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Hong-Jin Tang, Wei Li, Mei Zhou, Li-Ying Peng, Jin-Xin Wang, Jia-Huang Li, Jun Chen
Xanthine oxidase, which catalyzes the oxidative reaction of hypoxanthine and xanthine into uric acid, is a key enzyme to the pathogenesis of hyperuricemia and gout. In this study, for the purpose of discovering novel xanthine oxidase (XO) inhibitors, a series of 2-arylbenzo[b]furan derivatives (3a-3d, 4a-4o and 6a-6d) were designed and synthesized. All these compounds were evaluated their xanthine oxidase inhibitory and antioxidant activities by using in vitro enzymatic assay and cellular model. The results showed that a majority of the designed compounds exhibited potent xanthine oxidase inhibitory effects and antioxidant activities, and compound 4a emerged as the most potent xanthine oxidase inhibitor (IC50  = 4...
February 2, 2018: European Journal of Medicinal Chemistry
Chao Tian, Zifei Han, Yuanxin Li, Meng Wang, Jiajia Yang, Xiaowei Wang, Zhili Zhang, Junyi Liu
Checkpoint kinase 1 (CHK1) inhibitors can potentiate the effectiveness of deoxyribonucleic acid (DNA) damaging agents in the treatment of cancer. A novel series of 2,6-disubstituted-9H-purine (3a-p, 5a and 5b), 2,4-disubstituted-thieno[3,2-d]pyrimidine (8a-c) and 2,4-disbustituted-7H-pyrrolo[2,3-d]pyrimidine (11a-c) analogues were designed and synthesized as potent CHK1 inhibitors. Compounds (3a, 3d, 3f and 3j-l) with 9H-purine core displayed more potent inhibition against CHK1. The most potent compound (3l) also exhibited low anti-proliferative effects towards HT29 and Hek293 cell lines...
March 28, 2018: European Journal of Medicinal Chemistry
Mukul Joshi, Ravi Singh Baghel, Edna Fogelman, Raphael A Stern, Idit Ginzberg
Calyx-end cracking in 'Pink Lady' apple is treated by a solution of gibberellic acids 4 and 7 (GA4+7 ) and the cytokinin 6-benzyladenine (BA). Although the GA4+7 and BA mixture is applied early in apple fruit development, it mitigates cracking that becomes evident in the mature fruit, implying a long-term treatment effect. The reduced incidence of peel cracking is associated with increased epidermal cell density, which is maintained until fruit maturation. Presently, the expression of genes that have been previously reported to be associated with epidermal cell patterning and cuticle formation, or cracking resistance, was monitored in the peel during fruit development and following GA4+7 and BA treatment...
April 14, 2018: Plant Physiology and Biochemistry: PPB
Amilton Cesar Dos Santos, Alan James Conley, Moacir Franco de Oliveira, Antônio Chaves de Assis Neto
This study documented, for the first time, the morphological patterns of differentiation of male and female genital organs of Spix cavy (Galea spixii) using histological and ultrastructural analyses, with immuno-localization of steroidogenic enzymes, cytochromes P450 aromatase (P450arom) and 17α-hydroxylase/17, 20-lyase (P450c17), involved in the synthesis of estrogens and androgens respectively throughout fetal sexual development. Undifferentiated gonads of Spix cavy develop into ovaries in females after 25 days of gestation (DG), exhibiting P450arom immunoreactivity...
April 13, 2018: Differentiation; Research in Biological Diversity
Beijing Xue, Wenhao Wang, Litong Guo, Xuanru Ren, Xueyu Tao, Yinghuai Qiang
The titanium opaque porcelain was synthesized through sol-gel using borate-silicate system. The porcelain was characterized by DSC-TG, X-ray diffraction, N2 adsorption-desorption isotherms and scanning electron microscope tests. The results of DSC showed that the nitrates could be decomposed completely when the bioglass xerogel precursor was heat-treated at 760 ℃. The XRD results showed that the Na2 Ca3 Si6 O16 was the major phase of the opaque porcelain. The synthesized opaque porcelain powders had an average particle size of about 5-25 µm with nanopores of around 50-70 nm on the surface...
April 4, 2018: Journal of the Mechanical Behavior of Biomedical Materials
Zhiwei Lu, Wanlin Dai, Baichen Liu, Guangquan Mo, Junjun Zhang, Jiaping Ye, Jianshan Ye
In this work, we report a facile and green strategy for one pot and in-situ synthesis of a dandelion-like conductive polyaniline coated gold nanoparticle nanocomposites (Au@PANI). The Au@PANI was characterized by SEM, TEM, XRD, TGA, FTIR, UV-vis and conductivity measurement, respectively. Newly-designed Au@PANI materials possessed a significantly high conductivity and strong adsorption capability. Thus, the Au@PANI modified glassy carbon electrode (GCE) was utilized for construct a novel electrochemical sensor for the simultaneous assay of Pb2+ and Cu2+ using square wave anodic stripping voltammetry (SWASV)...
