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Susan R Mallery, Daren Wang, Brian Santiago, Ping Pei, Steven Schwendeman, Kari Nieto, Richard Spinney, Meng Tong, George Koutras, Byungdo B Han, Andrew S Holpuch, James C Lang
Over 1/3 of patients who have undergone oral squamous cell carcinoma (OSCC) surgical resections develop life-threatening and often untreatable recurrences. A variety of drugs, intended for management of recurrent or disseminated cancers, were designed to exploit cancer cells' reliance upon overexpressed receptors and gratuitous signaling. Despite their conceptual promise, clinical trials showed these agents lacked efficacy and were often toxic. These findings are consistent with evasion of pathway-targeted treatments via extensive signaling redundancies and compensatory mechanisms common to cancers...
October 18, 2016: Cancer Prevention Research
Prakasha Gowda, Thomas E Spratt
4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK) is a potent tobacco carcinogen that forms mutagenic DNA adducts including O(6)-methyl-2'-deoxyguanosine (O(6)-Me-dG), O(6)-[4-(3-pyridyl)-4-oxobut-1-yl]-dG (O6-POB-dG), O(2)-methylthymidine (O(2)-Me-dT), and O(2)-POB-dT. We evaluated the ability of human DNA polymerase ν to bypass this damage to evaluate the structural constraints on substrates for pol ν and to evaluate if there is kinetic evidence suggesting the in vivo activity of pol ν on tobacco-induced DNA damage...
October 14, 2016: Chemical Research in Toxicology
Sabzar Ahmad Dar, Abdul Rehman Yousuf, Masood-Ul-Hassan Balkhi, Bashir Ahmad Ganai, Mudasir Tantry, Farooz Ahmad Bhat
CONTEXT: Medicinal plants continue to act as a repository for novel drug leads with novel mechanisms of action. Podophyllum hexandrum Royale (Berberideceae) treats diverse conditions in folk medicine. OBJECTIVE: The antimutagenic potential of P. hexandrum was evaluated against endosulfan-induced clastogenicity in a piscine model by cytogenetic endpoints. MATERIALS AND METHODS: Podophyllum hexandrum rhizomes were subjected to successive solvent extraction...
October 8, 2016: Pharmaceutical Biology
Yu Zhang, Jeffrey L Petersen, Carsten Milsmann
Titanium and zirconium complexes carrying two 2,6-bis(pyrrolyl)pyridine ligands have been synthesized and characterized. The neutral complexes Ti((Me)PDP)2 and Zr((Me)PDP)2 ((Me)PDP = 2,6-bis(5-methyl-3-phenyl-1H-pyrrol-2-yl)pyridine) show intense ligand-to-metal charge-transfer bands in the visible region and undergo multiple reversible redox events under highly reducing conditions. Zr((Me)PDP)2 exhibits photoluminescent behavior and its excited state can be quenched by mild reductants to generate a powerful electron transfer reagent with a ground state potential of -2...
October 12, 2016: Journal of the American Chemical Society
Martha Moheb Morcoss, Nada Sayed Abdelwahab, Nouruddin Wagieh Ali, Mohammed Taha Elsaady
Two selective spectrophotometric and TLC-densitometric methods were developed for determination of mesalazine (ME) and its two toxic impurities, 4-amino phenol (4AP) and salicylic acid (SA) without preliminary separation. The proposed methods are: ratio difference in the subtracted spectra (RDSS) {Method 1}, area under the curve (AUC) {Method 2} and TLC-densitometric {Method 3}. In method {1} combination of measuring the amplitude of the constant at 350 nm (using standard spectrum of 10 µg/mL ME as a divisor) and ratio difference in the subtracted ratio spectrum for determination of 4AP and SA using the ratio difference at 221...
2016: Chemical & Pharmaceutical Bulletin
Yinsui Zheng, James T Dillon, Yifan Zhang, Yongsong Huang
Alkenones (C37 to C40 ) are highly specific biomarkers produced by certain haptophyte algae in ocean and lacustrine environments and have been widely used for paleoclimate studies. Unusual shorter-chain alkenones (e.g., C35 and C36 ) have been found in environmental and culture samples but the origin and structures of these compounds are much less understood. The marine alkenone producer, Emiliania huxleyi CCMP2758 strain was reported with abundant C35:2 Me (∆(12, 19) ) alkenone when cultured at 15°C (Prahl et al...
August 30, 2016: Journal of Phycology
Vineet Kumar Jakhar, Milan Kr Barman, Sharanappa Nembenna
The well-defined aluminum monohydride compound [{(2,4,6-Me3-C6H2)NC(Me)}2(Me)(H)]AlH·(NMe2Et) (1) catalyzes hydroboration of a wide range of aldehydes and ketones under mild reaction conditions. Moreover, compound 1 displayed chemoselective hydroboration of aldehydes over ketones at rt.
