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Chemico-biological Interactions

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https://www.readbyqxmd.com/read/28235427/efficient-t3p-%C3%A2-mediated-synthesis-differential-cytotoxicity-and-apoptosis-induction-by-indolo-triazolo-thiadiazoles-in-human-breast-adenocarcinoma-cells
#1
Pooja R Kamath, Dhanya Sunil, Shubhankar Das, Abdul A Ajees, B S Satish Rao
The limited efficacy of marketed anticancer agents demands the design of novel target-specific hybrid molecules incorporating multiple bioactive pharmacores to combat cancer. In the present study, a one-pot simple and efficient T3P(®) mediated procedure for the preparation of twelve new 3-(substituted- [1,2,4]triazolo[3,4-b] [1,3,4]thiadiazolo)-1H-indoles with short reaction times, easy workup procedure, good yields, and purity of products is described. Cytotoxicity assay (MTT), flow-cytometric univariate cell cycle analysis, Annexin V-FITC staining and DNA fragmentation for cell death mechanism suggested that compound 3d with chloro-substituted phenyl ring induced enhanced cytotoxicity by an apoptotic pathway with high differential toxicity to breast adenocarcinoma cells (MCF-7) when compared with normal human dermal fibroblast cells...
February 21, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28235426/antiproliferative-activity-and-apoptosis-induction-by-3-4-dibenzyloxyflavonol-on-human-leukemia-cells
#2
Mercedes Said, Ignacio Brouard, José Quintana, Francisco Estévez
In this study, we investigated the effects of synthetic 3',4'-dibenzyloxyflavonol on viabilities of eight human tumor cells. It was cytotoxic against leukemia cells (HL-60, U-937, MOLT-3, K-562, NALM-6, Raji), with significant effects against P-glycoprotein-overexpressing K-562/ADR and Bcl-2-overexpressing U-937/Bcl-2 cells, but had no significant cytotoxic effects against quiescent or proliferating human peripheral blood mononuclear cells. The IC50 value for the leukemia HL-60 cells was 0.8 ± 0.1 μM...
February 21, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28219640/identification-and-characterization-of-functional-antioxidant-response-elements-in-the-promoter-of-the-aldo-keto-reductase-akr1b10-gene
#3
Toru Nishinaka, Takeshi Miura, Kahori Shimizu, Tomoyuki Terada
AKR1B10 is a human-type aldo-keto reductase. The up-regulation of AKR1B10 has been associated with various cancers including non-small cell lung carcinoma, viral and bacterial infections, and skin diseases. However, the mechanisms underlying AKR1B10 gene regulation are not fully understood. We previously indicated the involvement of the transcription factor Nrf2 in AKR1B10 gene regulation. There are at least five potential Nrf2-responsive consensus sequences, so-called antioxidant response elements (AREs), and several ARE-like sequences in the 5'-flanking region up to -3282 bp of the AKR1B10 gene...
February 20, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28223025/transcriptional-regulation-of-human-paraoxonase-1-by-nuclear-receptors
#4
REVIEW
N Ponce-Ruiz, F E Murillo-González, A E Rojas-García, Mike Mackness, Y Y Bernal-Hernández, B S Barrón-Vivanco, C A González-Arias, I M Medina-Díaz
Paraoxonase 1 (PON1) is a calcium-dependent esterase synthesized primarily in the liver and secreted into the plasma, where it is associates with high density lipoproteins (HDL). PON1 acts as antioxidant preventing low-density lipoprotein (LDL) oxidation which is believed to be critical in the initiation and progression of atherosclerosis. Additionally, PON1 hydrolyzes and detoxifies some toxic metabolites of organophosphorus compounds (OPs). Thus, PON1 activity and expression levels are important for determining susceptibility to OPs intoxication and risk of diseases related to inflammation and oxidative stress...
