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https://www.readbyqxmd.com/read/28098433/synthesis-and-evaluation-of-anti-inflammatory-n-substituted-3-5-bis-2-trifluoromethyl-benzylidene-piperidin-4-ones
#1
Zixin Xie, Zaikui Zhang, Shufang Yu, Donghua Cheng, Huan Zhang, Chao Han, Handeng Lv, Faqing Ye
A total of 24 N-substituted 3,5-bis(2-(trifluoromethyl)benzylidene)piperidin-4-one derivatives were synthesized via aldol condensation, and their anti-inflammatory activities were evaluated. These compounds were found to have no significant cytotoxicity against mouse bone marrow cells in vitro. However, some compounds, such as c6 (N-(3-methylbenzoyl)-3,5-bis-(2-(trifluoromethyl)benzylidene)piperidin-4-one) and c10 (N-(2-chlorobenzoyl)-3,5-bis-(2-(trifluoromethyl)benzylidene)piperidin-4-one), displayed potent anti-inflammatory activity by inhibiting lipopolysaccharide (LPS)-stimulated tumor necrosis factor (TNF)-α, interleukin-6 (IL-6), IL-1β, prostaglandin E2 (PGE2), and nitric oxide (NO) production in RAW 264...
January 18, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28097508/preparation-and-evaluation-of-biopolymeric-nanoparticles-as-drug-delivery-system-in-effective-treatment-of-rheumatoid-arthritis
#2
Vijay Kumar, Ankita Leekha, Aakriti Tyagi, Ankur Kaul, Anil Kumar Mishra, Anita Kamra Verma
PURPOSE: The study purposes to evaluate nanocrystalline biopolymeric nanoparticles encapsulating methotrexate and dexamethasone with high biocompatibility, enhanced therapeutic efficacy and reduced toxicity. METHODS: Chitosan nanoparticles were prepared by ionic gelation, and Methotrexate (MTX) and Dexamethasone (DEX) were loaded during the preparation and screened for their in vitro efficacy in HEK and RAW264.7 cells, ex vivo and in vivo efficacy. RESULTS: FTIR confirmed the involvement of phosphoric group of sTPP with amine groups of chitosan and also role of hydrogen bonding involved in the preparation of MTXCHNP and DEXCHNP...
January 17, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28097040/effects-of-inhalable-microparticles-of-seonpyejeongcheon-tang-in-an-asthma-mouse-model-effects-of-microparticles-of-sjt
#3
Won-Kyung Yang, Chul-Hwa Lee, Min-Hee Kim, Seung-Hyeong Kim, Hae-Yoon Choi, Yoon Yeo, Yang-Chun Park
OBJECTIVES: Allergic asthma generally presents with symptoms of wheezing, coughing, breathlessness, and airway inflammation. Seonpyejeongcheon-tang (SJT) consists of 12 herbs. It originated from Jeongcheon-tang (JT), also known as Ding-chuan-tang, composed of 7 herbs, in She-sheng-zhong-miao-fang. This study aimed to evaluate the effects of local delivery of SJT via inhalable microparticles in an asthma mouse model. METHODS: Microparticles containing SJT were produced by spray-drying with leucine as an excipient...
December 2016: Journal of Pharmacopuncture
https://www.readbyqxmd.com/read/28096658/anticancer-and-anti-inflammatory-activities-of-girinimbine-isolated-from-murraya-koenigii
#4
Venoos Iman, Syam Mohan, Siddig Ibrahim Abdelwahab, Hamed Karimian, Noraziah Nordin, Mehran Fadaeinasab, Mohamad Ibrahim Noordin, Suzita Mohd Noor
Therapy that directly targets apoptosis and/or inflammation could be highly effective for the treatment of cancer. Murraya koenigii is an edible herb that has been traditionally used for cancer treatment as well as inflammation. Here, we describe that girinimbine, a carbazole alkaloid isolated from M. koenigii, induced apoptosis and inhibited inflammation in vitro as well as in vivo. Induction of apoptosis in human colon cancer cells (HT-29) by girinimbine revealed decreased cell viability in HT-29, whereas there was no cytotoxic effect on normal colon cells...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28095688/effect-of-gold-nanoparticle-size-and-coating-on-labeling-monocytes-for-ct-tracking
#5
Peter Chhour, Johoon Kim, Barbara Benardo, Alfredo Tovar, Shaameen Mian, Harold I Litt, Victor A Ferrari, David P Cormode
With advances in cell therapies, interest in cell tracking techniques to monitor the migration, localization, and viability of these cells continues to grow. X-ray computed tomography (CT) is a cornerstone of medical imaging but has been limited in cell tracking applications due to its low sensitivity toward contrast media. In this study, we investigate the role of size and surface functionality of gold nanoparticles for monocyte uptake to optimize the labeling of these cells for tracking in CT. We synthesized gold nanoparticles (AuNP) that range from 15 to 150 nm in diameter and examined several capping ligands, generating 44 distinct AuNP formulations...
