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methyl ester

Tomoko Kodama, Muneyoshi Okada, Hideyuki Yamawaki
Eukaryotic elongation factor 2 kinase (eEF2K) is a calmodulin-related protein kinase which regulates protein translation. A484954 is an inhibitor of eEF2K. In the present study, we investigated the acute effects of A484954 on contractility of isolated blood vessels. Isometric contraction of rat isolated aorta and main branch of superior mesenteric artery (MA) was measured. Expression of an inward rectifier K+ (Kir ) channel subtype mRNA and protein was examined. A484954 caused relaxation in endothelium-intact [E (+)] and -denuded [E (-)] aorta or MA precontracted with noradrenaline (NA)...
May 2, 2018: Journal of Pharmacological Sciences
Arpan Kumar Maiti, B C Spoorthi, Nimai Chandra Saha, Ashis Kumar Panigrahi
Although reactive oxygen species mediated oxidative stress is a well-documented mechanism of aging, recent evidences indicate involvement of nitrosative stress in the same. As mitochondrial dysfunction is considered as one of the primary features of aging, the present study was designed to understand the involvement of nitrosative stress by studying the impact of a mitochondria-targeted antioxidant MitoQ, a peroxynitrite (ONOO- ) scavenger, on mitochondrial functions. Four groups of rats were included in this study: Group I: Young-6 months (-MitoQ), Group II: Aged-22 months (- MitoQ), Group III: Young-6 months (+ MitoQ), Group IV: Aged-22 months (+ MitoQ)...
May 17, 2018: Biogerontology
Jianghong Zhong, Tatjana Scholz, Anthony C Y Yau, Simon Guerard, Ulrike Hüffmeier, Harald Burkhardt, Rikard Holmdahl
Previous identification of the inducible nitric oxide synthase (NOS2) gene as a risk allele for psoriasis (Ps) and psoriatic arthritis (PsA) suggests a possible pathogenic role of nitric oxide (NO). Using a mouse model of mannan-induced Ps and PsA (MIP), where macrophages play a regulatory role by releasing reactive oxygen species (ROS), we found that NO was detectable before disease onset in mice, independent of a functional nicotinamide adenine dinucleotide phosphate oxidase 2 complex. MIP was suppressed by either deletion of Nos2 or inhibition of NO synthases with NG-nitro-l-arginine methyl ester, demonstrating that Nos2-derived NO is pathogenic...
May 2018: Science Advances
Rohani Prasad Burman, Shantanu Gupta, Jyoti Bhatti, Krishan Verma, Devendra Rajak, Manjinder Singh Gill
First total synthesis of carpatamide-A 7a, cytotoxic arylamine derivative isolated from marine derived Streptomyces sp., was achieved in twelve steps with overall yield of 24% with seven longest linear steps. In the penultimate step, dienoic acid 13 and an amino-phenylpropionic acid methyl ester core 21 were coupled to synthesize methylated derivativative of carpatamide-A 22 followed by demethylation of the intermediate with BBr3 to accomplish carpatamide-A 7a. Both precursors 13 and 21 were synthesized from readily available starting materials i...
May 17, 2018: Natural Product Research
Hemlata Gupta, Shripad B Deshpande
BACKGROUND: Bisphenol A (BPA), a chemical used in the manufacture of plastics, has toxic effects on various systems of the human body including the reproductive system. BPA possesses estrogenic activity and is implicated in altering oogenesis, ovulation, and fertility. In addition to ovulatory changes, uterine contractility is an important factor for fertility. However, the effects of BPA on myometrial contractions are not known. Therefore, we examined the effect of BPA on rat uterine contractions...
May 16, 2018: Journal of Basic and Clinical Physiology and Pharmacology
Jianxin Yang, Feng Ruan, Zhongjun Zheng
BACKGROUND Microvascular endothelial inflammation and apoptosis are responsible for septic acute lung injury (ALI). Ripasudil is a novel Rho/Rho kinase (ROCK) inhibitor which shows therapeutic effects on several vascular diseases. The aim of this study was to investigate the protective effects and correlated molecular mechanisms of ripasudil on lipopolysaccharide- induced inflammation and apoptosis of pulmonary microvascular endothelial cells (PMVECs). MATERIAL AND METHODS Cultured PMVECs were exposed to lipopolysaccharide (LPS)...
