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Dieli Oliveira Nunes, Vinicius Bermond Marques, Camila Cruz Pereira Almenara, Wena Dantas Marcarini, Rogério Faustino Ribeiro Júnior, Alessandra Simão Padilha
We aimed to investigate the effect of linoleic acid (LA) treatment on the blood pressure and function of mesenteric resistance arteries (MRA) in spontaneous hypertensive rats (SHR). Male SHR were treated daily with LA (15 mg/kg) or vehicle (control) for 15 days. Compared with controls, LA treatment decreased blood pressure and showed the following in MRA: (1) increased lumen and external diameter, (2) decreased wall:lumen ratio and wall thickness, (3) decreased stiffness and (4) less collagen deposition. LA treatment reduced the contractile response to phenylephrine, although there were no changes observed in MRA in regard to the acetylcholine or sodium nitroprusside responses...
August 17, 2018: Journal of Nutritional Biochemistry
Mahmoud Mostafa, Eman Alaaeldin, Usama Farghaly Aly, Hatem A Sarhan
Thymoquinone, the major constituent of Nigella sativa oil has been found to have a promising topical anti-inflammatory activity; however, exaggerated heat and photo-sensitivity and lipophilicity prevent the best use of this promising product. The present work aimed to formulate an ideal thymoquinone liposomal system for topical delivery. Different liposomal systems were developed using thin film hydration method by applying different cholesterol molar concentrations, different total lipid molar concentrations, and different drug-to-lipid ratios...
September 14, 2018: AAPS PharmSciTech
Yasmine Ben Osman, Tatsiana Liavitskaya, Sergey Vyazovkin
The present study explores the hypothesis that a polymer can affect the thermal stability of a drug in solid polymer-drug dispersions. The hypothesis is tested in a systematic fashion by combining isoconversional kinetic analysis with thermogravimetric measurements on several solid dispersions. Experimental systems involve three drugs: indomethacin (IMC), felodipine (FD), and nifedipine (ND) and their solid dispersions with polyvinylpyrrolidone (PVP). It is found that PVP stabilizes IMC but destabilizes FD and ND...
September 11, 2018: International Journal of Pharmaceutics
Shahnawaz Ahmad Wani, Luqman Ahmad Khan, Seemi Farhat Basir
AIM: To investigate the mechanism of nickel augmented phenylephrine (PE)-induced contraction in isolated segments of Wistar rat aorta. MATERIALS AND METHODS: Effect of varying concentrations of nickel on PE-induced contraction were investigated in isolated segments of Wistar rat aorta using an organ bath system. Aortic rings were pre-incubated with verapamil (1 µM and 20 µM), gadolinium, apocynin, indomethacin or N-G-nitro-L-arginine methyl ester (L-NAME) separately before incubation with nickel...
2018: Journal of Smooth Muscle Research, Nihon Heikatsukin Gakkai Kikanshi
Chen Li, M B Sridhara, K P Rakesh, H K Vivek, H M Manukumar, C S Shantharam, Hua-Li Qin
Hydrazone compounds were considered as a useful moiety in drug design development. Therefore, these studies were aimed at the synthesis of new dihydrazones and were screened for their in vitro H+ /K+ -ATPase and anti-inflammatory activities. The results revealed that compounds 9 (22 ± 0.62 µg/mL), 10 (26 ± 0.91 µg/mL), 15 (24 ± 0.44 µg/mL), 16 (28 ± 0.63 µg/mL), 17 (12 ± 0.38 µg/mL), 18 (14 ± 0.47 µg/mL), 19 (26 ± 0.54 µg/mL), 20 (16 ± 0.41 µg/mL), 25 (06 ± 0...
September 1, 2018: Bioorganic Chemistry
Sahar M Jaffal, Manal A Abbas
Achillea biebersteinii is a perennial aromatic herb that grows in the Mediterranean area. The leaves of this plant are used in foods as bittering and appetizing agents. In folk medicine, it is used for the treatment of stomachache and abdominal pain. In this study, the analgesic effect of A. biebersteinii methanolic flower extract was tested in three pain models, namely: writhing, tail-flick and paw-licking (formalin) tests. A. biebersteinii extract inhibited abdominal cramps produced by acetic acid. The effect of A...
September 8, 2018: Inflammopharmacology
M J Gallardo-Altamirano, P Maza-Márquez, J M Peña-Herrera, B Rodelas, F Osorio, C Pozo
In this study, the removal rates of eight anti-inflammatory and/or analgesic pharmaceuticals, AIAPs (acetaminophen, ibuprofen, naproxen, ketoprofen, diclofenac, codeine, indomethacin and propyphenazone) were assessed in a pilot-scale A2 O system (including anaerobic/anoxic/aerobic zones), long term operated during two experimental phases using different sets of environmental conditions and operating parameters. qPCR was used to quantify the absolute abundances of total Bacteria, total Archaea, mycolic-acid containing filamentous Actinobacteria (Mycolata) and Fungi within the activated sludge microbial community developed in the system...
