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Na Fan, Rongzheng Liu, Pingping Ma, Xin Wang, Chang Li, Jing Li
In the current stage, the On-Off mechanism of chiral mesoporous silica nanoparticles (CMSN) for delivering achiral drug in chiral environment has rarely been reported. Herein, On-Off chiral mesoporous silica nanoparticles (On-Off-D-CMSN and On-Off-L-CMSN) were successfully synthesized and its particular contribution in delivering achiral drug indometacin (IMC) in chiral environment was mainly studied. The as-synthesized On-Off-D-CMSN and On-Off-L-CMSN were verified by fourier transform infrared spectrometer and circular dichroism...
December 26, 2018: Colloids and Surfaces. B, Biointerfaces
Jiuxia Yang, Bo Wang, Lu Ge, Xiaotian Yang, Xiangxiang Wang, Yixin Dai, Baolong Niu, Haijin Xu, Mingqiang Qiao
HGFI (hydrophobin found in Grifola frondosa) is a small surface-active protein, belonging to class I hydrophobins, and can form amphipathic protein films at hydrophobic- hydrophilic material interfaces. HGFI has a low isoelectric point (pI) because no basic amino acids are present in its sequence. Here we constructed two HGFI mutants using a site-directed mutation method. The two mutants were named MGF3 (E24K/D35K/D37K) and MGF6 (E12K/D19K/E24K/D35K/D37K/D66K). MGF3 was generated by replacing three acidic amino acids, namely Glu24, Asp35 and Asp37, with the basic amino acid Lys...
December 18, 2018: Colloids and Surfaces. B, Biointerfaces
Jiri Mikusek, Jeremy Nugent, Ping Lan, Martin G Banwell
A total synthesis of compound 3 from p-bromophenol is reported and thereby establishing that this, rather than its cyclodehydrated counterpart 1 (as postulated originally), is the correct structure of the natural product myrsinoic acid F. The biological evaluation of compound 3 in a mouse-ear edema assay established that it is a significantly more potent anti-inflammatory agent than the NSAID indometacin.
December 27, 2018: Journal of Natural Products
Tzu-Min Lin, Jia-En Chi, Chi-Ching Chang, Yi-No Kang
Background: Gout, a common medical condition that causes pain, can be treated by painkillers and anti-inflammatories. Indometacin and etoricoxib are two such drugs. However, no synthesized evidence exists comparing etoricoxib with indometacin in treating patients with gout. Methods: We searched PubMed, Embase, Ovid MEDLINE, Web of Science, ScienceDirect, and the Cochrane Library without restrictions on language or publication date for potential randomized clinical trials comparing etoricoxib with indometacin for gout...
2019: Journal of Pain Research
Nadiia I Gumerova, Amir Blazevic, Tania Caldera Fraile, Alexander Roller, Gerald Giester, Annette Rompel
The single-side Al-centred tris-functionalized hybrid organic-inorganic Anderson polyoxomolybdates (C16 H36 N)3 [Al(OH)3 Mo6 O18 (OCH2 )3 CNH(C10 H8 O)]·C9 H7 N·4CH3 OH·5H2 O (AlMo6 -NH-Cin; Cin is cinnamic acid, C10 H9 O2 ) and (C16 H36 N)3 [Al(OH)3 Mo6 O18 (OCH2 )3 CNH(C19 H15 ClNO3 )]·9H2 O (AlMo6 -NH-Indo; Indo is indometacin, C19 H16 ClNO4 ) have been prepared in a mild three-step synthesis and structurally characterized by single-crystal X-ray diffraction, 1 H NMR and IR spectroscopies and elemental analysis...
November 1, 2018: Acta Crystallographica. Section C, Structural Chemistry
Gwen M C Masclee, Huub Straatman, Andrea Arfè, Jordi Castellsague, Edeltraut Garbe, Ron Herings, Bianca Kollhorst, Silvia Lucchi, Susana Perez-Gutthann, Silvana Romio, René Schade, Tania Schink, Martijn J Schuemie, Lorenza Scotti, Cristina Varas-Lorenzo, Vera E Valkhoff, Marco Villa, Miriam C J M Sturkenboom
BACKGROUND: Use of selective COX-2 non-steroidal anti-inflammatory drugs (NSAIDs) (coxibs) has been associated with an increased risk of acute myocardial infarction (AMI). However, the risk of AMI has only been studied for very few NSAIDs that are frequently used. OBJECTIVES: To estimate the risk of AMI for individual NSAIDs. METHODS: A nested case-control study was performed from a cohort of new NSAID users ≥18 years (1999-2011) matching cases to a maximum of 100 controls on database, sex, age, and calendar time...
