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Chu Shan Tan, Mun Fei Yam
Previous studies have demonstrated that 3'-hydroxy-5,6,7,4'-tetramethoxyflavone (TMF) content in Orthosiphon stamineus fractions correlate with its vasorelaxation activity. Even with the availability of previous studies, there is still very little information on the vasorelaxation effect of TMF, and few scientific studies have been carried out. Therefore, the present study was designed to investigate the vasorelaxation activity and mechanism of action of the TMF. The vasorelaxation activity and the underlying mechanisms of TMF were evaluated on thoracic aortic rings isolated from Sprague Dawley rats...
March 19, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Jennifer Chia Wee Fern, Shuji Ohsaki, Satoru Watano, Robert Pfeffer
The synthesis of nano-size drug particles by antisolvent crystallization using a porous hollow fiber membrane provides promising benefits such as the capability of continuous operation, low energy input, and ease of scale-up for a variety of industrial processes. Porous hollow fiber membranes have also been shown to produce more efficient mixing than conventional mixing equipment mostly because in mixing binary fluids, they provide sufficient mixing time, retention time, and a large contact interface for the drug solution and the antisolvent, allowing for the precise control of nucleation and crystal growth necessary to form nano-size particles...
March 15, 2018: International Journal of Pharmaceutics
Mohamed K S El-Nagar, Hajjaj H M Abdu-Allah, Ola I A Salem, Abdel-Hamid N Kafafy, Hanan S M Farghaly
Three new series of 5-aminosalicylic acid derivatives; series I (14, 16-18), series II (19-30) and series III (31-41) were synthesized as potential dual COX-2/5-LOX inhibitors. Their chemical structures were confirmed using spectroscopic tools including IR,1 H NMR,13 C NMR, mass spectroscopy and elemental analyses. The anti-inflammatory activity for all target compounds was evaluated in vivo using carrageenan-induced paw edema. Compound 36 showed the highest anti-inflammatory activity (114.12%) relative to reference drug indomethacin at 4 h interval...
March 6, 2018: Bioorganic Chemistry
Mohamed A Abdelgawad, Madlen B Labib, Waleed A M Ali, Gehan Kamel, Amany A Azouz, El-Shaymaa El-Nahass
A series of newly synthesized 4-aryl-hydrazonopyrazolones were designed and their structures were confirmed by spectral and elemental analyses. All synthesized compounds were evaluated for their in vitro COXs, 5-LOX inhibition, in vivo analgesic and anti-inflammatory activities. Compounds 5d, 5f and 5i were found to be the most potent COX-2/5-LOX inhibitors with superior COX-2 selectivity index values (SI = 5.29-5.69) to reference standard celecoxib (SI = 3.52). Four compounds; 5b, 5c, 5d and 5f showed excellent anti-inflammatory activity (% edema inhibition = 72...
March 8, 2018: Bioorganic Chemistry
Alain N'guessan Yao, Mamadou Kamagaté, Augustin Kouao Amonkan, Philippe Chabert, Fidèle Kpahé, Camille Koffi, Mathieu N'goran Kouamé, Cyril Auger, Séraphin Kati-Coulibaly, Valérie Schini-Kerth, Henri Die-Kakou
BACKGROUND: Phyllanthus amarus (Schum & Thonn), a plant belonging to the family of Euphorbiaceae is used in Ivorian traditional medicine to treat cardiovascular disorders such as hypertension. However, although this plant has been described as a diuretic agent, the underlying mechanism remains unclear. Therefore, the aim of the present study was to investigate the mechanism action of diuretic effects of an ethanolic fraction of Phyllanthus amarus (EFPA) in rats. METHODS: Effects of EFPA on urinary excretion were carried out for doses ranging from 5 to 80 mg/kg given by intraperitoneal injection (i...
March 15, 2018: BMC Complementary and Alternative Medicine
Young Hee Nam, Colleen M Brensinger, Warren B Bilker, Charles E Leonard, Scott E Kasner, Tilo Grosser, Xuanwen Li, Sean Hennessy
OBJECTIVE: To examine the comparative safety of individual NSAIDs when given concomitantly with clopidogrel. METHODS: We conducted a retrospective cohort study using Medicaid claims from five US states during 1999-2010, supplemented with Medicare claims for dual-enrollees. The exposure of interest was the first concomitant use of clopidogrel and one of the 10 selected NSAIDs after a 1-year baseline period. The outcomes were: all-cause mortality; acute myocardial infarction (AMI)/ischemic stroke; and gastrointestinal bleeding (GIB)/intracranial hemorrhage (ICH)...
2018: PloS One
Jeanette I Beaute, Kevin G Friedman
This article reports a rare but potentially serious complication of ductus arteriosus closure resulting from second-trimester indomethacin exposure. Serial echocardiograms are indicated to monitor for development of right heart dysfunction and to ensure delivery prior to the onset of right heart failure and hydrops fetalis.