September 16, 2016: Organic Letters
Fabio Juliá, María-Dulce García-Legaz, Delia Bautista, Pablo González-Herrero
The synthesis, characterization, and photophysical properties of a wide variety of bis-cyclometalated Pt(IV) complexes featuring a C2-symmetrical or unsymmetrical {Pt(ppy)2} unit (sym or unsym complexes, respectively; ppy = C-deprotonated 2-phenylpyridine) and different ancillary ligands are reported. Complexes sym-[Pt(ppy)2X2] (X = OTf(-), OAc(-)) were obtained by chloride abstraction from sym-[Pt(ppy)2Cl2] using the corresponding AgX salts, and the triflate derivative was employed to obtain homologous complexes with X = F(-), Br(-), I(-), trifluoroacetate (TFA(-))...
August 1, 2016: Inorganic Chemistry
Haobing Wang, Yang Yang, Haiyan Ma
A series of tridentate chiral aminophenol proligands and corresponding zinc complexes, LZnX (L = (S)-2-{[(1-R(4)-2-pyrrolidinyl)CH2N(R(3))-]CH2}-6-R(1)-4-R(2)-C6H2O, X = N(SiMe3)2, R(3) = (n)Bu, R(4) = Bn: R(1) = R(2) = Cl (1), R(1) = R(2) = Me (2), R(1) = R(2) = (t)Bu (3); X = N(SiMe3)2, R(1) = trityl, R(2) = Me: R(3) = n-octyl, R(4) = Bn (4), R(3) = Bn, R(4) = Bn (5), R(3) = (n)Bu, R(4) = naphthalen-1-ylmethyl (6), R(3) = (n)Bu, R(4) = (i)Pr (7); R(1) = R(2) = cumyl, R(3) = Et, R(4) = Bn: X = N(SiMe3)2 (8), X = O(t)Bu (9), X = Et (10), X = Cl (11)), have been synthesized...
August 1, 2016: Inorganic Chemistry
Mathéo Berthet, Jean Martinez, Isabelle Parrot
In the field of peptide synthesis, the key to a successful access to synthetic targets lies on a pertinent combination of protecting groups. Their choice is directed by their selective removal conditions. We present here the behaviour of some of the most used protecting groups in peptide chemistry under experimental cleavage conditions, combining MgI2 with MW irradiation, using 2-Me-THF as a green solvent. In these experimental conditions, the benzyloxycarbonyl protecting group as well as the Merrifield resin can be re-considered in peptide chemistry...
July 8, 2016: Biopolymers
Shih-Hung Tsai, Po-Hsun Huang, Yu-Juei Hsu, Yi-Jen Peng, Chien-Hsing Lee, Jen-Chun Wang, Jaw-Wen Chen, Shing-Jong Lin
Hypoxia inducible factor-1α (HIF-1α) pathway is associated with many vascular diseases, including atherosclerosis, arterial aneurysms, pulmonary hypertension and chronic venous diseases. Significant HIF-1α expression could be found at the rupture edge at human abdominal aortic aneurysm (AAA) tissues. While our initial in vitro experiments had shown that deferoxamine (DFO) could attenuate angiotensin II (AngII) induced endothelial activations; we unexpectedly found that DFO augmented the severity of AngII-induced AAA, at least partly through increased accumulation of HIF-1α...
2016: Scientific Reports
Mario Bakardjiev, Bohumil Štíbr, Josef Holub, Oleg L Tok, Petr Švec, Zdeňka Růžičková, Aleš Růžička
Sequential methylation of arachno-6,9-C2B8H14 (1) led to a series of methyl derivatives and finally to the camouflaging of all boron positions by mixed persubstitution. Thus, deprotonation of 1 produced the [arachno-6,9-C2B8H13] anion (1(-)), the methylation of which with MeI in tetrahydrofuran proceeded on the open-face boron vertexes with the formation of 5-Me-arachno-6,9-C2B8H13 (2; yield 28%) and 5,8-Me2-arachno-6,9-C2B8H12 (3; yield 36%). Observed in this reaction was also a side formation of 2-Me-closo-1,6-C2B8H9 (4; yield 6%)...
July 18, 2016: Inorganic Chemistry
Smita S Mangalgi, Annapurna G Sajjan, Shivajirao T Mohite, Shivali Gajul
INTRODUCTION: In India, high incidence of human brucellosis may be expected, as the conditions conducive for human brucellosis exist. Limited studies have been undertaken on human brucellosis especially in occupationally-exposed groups. AIM: To estimate prevalence of anti-brucellar antibodies, evaluate the clinical manifestations, risk factors and Knowledge, Attitude and Practices (KAP) levels about brucellosis among occupationally exposed groups. MATERIALS AND METHODS: Blood samples were collected from 2337 occupationally exposed individuals...
