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https://www.readbyqxmd.com/read/28934138/inhibitory-effects-of-culinary-herbs-and-spices-on-the-growth-of-hca-7-colorectal-cancer-cells-and-their-cox-2-expression
#1
Andrius Jaksevicius, Mark Carew, Calli Mistry, Helmout Modjtahedi, Elizabeth I Opara
It is unclear if the anti-inflammatory properties of culinary herbs and spices (CHS) are linked to their ability to inhibit Colorectal cancer cell (CRC) growth. Furthermore, their therapeutic potential with regards to CRC is unknown. The aim of this study was to establish if the inhibition of HCA-7 CRC cell growth by a selection of culinary herbs and spices (CHS) is linked to the inhibition of the cells' cyclooxygenase-2 (COX-2 )expression, and to investigate their therapeutic potential. CHS inhibited the growth of Human colon adenocarcinoma-7 (HCA-7) cells; the order of potency was turmeric, bay leaf, ginger, sage, and rosemary; their combinations had a synergistic or additive effect on cell growth inhibition...
September 21, 2017: Nutrients
https://www.readbyqxmd.com/read/28929561/one-pot-three-component-sulfonimidamide-synthesis-exploiting-the-sulfinylamine-reagent-n-sulfinyltritylamine-trnso
#2
Thomas Q Davies, Adrian Hall, Michael C Willis
Sulfonimidamides are increasingly important molecules in medicinal chemistry and agrochemistry, but their preparation requires lengthy synthetic sequences, which has likely limited their use. We describe a one-pot de novo synthesis of sulfonimidamides from widely available organometallic reagents and amines. This convenient and efficient process uses a stable sulfinylamine reagent, N-sulfinyltritylamine (TrNSO), available in one step on 10 gram scale, as a linchpin. In contrast to classical approaches starting from thiols or their derivatives, our TrNSO-based approach facilitates the rapid assembly of the three reaction components into a variety of differentially substituted sulfonimidamides containing medicinally relevant moieties, including pyridines and indoles...
September 19, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28922386/new-carboxamide-derivatives-bearing-benzenesulphonamide-as-a-selective-cox-ii-inhibitor-design-synthesis-and-structure-activity-relationship
#3
David Izuchukwu Ugwu, Uchechukwu Chris Okoro, Hilal Ahmad
Sixteen new carboxamide derivatives bearing substituted benzenesulphonamide moiety (7a-p) were synthesized by boric acid mediated amidation of appropriate benzenesulphonamide with 2-amino-4-picoline and tested for anti-inflammatory activity. One compound 7c showed more potent anti-inflammatory activity than celecoxib at 3 h in carrageenan-induced rat paw edema bioassay. Compounds 7g and 7k also showed good anti-inflammatory activity comparable to celecoxib. Compound 7c appeared selectivity index (COX-2/COX-1) better than celecoxib...
2017: PloS One
https://www.readbyqxmd.com/read/28921415/comparing-the-safety-and-efficacy-of-celecoxib-for-the-treatment-of-osteoarthritis-in-asian-and-non-asian-populations-an-analysis-of-data-from-two-randomized-double-blind-placebo-controlled-active-comparator-trials
#4
Andri Lubis, Wei Wang, Graça Lima, Rana Fayyad, Chris Walker
INTRODUCTION: Celecoxib is an effective treatment for pain associated with osteoarthritis. There are differences in patient demographics among ethnic groups, with Asian populations typically smaller in body size. As a consequence, there may be a perception that celecoxib is less effective, or has poorer tolerability in Asian patients. METHODS: This analysis compares data from two multicenter, randomized, double-blind, placebo-controlled, active-comparator trials of celecoxib for the treatment of osteoarthritis of the knee: one study in Asian patients and the other in a mixed population comprised mostly of non-Asian patients (from which Asian patients were excluded for this analysis)...