2018: PloS One
Yan Fu, Huan-Qing Wu, Huai-Liang Cui, Yue-Yun Li, Chang-Zheng Li
Oxymatrine (OXY) has antioxidative and antiinflammatory activities. In the present work, we investigate the effects of OXY on gastric ulcer models and elucidate the underlying mechanisms of action. Ethanol, indometacin, and restraint water immersion stress-induced ulcerated models were used. The ulcer area was measured, and samples of gastric tissue were taken for pathological, histochemical, and biochemical analyses. OXY effectively reduced the area of gastric ulcers and improved the pathological changes of ulcerated tissue...
October 2018: Phytotherapy Research: PTR
Hai-Dong Xia, Yan-Dong Zhang, Yan-Hui Wang, Chi Zhang
A readily accessible and bench-stable water-soluble hypervalent iodine(III) reagent ( phenyl iodonio) sulfam ate (PISA) with an I-N bond was synthesized, and its structure was characterized by X-ray crystallography. With PISA, various indoles were synthesized via C-H amination of 2-alkenylanilines involving an aryl migration/intramolecular cyclization cascade with excellent regioselectivity in aqueous CH3 CN. Notably, using this new method as the key step, not only two drug molecules, indometacin and zidometacin, but also another bioactive molecule, pravadoline, were synthesized...
July 6, 2018: Organic Letters
Jiri Mikusek, Jeremy Nugent, Jas S Ward, Brett D Schwartz, Alison D Findlay, Jonathan S Foot, Martin G Banwell
The synthesis of the structure, 1, assigned to the anti-inflammatory natural product myrsinoic acid F is reported together with a means for preparing its Z-isomer 21. While neither of these compounds corresponds to the natural product, both of them are anti-inflammatory agents (as determined using a mouse ear edema assay) with congener 1 being notably more potent than the widely prescribed NSAID indometacin.
July 6, 2018: Organic Letters
Ozlem Akgul, Lorenzo Di Cesare Mannelli, Daniela Vullo, Andrea Angeli, Carla Ghelardini, Gianluca Bartolucci, Abdulmalik Saleh Alfawaz Altamimi, Andrea Scozzafava, Claudiu T Supuran, Fabrizio Carta
Herein we report the design as well as the synthesis of a new series of dual hybrid compounds consisting of the therapeutically used nonsteroidal-anti-inflammatory drugs (NSAIDs; i.e., indometacin, sulindac, ketoprofen, ibuprofen, diclofenac, ketorolac, etc., cyclooxygenase inhibitors) and the carbonic anhydrase inhibitor (CAIs) fragments of the sulfonamide type. Such compounds are proposed as new tools for the management of ache symptoms associated with rheumatoid arthritis (RA) and related inflammation diseases...
June 14, 2018: Journal of Medicinal Chemistry
Fouad Chraibi, Idriss Andaloussi Benatiya
No abstract text is available yet for this article.
2018: Pan African Medical Journal
Liankang Sun, Ke Chen, Zhengdong Jiang, Xin Chen, Jiguang Ma, Qingyong Ma, Wanxing Duan
Increasing evidence indicates that pancreatic stellate cells (PSCs) are responsible for the stromal reaction in pancreatic ductal adenocarcinoma (PDAC). The interaction between activated PSCs and PDAC cells and the resultant stromal reaction facilitate cancer progression. Previous findings suggested that cyclooxygenase‑2 (COX‑2) may have a profound role in regulating the proliferation and activation of PSCs in response to pancreatic cancer. Indometacin, a well‑known anti‑inflammatory drug and a non‑selective inhibitor of COX‑2, has been shown to exert anticancer effects in various types of cancer, including PDAC...
May 2018: Oncology Reports
L A Dowd, B J Wheeler, H S Al-Sallami, R S Broadbent, L K Edmonds, N J Medlicott
AIM: To describe the current clinical practices and attitudes of neonatologists towards paracetamol treatment of PDA in Australia (AU) and New Zealand (NZ). METHOD: A web-based survey of all neonatologists registered under the 2017 Australia New Zealand Neonatal Network (ANZNN) was conducted. RESULTS: The response rate for the survey was 67%, (141/210). Of those respondents, 37% stated their unit had a written policy outlining how to treat patent ductus arteriosus (PDA)...
April 3, 2018: Journal of Maternal-fetal & Neonatal Medicine
Sina Andalib, Pezhman Molhemazar, Hossein Danafar
Statins have been shown to exert 'pleiotropic effects' independent of their cholesterol lowering actions that include anti-inflammatory properties. In this study we synthesized mono methoxy poly (ethylene glycol)-poly (ε-caprolactone) (mPEG-PCL) di block copolymers. The structure of the copolymers was characterized by H nuclear magnetic resonance, Fourier-transform infrared spectroscopy, differential scanning calorimetry and gel permeation chromatography techniques. In this method, atorvastatin was encapsulated within micelles through a single-step nano-precipitation method, leading to the formation of atorvastatin-loaded mPEG-PCL (atorvastatin/mPEG-PCL) micelles...