March 2018: Clinical Case Reports
Deonne Dersch-Mills, Belal Alshaikh, Amuchou S Soraisham, Albert Akierman, Kamran Yusuf
Background: There is no injectable ibuprofen product marketed to treat patent ductus arteriosus (PDA) in newborns in Canada. The authors' institution has used ibuprofen arginine in the past. In the absence of published evidence supporting use of this salt form of ibuprofen for neonatal PDA, a retrospective analysis was undertaken. Objective: To compare the effectiveness and adverse effects of ibuprofen arginine, ibuprofen tromethamine, and indomethacin in the treatment of PDA...
January 2018: Canadian Journal of Hospital Pharmacy
Hasan Kırmızıbekmez, Yiğit İnan, Rengin Reis, Hande Sipahi, Ahmet C Gören, Erdem Yeşilada
Phytochemical investigations on the EtOH extract of Clematis viticella led to the isolation of six flavonoid glycosides, isoorientin (1), isoorientin 3'-O-methyl ether (2), quercetin 7-O-α-L-rhamnopyranoside (3), quercetin 3,7-di-O-α-L-rhamnopyranoside (4), manghaslin (5) and chrysoeriol 7-O-β-D-glucopyranoside (6), one phenylethanol derivative, hydroxytyrosol (7), along with three phenolic acids, caffeic acid (8), (E)-p-coumaric acid (9) and p-hydroxybenzoic acid (10). The structures of the isolates were elucidated on the basis of NMR and HR-MS data...
March 12, 2018: Natural Product Research
M Tavares-Silva, D Ferreira, S Cardoso, A R Raimundo, J Barbosa-Breda, A Leite-Moreira, A Rocha-Sousa
Urocortin 2 (UCN2) is a peptide related to corticotropin-releasing factor, capable of activating CRF-R2. Among its multisystemic effects, it has actions in all 3 muscle subtypes. This study's aim was to determine its potential role in two of the intrinsic eye muscle kinetics. Strips of iris sphincter (rabbit) and ciliary (bovine) muscles were dissected and mounted in isometric force-transducer systems filled with aerated-solutions. Contraction was elicited using carbachol (10(-6) M for iris sphincter, 10(-5) M for ciliary muscle), prior to all testing substances...
March 12, 2018: Physiological Research
Akintayo Lanre Ogundajo, Lateef Apollo Adeniran, Anofi Omotayo Ashafa
OBJECTIVE: This study evaluates the phytochemical constituents, antioxidant and anti-inflammatory activity, cytotoxicity, and inhibitory activity against carbohydrate metabolism of extracts from Ocotea bullata stem bark. METHODS: Hexane, ethyl acetate, methanol and water were used to extract the air-dried sample. The phytochemical investigation and antioxidant assays were carried out on the extracts using standard procedures. The antidiabetic and anti-inflammatory potentials were evaluated using α-amylase, α-glucosidase and 5-lipoxygenase enzymes respectively...
March 2018: Journal of Integrative Medicine
Zhongjian Cheng, Xinggui Shen, Xiaohua Jiang, Huimin Shan, Maria Cimini, Pu Fang, Yong Ji, Joon Young Park, Konstantinos Drosatos, Xiaofeng Yang, Christopher G Kevil, Raj Kishore, Hong Wang
Insufficient hydrogen sulfide (H2 S) has been implicated in Type 2 diabetic mellitus (T2DM) and hyperhomocysteinemia (HHcy)-related cardiovascular complications. We investigated the role of H2 S in T2DM and HHcy-induced endothelial dysfunction in small mesenteric artery (SMA) of db/db mice fed a high methionine (HM) diet. HM diet (8 weeks) induced HHcy in both T2DM db/db mice and non-diabetic db/+ mice (total plasma Hcy: 48.4 and 31.3 µM, respectively), and aggravated the impaired endothelium-derived hyperpolarization factor (EDHF)-induced endothelium-dependent relaxation to acetylcholine (ACh), determined by the presence of eNOS inhibitor N(ω)-nitro-L-arginine methyl ester (L-NAME) and prostacyclin (PGI2 ) inhibitor indomethacin (INDO), in SMA from db/db mice but not that from db/+ mice...
February 14, 2018: Redox Biology
Paul C Norris, Charles N Serhan
Metabolomics enables a systems approach to interrogate the bioactive mediators, their pathways and further metabolites involved in the physiology and pathophysiology of human and animal tissues. New metabololipidomic approaches with mass spectrometry presented in this brief review can now be utilized for the identification and profiling of lipid mediator networks that control inflammation-resolution in human blood and healthy and diseased solid tissues. Coagulation of blood is a protective response that prevents excessive bleeding on injury of blood vessels...