September 18, 2017: Pain and Therapy
https://www.readbyqxmd.com/read/28919798/comparative-effects-of-the-%C3%AF-3-polyunsaturated-fatty-acid-derivatives-resolvins-e1-and-d1-and-protectin-dx-in-models-of-inflammation-and-pain
#5
Flávia Cs Fonseca, Ricardo M Orlando, Regina Mm Turchetti-Maia, Janetti Nogueira de Francischi
PURPOSE: Specialized pro-resolving lipid mediators (SPMs), also known as lipoxins, resolvins (Rvs), protectins and maresins, have been implicated in the resolution of the inflammatory process. However, a systematic comparison of their activity in the relief of inflammation and pain models is still lacking. MATERIALS AND METHODS: The effects of Rvs E1 and D1 and protectin DX (PDX) were assessed in rat paws inflamed by the standard proinflammatory stimulus carrageenan or by histamine, 5-hydroxytryptamine, substance P or prostaglandin E2...
2017: Journal of Inflammation Research
https://www.readbyqxmd.com/read/28906164/comparative-pharmacokinetics-study-of-anastrozole-after-single-administration-and-combination-with-celecoxib
#6
Xiaoyang Sun, Mingming Lv, Binjie Wang, Simin Zhao, Ping Guo, Shixiao Wang, Liqiang Gu, Xiaohui Chen
1. There are numerous investigations demonstrating that the cyclooxygenase-2 (COX-2) inhibitors might enhance the efficiency of anastrozole in breast cancer. Hence, this study was conducted to investigate the comparative pharmacokinetics of anastrozole after single administration and combination with celecoxib. 2. A simple protein precipitation procedure was adopted for the sample preparation with satisfactory extraction recovery for both anastrozole and the internal standard, and then anastrozole was separated and analysed on an ACQUITY BEH UPLC C18 column (50 × 2...
September 14, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28901847/micrornas-to-monitor-pain-migraine-and-drug-treatment
#7
Luca Gallelli, Erika Cione, Maria Cristina Caroleo, Marco Carotenuto, Pasqualina Lagana, Antonio Siniscalchi, Vincenzo Guidetti
Migraine is a prevalent neurovascular disorders with a complex pathophysiology and therapeutic options characterized by important side effects or problems related to drug abuse. No specific biomarkers are recognized to be univocal for this subclinical condition, yet. In this concern microRNAs have been suggested as potentially useful screening/diagnostic tool, and research is underway to recognize the most effective candidate(s). microRNAs, able to regulate immune and neuronal processes are herein reported for both, mice models with multiple induced pain conditions and human subjects...
September 12, 2017: MicroRNA
https://www.readbyqxmd.com/read/28888220/pharmacokinetics-of-multiple-doses-of-co-crystal-of-tramadol-celecoxib-findings-from-a-4-way-randomized-open-label-phase-i-clinical-trial
#8
Sebastián Videla, Mounia Lahjou, Anna Vaqué, Mariano Sust, Marisol Escriche, Lluis Soler, Artur Sans, Eric Sicard, Neus Gascón, Gregorio Encina, Carlos Plata-Salamán
AIM: We compared the pharmacokinetic (PK) profiles of Co-Crystal of Tramadol-Celecoxib (CTC) versus each reference product (alone and in open combination) after single (first dose) and multiple dosing. METHODS: Healthy adults aged 18-50 years received, under fasted conditions, 15 twice-daily doses of the following treatments (separated by ≥14-day wash-out): 200 mg immediate-release (IR) CTC (equivalent to 88 mg tramadol and 112 mg celecoxib; Treatment-1); 100 mg IR tramadol (Treatment-2), 100 mg celecoxib (Treatment-3); and 100 mg IR tramadol and 100 mg celecoxib (Treatment-4)...