May 16, 2018: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
Chao-Hsuan Chen, Zhi-Wei Lin, Kuan-Min Huang, Hsin-Fei Meng, Ziyi Ge, Hsiao-Wen Zan, Chih-Yu Chang, Yu-Chiang Chao, Sheng-Fu Horng
Interfacial engineering plays an important role in determining the performance and stability of polymer solar cells (PSCs). In this study, we demonstrate thermally stable highly-efficient PSCs by incorporating solution-processed cathode interfacial layer (CIL), including 4,4'-(((methyl(4-sulphonatobutyl)ammonio) bis(propane-3,1-diyl)) bis(dimethyl-ammoniumdiyl)) bis-(butane-1-sulphonate) (MSAPBS) and polyethylenimine (PEI). For PSCs based on blends of poly [4,8-bis (5-(2-ethyl-hexyl) thiophen-2-yl) benzo [1,2-b;4,5-b'] dithiophene-2,6-diyl-alt-(4-(2-ethylhexyl)-3-fluorothieno[3,4-b]thiophene-2-carboxylate-2,6-diyl)] (PBDTTT-EFT) and [6,6]-phenyl C71-butyric acid methyl ester (PC71BM), the maximum power conversion efficiency (PCE) of inverted PSCs reaches 8...
May 16, 2018: ChemSusChem
Julio Zukerman-Schpector, Monica Soto-Monsalve, Regina H De Almeida Santos, Angelo H L Machado, Carlos Roque D Correia, Mukesh M Jotani, Edward R T Tiekink
In the title compound, C28 H34 N2 O5 , the adjacent ester and nitro-benzene substituents are connected via an intra-molecular methyl-ene-C-H⋯π(nitrobenzene) inter-action and the mol-ecule approximates to a U-shape. The di-hydro-pyrrole ring (r.m.s. deviation = 0.003 Å) is almost co-planar with the carboxyl-ate residue [Cm -N-C1-Oc (m = methine, c = carbox-yl) torsion angle = 1.8 (4)°] but is orthogonal to the 4-meth-oxy-benzene ring [dihedral angle = 84.34 (17)°]. In the crystal, methyl-ene- C - H ⋯ O (carbon-yl) inter-actions lead to linear supra-molecular chains along the b -axis direction, which pack without directional inter-actions between them...
March 1, 2018: Acta Crystallographica. Section E, Crystallographic Communications
Yue Liu, Nan Sun, Jianshe Hu, Song Li, Gaowu Qin
The phthalate ester compounds in industrial wastewater, as kinds of environmental toxic organic pollutants, may interfere with the body's endocrine system, resulting in great harm to humans. In this work, the photocatalytic degradation properties of dibutyl phthalate (DBP) were investigated using α-Fe2 O3 nanoparticles and H2 O2 in aqueous solution system. The optimal parameters and mechanism of degradation were discussed by changing the morphology and usage amount of catalysts, the dosage of H2 O2 , pH value and the initial concentration of DBP...
April 2018: Royal Society Open Science
Nada A Noureldin, Hend Kothayer, El-Sayed M Lashine, Mohamed M Baraka, Yanrong Huang, Bing Li, Qinggang Ji
A series of (2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl) acetamido) acids) (6 a-m), (7) has been designed to inhibit the action of fungus chitin synthase enzyme (CHS). The synthesis of the designed compounds was carried out in four steps starting from the reaction between 1-methylquinazoline-2,4(1H,3H)-dione and ethyl chloroacetate to yield the ethyl acetate derivative. This ester was hydrolyzed to the corresponding carboxylic acid derivative that was then utilized to couple several amino acids getting the final designed compounds...
