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https://www.readbyqxmd.com/read/28645884/investigation-of-the-effects-of-lycium-barbarum-polysaccharides-against-cadmium-induced-damage-in-testis
#1
Maria Vittoria Varoni, Sergio Domenico Gadau, Valeria Pasciu, Elena Baralla, Elisa Serra, Domenico Palomba, Maria Piera Demontis
This study describes the effects of Lycium barbarum polysaccharides (LBP) on testicular damage induced by cadmium (Cd). Adult male rats were i.p. injected with CdCl2 (4mg/Kg, once) with or without LBP pretreatment (300mg/Kg orally, once a day, for 30days). Testis weight, morphological/histological structure and oxidative stress parameters were evaluated. Several adverse effects were observed after CdCl2 injection, with a significant decrease in body/testis weight ratio (P<0.05), gross morphological changes with hyperemia of the parenchyma, increased volume and alteration in the structure of the seminiferous tubules...
June 20, 2017: Experimental and Molecular Pathology
https://www.readbyqxmd.com/read/28645873/generation-of-nitric-oxide-by-olive-olea-europaea-l-pollen-during-in-vitro-germination-and-assessment-of-the-s-nitroso-and-nitro-pollen-proteomes-by-computational-predictive-methods
#2
María José Jimenez-Quesada, Rosario Carmona, Elena Lima-Cabello, José Ángel Traverso, Antonio Jesús Castro, M Gonzalo Claros, Juan de Dios Alché
Nitric oxide is recognized as a signaling molecule involved in a broad range of physiological processes in plants including sexual reproduction. NO has been detected in the pollen grain at high levels and regulates pollen tube growth. Previous studies demonstrated that NO as well as ROS are produced in the olive reproductive tissues in a stage- and tissue-specific manner. The aim of this study was to assess the production of NO throughout the germination of olive (Olea europaea L.) pollen in vitro. The NO fluorescent probe DAF-2DA was used to image NO production in situ, which was correlated to pollen viability...
June 20, 2017: Nitric Oxide: Biology and Chemistry
https://www.readbyqxmd.com/read/28645860/gper-agonist-dilates-mesenteric-arteries-via-pi3k-akt-enos-and-potassium-channels-in-both-sexes
#3
Pollyana Peixoto, Rosária Dias Aires, Virgínia Soares Lemos, Nazaré Souza Bissoli, Roger Lyrio Dos Santos
AIM: The action of oestrogen has traditionally been attributed to the activation of nuclear receptors (ERα and ERβ). A third receptor, the G protein-coupled oestrogen receptor (GPER), has been described as mediator of the rapid action of oestrogen. Based on the possible protective role of oestrogen in the cardiovascular system, the present study was designed to determine whether selective GPER activation induces relaxation of mesenteric resistance arteries in both sexes and which signalling pathways are involved...
June 20, 2017: Life Sciences
https://www.readbyqxmd.com/read/28644035/influence-of-a-basic-side-chain-on-the-properties-of-hypoxia-selective-nitro-analogues-of-the-duocarmycins-demonstration-of-substantial-anticancer-activity-in-combination-with-irradiation-or-chemotherapy
#4
Moana Tercel, Ho H Lee, Sunali Y Mehta, Jean-Jacques Youte Tendoung, Sally Y Bai, H D Sarath Liyanage, Frederik B Pruijn
A new series of nitro analogues of the duocarmycins was prepared and evaluated for hypoxia-selective anticancer activity. The compounds incorporate 13 different amine-containing side chains designed to bind in the minor groove of DNA while spanning a wide range of base strength from pKa 9.64 to 5.24. The most favorable in vitro properties were associated with strongly basic side chains, but the greatest in vivo antitumor activity was found for compounds containing a weakly basic morpholine. This applies to single-agent activity and for activity in combination with irradiation or chemotherapy (gemcitabine or docetaxel)...
June 23, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28643514/nitroalkenes-as-latent-1-2-biselectrophiles-a-multicatalytic-approach-for-the-synthesis-of-1-4-diketones-and-their-application-in-a-4-step-one-pot-reaction-to-polysubstituted-pyrroles
#5
Patrick J W Fuchs, Kirsten Zeitler
A NHC-catalyzed Nitro-Stetter/elimination/Stetter reaction sequence employs nitroalkenes as latent 1,2-dication synthons providing a novel access to highly useful symmetrical and unsymmetrical 2-aryl substituted 1,4 diketone building blocks from commercially available aldehyde precursors. For less activated (aliphatic) aldehydes a cooperative catalytic strategy has been developed via the merger of NHC and H-bonding catalysis. To further showcase the versatility of our approach a great variety of these unprecedented 1,4 diketones are used to efficiently synthesize polysubstituted pyrroles - including those with hetaryl substituents - in good to excellent yields in a multicatalytic metal-free, 4-step one-pot-cascade reaction under mild, yet robust conditions...