September 9, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28882733/-risk-of-fatal-non-fatal-events-in-patients-with-previous-coronary-heart-disease-acute-myocardial-infarction-and-treatment-with-non-steroidal-anti-inflammatory-drugs
#9
REVIEW
L Muñoz Olmo, J Juan Armas, J J Gomariz García
BACKGROUND: Primary Care is the fundamental axis of our health system and obliges us to be consistent with our prescriptions. The non-steroidal anti-inflammatory drugs (NSAIDs) have been associated with increased cardiovascular risk and increased risk of all causes of death, as well as acute myocardial infarction (AMI) in patients with a previous myocardial infarction. Pain and cardiac patient management are 2 basic pillars in our daily activity, and we must know the limitations of NSAIDs in patients with established cardiovascular risk...
September 4, 2017: Semergen
https://www.readbyqxmd.com/read/28881683/inhibition-of-cox2-enhances-the-chemosensitivity-of-dichloroacetate-in-cervical-cancer-cells
#10
Bo Li, Xinzhe Li, Haojun Xiong, Peng Zhou, Zhenhong Ni, Teng Yang, Yan Zhang, Yijun Zeng, Jintao He, Fan Yang, Nan Zhang, Yuting Wang, Yingru Zheng, Fengtian He
Dichloroacetate (DCA), a traditional mitochondria-targeting agent, has shown promising prospect as a sensitizer in fighting against malignancies including cervical cancer. But it is unclear about the effect of DCA alone on cervical tumor. Moreover, previous reports have demonstrated that the increased cyclooxygenase-2 (COX2) expression is associated with chemoresistance and poor prognosis of cervical cancer. However, it is still unknown whether COX2 can affect the sensitivity of DCA in cervical cancer cells...
August 1, 2017: Oncotarget
https://www.readbyqxmd.com/read/28881160/effective-treatment-of-aggressive-fibromatosis-with-celecoxib-guided-by-genetic-testing
#11
Shanshan Yang, Xufu Wang, Haiping Jiang, Yongjie Wang, Zhuokun Li, Haijun Lu
Aggressive fibromatosis (AF) or desmoid tumors is an aggressive fibroblastic proliferation which is locally invasive but can not metastasize. The treatment of AF is challenging. Surgery was the main treatment modality for AF in the past, other strategies including radiotherapy, systemic therapies and wait-and-see policy. The use of non-steroidal anti-inflammatory drugs (NSAIDs) and targeted therapies has demonstrated good results. In the case report, a 39-year-old man presented with progressive chest wall pain...
September 7, 2017: Cancer Biology & Therapy
https://www.readbyqxmd.com/read/28865485/combination-therapy-of-pkc%C3%AE-and-cox-2-inhibitors-synergistically-suppress-melanoma-metastasis
#12
Ping Zhou, Jiaqi Qin, Yuan Li, Guoxia Li, Yinsong Wang, Ning Zhang, Peng Chen, Chunyu Li
BACKGROUND: Metastatic malignant melanoma is one of the most aggressive malignancies and its treatment remains challenging. Recent studies demonstrate that the melanoma metastasis has correlations with the heightened activations of protein kinase C ζ (PKCζ) and cyclooxygenase-2 (COX-2) signaling pathways. Targeted inhibitions for PKCζ and COX-2 have been considered as the promising strategies for the treatment of melanoma metastasis. Thus, the PKCζ inhibitor J-4 and COX-2 inhibitor Celecoxib were combined to treat melanoma metastasis in this study...
September 2, 2017: Journal of Experimental & Clinical Cancer Research: CR
https://www.readbyqxmd.com/read/28865292/pyrazole-hydrazone-derivatives-as-anti-inflammatory-agents-design-synthesis-biological-evaluation-cox-1-2-5-lox-inhibition-and-docking-study
#13
Mohamed A Abdelgawad, Madlen B Labib, Mahmoud Abdel-Latif
A new series of pyrazole-hydrazone derivatives 4a-i were designed and synthesized, their chemical structures were confirmed by IR, (1)H NMR, (13)C NMR, MS spectral data and elemental analysis. IC50 values for all prepared compounds to inhibit COX-1, COX-2 and 5-LOX enzymes were determined in vitro. Compounds 4a (IC50=0.67μM) and 4b (IC50=0.58μM) showed better COX-2 inhibitory activity than celecoxib (IC50=0.87μM) with selectivity index (SI=8.41, 10.55 in sequent) relative to celecoxib (SI=8.85). Also, compound 4a and 4b exhibited superior inhibitory activity against 5-LOX (IC50=1...