May 4, 2018: European Journal of Medicinal Chemistry
Amani N Shafik, Mahmoud A Khattab, Ahmed H Osman
OBJECTIVE: Preeclampsia represents a major complication of pregnancy, associated with greater maternal and fetal complications. We compared the effects of esomeprazole (a proton pump inhibitor) and magnesium sulfate (MgSO4) on the deleterious effects observed on the mother and neonates in experimentally induced preeclampsia in rats. STUDY DESIGN: Preeclampsia was induced in pregnant rats with NG-nitro-l-arginine methyl ester (L-NAME) starting from day 10-till end of pregnancy...
May 8, 2018: European Journal of Obstetrics, Gynecology, and Reproductive Biology
Jaishabanu Ameeramja, Vishnu Vignesh Kanagaraj, Ekambaram Perumal
We have found that protocatechuic acid methyl ester (PCAME) attenuates fluoride (F- ) toxicity in lung epithelial cells (A549). However, these finding has to be confirmed with in vivo studies. Further, the effect of PCAME on F- induced pulmonary fibrosis and inflammation remains limited. Hence, the present study is aimed to determine the protective effect PCAME against F- induced pulmonary toxicity in female albino Wistar rats. The animals were treated with sodium fluoride (NaF, 300 ppm in drinking water ad libitum) alone or in combination with PCAME (25 or 50 mg/kg bw/day by oral intubation) for 60 days and analyzed for changes in lung histology, oxidative stress, inflammation, apoptosis and fibrosis markers...
May 11, 2018: Food and Chemical Toxicology
A Arreguín, J Ribot, H Musinovic, J von Lintig, A Palou, M L Bonet
We previously showed that vitamin A supplementation in early life impacts white adipose tissue (WAT) biology. We here studied the vitamin's effects on DNA methylation of genes crucial for WAT cell development, determination and metabolism. CpG promoter methylation and mRNA expression of Pparg, Zfp423, Pcna, and Rbp4 was compared in inguinal WAT of 21-day-old rats supplemented during the suckling period with vehicle (controls) or an emulsion of vitamin A as retinyl ester (RE) or β-carotene (BC). The methylation profile of promoters was affected by vitamin A supplementation with pronounced differences between the RE and BC groups...
May 11, 2018: Archives of Biochemistry and Biophysics
Ming-Yi Lin, Shang-Hsuan Wu, Li-Jen Hsiao, Widhya Budiawan, Shih-Lun Chen, Wei-Chen Tu, Chia-Yen Lee, Yia-Chung Chang, Chih-Wei Chu
This manuscript describes how to design and fabricate efficient inverted solar cells, which are based on a two-dimensional conjugated small molecule (SMPV1) and [6,6]-phenyl-C71-butyric acid methyl ester (PC71BM), by utilizing ZnO nanorods (NRs) grown on a high quality Al-doped ZnO (AZO) seed layer. The inverted SMPV1:PC71BM solar cells with ZnO NRs that grew on both a sputtered and sol-gel processed AZO seed layer are fabricated. Compared with the AZO thin film prepared by the sol-gel method, the sputtered AZO thin film exhibits better crystallization and lower surface roughness, according to X-ray diffraction (XRD) and atomic force microscope (AFM) measurements...
April 25, 2018: Journal of Visualized Experiments: JoVE
Tian Lan, Francesca Soavi, Massimo Marcaccio, Pierre-Louis Brunner, Jonathan Sayago, Clara Santato
The n-type organic semiconductor phenyl-C61-butyric acid methyl ester (PCBM), a soluble fullerene derivative well investigated for organic solar cells and transistors, can undergo several successive reversible, diffusion-controlled, one-electron reduction processes. We exploited such processes to shed light on the correlation between electron transfer properties, ionic and electronic transport as well as device performance in ionic liquid (IL)-gated transistors. Two ILs were considered, based on bis(trifluoromethylsulfonyl)imide [TFSI] as the anion and 1-ethyl-3-methylimidazolium [EMIM] or 1-butyl-1-methylpyrrolidinium [PYR14] as the cation...
