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https://www.readbyqxmd.com/read/29475165/non-acidic-1-3-4-trisubstituted-pyrazole-derivatives-as-lonazolac-analogs-with-promising-cox-2-selectivity-anti-inflammatory-activity-and-gastric-safety-profile
#1
Khaled R A Abdellatif, Wael A A Fadaly, Yaseen A M M Elshaier, Waleed A M Ali, Gehan M Kamel
Twelve new compounds of 1,3,4-trisubstituted-pyrazole derivatives possessing two cyclooxygenase-2 (COX-2) pharmacophoric moieties (SO2 Me or/and SO2 NH2 ) 11a-c, 12a-c, 13a-c and 14a-c were designed and synthesized to be evaluated for their COX inhibition, anti-inflammatory activity, ulcerogenic liability. All compounds were more selective for COX-2 isozyme and showed good in vivo anti-inflammatory activity. The bisaminosulphonyl derivatives (14a-c) were the most COX-2 selective compounds (S.I. = 9.87, 9...
February 16, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29473125/sulforaphane-attenuated-the-pro-inflammatory-state-induced-by-hydrogen-peroxide-in-sh-sy5y-cells-through-the-nrf2-ho-1-signaling-pathway
#2
Marcos Roberto de Oliveira, Flávia Bittencourt Brasil, Cristina Ribas Fürstenau
Sulforaphane (SFN), an isothiocyanate obtained from cruciferous vegetables, exerts antioxidant, antiapoptotic, and antitumor activities in different cell types. Moreover, SFN has been viewed as an anti-inflammatory agent. Nonetheless, the mechanism underlying the ability of SFN in modulating the immune response in mammalian cells is not completely understood yet. Therefore, we investigated here whether and how SFN would be effective in preventing inflammation induced by a pro-oxidant agent (hydrogen peroxide, H2 O2 ) in the human neuroblastoma SH-SY5Y cells...
February 23, 2018: Neurotoxicity Research
https://www.readbyqxmd.com/read/29473075/monascin-inhibits-il-1%C3%AE-induced-catabolism-in-mouse-chondrocytes-and-ameliorates-murine-osteoarthritis
#3
Gang Zheng, Yu Zhan, Qian Tang, Tianhe Chen, Fanghong Zheng, Haoli Wang, Jianle Wang, Dengying Wu, Xiaobing Li, Ying Zhou, Xiaobin Wang, Yaosen Wu, Yifei Zhou, Huazi Xu, Naifeng Tian, Xiaolei Zhang
Osteoarthritis (OA) is an age-related degenerative disease and is the fourth major cause of disability, but there are no effective therapies because of its complex pathology and the side effects of the drugs. Previous research demonstrated that inflammation and ECM degradation play major roles in OA development. Monascin is an azaphilonoid pigment extracted from Monascus-fermented rice with a potential anti-inflammatory effect reported in various preclinical studies. In the present study, we investigated the protectiveness of monascin on interleukin (IL)-1β-induced mouse chondrocytes and surgical destabilization of the medial meniscus mouse (DMM) OA models...
February 23, 2018: Food & Function
https://www.readbyqxmd.com/read/29471006/astilbin-ameliorates-cisplatin-induced-nephrotoxicity-through-reducing-oxidative-stress-and-inflammation
#4
Si-Wei Wang, Yi Xu, Yuan-Yuan Weng, Xue-Yu Fan, Yong-Feng Bai, Xiao-Yan Zheng, Li-Jun Lou, Feng Zhang
Oxidative stress and inflammation are considered to be the main pathogenesis of cisplatin nephrotoxicity. Astilbin, a flavonoid with anti-oxidation and anti-inflammation function, has been used to treat heavy metal induced kidney injury. In this study, we investigated the protective effects of astilbin on cisplatin-induced nephrotoxicity and its underlying mechanisms. Our results showed that astilbin markedly inhibited cisplatin-induced cell apoptosis and recovered cell growth. Astilbin significantly decreased reactive oxygen species (ROS) accumulation and alleviated ROS-induced activation of p53, MAPKs and AKT signaling cascades, which in turn attenuated cisplatin-induced HEK-293 cell apoptosis...