April 2016: Journal of Clinical and Diagnostic Research: JCDR
Vera A Machado, Daniela Peixoto, Maria João Queiroz, Raquel Soares
Breast cancer is the most frequently diagnosed cancer and the second leading cause of cancer related deaths among women worldwide. The purpose of this study is to evaluate the cytotoxic effects and possible molecular mechanisms of the antiproliferative properties of the antiangiogenic 1-aryl-3-[3-(thieno[3,2-b]pyridin-7-ylthio)phenyl]ureas 1a-e, prepared earlier by us, on two human breast cancer cell lines of distinct histological types: hormone-dependent MCF-7 (ER positive), and hormone independent MDA-MB-231 (ER/PR/HER2 negative), this latter being the most aggressive and difficult to treat...
May 5, 2016: Journal of Cellular Biochemistry
Mojtaba Kamali Aghdam, Kambiz Davari, Kambiz Eftekhari
Severe thrombocytopenia with bleeding is rarely reported in children with brucellosis, and recurrent epistaxis is extremely rare. Brucellosis with hemorrhage should be differentiated from viral hemorrhagic fever, malignancy, and other blood disorders. Bone marrow aspiration (BMA) is mandatory to differentiate from other blood diseases. An 8-year-old boy was admitted with recurrent epistaxis, petechiae and purpura on face and extremities and bleeding from the gums. During the hospitalization, he was febrile and complained of muscle pain...
March 2016: Acta Medica Iranica
Jianwai Ren, George G Chen, Yi Liu, Xianwei Su, Baoguang Hu, Billy C S Leung, Y Wang, Rocky L K Ho, Shengli Yang, Gang Lu, C G Lee, Paul B S Lai
Hepatocellular carcinoma (HCC) occurs more frequently in men than in women. It is commonly agreed that estrogen plays important roles in suppressing HCC development, however, the underlying mechanism remains largely unknown. Since estrogen is mainly metabolized in liver and its metabolites affect cell proliferation, we sought to investigate if the liver-specific cytochrome P450 1A2 (CYP1A2) mediated the inhibitory effect of estrogen on HCC. In this study, the expression of estrogen-metabolizing enzyme CYP1A2 was determined in HCC tissues and cell lines...
2016: PloS One
Edward Oliveira, Juliana Wilke Saliba, Diana Oliveira, Edelberto Santos Dias, Gustavo Fontes Paz
This report describes the stege I/II development of a new direct agglutination test (DAT) for the diagnosis of canine visceral leishmaniasis (CVL) using freeze-dried antigen produced Coomassie blue-stained Leishmania (Leishmania) infantum promastigotes. In stage I, 16 canine serum samples, collected from eight dogs carrying CVL and eight healthy dogs, were assessed with the DAT using 2-mercaptoethanol (2-ME), N-acetyl-cysteine (NAC), kaolin or NAC plus urea (NAC+U) to improve the assay conditions. Stage II assessed the diagnostic accuracy with 100 serum samples collected from dogs with symptomatic CVL and clinically healthy dogs, comparing the four different sample diluents...
May 15, 2016: Veterinary Parasitology
Shashank Purwar, Sharada C Metgud, Manohar B Mutnal, Mahantesh B Nagamoti, Chidanand S Patil
BACKGROUND: The culture has always been the gold standard test for diagnosis of human brucellosis but the conventional Brucella diagnostic tests viz. serology and culture are often beset with poor specificity & sensitivity respectively. The culture positivity rates for Brucella vary from 92% for bone marrow to 10% for non-blood samples and also dependent on the type of sample. The primary immune-determinant for Brucella species is the cell wall surface lipopolysaccharide, which is antigenically similar to other gram-negative rods...
February 2016: Journal of Clinical and Diagnostic Research: JCDR
Felix Mader, Ludwig Krause, Tursonjan Tokay, Oliver W Hakenberg, Rüdiger Köhling, Timo Kirschstein
AIM: Purinergic signaling plays a major role in the enteric nervous system, where it governs gut motility through a number of P2X and P2Y receptors. The aim of this study was to investigate the P2Y receptor-mediated motility in rat longitudinal ileum preparations. METHODS: Ileum smooth muscle strips were prepared from rats, and fixed in an organ bath. Isometric contraction and relaxation responses of the muscle strips were measured with force transducers. Drugs were applied by adding of stock solutions to the organ bath to yield the individual final concentrations...
May 2016: Acta Pharmacologica Sinica
H F Dos Santos, M A Vieira, G Y Sánchez Delgado, D Paschoal
The chemotherapy with gold complexes has been attempted since the 90s after the clinical success of auranofin, a gold(I) coordination complex. Currently, the organometallics compounds have shown promise in cancer therapy, mainly in those complexes containing N-heterocylic carbenes (NHC) as a ligand. The present study shows a kinetic analysis of the reaction of six alkyl-substituted NHC with cysteine (Cys), which is taken as an important bionucleophile representative. The first and second ligand exchange processes were analyzed with the complete description of the mechanism and energy profiles...
April 14, 2016: Journal of Physical Chemistry. A
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