June 23, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28641232/on-the-aquatic-toxicity-of-substituted-phenols-to-chlorella-vulgaris-qstr-with-an-extended-novel-data-set-and-interspecies-models
#6
Gulcin Tugcu, M Doğa Ertürk, Melek Türker Saçan
This study provides for the first time the 96-h toxicity of 16 nitro- and methyl- substituted phenols to Chlorella vulgaris. Enabling the circulation of new ecotoxicity data has expanded the previously reported toxicity data set of 30 phenols to C. vulgaris by our laboratory. In this respect, high quality, single source algal toxicity data, generated in the same laboratory according to a REACH (Registration, Evaluation, Authorization and Restriction of CHemicals) compatible endpoint, provided a sound basis to explore quantitative structure-toxicity relationship (QSTR), which can be used for regulatory purposes...
June 15, 2017: Journal of Hazardous Materials
https://www.readbyqxmd.com/read/28641156/mild-c-sp-3-h-functionalization-of-dihydrosanguinarine-and-dihydrochelerythrine-for-development-of-highly-cytotoxic-derivatives
#7
Adriana Romo-Pérez, Luis Demetrio Miranda, Alma D Chávez-Blanco, Alfonso Dueñas-González, María Del Rayo Camacho-Corona, Alejandrina Acosta-Huerta, Abraham García
A series of C(6)-substituted dihydrobenzo[c]phenanthridines were synthesized by mild copper-catalyzed C(sp(3))-H functionalization of dihydrosanguinarine (2) and dihydrochelerythrine (3) with certain nucleophiles selected to enhance cytotoxicity against human breast, colorectal, and prostate cancer cell lines. We also investigated the cytotoxicity of our previously reported C(6)-functionalized N-methyl-5,6-dihydrobenzo[c]phenanthridines 1a-1e to perform structure-activity relationship (SAR) studies. Among the target compounds, five β-aminomalonates (1a, 1b, 2a, 2b, and 3b), one α-aminophosphonate (2c), and one nitroalkyl derivative (2h) exhibited half maximal inhibitory concentration (IC50) values in the range of 0...
June 13, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28640960/ferulic-acid-alleviates-symptoms-of-preeclampsia-in-rats-by-upregulating-vascular-endothelial-growth-factor
#8
Weiyan Gong, Jipeng Wan, Qing Yuan, Quanzhan Man, Xiaojing Zhang
Preeclampsia is a complication affecting pregnant women worldwide, which leads to maternal and fetal morbidity and mortality. In this study, we evaluated the efficacy of ferulic acid (FA) on an N(ω) -nitro-L-arginine methyl ester hydrochloride (L-NAME) induced rat model of preeclampsia. L-NAME was administered to pregnant rats to induce preeclampsia. 48 rats were divided into three experimental groups (n=16 each): control group, preeclampsia group and preeclampsia with FA treatment (preeclampsia+FA). Physiological characteristics such as urine volume, total urine protein and blood pressure were assessed...
June 22, 2017: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/28640644/nebivolol-alleviates-aortic-remodeling-through-enos-upregulation-and-inhibition-of-oxidative-stress-in-l-name-induced-hypertensive-rats
#9
Yan Wang, Fei Zhang, Yu Liu, Sha Yin, Xuefen Pang, Zhidong Li, Zehui Wei
PURPOSE: To investigate the effect and mechanism of nebivolol on aortic remodeling in N-nitro-l-arginine methyl ester (l-NAME)-induced hypertension. METHODS: Male Sprague-Dawley rats were treated with equal volumes of drinking water or l-NAME (60 mg/kg/day), alone or in combination with nebivolol (8 mg/kg/day) or atenolol (80 mg/kg/day) by gavage for 8 weeks. Systolic blood pressure (SBP), aortic morphometry, plasma nitric oxide (NO) levels, nitric oxide synthase (NOS) activity, and relaxation of aorta to acetylcholine were determined...
June 22, 2017: Clinical and Experimental Hypertension: CHE
https://www.readbyqxmd.com/read/28640305/immobilization-of-catalytic-virus-like-particles-in-a-flow-reactor
#10
A Liu, L Yang, C H-H Traulsen, J J L M Cornelissen
A functional microfluidic reactor is constructed by the immobilization of gold containing virus-based protein cages that catalyze the reduction of nitro-arenes with high efficiency.