August 30, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28865290/erythrocyte-membrane-encapsulated-celecoxib-improves-the-cognitive-decline-of-alzheimer-s-disease-by-concurrently-inducing-neurogenesis-and-reducing-apoptosis-in-app-ps1-transgenic-mice
#14
Jing-Wen Guo, Pei-Pei Guan, Wei-Yan Ding, Si-Ling Wang, Xue-Shi Huang, Zhan-You Wang, Pu Wang
Alzheimer's disease (AD) is characterized by the loss of neurogenesis and excessive induction of apoptosis. The induction of neurogenesis and inhibition of apoptosis may be a promising therapeutic approach to combating the disease. Celecoxib (CB), a cyclooxygenase-2 specific inhibitor, could offer neuroprotection. Specifically, the CB-encapsulated erythrocyte membranes (CB-RBCMs) sustained the release of CB over a period of 72 h in vitro and exhibited high brain biodistribution efficiency following intranasal administration, which resulted in the clearance of aggregated β-amyloid proteins (Aβ) in neurons...
July 14, 2017: Biomaterials
https://www.readbyqxmd.com/read/28865237/dose-dependent-acute-liver-injury-with-hypersensitivity-features-in-humans-due-to-a-novel-microsomal-prostaglandin-e-synthase-1-inhibitor
#15
Yan Jin, Arie Regev, Jeanelle Kam, Krista Phipps, Claire Smith, Judith Henck, Kristina Campanale, Leijun Hu, D Greg Hall, Xiao Yan Yang, Masako Nakano, Terry Ann McNearney, Jack Uetrecht, William Landschulz
AIM: LY3031207, a novel microsomal prostaglandin E synthase 1 inhibitor, was evaluated in a multiple ascending dose study after nonclinical toxicology studies and a single ascending dose study demonstrated an acceptable toxicity, safety, and tolerability profile. METHODS: Healthy subjects were randomised to receive LY3031207 (25, 75, and 275 mg), placebo, or celecoxib (400 mg) once daily for 28 days. The safety, tolerability, and pharmacokinetic and pharmacodynamic profiles of LY3031207 were evaluated...
September 2, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28857461/ly3127760-a-selective-prostaglandin-e4-ep4-receptor-antagonist-and-celecoxib-a-comparison-of-pharmacological-profiles
#16
Yan Jin, Claire Smith, Leijun Hu, David E Coutant, Kelly Whitehurst, Krista Phipps, Terry Ann McNearney, Xiao Yang, Bradley Ackermann, Thomas Pottanat, William Landschulz
Safety, tolerability, and pharmacology profiles of LY3127760, an EP4 antagonist, were explored in healthy subjects in a subject/investigator-blind, parallel-group, multiple-ascending dose study. Cohorts consisted of 13 patients randomized to LY3127760, celecoxib (400 mg), or placebo (9:2:2 ratio) for 28 days. LY3127760 was well tolerated; the most commonly observed adverse events were gastrointestinal, similar to celecoxib. LY3127760 increased release of ex vivo tumor necrosis factor alpha after lipopolysaccharide/prostaglandin E2 stimulation when compared with placebo, suggesting a dose-dependent blockade of the EP4 receptor...