February 19, 2018: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/29470957/kaempferol-7-o-%C3%AE-d-glucoside-isolated-from-the-leaves-of-cudrania-tricuspidata-inhibits-lps-induced-expression-of-pro-inflammatory-mediators-through-inactivation-of-nf-%C3%AE%C2%BAb-ap-1-and-jak-stat-in-raw-264-7-macrophages
#5
Seung-Bin Lee, Ji-Sun Shin, Hee-Soo Han, Hwi-Ho Lee, Jong Cheol Park, Kyung-Tae Lee
Kaempferol 7-O-β-D-glucoside (KPG), a natural flavonol isolated from Cudrania tricuspidata, has been reported to exert anti-cancer effects; however, its anti-inflammatory effects have not yet been reported. In this study, we demonstrate the suppressive effect of KPG on the production of nitric oxide (NO), prostaglandin E2 (PGE2 ), tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), and interleukin-6 (IL-6) in lipopolysaccharide (LPS)-induced RAW 264.7 macrophages and mouse bone marrow-derived macrophages...
February 19, 2018: Chemico-biological Interactions
https://www.readbyqxmd.com/read/29468988/cox-2-in-radiotherapy-a-potential-target-for-radioprotection-and-radiosensitization
#6
Mohsen Cheki, Rasoul Yahyapour, Bagher Farhood, Abolhassan Rezaeyan, Dheyauldeen Shabeeb, Peyman Amini, Saeed Rezapoor, Masoud Najafi
BACKGROUND: Each year, millions of people die from cancer. Radiotherapy is one of the main treatment strategies for cancer patients. Despite the beneficial roles of treatment with radiation, several side effects may threaten normal tissues of patients in the years after treatment. Moreover, high incidences of second primary cancers may reduce therapeutic ratio of radiotherapy. The search for appropriate targets of radiosensitization of tumor cells as well as radioprotection of normal tissues is one of the most interesting aims in radiobiology...
February 18, 2018: Current Molecular Pharmacology
https://www.readbyqxmd.com/read/29468706/comparative-cardiovascular-safety-of-non-steroidal-anti-inflammatory-drugs-in-patients-with-hypertension-a-population-based-cohort-study
#7
Yaa-Hui Dong, Chia-Hsuin Chang, Li-Chiu Wu, Jing-Shiang Hwang, Sengwee Toh
AIMS: Prior studies have suggested that non-steroidal anti-inflammatory drugs (NSAIDs) may be associated with higher cardiovascular risks. Few were active-comparison studies that directly assessed potential differential cardiovascular risk between NSAID classes or across individual NSAIDs. We compared the risk of major cardiovascular events between cyclooxygenase-2 enzyme (COX-2) selective NSAIDs and nonselective NSAIDs in patients with hypertension. METHODS: We conducted a cohort study of patients with hypertension who initiated COX-2 selective NSAIDs or nonselective NSAIDs in a population-based Taiwanese database...
February 22, 2018: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29468666/eicosanoids-prostacyclin-and-cyclooxygenase-in-the-cardiovascular-system
#8
REVIEW
Jane A Mitchell, Nicholas S Kirkby
Eicosanoids represent a diverse family of lipid mediators with fundamental roles in controlling physiology and disease. Within the eicosanoid super family are prostanoids, which are specifically derived from arachidonic acid by the enzyme cyclooxygenase (COX). COX has two isoforms; COX-1 and COX-2. COX-2 is the therapeutic target for the nonsteroidal anti-inflammatory drug (NSAID) class of pain medications. Of the prostanoids, prostacyclin, first discovered by Sir Professor John Vane in 1976, remains amongst the best studied and retains an impressive pedigree as one the bodies fundamental cardiovascular protective pathways...