April 18, 2018: Journal of Colloid and Interface Science
Yuxi Zhang, Qunqun Ruan, Yaguang Peng, Guopeng Han, Hongliang Huang, Chongli Zhong
Large organic pollutants in wastewater are harmful to human health and environmental ecosystem, and it is of great importance to remove them from waste water. In this report, hierarchical-pore metal-organic frameworks with different mesopore sizes (H-UiO-66-3.8 nm and H-UiO-66-17.3 nm) have been successfully synthesized at reflux condition. The resulting MOFs are characterized by N2 adsorption-desorption analysis and the results show that the samples have hierarchical-pore structures, which indicate the heat reflux method is efficient for the synthesis of H-UiO-66s on liter scale...
April 17, 2018: Journal of Colloid and Interface Science
Alaknanda J Adur, N Nandini, K Shilpashree Mayachar, R Ramya, N Srinatha
Silver nanoparticles were prepared through eco-friendly, cost effective, bio-mediated technique using anaerobically digested Parthenium hysterophorous digested slurry (PDS) for the first time. The synthesized nanoparticles were characterized through different techniques such as UV-Vis spectrophotometer for optical properties; X-ray diffractometer (XRD), high resolution transmission electron spectroscopy (HR-TEM) and Fourier Transform Infra Red (FTIR) Spectroscopy for structural property investigations. It was observed that the prepared silver nanoparticles were crystallized in face centered cubic crystal structure with an average particle size of 19 nm as confirmed from XRD...
April 16, 2018: Journal of Photochemistry and Photobiology. B, Biology
Waleed H Malki, Ahmed M Gouda, Hamdy E A Ali, Rabaa Al-Rousan, Doaa Samaha, Ashraf N Abdalla, Juan Bustamante, Zakaria Y Abd Elmageed, Hamed I Ali
Protein kinases are promising therapeutic targets for cancer therapy. Here, we applied multiple approaches to optimize the potency and selectivity of our reported alloxazine scaffold. Flexible moieties at position 2 of the hetero-tricyclic system were incorporated to fit into the ATP binding site and extend to the adjacent allosteric site and selectively inhibit protein kinases. This design led to potential selective inhibition of ABL1, CDK1/Cyclin A1, FAK, and SRC kinase by 30-59%. Cytotoxicity was improved by ∼50 times for the optimized lead (10b; IC50  = 40 nM) against breast cancer (MCF-7) cells...
April 17, 2018: European Journal of Medicinal Chemistry
Ratna Kancana Wolfram, Lucie Heller, René Csuk
Triterpenoic acids, ursolic acid (1), oleanolic acid (2), glycyrrhetinic acid (3) and betulinic acid (4) were converted into their corresponding methyl 5-8 and benzyl esters 9-12 or benzyl amides 21-24. These derivatives served as starting materials for the synthesis of pink colored rhodamine B derivatives 25-36 which were screened for cytotoxicity in colorimetric SRB assays. All of the compounds were cytotoxic for a variety of human tumor cell lines. The activity of the benzyl ester derivatives 29-32 was lower than the cytotoxicity of the methyl esters 25-28...
April 17, 2018: European Journal of Medicinal Chemistry
Evgeny V Buravlev, Oksana G Shevchenko, Aleksei A Anisimov, Kyrill Yu Suponitsky
A series of new C-4- and C-4/C-5-aminomethyl derivatives were synthesized on the basis of α- and γ-mangostins. A comparative evaluation of their chelating ability, radical scavenging activity and hemolytic activity, as well as antioxidant and membrane-protective properties, was carried out on the model of H2 O2 -induced hemolysis of mammalian red blood cells. It was shown that γ-mangostin and its C-4/C-5-derivatives were superior to α-mangostin and its derivatives in all the investigated parameters characterizing the antioxidant activity in the test systems used...
April 13, 2018: European Journal of Medicinal Chemistry
Hany S Ibrahim, Heba Abdelrasheed Allam, Walaa R Mahmoud, Alessandro Bonardi, Alessio Nocentini, Paola Gratteri, Eslam S Ibrahim, Hatem A Abdel-Aziz, Claudiu T Supuran
The synthesis and characterization of two new sets of arylsulfonehydrazone benzenesulfonamides (4a-4i with phenyl tail and 4j-4q with tolyl tail) are reported. The compounds were designed according to a dual-tails approach to modulate the interactions of the ligands portions at the outer rim of both hydrophobic and hydrophilic active site halves of human isoforms of carbonic anhydrase (CA, EC The synthesized sulfonamides were evaluated in vitro for their inhibitory activity against the following human (h) isoforms, hCA I, II, IV and IX...
