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Chemico-biological Interactions

Salvatore Nesci, Fabiana Trombetti, Maurizio Pirini, Vittoria Ventrella, Alessandra Pagliarani
In spite of the known widespread toxicity of mercury, its impact on mitochondrial bioenergetics is a still poorly explored topic. Even if many studies have dealt with mercury poisoning of mitochondrial respiration, as far as we are aware Hg(2+) effects on individual complexes are not so clear. In the present study changes in swine heart mitochondrial respiration and F1FO-ATPase (F-ATPase) activity promoted by micromolar Hg(2+) concentrations were investigated. Hg(2+) was found to inhibit the respiration of NADH-energized mitochondria, whereas it was ineffective when the substrate was succinate...
October 22, 2016: Chemico-biological Interactions
Ana Roseli S Ribeiro, José Diego do Nascimento Valença, Jeferson da Silva Santos, Thaise Boeing, Luisa Mota da Silva, Sérgio Faloni de Andrade, Ricardo L C Albuquerque-Júnior, Sara Maria Thomazzi
Many flavonoids have been shown to present good results for the treatment of gastric ulcers. Baicalein, a bioactive flavonoid derived from the Scutellaria baicalensis Georgi root, possesses several biological effects, such as anti-inflammatory and antioxidant. This study was conducted to assess the gastroprotective properties of baicalein. Anti-ulcerogenic assay was performed using the protocol of ulcer induced by ethanol/HCl in mice; then, the role of presynaptic α2-receptors, sulfhydryl (SH) compounds, nitric oxide (NO), prostaglandin (PG) and ATP-sensitive K(+) (KATP) channels in gastroprotection of baicalein was investigated...
October 22, 2016: Chemico-biological Interactions
Lenka Roubalová, David Biedermann, Barbora Papoušková, Jan Vacek, Marek Kuzma, Vladimír Křen, Jitka Ulrichová, Albena T Dinkova-Kostova, Jiří Vrba
The natural flavonoid quercetin is known to activate the transcription factor Nrf2, which regulates the expression of cytoprotective enzymes such as heme oxygenase-1 (HO-1) and NAD(P)H:quinone oxidoreductase 1 (NQO1). In this study, a novel semisynthetic flavonoid 7-O-galloylquercetin (or quercetin-7-gallate, 3) was prepared by direct galloylation of quercetin, and its effect on the Nrf2 pathway was examined. A luciferase reporter assay showed that 7-O-galloylquercetin, like quercetin, significantly activated transcription via the antioxidant response element in a stably transfected human AREc32 reporter cell line...
October 21, 2016: Chemico-biological Interactions
Chao-Ming Hung, Ying-Chao Lin, Liang-Chih Liu, Sheng-Chu Kuo, Chi-Tang Ho, Tzong-Der Way
CWF-145, a synthetic 2-phenyl-4-quinolone derivative exerted potent cytotoxicity against prostate cancer. CWF-145 inhibited prostate cancer cell lines PC-3, DU-145 and LNCap. It had a very low IC50 about 200 nM against castrate-resistant prostate cancer (CRPC) PC-3. We found that CWF-145 had a similar effect to clinical trial antimitotic agents in cancer cells and normal cells. CWF-145 arrested cell cycle at G2/M phase by binding to the β-tubulin at the colchicine-binding site then disrupted microtubule polymerization...
October 18, 2016: Chemico-biological Interactions
Ra-Yeong Choi, Ju Ri Ham, Mi-Kyung Lee
This study investigated the effects and mechanism of esculetin (6,7-dihydroxycoumarin) on non-alcoholic fatty liver in diabetic mice fed high-fat diet (HFD). The diabetic mice model was induced by injection of streptozotocin, after which they were fed HFD diet with or without esculetin for 11 weeks. Non-diabetic mice were provided a normal diet. Diabetes induced hepatic hypertrophy, lipid accumulation and droplets; however, esculetin reversed these changes. Esculetin treatment in diabetic mice fed HFD significantly down-regulated expression of lipid synthesis genes (Fasn, Dgat2 and Pap) and inflammation genes (Tlr4, Myd88, Nfkb, Tnfα and Il6)...
October 18, 2016: Chemico-biological Interactions
Francislaine A Dos Reis Lívero, Gracianny Gomes Martins, José Ederaldo Queiroz Telles, Olair Carlos Beltrame, Stellee Marcela Petris Biscaia, Célia Regina Cavichiolo Franco, Ronald P J Oude Elferink, Alexandra Acco
Ethanol abuse is a serious public health problem that is associated with several stages of alcoholic liver disease (ALD) and a high incidence of morbidity and mortality. Alcoholic fatty liver disease (AFLD), the earliest stage of ALD, is a multifactorial injury that involves oxidative stress and disruptions of lipid metabolism. Although benign and reversible, no pharmacological treatments are available for this condition. In the present study, we induced AFLD in mice with 10% ethanol and a low-protein diet and then orally treated them with a hydroethanolic extract of Baccharis trimera (HEBT; 30 mg kg(-1))...