February 21, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29468499/resveratrol-improves-neuroimmune-dysregulation-through-the-inhibition-of-neuronal-toll-like-receptors-and-cox-2-signaling-in-btbr-t-itpr3-tf-j-mice
#9
Sheikh F Ahmad, Mushtaq A Ansari, Ahmed Nadeem, Mohammad Z Alzahrani, Saleh A Bakheet, Sabry M Attia
Autism is a neurodevelopmental disorder characterized by deficits in qualitative impairments in communication, repetitive and social interaction, restricted, and stereotyped patterns of behavior. Resveratrol has been extensively studied pharmacologically and biologically and has anti-inflammatory, antioxidant, and neuroprotective effects on neuronal damage in neurodegenerative disorders. The BTBR T+ Itpr3tf /J (BTBR) autistic mouse model has been explored for treatment of autism, which shows low reciprocal social interactions, impaired juvenile play, and decreased social approach...
February 21, 2018: Neuromolecular Medicine
https://www.readbyqxmd.com/read/29466245/effect-of-the-arctic-terrestrial-plant-ranunculus-hyperboreus-on-lps-induced-inflammatory-response-via-mapk-pathways
#10
Chang-Suk Kong, Jung Im Lee, Fatih Karadeniz, Hojun Kim, Youngwan Seo
The Arctic flora hosts a limited number of species due to its extreme environmental conditions which also yield novel and unique secondary metabolites from withstanding plants. Considering a lack of research on bioactivity potential of Arctic flora, Ranunculus hyperboreus, an Arctic plant, was studied for its anti-inflammatory potential as a part of ongoing research on discovering novel natural bioactive products. Solvent-based fractions (H2O, n-BuOH, 85% aq. MeOH, n-hexane) from R. hyperboreus extract were observed to decrease the elevated nitrate amount during the inflammatory response of lipopolysaccharide-induced mouse macrophage RAW264...
February 21, 2018: Zeitschrift Für Naturforschung. C, A Journal of Biosciences
https://www.readbyqxmd.com/read/29463423/-is-celecoxib-a-safe-alternative-for-the-fernand-widal-syndrome
#11
REVIEW
A Schaller, C Metz-Favre, L Guenard-Bilbaut, F De Blay
The Fernand Widal syndrome is a set of associations between asthma, nasal polyposis and aspirin sensitivity. Selective cyclo-oxygenase 2 (COX 2) inhibitors are recognized as being a therapeutic alternative in cases needing analgesic or anti-inflammatory treatment. In a retrospective study, we have compiled data concerning oral provocation tests (OPT) undertaken with celecoxib, one of most the selective COX 2 inhibitors, in eight patients with the Fernand Widal syndrome. They were compared with twenty-seven control patients with sensitivity to aspirin or non-steroidal anti-inflammatories, manifesting as asthma, urticaria or rhino-conjunctivitis...
February 17, 2018: Revue des Maladies Respiratoires
https://www.readbyqxmd.com/read/29463104/momordica-charantia-inhibits-inflammatory-responses-in-murine-macrophages-via-suppression-of-tak1
#12
Woo Seok Yang, Eunju Yang, Min-Jeong Kim, Deok Jeong, Deok Hyo Yoon, Gi-Ho Sung, Seungihm Lee, Byong Chul Yoo, Seung-Gu Yeo, Jae Youl Cho
Momordica charantia known as bitter melon is a representative medicinal plant reported to exhibit numerous pharmacological activities such as antibacterial, antidiabetic, anti-inflammatory, anti-oxidant, antitumor, and hypoglycemic actions. Although this plant has high ethnopharmacological value for treating inflammatory diseases, the molecular mechanisms by which it inhibits the inflammatory response are not fully understood. In this study, we aim to identify the anti-inflammatory mechanism of this plant. To this end, we studied the effects of its methanol extract (Mc-ME) on lipopolysaccharide (LPS)-stimulated RAW264...