May 14, 2018: Chemical Communications: Chem Comm
S R Sathish Kumar, K V Bhaskara Rao
The current study was carried out to evaluate the in-vitro and in-vivo efficiency of alpha glucosidase inhibitor of marine actinobacteria in the control of postprandial hyperglycaemia. Soil samples were collected from salterns, coastal area in Kothapatnam, Ongole, Andhra Pradesh, India. Among the actinobacterial isolates tested for yeastα-glucosidase inhibitory activity, only three isolates showed prominent inhibition. The patient isolate was selected and identified as Streptomyces coelicoflavus SRBVIT13 using 16S r-RNA gene sequencing...
2018: Iranian Journal of Pharmaceutical Research: IJPR
Herbert J Dias, Andressa B Patrocínio, Mariana C Pagotti, Murilo J Fukui, Vanderlei Rodrigues, Lizandra G Magalhães, Antônio E M Crotti
We have evaluated the antischistosomal activity of synthetic dihydrobenzofuran neolignans (DBNs) derived from (±)-trans-dehydrodicoumarate dimethyl ester (1) and (±)-trans-dehydrodiferulate dimethyl ester (2) against adult Schistosoma mansoni worms in vitro. Compound 4 ((±)-4-O-acetyl-trans-dehydrodiferulate dimethyl ester) displays the most promising activity; at 200 μM, it kills 100±0% of worms after 24 h, which resembles the result achieved with praziquantel (positive control) at 1.56 μM. Hydrogenation of the double bond between C7' and C8', introduction of an additional methyl group at C3', and a double bond between C7 and C8 decreases the schistosomicidal activity of DBNs...
May 13, 2018: Chemistry & Biodiversity
Cristian Adrián Márquez-Ramírez, José Lucio Hernández de la Paz, Omar Ortiz-Avila, Andrés Raya-Farias, Juan Carlos González-Hernández, Alain Raimundo Rodríguez-Orozco, Rafael Salgado-Garciglia, Alfredo Saavedra-Molina, Daniel Godínez-Hernández, Christian Cortés-Rojo
OBJECTIVE: Angiotensin II (Ang-II) antagonism alleviates hypertensive kidney damage by improving mitochondrial function and decreasing oxidative stress. This condition also is associated with altered renal vascular tone due to enhanced constriction by Ang-II. Thus, approaches ameliorating these events are desirable to alleviate kidney damage. Avocado oil, a source of antioxidants and oleic acid, is known to improve mitochondrial function, while oleic acid has antihypertensive effects...
March 20, 2018: Nutrition
Carlos A Valdez, Mira K Marchioretto, Roald N Leif, Saphon Hok
Trimethyloxonium tetrafluoroborate (TMO·BF4 ) has been used in the simultaneous derivatization of phosphonic and 2-aminoethylsulfonic acids related to nerve agents in different soils for their enhanced detection and identification by electron ionization gas chromatography-mass spectrometry (EI-GC-MS). The panel of acids consisted of five Schedule 2 phosphonic acids (methyl methylphosphonic acid, ethyl methylphosphonic acid, isopropyl methylphosphonic acid, pinacolyl methylphosphonic acid and cyclohexyl methylphosphonic acid) along with two sulfonic acids, N,N-diethyl-2-aminoethylsulfonic acid and N,N-diisopropyl-2-aminoethylsulfonic acid...
April 27, 2018: Forensic Science International
Xinyu Zhang, Rui Zhao, Meng Chen, Tao Ma, Gaorong Wu, Nannan Xue, Guoliang Li, Hui Wang, Kang Fang, Wenxi Zhang, Penglong Wang, Haimin Lei
The neuroprotective evaluation of ligustrazine derivatives has become a research focus all over the world. A novel ligustrazine derivative, (3,5,6-Trimethylpyrazin-2-yl)methyl(E)-3-(4-((3,5,6-trimethylpyrazin-2-l)methoxy)phenyl)acrylate (T-CA), has shown protective effects against CoCl₂-induced neurotoxicity in a differentiated PC12 cell model and middle cerebral artery occlusion (MCAO) model in our previous studies. However, nearly none of the parent drugs existed after rapid metabolism due to uncertain reasons...
May 11, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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