October 15, 2016: Chemico-biological Interactions
Ali Roohbakhsh, Kobra Shirani, Gholamreza Karimi
Methamphetamine (METH) is a highly potent and addictive drug with major medical, psychiatric, cognitive, socioeconomic, and legal consequences. It is well absorbed following different routes of administration and distributed throughout the body. METH is known as psychomotor stimulant with potent physiological outcomes on peripheral and central nervous systems, resulting in physical and psychological disorders. Autophagy is a highly conserved and regulated catabolic pathway which is critical for maintaining cellular energy homeostasis and regulating cell growth...
October 13, 2016: Chemico-biological Interactions
Seon Min Woo, Taeg Kyu Kwon
Jaceosidin is a flavonoid isolated from Artemisia vestita that has been reported to possess anti-tumor and anti-proliferative activities in many cancer cells. In this study, we investigated the anti-tumor activity of jaceosodin in renal carcinoma cells. Jaceosidin induced apoptosis in multiple human renal carcinoma cells (Caki, ACHN, A498, and 786-O), lung cancer cells (A549) and glioma cells (U251MG). In contrast, jaceosidin does not induce apoptosis in normal human umbilical vein cells (EA.hy926). Apoptotic cell death was associated with the activation of caspase-3 and cleavage of poly (ADP-ribose) polymerase...
October 8, 2016: Chemico-biological Interactions
Suchismita Daw, Ritam Chatterjee, Aditya Law, Sujata Law
Hematological disorders like myelodysplastic syndrome (MDS) may arise due to cumulative dysregulation of various signalling pathways controlling proliferation, differentiation, maturation and apoptosis of bone marrow cells. This devastating bone marrow condition can be due to consequential abnormalities in haematopoiesis as well as its supportive microenvironment. Although mutations related to JAK/STAT pathway are common in myeloproliferative neoplasms, further studies are required to fully explore the myelodysplastic scenario regarding the concerned pathway...
October 7, 2016: Chemico-biological Interactions
Bhumika Wadhwa, Rashmi Dumbre
Prostate (CaP) cancer is the second-leading cause of cancer-related mortality in men in Western societies. Androgen receptor (AR) signaling is a critical survival pathway for prostate cancer cells, and androgen-deprivation therapy (ADT) remains the principal treatment for patients with locally advanced and metastatic disease. Although a majority of patients initially respond to ADT, most will eventually develop castrate resistance. The recent discovery that AR signaling persists during systemic castration via intratumoral production of androgens led to the development of novel anti-androgen therapies...
October 6, 2016: Chemico-biological Interactions
Chun Pang, Liang Shi, Yuchen Sheng, Zhiyong Zheng, Hai Wei, Zhengtao Wang, Lili Ji
Caffeic acid (CA) is a natural compound abundant in fruits, coffee and plants. This study aims to investigate the involved mechanism of the therapeutic detoxification of CA against acetaminophen (APAP)-induced hepatotoxicity. CA (10, 30 mg/kg) was orally given to mice at 1 h after mice were pre-administrated with APAP (300 mg/kg). The therapeutic detoxification of CA against APAP-induced hepatotoxicity was observed by detecting serum aminotransferases, liver malondialdehyde (MDA) amount and liver histological evaluation in vivo...
October 6, 2016: Chemico-biological Interactions
Buse Cevatemre, Bruno Botta, Mattia Mori, Simone Berardozzi, Cinzia Ingallina, Engin Ulukaya
Despite the rapid advances in chemotherapy regimens, the outcome of patients with breast cancer is not satisfactory. One of the reasons of this dissatisfaction is that subsets of cells in tumors which referred as cancer stem cells (CSCs) show and/or gain resistance to therapies. Thus, compounds that target CSCs are urgently needed. Since some are already used in the clinic, natural products have great potential for further development as anti cancer drugs. The aim of this study is to investigate the cytotoxic activity of tingenin b (or 22β-hydroxytingenone) which is a quinone-methide triterpenoid structurally related to tingenone, against breast CSCs (stem-cell enriched population from MCF-7 cell line, MCF-7s)...
October 5, 2016: Chemico-biological Interactions
Hye-Eun Choi, Ji-Sun Shin, Dong-Gyu Leem, Soo-Dong Kim, Won-Jea Cho, Kyung-Tae Lee
Previously, we reported that 6-(3,4-dihydro-1H-isoquinolin-2-yl)-N-(6-methylpyridin-2-yl) nicotinamide (DIMN) analogues inhibited the growth of prostate cancer cells as an anti-androgenic compound. In the present study, we evaluated cytotoxic effects of these DIMN derivatives and found that DIMN-26 most potently inhibited the proliferation of the LNCap-LN3 androgen-dependent and DU145 androgen-independent prostate cancer cells through induction of G2/M phase cell cycle arrest and subsequent apoptosis. The G2/M phase arrest was found due to increases in the activation of cdc2 (also known as cyclin-dependent kinase 1, CDK1)/cyclin B1 complex...