April 10, 2018: European Journal of Medicinal Chemistry
Grégory Legrave, Ramzi Ait Youcef, Damien Afonso, Angélique Ferry, Jacques Uziel, Nadège Lubin-Germain
The synthesis of four C-pyrimidyl nucleosides is described by condensation of small nitrogen molecules (amidines and ureas) onto alkynyl riboside derivatives. These last compounds were obtained by indium mediated stereoselective alkynylation of suitably protected ribose derivatives and the condensation reaction conditions were studied in order to favor the N-attack of the nitrogen molecules leading to the pyrimidine ring formation.
April 13, 2018: Carbohydrate Research
Juan Wang, Jiacai Wu, Xumei Li, Haowei Liu, Jianli Qin, Zhun Bai, Bixia Chi, Chen Xu
Identification of the specific protein target(s) of a drug is a critical step in unraveling its mechanisms of action (MOA) in many natural products. Curcumol, isolated from well known Chinese medicinal plant Curcuma zedoary, has been shown to possess multiple biological activities. It can inhibit nasopharyngeal carcinoma (NPC) proliferation and induce apoptosis, but its target protein(s) in NPC cells remains unclear. In this study, we employed a mass spectrometry-based chemical proteomics approach reveal the possible protein targets of curcumol in NPC cells...
April 20, 2018: Journal of Proteomics
Ker Woon Choy, Dharmani Murugan, Mohd Rais Mustafa
Endoplasmic reticulum (ER) is the main organelle for the synthesis, folding, and processing of secretory and transmembrane proteins. Pathological stimuli including hypoxia, ischaemia, inflammation and oxidative stress interrupt the homeostatic function of ER, leading to accumulation of unfolded proteins, a condition referred to as ER stress. ER stress triggers a complex signalling network referred as the unfolded protein response (UPR). Extensive studies have demonstrated that ER stress plays an important role in the pathogenesis of various cardiovascular diseases such as heart failure, ischemic heart disease and atherosclerosis...
April 20, 2018: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
Crist N Filer
This article reviews the methods and strategies to radiolabel and characterise substances with tritium.
March 8, 2018: Applied Radiation and Isotopes
Karoline Kragelund Nielsen, Peter Damm, Ib C Bygbjerg, Anil Kapur
AIMS: An estimated 87.6% of hyperglycaemia in pregnancy cases is in low and middle income countries (LMICs). The aim of this study is to review the evidence on barriers and facilitators to programmes and services addressing hyperglycaemia in pregnancy in LMICs. METHODS: A systematic review and narrative synthesis was conducted based on searches in PubMed. A total of 23 qualitative and quantitative studies were included. RESULTS: Barriers and facilitators exist at the health system level, individual level and social and societal levels and are often interacting...
April 20, 2018: Diabetes Research and Clinical Practice
Carolina P Bernardes, Neife A G Santos, Flavia M Sisti, Rafaela Scalco Ferreira, Norival A Santos-Filho, Adélia C O Cintra, Eduardo M Cilli, Suely V Sampaio, Antonio C Santos
Venom small peptides that target neurotrophin receptors might be beneficial in neurodegeneration, including Parkinsońs disease (PD). Their small size, ease of synthesis, structural stability and target selectivity make them important tools to overcome the limitations of endogenous neurotrophins as therapeutic agents. Additionally, they might be optimized to improve resistance to enzymatic degradation, bioavailability, potency and, mainly, lipophilicity, important to cross the blood brain barrier (BBB). Here, we evaluated the neuroprotective effects and mechanisms of the synthetic snake-venom-based peptide p-BTX-I (Glu-Val-Trp) in PC12 cells treated with MPP+ (1-methyl-4-phenylpyridinium), a dopaminergic neurotoxin that induces Parkinsonism in vivo...
April 20, 2018: Peptides
Lamei Yu, Byung Mun Park, Yong Jin Ahn, Gi-Ja Lee, Suhn Hee Kim
Hydrogen sulfide (H2 S) is normally produced from L-cysteine in mammalian tissues and related to the pathogenesis of cardiovascular diseases. The aim of this study is to investigate the effects of H2 S donor on atrial natriuretic peptide (ANP) secretion and define its mechanism using normal and isoproterenol (ISP)-treated rats. Several H2 S donors were perfused into isolated beating rat atria, and atrial pressure (AP) and ANP secretion were measured. NaHS augmented high stretch-induced ANP secretion and decreased AP in a dose-dependent manner...
April 20, 2018: Peptides
Jung-Ung An, Seung-Hye Hong, Deok-Kun Oh
Lipoxygenase (LOX) is the key enzyme involved in the synthesis of oxylipins as signaling compounds that are important for cell growth and development, inflammation, and pathogenesis in various organisms. The regiospecificity of LOX from Myxococcus xanthus, a gram-negative bacterium, was investigated. The enzyme catalyzed oxygenation at the n-9 position in C20 and C22 polyunsaturated fatty acids (PUFAs) to form 12S- and 14S-hydroxy fatty acids (HFAs), respectively, and oxygenation at the n-6 position in C18 PUFAs to form 13-HFAs...
April 20, 2018: Biochimica et Biophysica Acta
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