March 7, 2018: Biochemical and Biophysical Research Communications
Nancy N Shahin, Noha F Abdelkader, Marwa M Safar
The advent of angiotensin II type 1 receptor blockers (ARBs) as intriguing gastroprotective candidates and the superior pharmacokinetics and pharmacodynamics displayed by irbesartan compared to many other ARBs raised the interest to investigate its gastroprotective potential in a rat model of gastric injury. Irbesartan (50 mg/Kg) was orally administered to male Wistar rats once daily for 14 days; thereafter gastric injury was induced by indomethacin (60 mg/Kg, p.o). Irbesartan reduced gastric ulcer index, gastric acidity, and ameliorated indomethacin-induced gastric mucosal apoptotic and inflammatory aberrations, as demonstrated by hampering caspase-3, prostaglandin E2 and tumor necrosis factor-alpha levels and cyclooxygenase-2 mRNA expression...
March 9, 2018: Scientific Reports
Carla Blum-Johnston, Richard B Thorpe, Chelsea Wee, Raechel Opsahl, Monica Romero, Samuel Murray, Alexander Brunelle, Quintin Blood, Rachael Wilson, Arlin B Blood, Lubo Zhang, Lawrence D Longo, William J Pearce, Sean M Wilson
Bradykinin-induced activation of the pulmonary endothelium triggers a rise in intracellular Ca2+ , which activates nitric oxide (NO)-dependent vasorelaxation. Chronic hypoxia is commonly associated with increased pulmonary vascular tone, which can cause pulmonary hypertension in responsive individuals. In the present study, we tested the hypothesis that long-term high altitude hypoxia (LTH) diminishes bradykinin-induced Ca2+ signals and inhibits eNOS, PGI2 and BKCa channels in sheep, which are moderately responsive to LTH, resulting in decreased pulmonary arterial vasorelaxation...
March 7, 2018: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
Kazumi Sugihara
 In recent years, pharmaceuticals and personal care products (PPCPs) have emerged as significant pollutants of aquatic environments and have been detected at levels in the range of ng/L to μg/L. The source of PPCPs is humans and livestock that have been administered pharmaceuticals and subsequently excreted them via urine and feces. Unlike agricultural chemicals, the environmental dynamics of PPCPs is not examined and they would undergo structural transformation by environmental factors, e.g., sunlight, microorganisms and treatments in sewage treatment plants (STPs)...
2018: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
Masato Takahashi, Tomohiro Ogawa, Hiroshi Kashiwagi, Fumiya Fukushima, Misaki Yoshitsugu, Masami Haba, Masakiyo Hosokawa
It is necessary to consider the affinity of prodrugs for metabolic enzymes for efficient activation of the prodrugs in the body. Although many prodrugs have been synthesized with consideration of these chemical properties, there has been little study on the design of a structure with consideration of biological properties such as substrate recognition ability of metabolic enzymes. In this report, chemical synthesis and evaluation of indomethacin prodrugs metabolically activated by human carboxylesterase 1 (hCES1) are described...
February 21, 2018: Bioorganic & Medicinal Chemistry Letters
Juliana Pavan Zuliani, José María Gutiérrez, Catarina Teixeira
Phagocytosis, a process involved in host defense, requires coordination of a variety of signaling reactions. MT-II, a catalytically-inactive Lys49-PLA2 ¸ and MT-III, an active Asp49-PLA2 isolated from Bothrops asper snake venom, activate phagocytosis in macrophages. In this study the signal pathways mediating zymosan phagocytosis, focusing in lipidic second messengers, were investigated. Macrophages collected from male Swiss mouse peritoneum were obtained 96 h after i.p. injection of thioglycollate. Phagocytosis was evaluated with non-opsonized zymosan in the presence or absence of specific inhibitors...
February 28, 2018: International Journal of Biological Macromolecules
Ines Tofe, Maria Dolores Ruiz-González, Maria Dolores Cañete, Asuncion Pino, Rosa Lorena Rueda, Maria Jose Parraga, Juan Luis Perez-Navero
Background: Standard medical treatment for patent ductus arteriosus (PDA) closure has been indomethacin/ibuprofen or surgical ligation. Up to date, new strategies have been reported with paracetamol. The aim of this study was to present our experience with intravenous paracetamol for closing PDA in preterm neonates presenting contraindication to ibuprofen or ibuprofen had failed and no candidates for surgical ligation because of huge instability. Materials and methods: We conducted a retrospective case series study in a neonatal intensive care unit from a tertiary hospital...
2018: Frontiers in Pediatrics
Kelli Monteiro da Costa, Raphael C Valente, Eduardo J Salustiano, Luciana B Gentile, Leonardo Freire-de-Lima, Lucia Mendonça-Previato, José O Previato
Chagas disease is a neglected disease caused by the protozoan Trypanosoma cruzi and affects 8 million people worldwide. The main chemotherapy is based on benznidazole. The efficacy in the treatment depends on factors such as the parasite strain, which may present different sensitivity to treatment. In this context, the expression of ABC transporters has been related to chemotherapy failure. ABC transporters share a well-conserved ABC domain, responsible for ATP binding and hydrolysis, whose the energy released is coupled to transport of molecules through membranes...
2018: Frontiers in Microbiology
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