June 22, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28639634/copper-ii-catalyzed-iodine-promoted-oxidative-cyclization-of-2-amino-1-3-5-triazines-and-chalcones-synthesis-of-aroylimidazo-1-2-a-1-3-5-triazines
#11
Jin Jing Li, Chan Song, Dong-Mei Cui, Chen Zhang
An efficient copper(ii) catalyzed iodine-promoted synthesis of aroylimidazo[1,2-a][1,3,5]triazines from 2-amino-1,3,5-triazines and chalcones under mild conditions has been developed. The reaction occurred with good yields and excellent regioselectivities, and tolerated chalcone containing functionalities such as ethers, halogens, and nitro groups. The successful application of this methodology for a gram-scale reaction indicates its potential for bulk synthesis.
June 22, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28638637/crystal-structure-of-chlorido-1-4-nitro-phen-yl-thio-urea-%C3%AE%C2%BAs-bis-tri-phenyl-phosphane-%C3%AE%C2%BAp-silver-i
#12
Arunpatcha Nimthong-Roldán, Paramee Sripa, Yupa Wattanakanjana
In the title compound, [AgCl(C7H7N3O2S)(C18H15P)2], the Ag(I) ion is in a distorted tetra-hedral coordination environment formed by P atoms from two tri-phenyl-phosphane ligands, one terminal S atom from the 1-(4-nitro-phen-yl)thio-urea ligand and a chloride ion. In the crystal, bifurcated (N-H)2⋯Cl hydrogen bonds [with graph-set motif R2(1)(6)] connect complex mol-ecules, forming zigzag chains along [001]. These chains are linked via weak C-H⋯O hydrogen bonds, forming a two-dimensional network parallel to (100)...
June 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28636367/cobalt-catalyzed-regioselective-ortho-c-sp2-h-bond-nitration-of-aromatics-through-proton-coupled-electron-transfer-pcet-assistance
#13
Desaboini Nageswar Rao, Sk Rasheed, Gaurav Raina, Qazi Naveed Ahmed, Chaitanya Kumar Jaladanki, Prasad V Bharatam, Parthasarathi Das
A cobalt-catalyzed proton-coupled electron transfer (PCET) mediated regioselective ortho-specific nitration of aromatic C(sp2)-H bonds using chelation assisted removable vicinal diamine directing groups has been developed. The reaction proceeded under mild conditions in the presence of Co(OAc)2•4H2O as the catalyst and AgNO2 utilized as nitro source as well as terminal oxidant in the presence of O2 as a external oxidant, no external base and additives were required for this process. By doing controlled experiments and mechanistic investigations with DFT calculations revealed that the reaction proceeds through PCET promoted nitro functional group transfer pathway...
June 21, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28636362/corey-chaykovsky-reactions-of-nitro-styrenes-enable-cis-configured-trifluoromethyl-cyclopropanes
#14
Katharina J Hock, Renè Hommelsheim, Lucas Mertens, Junming Ho, Thanh Vinh Nguyen, Rene M Koenigs
Trifluoromethyl-substituted cyclopropanes are an attractive family of building blocks for the construction of pharmaceutical and agrochemical agents. This work demonstrated the utilization of fluorinated sulfur ylides as versatile reagents for Corey-Chaykovsky cyclopropanation reactions of nitro styrenes. This protocol favored the synthesis of cis-configured trifluoromethyl cyclopropanes on a broad range of substrates with excellent yields and good diastereoselectivity.
June 21, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28636336/a-mg-cp-with-in-situ-encapsulated-photochromic-guest-as-sensitive-fluorescence-sensor-for-fe-3-cr-3-ions-and-nitro-explosives
#15
Zhao-Feng Wu, Liao-Kuo Gong, Xiao-Ying Huang
Here we report a fluorescent magnesium coordination polymer (Mg-CP), namely, [CH3-dpb]2[Mg3(1,4-NDC)4(μ-H2O)2(CH3OH)(H2O)]·1.5H2O (1, 1,4-H2NDC = 1,4-naphthalene dicarboxylic acid, dpb = 1,4-bis(pyrid-4-yl)benzene). Compound 1 possesses a three-dimensional (3D) host-guest structure constructed by the 1,4-NDC linkers bridging the linear trinuclear secondary building units of [Mg3(COO)8(μ-H2O)2]. The dpb molecules were in situ reacted with CH3OH resulting in photochromic cations of [CH3-dpb](+) that acted as guests located in the channels parallel to the b-axis...