December 1, 2018: Science of the Total Environment
Tiffany K Rundstadler, Arvin Eskandari, Sarah M Norman, Kogularamanan Suntharalingam
Cancer stem cells (CSCs) are thought of as a clinically pertinent subpopulation of tumors, partly responsible for cancer relapse and metastasis. Research programs aimed at discovering anti-CSC agents have largely focused on biologics and purely organic molecules. Recently, we showed that a family of redox-active copper(II) complexes with phenanthroline-based ligands and nonsteroidal anti-inflammatory drugs (NSAIDs) such as indomethacin, are capable of potently and selectively killing breast CSCs. Herein we present analogous redox-inactive, zinc(II)-phenanthroline-indomethacin complexes with the ability to kill breast CSCs and bulk breast cancer cells with equal potency (in the submicro- or micromolar range)...
September 4, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Jun Wu, Shu-Yun Bi, Xiao-Yue Sun, Rui Zhao, Ji-Hong Wang, Hui-Feng Zhou
The interaction of fisetholz with bovine serum albumin (BSA) and human serum albumin (HSA) was investigated by multi-spectroscopic, cyclic voltammetric and molecular docking technique. The results revealed that there was a static quenching of BSA/HSA induced by fisetholz. The binding constants (Ka ) and binding sites (n) were calculated at different temperatures (293 K, 303 K and 311 K). The enthalpy change (ΔH) were calculated to be -17.20 kJ mol-1 (BSA) and -18.28 kJ mol-1 (HSA) and the entropy change (ΔS) were calculated to be 35...
September 4, 2018: Journal of Biomolecular Structure & Dynamics
Akihito Kiguchiya, Reiko Teraoka, Toshiyasu Sakane
Evaluating the stability of drugs over ranges of various environmental conditions is necessary to ensure the quality of the drug throughout the shelf life. In this study, we used indomethacin, which is well known as a photosensitive drug, and evaluated the photostability of prepared crystals. HPLC analysis revealed that all the indomethacin crystals were degraded by light exposure. However, the indomethacin crystals involving solvates had different degrees of photodegradation and different solid-state UV/Vis spectra...
2018: Chemical & Pharmaceutical Bulletin
Porntip Benjasirimongkol, Keisuke Ueda, Kenjirou Higashi, Pornsak Sriamornsak, Kunikazu Moribe
We examined the effect of hot-melt extrusion condition on the physical stability of the solid dispersion prepared using partially hydrolyzed polyvinyl alcohol (PVOH). The hot-melt extrusion of indomethacin (IMC) and PVOH mixed at the weight ratio of 3 : 7, 5 : 5 and 7 : 3 was performed either at 170 or 190°C to prepare the IMC/PVOH hot-melt extrudate (HME). Differential scanning calorimetry represented that IMC was mixed with PVOH on a scale of several tens of nanometer in all the HMEs with different weight ratio...
2018: Chemical & Pharmaceutical Bulletin
Chaonan Huang, Yun Li, Jiajia Yang, Junyu Peng, Jun Tan, Yun Fan, Longxing Wang, Jiping Chen
This paper describes the poly(divinylbenzene) (PDVB) supported synthesis of quaternized hyperbranched macromolecules (QHMs) and its use as a highly selective, high-capacity mixed-mode anion-exchange (MAX) sorbent. In detail, the aminated PDVB support was firstly synthesized by copolymerization of divinylbenzene and 2-(diethylamino)ethyl methacrylate via Pickering emulsion polymerization. The QHMs were then grafted on PDVB by a divergent synthesis involving consecutive reactions of resorcinol diglycidyl ether with methylamine (N, N-dimethylethanolamine for terminal epoxides), which brought in a high density of quaternary ammonium functionalities...
December 1, 2018: Talanta
Raquel Díaz Ruiz, Virginia Flores Fernández, Jose Antonio Pajares Díaz
Desmoid fibromatosis is a mesenchymal clonal proliferation, which lacks metastatic potential. Nevertheless, it has an infiltrative growth and thus implies a high morbidity1. Although the etiology remains unclear, mutations in the B-catenin or APC genes are involved. Some risk factors include pregnancy, hormonal exposure or surgery. Desmoid fibromatosis can be sporadic (80%) or FAP-associated2. In sporadic cases, it is caused by mutations in the B-catenin (CTNNB1) gene. Whether it is FAP-associated or not should be determined, as the treatment for each condition is different...
August 28, 2018: Revista Española de Enfermedades Digestivas
Shamim Khan, Taous Khan, Abdul Jabbar Shah
BACKGROUND: Calamintha vulgaris L., has been used medicinally in the management hypertension. PURPOSE: To investigate the antihypertensive mechanisms of extract of C. vulgaris L., in Sprague-Dawley (SD) rat. STUDY DESIGN: Total phenol and total flavonoid contents were determined in the crude extract through HPLC. In vivo and in vitro pharmacological approaches were utilized to test the crude extract and fractions of C. vulgaris in Sprague-Dawley (SD) rats...