March 2018: Journal of Biomaterials Applications
Chaodan Luo, Hanbin Chen, Yongfu Wang, Guosheng Lin, Cailan Li, Lihua Tan, Ziren Su, Xiaoping Lai, Jianhui Xie, Huifang Zeng
AIMS: The aim of this study was to comparatively investigate the potential gastroprotective effect and underlying mechanisms of coptisine free base (CFB, 8-hydroxy-7, 8-dihydrocoptisine), berberine and lansoprazole against indomethacin-induced gastric ulcer in rats. MATERIALS AND METHODS: CFB (10, 20 and 40mg/kg), berberine (20mg/kg) and lansoprazole (30mg/kg) were orally administrated to rats prior to indometacin ingestion, and gastric lesions were evaluated macroscopically and histologically, and further analyzed by ELISA, qRT-PCR and Western blot...
January 15, 2018: Life Sciences
Hesham M Tawfeek, Ahmed A H Abdellatif, Thomas J Dennison, Afzal R Mohammed, Younis Sadiq, Imran Y Saleem
The aim of this work was to investigate the efficient targeting and delivery of indometacin (IND), as a model anti-inflammatory drug to the colon for treatment of inflammatory bowel disease. We prepared fast disintegrating tablets (FDT) containing IND encapsulated within poly(glycerol-adipate-co-ɷ-pentadecalactone), PGA-co-PDL, microparticles and coated with Eudragit L100-55 at different ratios (1:1.5, 1:1, 1:0.5). Microparticles encapsulated with IND were prepared using an o/w single emulsion solvent evaporation technique and coated with Eudragit L-100-55 via spray drying...
October 5, 2017: International Journal of Pharmaceutics
Zhijian Yao, Qingqing Zhao, Yan Ma, Wei Wang, Qing Zhou, Aimin Li
In this research a new magnetic material called M88 was fully synthetized and characterized for the extraction of pharmaceutical and personal care products in water samples. In addition, a portable prototype of magnetic solidphase extraction (MSPE) device was developed for the onsite preconcentration. The MSPE coupling with high performance liquid chromatography-Diode array detector (HPLC-DAD) method was developed and validated for simultaneous analysis of 11 PPCPs (mefenamic acid, chloroamphenicol, ketoprofen, clofibric acid, indometacin, acetylsalicylic acid, bisphenol A, phenylphenol, gemfibrozil, triclosan, and ibuprofen) in environmental water samples...
August 14, 2017: Scientific Reports
Jing Li, Yingyu Guo, Heran Li, Lei Shang, Sanming Li
The present study established indometacin (IMC) delivery system with chiral mesoporous silica nanoparticles (CMSNs) and amino-modified chiral mesoporous silica nanoparticles (Amino-CMSNs) that previously reported as pharmaceutical excipients, and their systemic biological effects, mainly consisting of in vitro drug intestinal permeability, haemolysis assay, in vivo pharmacokinetics, anti-inflammation pharmacodynamics and gastric irritation, were addressed. It turned out that the two IMC delivery systems established by CMSN and Amino-CMSN significantly improved drug intestinal permeability due to the improved drug dissolution caused by conversion of drug crystalline state to amorphous phase...
August 2018: Artificial Cells, Nanomedicine, and Biotechnology
Min He, Qian Wang, Zhenqiang Shi, Yi Xie, Weifeng Zhao, Changsheng Zhao
Heterotopic ossification(HO) is a potential severe complication after many biomaterial implanting surgeries, and the inflammation environment caused by the implanting-associated infections is considered as the main nosogenesis. Herein, an inflammation-responsive drug release system was designed by chemically conjugating indometacin (via ester group) onto hydrogel coating to realize local self-regulated drug release to prevent HO. In our strategy, poly(3-mercaptopropyl)trimethoxysilane-co-acrylic acrylate and polyvinyl alcohol (providing anchoring sites for drug molecules) were firstly synthesized and functionalized with ene-groups, then a hydrogel layer was formed and covalently attached onto thiol-modified substrate via thiol-ene click chemistry, followed by grafting indometacin...
October 1, 2017: Colloids and Surfaces. B, Biointerfaces
Chao Chen, Binbin Wang
This study was conducted to evaluate the efficacy and possible mechanism of Brucea javanica oil emulsion (BJOE) on cachexia, by observing changes in related indexes in mice with cachexia and identifying the genes responsible based on gene chip analysis. In the BJOE treatment group, body weight loss, tumour growth and metastasis were found obviously inhibited, food and water intake had markedly increased, and survival time was significantly prolonged, as compared to the control group. Moreover, the BJOE witnessed improvement in body weight, prevention of tumour metastasis and overall increase in survival time, as compared to Indometacin (IND, the positive control medicine)...
March 2018: Journal of Drug Targeting
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