February 18, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28219639/leishmania-l-amazonensis-induces-hyperalgesia-in-balb-c-mice-contribution-of-endogenous-spinal-cord-tnf%C3%AE-and-nf%C3%AE%C2%BAb-activation
#5
Sergio M Borghi, Victor Fattori, Kenji W Ruiz-Miyazawa, Milena M Miranda-Sapla, Rúbia Casagrande, Phileno Pinge-Filho, Wander R Pavanelli, Waldiceu A Verri
: Cutaneous leishmaniasis (CL) is the most common form of the leishmaniasis in humans. Ulcerative painless skin lesions are predominant clinical features of CL. Wider data indicate pain accompanies human leishmaniasis, out with areas of painless ulcerative lesions per se. In rodents, Leishmania (L.) major infection induces nociceptive behaviors that correlate with peripheral cytokine levels. However, the role of the spinal cord in pain processing after Leishmania infection has not been investigated...
February 17, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28216341/mechanisms-of-protection-against-irreversible-oxidation-of-the-catalytic-cysteine-of-aldh-enzymes-possible-role-of-vicinal-cysteines
#6
Rosario A Muñoz-Clares, Lilian González-Segura, Dario S Murillo-Melo, Héctor Riveros-Rosas
The catalytic mechanism of the NAD(P)(+)-dependent aldehyde dehydrogenases (ALDHs) involves the nucleophilic attack of the essential cysteine (Cys302, mature HsALDH2 numbering) on the aldehyde substrate. Although oxidation of Cys302 will inactivate these enzymes, it is not yet well understood how this oxidation is prevented. In this work we explore possible mechanisms of protection by systematically analyzing the reported three-dimensional structures and amino acid sequences of the enzymes of the ALDH superfamily...
February 17, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28212821/cloning-and-molecular-characterization-of-the-betaine-aldehyde-dehydrogenase-involved-in-the-biosynthesis-of-glycine-betaine-in-white-shrimp-litopenaeus-vannamei
#7
María F Delgado-Gaytán, Jesús A Rosas-Rodríguez, Gloria Yepiz-Plascencia, Ciria G Figueroa-Soto, Elisa M Valenzuela-Soto
The enzyme betaine aldehyde dehydrogenase (BADH) catalyzes the irreversible oxidation of betaine aldehyde to glycine betaine (GB), a very efficient osmolyte accumulated during osmotic stress. In this study, we determined the nucleotide sequence of the cDNA for the BADH from the white shrimp Litopenaeus vannamei (LvBADH). The cDNA was 1882 bp long, with a complete open reading frame of 1524 bp, encoding 507 amino acids with a predicted molecular mass of 54.15 kDa and a pI of 5.4. The predicted LvBADH amino acid sequence shares a high degree of identity with marine invertebrate BADHs...
February 15, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28209544/sestrin2-protects-against-acetaminophen-induced-liver-injury
#8
Seung Jung Kim, Kyu Min Kim, Ji Hye Yang, Sam Seok Cho, Sang Kyu Lee, Sae Kwang Ku, Il Je Cho, Sung Hwan Ki
Acetaminophen (APAP) overdose accounts for half of the cases of acute liver failure worldwide. We previously reported that that Sestrin2 (Sesn2) protects against d-galactosamine/lipopolysaccharide-induced acute fulminant liver failure. In this study, we demonstrated that Sesn2 protects APAP-induced liver injury in mice, using a recombinant adenovirus encoding Sesn2 (Ad-Sesn2). First, we found that treatment of mice with toxic levels of APAP significantly reduced Sesn2 expression. Tail-vein injection with Ad-Sesn2 inhibited APAP-induced serum alanine aminotransferase and aspartate aminotransferase levels and markedly reduced hepatocyte degeneration and inflammatory cell infiltration...
February 13, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28190539/corrigendum-to-evodiamine-a-plant-alkaloid-induces-calcium-jnk-mediated-autophagy-and-calcium-mitochondria-mediated-apoptosis-in-human-glioblastoma-cells-chem-biol-interact-205-1-2013-sep-5-20-28
#9
Ann-Jeng Liu, Sheng-Hao Wang, Ku-Chung Chen, Hsiu-Ping Kuei, Yung-Luen Shih, Sz-Ying Hou, Wen-Ta Chiu, Sheng-Huang Hsiao, Chwen-Ming Shih
No abstract text is available yet for this article.
