmd.com/read/29538422/bidesmosidic-betulin-saponin-bearing-l-rhamnopyranoside-moieties-induces-apoptosis-and-inhibition-of-lung-cancer-cells-growth-in-vitro-and-in-vivo
#15
Mouadh Mihoub, André Pichette, Balla Sylla, Charles Gauthier, Jean Legault
Betulin has a wide range of biological and pharmacological properties with its anticancer activity attracting most of the attention as it offers a possible alternative treatment to chemotherapy. However, betulin's in vivo biological effectiveness is limited by its poor solubility. As such, we synthesized polar glycosylated derivatives to increase its hydrosolubility and enhance its pharmacological properties. Among these synthesized compounds, 28-O-α-l-rhamnopyranosylbetulin 3β-O-α-l-rhamnopyranoside (Bi-L-RhamBet) was assessed for its cytotoxic effects against a suite of lung cancer cell lines...
2018: PloS One
https://www.readbyqxmd.com/read/29495001/akt-independent-activation-of-p38-map-kinase-promotes-vascular-calcification
#16
Youfeng Yang, Yong Sun, Jianye Chen, Wayne E Bradley, Louis J Dell'Italia, Hui Wu, Yabing Chen
Vascular calcification is prevalent in patients with atherosclerosis, and oxidative stress promotes pathogenesis of atherosclerosis. We have previously reported that activation of AKT by oxidative stress induces vascular calcification. Using sodium dichloroacetate (DCA), a previously reported small molecule inhibitor of AKT, the present studies uncovered an AKT-independent mechanism in regulating vascular calcification. We found that DCA dose-dependently induced calcification of vascular smooth muscle cells (VSMC) in vitro and aortic rings ex vivo...
June 2018: Redox Biology
https://www.readbyqxmd.com/read/29485148/enhancing-anticancer-cytotoxicity-through-bimodal-drug-delivery-from-ultrasmall-zr-mof-nanoparticles
#17
Isabel Abánades Lázaro, Sandra Abánades Lázaro, Ross S Forgan
Dual delivery of dichloroacetate and 5-fluorouracil from Zr MOFs into cancer cells is found to enhance in vitro cytotoxicity. Tuning particle size and, more significantly, surface chemistry, further improves cytotoxicity by promoting caveolae-mediated endocytosis and cytosolic cargo delivery.
March 13, 2018: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/29471628/activation-of-pyruvate-dehydrogenase-by-sodium-dichloroacetate-shifts-metabolic-consumption-from-amino-acids-to-glucose-in-ipec-j2-cells-and-intestinal-bacteria-in-pigs
#18
Rui An, Zhiru Tang, Yunxia Li, Tiejun Li, Qingqing Xu, Jifu Zhen, Feiru Huang, Jing Yang, Cheng Chen, Zhaoliang Wu, Mao Li, Jiajing Sun, Xiangxin Zhang, Jinchao Chen, Liuting Wu, Shengjun Zhao, Jiang Qingyan, Weiyun Zhu, Yulong Yin, Zhihong Sun
The extensive metabolism of amino acids (AA) as fuel is an important reason for the low use efficiency of protein in pigs. In this study, we investigated whether regulation of the pyruvate dehydrogenase kinase (PDK)/pyruvate dehydrogenase alpha 1 (PDHA1) pathway affected AA consumption by porcine intestinal epithelial (IPEC-J2) cells and intestinal bacteria in pigs. The effects of knockdown of PDHA1 and PDK1 with small interfering RNA (siRNA) on nutrient consumption by IPEC-J2 cells were evaluated. IPEC-J2 cells were then cultured with sodium dichloroacetate (DCA) to quantify AA and glucose consumption and nutrient oxidative metabolism...
April 18, 2018: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/29451305/treading-slowly-through-hypoxic-waters-dichloroacetate-to-the-rescue
#19
Golam Mezbah Uddin, Kim L Ho, Gary D Lopaschuk
No abstract text is available yet for this article.
February 16, 2018: Journal of Physiology
https://www.readbyqxmd.com/read/29431735/vhl-deletion-in-osteoblasts-boosts-cellular-glycolysis-and-improves-global-glucose-metabolism
#20
Naomi Dirckx, Robert J Tower, Evi M Mercken, Roman Vangoitsenhoven, Caroline Moreau-Triby, Tom Breugelmans, Elena Nefyodova, Ruben Cardoen, Chantal Mathieu, Bart Van der Schueren, Cyrille B Confavreux, Thomas L Clemens, Christa Maes
The skeleton has emerged as an important regulator of systemic glucose homeostasis, with osteocalcin and insulin representing prime mediators of the interplay between bone and energy metabolism. However, genetic evidence indicates that osteoblasts can influence global energy metabolism through additional, as yet unknown, mechanisms. Here, we report that constitutive or postnatally induced deletion of the hypoxia signaling pathway component von Hippel-Lindau (VHL) in skeletal osteolineage cells of mice led to high bone mass as well as hypoglycemia and increased glucose tolerance, not accounted for by osteocalcin or insulin...
March 1, 2018: Journal of Clinical Investigation
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