January 18, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28095354/heliangin-inhibited-lipopolysaccharide-induced-inflammation-through-signaling-nf-%C3%AE%C2%BAb-pathway-on-lps-induced-raw-264-7-cells
#6
XinGang Lu, Li Min, JiongLin Wei, HaiXin Gou, ZhiJun Bao, JiaoFeng Wang, Zheng Wang, YiZhi Huang, BingChen An
The heliangin is a natural agent mainly isolated from Helianthus tuberosus L. (Asteraceae). In order to investigate the anti-inflammatory effect of heliangin, several typical models in vivo and in vitro were performed. The RAW264.7 mouse macrophages cells were employed in vitro and dexamethasone were conducted as positive. The cytotoxicity results of heliangin on RAW 264.7 cells provided the safety in vitro for further study. The mRNA of TNF-α, IL-6, iNOS and COX-2 were degraded under heliangin exposure in LPS-stimulated RAW 264...
January 14, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28095349/anti-inflammatory-effects-of-ononin-on-lipopolysaccharide-stimulated-raw-264-7-cells
#7
Lin Dong, Lei Yin, Yuanbin Zhang, Xueyan Fu, Jincai Lu
Increasing evidence has shown that ononin, a major isoflavone, has anti-inflammatory effects on lipopolysaccharide (LPS)-induced inflammation. However, the molecular mechanisms underlying the anti-inflammatory effects of ononin are still unclear. In the present study, we investigated these effects and the underlying mechanisms of ononin on LPS-induced inflammatory responses. Mouse RAW 264.7 cells were treated with 1μg/mL LPS and 5, 25, 50, 100 or 150μM ononin for 18h. Cell viability was assessed using MTT assays, and the production of nitric oxide (NO), prostaglandin E2 (PGE2) and the pro-inflammatory cytokines TNF-α, IL-1β and IL-6 in cultures was examined by Griess and ELISA analyses...
January 14, 2017: Molecular Immunology
https://www.readbyqxmd.com/read/28095306/the-role-of-pten-in-regulation-of-hepatic-macrophages-activation-and-function-in-progression-and-reversal-of-liver-fibrosis
#8
Yahui Cheng, Yuanyao Tian, Jialu Xia, Xiaoqin Wu, Yang Yang, Xiaofeng Li, Cheng Huang, Xiaoming Meng, Taotao Ma, Jun Li
Activation of Kupffer cells (KCs) plays a pivotal role in the pathogenesis of liver fibrosis. The progression and reversal of CCl4-induced mouse liver fibrosis showed a mixed induction of hepatic classical (M1) and alternative (M2) macrophage markers. Although the role of phosphatase and tensin homolog deleted on chromosome 10 (PTEN) in modulating myeloid cell activation has recently been identified, its function in macrophage activation during hepatic fibrosis remains to be fully appreciated. In our study, PTEN expression of KCs was remarkably decreased in CCl4-induced mice but increased to a near-normal level in reversed mice...
January 14, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28094275/sulfated-cyclocarya-paliurus-polysaccharides-markedly-attenuates-inflammation-and-oxidative-damage-in-lipopolysaccharide-treated-macrophage-cells-and-mice
#9
Zhijun Wang, Jianhua Xie, Yujiao Yang, Fan Zhang, Shengnan Wang, Ting Wu, Mingyue Shen, Mingyong Xie
Natural polysaccharides and their modified derivatives are crucial supplements to the prevention of inflammation. This study aimed to evaluate the effect of sulfated modification on the anti-inflammatory and anti-oxidative activities of Cyclocarya paliurus polysaccharides (CP). A sulfated CP, S-CP1-4 was obtained using chlorosulfonic acid-pyridine method. The chemical components and FT-IR spectrum confirmed that sulfated group was synthesized to the polysaccharide chains successfully. S-CP1-4 was found to inhibit nitric oxide production, phagocytic activity and the release of interleukin (IL)-6 and IL-1β in lipopolysaccharide-treated macrophage cells, RAW 264...