August 1, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Changxing Qi, Weixi Gao, Jianping Wang, Mengting Liu, Jinwen Zhang, Chunmei Chen, Zhengxi Hu, Yongbo Xue, Dongyan Li, Qing Zhang, Yongji Lai, Qun Zhou, Hucheng Zhu, Yonghui Zhang
Terrusnolides A-D (1-4), four butenolides were isolated from an endophytic Aspergillus from Tripterygium wilfordii. The structures of 1-4 were established by comprehensive spectroscopic analyses and electronic circular dichroism (ECD) calculation. It is interesting that 1 was a butenolide derived by a triple decarboxylation, while 2-4 were the metabolites with 4-benzyl-3-phenyl-5H-furan-2-one motif possessing an isopentene group fused to the benzene ring. In vitro anti-inflammatory effects of these isolates were evaluated in lipopolysaccharide (LPS)-stimulated RAW264...
August 27, 2018: Fitoterapia
Mansi Shah, Meixiang Xu, Poonam Shah, Xiaoming Wang, Shannon M Clark, Maged Costantine, Holly A West, Tatiana N Nanovskaya, Mahmoud S Ahmed, Sherif Z Abdel-Rahman, Raman Venkataramanan, Steve N Caritis, Gary D V Hankins, Erik Rytting
BACKGROUND AND OBJECTIVE: Cytochrome P450 (CYP) 2C9 catalyzes the biotransformation of indomethacin to its inactive metabolite O-desmethylindomethacin (DMI). The aim of this work was to determine the effect of CYP2C9 polymorphisms on indomethacin metabolism in pregnant women. METHODS: Plasma concentrations of indomethacin and DMI at steady state were analyzed with a validated LC-MS/MS method. DNA was isolated from subject blood and buccal smear samples. Subjects were grouped by genotype for comparisons of pharmacokinetic parameters...
August 29, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Lisa W Howley, Debnath Chatterjee, Sonali S Patel, Bettina F Cuneo, Timothy M Crombleholme, Nicholas Behrendt, Michael V Zaretsky, Ahmed I Marwan, Jeannie Zuk, Henry L Galan, Cristina Wood
INTRODUCTION: The use of perioperative tocolytic agents in fetal surgery is imperative to prevent preterm labor. Indomethacin, a well-known tocolytic agent, can cause ductus arteriosus (DA) constriction. We sought to determine whether a relationship exists between preoperative indomethacin dosing and fetal DA constriction. MATERIALS AND METHODS: This is an IRB-approved, single-center retrospective observational case series of 42 pregnant mothers who underwent open fetal myelomeningocele repair...
August 29, 2018: Fetal Diagnosis and Therapy
Md Mohaimenul Islam, Tahmina Nasrin Poly, Bruno Andreas Walther, Hsuan-Chia Yang, Ming-Chin Lin, Yu-Chuan Li
BACKGROUND AND AIM: Nonsteroidal anti-inflammatory drugs (NSAIDs) are one of the most common pain relief medications, but the risk of hemorrhagic stroke in patients taking these medications is unclear. In this study, our aim was to systematically review, synthesize, and critique the epidemiological studies that evaluate the association between NSAIDs and hemorrhagic stroke risk. We therefore assessed the current state of knowledge, filling the gaps in our existing concern, and make a recommendation for future research...
August 28, 2018: Neuroepidemiology
Licia Grazzi, Eleonora Grignani, Domenico D'Amico, Emanuela Sansone, Alberto Raggi
PURPOSE OF REVIEW: The aim is twofold. First, to give an insight on the role exerted by different classes of drugs in favouring migraine chronification. Second, to explore the relationship between type and amount of overused medications and history of previous withdrawal treatment and of frequent relapses. RECENT FINDINGS: All drug classes were found to favour migraine chronification. No data are available for the association with relapses into CM-MOH. Our clinical study shows that patients who underwent previous withdrawal treatments were more likely to be overusers of multiple drug classes and overuse higher amounts of symptomatic medications, particularly, indomethacin, eletriptan and tramadol...
August 27, 2018: Current Pain and Headache Reports
Patrycja Garbacz, Marek Wesolowski
Co-crystals have garnered increasing interest in recent years as a beneficial approach to improving the solubility of poorly water soluble active pharmaceutical ingredients (APIs). However, their preparation is a challenge that requires a simple approach towards co-crystal detection. The objective of this work was, therefore, to verify to what extent a multivariate statistical approach such as principal component analysis (PCA) and cluster analysis (CA) can be used as a supporting tool for detecting co-crystal formation...
August 24, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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