February 20, 2018: American Journal of Chinese Medicine
https://www.readbyqxmd.com/read/29462911/anti-inflammatory-and-gastroprotective-roles-of-rabdosia-inflexa-through-downregulation-of-pro-inflammatory-cytokines-and-mapk-nf-%C3%AE%C2%BAb-signaling-pathways
#13
Md Rashedunnabi Akanda, In-Shik Kim, Dongchoon Ahn, Hyun-Jin Tae, Hyeon-Hwa Nam, Byung-Kil Choo, Kyunghwa Kim, Byung-Yong Park
Globally, gastric ulcer is a vital health hazard for a human. Rabdosia inflexa (RI) has been used in traditional medicine for inflammatory diseases. The present study aimed to investigate the protective effect and related molecular mechanism of RI using lipopolysaccharide (LPS)-induced inflammation in RAW 246.7 cells and HCl/EtOH-induced gastric ulcer in mice. We applied 3-(4,5-dimethyl-thiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), nitric oxide (NO), reactive oxygen species (ROS), histopathology, malondialdehyde (MDA), quantitative real-time polymerase chain reaction (qPCR), immunohistochemistry (IHC), and Western blot analyses to evaluate the protective role of RI...
February 16, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29462704/enhancement-of-endocannabinoid-dependent-depolarization-induced-suppression-of-excitation-in-glycinergic-neurons-by-prolonged-exposure-to-high-doses-of-salicylate
#14
João Zugaib, Ricardo M Leão
The Dorsal Cochlear Nucleus (DCN) is a region which has been traditionally linked to the genesis of tinnitus, the constant perception of a phantom sound. Sodium salicylate, a COX-2 inhibitor, can induce tinnitus in high doses. Hyperactivity of DCN neurons is observed in several animal models of tinnitus, including salicylate-induced tinnitus. The DCN presents several forms of endocannabinoid (EC) dependent synaptic plasticity and COX-2 can also participate in the oxidative degradation of ECs. We recently demonstrated that short-term perfusion of sodium salicylate and other inhibitors of both oxidative and hydrolytic EC degradation did not affect depolarization-induced suppression of excitation (DSE), a form of EC- dependent short-term synaptic plasticity...
February 17, 2018: Neuroscience
https://www.readbyqxmd.com/read/29461477/anti-renal-fibrotic-effect-of-exercise-training-in-hypertension
#15
Ching Huang, Yi-Yuan Lin, Ai-Lun Yang, Tang-Wei Kuo, Chia-Hua Kuo, Shin-Da Lee
The purpose of this study was to evaluate the effects of exercise training on renal fibrosis in hypertensive rats. Masson's trichrome staining and Western blotting were performed on the excised renal cortex from sixteen male spontaneously hypertensive rats (SHR), which were randomly divided into either a sedentary hypertensive group (SHR) or exercise hypertensive group (SHR-EX, running on an exercise treadmill for 60 min/day, 5 sessions/week, for 12 weeks), and from eight male Wistar-Kyoto rats which served as a sedentary normotensive group (WKY)...
February 20, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29460212/involvement-of-nf-%C3%AE%C2%BAb-in-mediating-the-anti-tumour-effects-of-combretastatins-in-t-cells
#16
Jade K Pollock, Lisa M Greene, Seema M Nathwani, Paula Kinsella, Niamh M O'Boyle, Mary J Meegan, Daniela M Zisterer
Purpose The combretastatins (CAs) are known to exhibit anti-tumour activity but the underlying mechanism remains to be fully elucidated. Inflammation plays a critical role in altering the function of cancer cells and evasion of cell death and increased proliferation are characteristics of transformed malignancies. Many of the proteins involved in these pathways are regulated by the transcription factor NF-κB which can be activated by tumour necrosis factor (TNF-α), a pro-inflammatory cytokine released by both malignant and immune cells within the tumour microenvironment...