February 9, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28189703/characterization-of-butyrylcholinesterase-in-bovine-serum
#10
Alicia J Dafferner, Sofya Lushchekina, Patrick Masson, Gaoping Xiao, Lawrence M Schopfer, Oksana Lockridge
Human butyrylcholinesterase (HuBChE) protects from nerve agent toxicity. Our goal was to determine whether bovine serum could be used as a source of BChE. Bovine BChE (BoBChE) was immunopurified from 100 mL fetal bovine serum (FBS) or 380 mL adult bovine serum by binding to immobilized monoclonal mAb2. Bound proteins were digested with trypsin and analyzed by liquid chromatography-tandem mass spectrometry. The results proved that FBS and adult bovine serum contain BoBChE. The concentration of BoBChE was estimated to be 0...
February 8, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28187856/corrigendum-to-pcb153-tcdd-and-estradiol-compromise-the-benzo-a-pyrene-induced-p53-response-via-foxo3a-chem-biol-interact-219-2014
#11
Lauy Al-Anati, Sandeep Kadekar, Johan Högberg, Ulla Stenius
No abstract text is available yet for this article.
February 7, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28187855/corrigendum-to-inhibition-of-rna-transportation-induces-glioma-cell-apoptosis-via-downregulation-of-rangap1-expression-chem-biol-interact-232-2015-may-5-49-57
#12
Tsung-Yao Lin, Chin-Cheng Lee, Ku-Chung Chen, Chien-Ju Lin, Chwen-Ming Shih
No abstract text is available yet for this article.
February 7, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28185768/antitumor-activity-of-paederosidic-acid-in-human-non-small-cell-lung-cancer-cells-via-inducing-mitochondria-mediated-apoptosis
#13
Ping Yu, Lifeng Shi, Meiyan Song, Yu Meng
This study was aimed to investigate antitumor activity of paederosidic acid (PA) in human non-small cell lung cancer cells and explore the related mechanisms. The anti-proliferative effects of PA on A549 cells were evaluated by MTT method and the IC50 values were calculated. Furthermore, the PA-induced apoptosis in A549 cells was determined by fluorescence microscope via staining with DAPI and by flow cytometer via staining with FITC conjugated Annexin V/PI. The expression of apoptosis-related or signaling proteins was investigated by Western blotting...
February 6, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28174098/effects-of-organophosphates-on-the-regulation-of-mesenchymal-stem-cell-proliferation-and-differentiation
#14
Amber M Prugh, Stephanie D Cole, Trevor Glaros, Daniel J Angelini
Mesenchymal stem cells (MSCs) are multipotent cells located within various adult tissues. Recent literature has reported that human bone marrow-derived MSCs express active acetylcholinesterase (AChE) and that disruption of AChE activity by organophosphate (OP) chemicals decreases the ability of MSCs to differentiate into osteoblasts. The potential role of AChE in regulating MSC proliferation and differentiation is currently unknown. In the present study, we demonstrate that MSCs exposed to OPs have both decreased AChE activity and abundance...
February 4, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28174097/synthetic-2-aryl-3-piperidin-1-yl-ethyl-thiazolidin-4-ones-exhibit-selective-in%C3%A2-vitro-antitumoral-activity-and-inhibit-cancer-cell-growth-in-a-preclinical-model-of-glioblastoma-multiforme
#15
Elita F da Silveira, Juliana H Azambuja, Taíse Rosa de Carvalho, Alice Kunzler, Daniel S da Silva, Fernanda C Teixeira, Rodrigo Rodrigues, Fátima T Beira, Rita de Cássia Sant Anna Alves, Roselia M Spanevello, Wilson Cunico, Francieli M Stefanello, Ana P Horn, Elizandra Braganhol
Glioblastoma multiforme (GBM) is the worst form of primary brain tumor, which has a high rate of infiltration and resistance to radiation and chemotherapy, resulting in poor prognosis for patients. Recent studies show that thiazolidinones have a wide range of pharmacological properties including antimicrobial, anti-inflammatory, anti-oxidant and anti-tumor. Here, we investigate the effect antiglioma in vitro of a panel of sixteen synthetic 2-aryl-3-((piperidin-1-yl)ethyl)thiazolidin-4-ones where 13 of these decreased the viability of glioma cells 30-65% (100 μM) compared with controls...