August 30, 2017: Clinical and Translational Science
https://www.readbyqxmd.com/read/28855534/celecoxib-normalizes-the-tumor-microenvironment-and-enhances-small-nanotherapeutics-delivery-to-a549-tumors-in-nude-mice
#17
Bo Zhang, Kai Jin, Ting Jiang, Lanting Wang, Shun Shen, Zimiao Luo, Yanyan Tuo, Xianping Liu, Yu Hu, Zhiqing Pang
Barriers presented by the tumor microenvironment including the abnormal tumor vasculature and interstitial matrix invariably lead to heterogeneous distribution of nanotherapeutics. Inspired by the close association between cyclooxygenase-2 (COX-2) and tumor-associated angiogenesis, as well as tumor matrix formation, we proposed that tumor microenvironment normalization by COX-2 inhibitors might improve the distribution and efficacy of nanotherapeutics for solid tumors. The present study represents the first time that celecoxib, a special COX-2 inhibitor widely used in clinics, was explored to normalize the tumor microenvironment and to improve tumor nanotherapeutics delivery using a human-derived A549 tumor xenograft as the solid tumor model...
August 30, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28851954/interleukin-6-tumor-necrosis-factor-alpha-and-receptor-activator-of-nuclear-factor-kappa-ligand-are-elevated-in-hypertrophic-gastric-mucosa-of-pachydermoperiostosis
#18
Hui Huang, Yongjun Wang, Yong Cao, Boda Wu, Yonggui Li, Liangliang Fan, Zhiping Tan, Yi Jiang, Jianguang Tang, Jianzhong Hu, Xiaoliu Shi
Pachydermoperiostosis (PDP) is a rare inherited multisystem disease characterized with digital clubbing, pachydermia and periostosis. Variants in either HPGD or SLCO2A1 that interrupt the prostaglandin E2 (PGE2) pathway have been shown to be involved in PDP. Here, in addition to six confirmed variants in HPGD or SLCO2A1, we identified four novel SLCO2A1 variants in eight PDP patients from seven Chinese Han families. In addition, gastric mucosa hyperplasia was observed in all affected individuals and interleukin-6 (IL-6), tumor necrosis factor-alpha (TNFα) and receptor activator of nuclear factor kappa ligand (RANKL) expression were elevated in hypertrophic gastric mucosa...
August 29, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28851389/immunohistochemical-staining-with-non-phospho-%C3%AE-catenin-as-a-diagnostic-and-prognostic-tool-of-cox-2-inhibitor-therapy-for-patients-with-extra-peritoneal-desmoid-type-fibromatosis
#19
Tomohisa Sakai, Yoshihiro Nishida, Shunsuke Hamada, Hiroshi Koike, Kunihiro Ikuta, Takehiro Ota, Naoki Ishiguro
BACKGROUND: Immunohistochemical staining with conventional anti-β-catenin antibody has been applied as a diagnostic tool for desmoid-type fibromatosis (DF). This study aimed to evaluate the diagnostic and prognostic value of immunohistochemical staining with anti-non-phospho β-catenin antibody, which might more accurately reflect the aggressiveness of DF, in comparison to the conventional anti-β-catenin antibody. METHODS: Between 2003 and 2015, 40 patients with extra-peritoneal sporadic DF were prospectively treated with meloxicam or celecoxib, a COX-2 inhibitor, therapy...
August 29, 2017: Diagnostic Pathology
https://www.readbyqxmd.com/read/28843794/photochemical-thermal-biological-and-long-term-degradation-of-celecoxib-in-river-water-degradation-products-and-adsorption-to-sediment
#20
Juan J Jiménez, Rafael Pardo, María I Sánchez, Beatriz E Muñoz
Celecoxib is an anti-inflammatory drug with antibacterial activity whose fate in surface water is unknown. Thus, some assays have been conducted under forced biological, photochemical and thermal conditions, and non-forced conditions, to establish its persistence and degradation products in river water. The results suggest that celecoxib dissolved in river water is not biologically degraded while it is minimally altered after its exposure to sunlight or high temperature (70°C). Only the irradiation at 254nm promotes its complete degradation...
August 19, 2017: Journal of Hazardous Materials
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