January 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28093936/biological-activities-of-rosmarinus-officinalis-l-rosemary-extract-as-analyzed-in-microorganisms-and-cells
#10
Jonatas Rafael de Oliveira, Daiane de Jesus, Leandro Wagner Figueira, Felipe Eduardo de Oliveira, Cristina Pacheco Soares, Samira Estves Afonso Camargo, Antonio Olavo Cardoso Jorge, Luciane Dias de Oliveira
R. officinalis L. is an aromatic plant commonly used as condiment and for medicinal purposes. Biological activities of its extract were evaluated in this study, as antimicrobial effect on mono- and polymicrobial biofilms, cytotoxicity, anti-inflammatory capacity, and genotoxicity. Monomicrobial biofilms of Candida albicans, Staphylococcus aureus, Enterococcus faecalis, Streptococcus mutans and Pseudomonas aeruginosa and polymicrobial biofilms composed of C. albicans with each bacterium were formed in microplates during 48 h and exposed for 5 min to R...
January 1, 2017: Experimental Biology and Medicine
https://www.readbyqxmd.com/read/28093915/oscarellin-an-anthranilic-acid-derivative-from-a-philippine-sponge-oscarella-stillans-as-an-inhibitor-of-inflammatory-cytokines-in-macrophages
#11
Ii-Seul Kwon, Jong Hwan Kwak, Suhkneung Pyo, Hee-Weon Lee, AeRyon Kim, Francis J Schmitz
A new anthranilic acid derivative (1) was isolated from a Philippine sponge, Oscarella stillans (Bergquist and Kelly). The structure of compound 1, named oscarellin, was determined as 2-amino-3-(3'-aminopropoxy)benzoic acid from spectroscopic data and confirmed by synthesis. We examined the immunomodulating effect of compound 1 and its mechanism in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. Our data indicated that the expression of tumor necrosis factor-α (TNF-α) and interleukin (IL)-6 were significantly reduced by the pretreatment of 1 (0...
January 17, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28092793/high-dilutions-of-antimony-modulate-cytokines-production-and-macrophage-leishmania-l-amazonensis-interaction-in-vitro
#12
Fabiana Rodrigues de Santana, Luciane C Dalboni, Kátia F Nascimento, Fabiana Toshie Konno, Anuska M Alvares-Saraiva, Michelle S F Correia, Maristela Dutra Correa Bomfim, Renato C V Casarin, Elizabeth C Perez, Maria Anete Lallo, Giovani B Peres, Márcia Dalastra Laurenti, Nilson R Benites, Dorly F Buchi, Leoni Villano Bonamin
BACKGROUND: In previous results mice treated with high dilutions of antimony presented reduction of monocyte migration to the site of infection with increase in B lymphocytes population in the local lymph node. AIMS: To know the mechanisms involved, a series of in vitro studies was done, using co-cultures of macrophages (RAW 264.7) and Leishmania (L.) amazonensis treated with different dilutions of antimony (Antimonium crudum or AC), in different times. METHODOLOGY: Spreading, phagocytosis, the oxidative activity of macrophages, the viability of free promastigotes and the cytokines/chemokines concentration in the supernatant were evaluated...
January 13, 2017: Cytokine
https://www.readbyqxmd.com/read/28089586/natural-uranium-impairs-the-differentiation-and-the-resorbing-function-of-osteoclasts
#13
Tatiana Gritsaenko, Valérie Pierrefite-Carle, Thomas Lorivel, Véronique Breuil, Georges F Carle, Sabine Santucci-Darmanin
BACKGROUND: Uranium is a naturally occurring radionuclide ubiquitously present in the environment. The skeleton is the main site of uranium long-term accumulation. While it has been shown that natural uranium is able to perturb bone metabolism through its chemical toxicity, its impact on bone resorption by osteoclasts has been poorly explored. Here, we examined for the first time in vitro effects of natural uranium on osteoclasts. METHODS: The effects of uranium on the RAW 264...
January 9, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28088779/comprehensive-proteome-analysis-of-lysosomes-reveals-the-diverse-function-of-macrophages-in-immune-responses
#14
Yanpan Gao, Yanyu Chen, Shaohua Zhan, Wenhao Zhang, Feng Xiong, Wei Ge
Phagocytosis and autophagy in macrophages have been shown to be essential to both innate and adaptive immunity. Lysosomes are the main catabolic subcellular organelles responsible for degradation and recycling of both extracellular and intracellular material, which are the final steps in phagocytosis and autophagy. However, the molecular mechanisms underlying lysosomal functions after infection remain obscure. In this study, we conducted a quantitative proteomics analysis of the changes in constitution and glycosylation of proteins in lysosomes derived from murine RAW 264...