February 19, 2018: Investigational New Drugs
https://www.readbyqxmd.com/read/29459872/the-neurokinin-1-receptor-contributes-to-the-early-phase-of-lipopolysaccharide-induced-fever-via-stimulation-of-peripheral-cyclooxygenase-2-protein-expression-in-mice
#17
Eszter Pakai, Valeria Tekus, Csaba Zsiboras, Zoltan Rumbus, Emoke Olah, Patrik Keringer, Nora Khidhir, Robert Matics, Laszlo Deres, Katalin Ordog, Nikolett Szentes, Krisztina Pohoczky, Agnes Kemeny, Peter Hegyi, Erika Pinter, Andras Garami
Neurokinin (NK) signaling is involved in various inflammatory processes. A common manifestation of systemic inflammation is fever, which is usually induced in animal models with the administration of bacterial lipopolysaccharide (LPS). A role for the NK1 receptor was shown in LPS-induced fever, but the underlying mechanisms of how the NK1 receptor contributes to febrile response, especially in the early phase, have remained unknown. We administered LPS (120 µg/kg, intraperitoneally) to mice with the Tacr1 gene, i...
2018: Frontiers in Immunology
https://www.readbyqxmd.com/read/29459868/characteristics-of-infection-immunity-regulated-by-toxoplasma-gondii-to-maintain-chronic-infection-in-the-brain
#18
Young Sang Hwang, Ji-Hun Shin, Jung-Pyo Yang, Bong-Kwang Jung, Sang Hyung Lee, Eun-Hee Shin
To examine the immune environment of chronic Toxoplasma gondii infection in the brain, the characteristics of infection-immunity (premunition) in infection with T . gondii strain ME49 were investigated for 12 weeks postinfection (PI). The results showed that neuronal cell death, microglia infiltration and activation, inflammatory and anti-inflammatory cytokine expression, Stat1 phosphorylation, and microglia activation and inflammatory gene transcripts related to M1 polarization in the brain were increased during the acute infection (AI) stage (within 6 weeks PI), suggesting that innate and cellular inflammatory response activation and neurodegeneration contributed to excessive inflammatory responses...
2018: Frontiers in Immunology
https://www.readbyqxmd.com/read/29458016/renal-toxicological-evaluations-of-sulphonated-nanocellulose-from-khaya-sengalensis-seed-in-wistar-rats
#19
Adewale Adewuyi, Chiagoziem A Otuechere, Olusegun L Adebayo, Chibuzo Anazodo, Fabiano V Pereira
Nanocellulose is currently gaining attention due to its unique properties. This attention includes its application as building blocks for developing novel functional materials, plant drug and also in drug delivery systems. However, its safety remains largely untested or less understood. Thus, sulphonated nanocellulose (KSS) was prepared from cellulose (KSC) isolated from Khaya senegalensis seed (KS). KS, KSC and KSS were characterized using Fourier transformed infrared (FTIR), X-ray diffraction (XRD), thermogravimetric analysis (TG), particle size distribution (PSD), zeta potential and scanning electron microscopy (SEM)...
February 16, 2018: Chemico-biological Interactions
https://www.readbyqxmd.com/read/29458014/topical-delivery-of-l-theanine-ameliorates-tpa-induced-acute-skin-inflammation-via-downregulating-endothelial-pecam-1-and-neutrophil-infiltration-and-activation
#20
Wei-Jie Zeng, Zhi Tan, Xing-Fei Lai, Ya-Nan Xu, Chun-Lin Mai, Jun Zhang, Zhen-Jia Lin, Xian-Guo Liu, Shi-Li Sun, Li-Jun Zhou
l-theanine, the most abundant free amino acid in tea, has been documented to possess many different bioactive properties through oral or intragastrical delivery. However, little is known about the effect of topical delivery of l-theanine on acute inflammation. In the present study, by using 12-O-tetradecanoylphorbol-13-acetate (TPA, 2.5 μg/ear)-induced ear edema model in mice, we first found that single-dose local pretreatment of l-theanine 30 min before TPA time- and dose-dependently suppressed the increases in both skin thickness and weight...
February 16, 2018: Chemico-biological Interactions
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