June 21, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28633978/airborne-nitro-pahs-induce-nrf2-are-defense-system-against-oxidative-stress-and-promote-inflammatory-process-by-activating-pi3k-akt-pathway-in-a549-cells
#16
Yu Shang, Qian Zhou, Tiantian Wang, Yuting Jiang, Yufang Zhong, Guangren Qian, Tong Zhu, Xinghua Qiu, Jing An
Ambient particulate matter (PM) is a worldwide health issue of concern. However, limited information is available regarding the toxic contributions of the nitro-derivatives of polycyclic aromatic hydrocarbons (nitro-PAHs). This study intend to examine whether 1-nitropyrene (1-NP) and 3-nitrofluoranthene (3-NF) could activate the nuclear factor-erythroid 2-related factor 2/antioxidant response element (Nrf2/ARE) antioxidant defense system, and whether the phosphatidylinositol 3-kinase/protein kinase B (PI3K/Akt) pathway participates in regulating pro-inflammatory responses in A549 cells...
June 17, 2017: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/28632402/3-benzyloxy-1-5-18-f-fluoropentyl-5-nitro-1h-indazole-a-pet-radiotracer-to-measure-acetylcholinesterase-in-brain
#17
Soledad Fernández, Javier Giglio, Ana Laura Reyes, Andrés Damián, Concepción Pérez, Daniel I Pérez, Mercedes González, Patricia Oliver, Ana Rey, Henry Engler, Hugo Cerecetto
AIM: Noninvasive studies of the acetylcholinesterase (AChE) level in Alzheimer's disease (AD) patients can contribute to a better understanding of the disease and its therapeutic. We propose 3-(benzyloxy)-1-(5-[(18)F]fluoropentyl)-5-nitro-1H-indazole, [(18)F]-IND1, structurally related to the AChE-inhibitor CP126,998, as a new positron emission tomography-radiotracer. EXPERIMENTAL: Radiosynthesis, with 18F, stability, lipophilicity and protein binding of [18F]-IND1 were studied...
June 20, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28629630/design-synthesis-and-tumor-cell-growth-inhibitory-activity-of-3-nitro-2h-cheromene-derivatives-as-histone-deacetylaes-inhibitors
#18
Shuai Tan, Feng He, Tingting Kong, Jingde Wu, Zhaopeng Liu
As a continuous research for the discovery of coumarin-based targeted anticancer agents, we designed and synthesized a series of novel histone deacetylases (HDAC) inhibitors using the 8-ethoxy-3-nitro-2H-chromene as the surface binding or cap group, linear dicarboxylic acid or ω-amino acid moiety with different length as the linking motif, ortho-aminoanilides, amides or α-aminoamides as the zinc binding group and the internal cavity motifs. Most of these 3-nitro-2H-chromene derivatives exhibited good growth inhibitory activity against K562, A549, MCF-7, PC3 and Hela cells and were more potent than the reference drug SAHA and MS-275...
June 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28628311/pushing-the-limits-of-oxygen-balance-in-1-3-4-oxadiazoles
#19
Qiong Yu, Ping Yin, Jiaheng Zhang, Chunlin He, Gregory H Imler, Damon A Parrish, Jean'ne M Shreeve
Gem-trinitromethyl groups were introduced into a 1,3,4-oxadiazole ring to give the first example of a bifunctionalized single five-membered ring with six nitro groups. 2,5-Bis(trinitromethyl)-1,3,4-oxadiazole (12) has a high calculated crystal density of 2.007 g cm(-3) at 150 K (1.941 g cm(-3) at 293 K) and a very high positive oxygen balance (39.12%), which makes it a strong candidate as a high energy dense oxidizer. The dihydroxylammonium and dihydrazinium salts of bis(trinitromethyl)-1,3,4-oxadiazole (5 and 6) exhibit excellent calculated detonation properties (5, vD = 9266 m s(-1), P = 38...
June 21, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28626525/identification-of-better-pharmacokinetic-benzothiazinone-derivatives-as-new-antitubercular-agents
#20
Kai Lv, Xuefu You, Bin Wang, Zengquan Wei, Yun Chai, Bo Wang, Apeng Wang, Guocheng Huang, Mingliang Liu, Yu Lu
A series of new 8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one(BTZ) derivatives containing a C-2 nitrogen spiro-heterocycle moiety based on the structures of BTZ candidates BTZ043 and PBTZ169 were designed and synthesized as new antitubercular agents. Many of them were found to have excellent in vitro activity (MIC < 0.15 μM) against the drug susceptive Mycobacterium tuberculosis H37Rv strain and two clinically isolated multidrug-resistant strains. Compounds 11l and 11m display acceptable safety, greater aqueous solubility, and better pharmacokinetic profiles than PBTZ169, suggesting their promising potential to be lead compounds for future antitubercular drug discovery...
June 8, 2017: ACS Medicinal Chemistry Letters
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