October 5, 2016: Chemico-biological Interactions
Priyanka Pahwa, Rajesh Kumar Goel
Asparagus adscendens Roxb. commonly known as safed musli and belonging to the Liliaceae family is cultivated mainly in Asian countries. In traditional medicine, safed musli is recommended as nerve tonic and remedy for memory impairment. The present study was aimed to evaluate nootropic and antiamnesic activities of Asparagus adscendens extract (AAE) using in silico and in vivo approach. Phytoconstituents of A. adscendens root reported in literature were subjected to in silico prediction using PASS and Pharmaexpert...
October 4, 2016: Chemico-biological Interactions
Xiang-Bin Song, Gang Liu, Zhen-Yong Wang, Lin Wang
Puerarin (PU) is a potent free radical scavenger with a protective effect in nephrotoxin-mediated oxidative damage. Here, we show a novel molecular mechanism by which PU exerts its anti-apoptotic effects in cadmium (Cd)-exposed primary rat proximal tubular (rPT) cells. Morphological assessment and flow cytometric analysis revealed that PU significantly decreased Cd-induced apoptotic cell death of rPT cells. Administration of PU protected cells against Cd-induced depletion of mitochondrial membrane potential (ΔΨm) and lipid peroxidation...
October 4, 2016: Chemico-biological Interactions
Majid Mahdavi, Malihe Mohseni Lavi, Reza Yekta, Mohammad Amin Moosavi, Mahnaz Nobarani, Saeed Balalei, Sanam Arami, Mohammad Reza Rashidi
Previous studies have suggested that quinazolinone derivatives are potent apoptosis-inducing agents in various cancer cell lines. In the present study, we have investigated cytotoxic, apoptosis induction, and molecular docking activities of the spiroquinazolinone benzamide derivatives family on MCF-7 human breast cancer cells. The MTT cytotoxicity assays and docking studies showed that 4t-CHQB was the most active compound among the prepared spiroquinazolinone benzamide compounds with IC50 of 50 ± 1.2 μM and was selected for further assessments...
October 3, 2016: Chemico-biological Interactions
Neetu Gupta, Romain Noël, Amélie Goudet, Karen Hinsinger, Aurélien Michau, Valérie Pons, Hajer Abdelkafi, Thomas Secher, Ayaka Shima, Olena Shtanko, Yasuteru Sakurai, Sandrine Cojean, Sébastien Pomel, Vanessa Liévin-Le Moal, Véronique Leignel, Jo-Ana Herweg, Annette Fischer, Ludger Johannes, Kate Harrison, Philippa M Beard, Pascal Clayette, Roger Le Grand, Jonathan O Rayner, Thomas Rudel, Joël Vacus, Philippe M Loiseau, Robert A Davey, Eric Oswald, Jean-Christophe Cintrat, Julien Barbier, Daniel Gillet
Medical countermeasures to treat biothreat agent infections require broad-spectrum therapeutics that do not induce agent resistance. A cell-based high-throughput screen (HTS) against ricin toxin combined with hit optimization allowed selection of a family of compounds that meet these requirements. The hit compound Retro-2 and its derivatives have been demonstrated to be safe in vivo in mice even at high doses. Moreover, Retro-2 is an inhibitor of retrograde transport that affects syntaxin-5-dependent toxins and pathogens...
October 3, 2016: Chemico-biological Interactions
Aurélie Jacquart, Roberta Brayner, Jean-Michel El Hage Chahine, Nguyet-Thanh Ha-Duong
Phytochelatins or PCn, (γGlu-Cys)n-Gly, and their glutathione (GSH) precursor are thiol-rich peptides that play an important role in heavy metal detoxification in plants and microorganisms. Complex formation between Cd(2+) and Pb(2+) and GSH or PCn (n = 2, 4 and 6) are investigated by microcalorimetry, absorption spectrophotometry and T-jump kinetics. Complex formation with Pb(2+) or Cd(2+) is exothermic, and induces ligand metal charge transfer bands in UV absorption spectral range, which implies the formation of a coordination bond between the metal and the thiol groups of the phytochelatins...
September 6, 2016: Chemico-biological Interactions
Shweta Sharma, Monika Yadav, Surendra P Gupta, Kumud Pandav, Surat Kumar
Harmine, a tricyclic β-carboline alkaloid possesses anticancer properties. Thus, its binding studies with DNA are considerably important because mechanism of action of anticancer drug involves DNA binding. On the other hand, the DNA binding study is also useful in drug designing and synthesis of new compounds with enhanced biological properties. Hence, the binding of harmine with sequence specific DNA oligonucleotides has been studied using various biophysical techniques i.e. absorption, fluorescence and molecular docking techniques...
August 30, 2016: Chemico-biological Interactions
Xingyu Liu, Jie Zhang, Limeng Wang, Bicheng Yang, Chen Zhang, Wei Liu, Jun Zhou
N'-Nitrosonornicotine (NNN) is considered to be one of the most carcinogenic compounds of the four conventionally measured tobacco-specific N-nitrosamines (TSNAs). In order to evaluate the significance of metabolic activation for the carcinogenic potential of NNN, its catalysis by different phase I enzymes and its interaction with nicotine and nicotine-derived TSNAs need to be investigated. Using an in vitro model system, NNN was found to interact with various cytochrome P450 enzymes, predominantly CYP2A13...
August 24, 2016: Chemico-biological Interactions
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