February 4, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28161411/structural-basis-for-the-inhibition-of-akr1b10-by-the-c3-brominated-ttnpb-derivative-uvi2008
#16
Francesc X Ruiz, Isidro Crespo, Susana Álvarez, Sergio Porté, Joan Giménez-Dejoz, Alexandra Cousido-Siah, André Mitschler, Ángel R de Lera, Xavier Parés, Alberto Podjarny, Jaume Farrés
UVI2008, a retinoic acid receptor (RAR) β/γ agonist originated from C3 bromine addition to the parent RAR pan-agonist 4-[(E)-2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)-1-propenyl]benzoic acid (TTNPB), is also a selective inhibitor of aldo-keto reductase family member 1B10 (AKR1B10). Thus, it might become a lead drug for the design of compounds targeting both activities, as an AKR1B10 inhibitor and RAR agonist, which could constitute a novel therapeutic approach against cancer and skin-related diseases...
February 1, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28161410/methylseleninic-acid-and-sodium-selenite-induce-severe-er-stress-and-subsequent-apoptosis-through-upr-activation-in-pel-cells
#17
Zenpei Shigemi, Kazuki Manabe, Naoko Hara, Yusuke Baba, Kohei Hosokawa, Hiroki Kagawa, Tadashi Watanabe, Masahiro Fujimuro
Selenium compounds such as methylseleninic acid (MSA) and sodium selenite (SS) have been widely evaluated as potential anti-cancer agents in the clinical setting. Primary effusion lymphoma (PEL) is a non-Hodgkin's B-cell lymphoma, associated with immunosuppressed individuals, such as post-transplant or AIDS patients. Kaposi's sarcoma-associated herpesvirus (KSHV) is the causative agent of PEL and Kaposi's sarcoma. Here, we found that MSA and SS markedly inhibited the growth of PEL cells compared with KSHV-uninfected B cells...
February 1, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28159580/editorial-for-the-special-issue-of-the-1st-international-conference-cbrn-research-and-innovation-antibes-juan-les-pins-france-march-16-19-2015
#18
EDITORIAL
Frederic Dorandeu, Daniel Gillet
No abstract text is available yet for this article.
January 31, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28159579/edible-vegetables-as-a-source-of-aldose-reductase-differential-inhibitors
#19
Francesco Balestri, Carlo Sorce, Roberta Moschini, Mario Cappiello, Livia Misuri, Antonella Del Corso, Umberto Mura
The hyperactivity of aldose reductase (AR) on glucose in diabetic conditions or on glutathionyl-hydroxynonenal in oxidative stress conditions, the source of cell damage and inflammation, appear to be balanced by the detoxifying action exerted by the enzyme. This detoxification acts on cytotoxic hydrophobic aldehydes deriving from membrane peroxidative processes. This may contribute to the failure in drug development for humans to favorably intervene in diabetic complications and inflammation, despite the specificity and high efficiency of several available aldose reductase inhibitors...
January 31, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28153595/phenolic-compounds-the-inhibition-effect-on-polyol-pathway-enzymes
#20
Hatice Esra Aslan, Şükrü Beydemir
The polyol pathway called as sorbitol way is a small part of glycose metabolism. The pathway is regarded as an important element in the pathogenesis of various diabetic complications in individuals with diabetes mellitus. The pathway plays a crucial role in hyperglycemia. The polyol pathway contains two enzymes as aldose reductase (AR) and sorbitol dehydrogenase (SDH). In the present study, AR and SDH were purified from sheep liver by using simple chromatographic methods. AR was purified with a yield of 2.11% and approximately 162 fold and SDH was purified with a yield of 0...
January 30, 2017: Chemico-biological Interactions
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