January 8, 2017: Oncotarget
https://www.readbyqxmd.com/read/28087839/understanding-the-property-activity-relationships-of-polyhedral-cuprous-oxide-nanocrystals-in-terms-of-reactive-crystallographic-facets
#15
Yanlin Feng, Yun Chang, Xiujuan Sun, Ning Liu, Yan Cheng, Yuqing Feng, Haiyuan Zhang, Xi Li
The property-activity relationship is usually established to understand the toxicity mechanism of nanomaterials. In the present study, different morphological Cu2O nanocrystals, octahedrons, truncated octahedrons, cuboctahedrons, and cubes, were synthesized to precisely tuning the {100} and {111} facet percentages in purpose of systematically investigating the toxicity role of crystallographic facets in BEAS-2B and RAW 264.7 cells. It was found that the toxicity of polyhedral Cu2O nanocrystals was highly dependent on the exposed {100} surface after short-term exposure because {100} facets could produce more reactive oxygen species (ROS) than {111} facets, however, after long-term exposure, their toxicity showed again the correlation with total surface property because toxic copper ions were largely released from the whole nanocrystal surface irrespective of {100} or {111} facet and this copper dissolution caused the collapse of surface crystals and the vanishing of ROS...
January 13, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/28086859/cheongsangbangpung-tang-ameliorated-the-acute-inflammatory-response-via-the-inhibition-of-nf-%C3%AE%C2%BAb-activation-and-mapk-phosphorylation
#16
Seon Young Kim, Sang Mi Park, Min Hwangbo, Jong Rok Lee, Sung Hui Byun, Sae Kwang Ku, Il Je Cho, Sang Chan Kim, Seon Young Jee, Sook Jahr Park
BACKGROUND: Cheongsangbangpung-tang (CBT) is a traditional herbal formula used in Eastern Asia to treat heat-related diseases and swellings in the skin. The present study was conducted to evaluate the anti-inflammatory effects of cheongsangbangpung-tang extract (CBTE) both in vitro and in vivo. METHODS: The in vitro effects of CBTE on the lipopolysaccharide (LPS)-induced production of inflammation-related proteins were examined in RAW 264.7 cells. The levels of nitric oxide (NO) were measured with the Griess reagent...
January 13, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28086773/pleurotus-giganteus-berk-karun-hyde-the-giant-oyster-mushroom-inhibits-no-production-in-lps-h2o2-stimulated-raw-264-7-cells-via-stat-3-and-cox-2-pathways
#17
Asweni Baskaran, Kek Heng Chua, Vikineswary Sabaratnam, Mani Ravishankar Ram, Umah Rani Kuppusamy
BACKGROUND: Pleurotus giganteus (Berk. Karunarathna and K.D. Hyde), has been used as a culinary mushroom and is known to have medicinal properties but its potential as an anti-inflammatory agent to mitigate inflammation triggered diseases is untapped. In this study, the molecular mechanism underlying the protective effect of ethanol extract of P. giganteus (EPG) against lipopolysaccharide (LPS) and combination of LPS and hydrogen peroxide (H2O2)-induced inflammation on RAW 264.7 macrophages was investigated...
January 13, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28071803/effects-of-catechol-o-methyl-transferase-inhibition-on-anti-inflammatory-activity-of-luteolin-metabolites
#18
Sang Keun Ha, Jin-Ah Lee, Eun Jung Cho, Inwook Choi
Although luteolin is known to have potent anti-inflammatory activities, much less information has been provided on such activities of its hepatic metabolites. Luteolin was subjected to hepatic metabolism in HepG2 cells either without or with catechol O-methyl transferase (COMT) inhibitor. To identify hepatic metabolites of luteolin without (luteolin metabolites, LMs) or with COMT inhibitor (LMs+CI), metabolites were treated by β-glucuronidase and sulfatase, and found that they were composed of glucuronide and sulfate conjugates of diosmetin in LMs or these conjugates of luteolin in LMs+CI...
January 10, 2017: Journal of Food Science
https://www.readbyqxmd.com/read/28070931/anti-rheumatoid-arthritis-effect-of-kaejadan-via-analgesic-and-antiinflammatory-activity-in-vivo-and-in-vitro
#19
Jung Jae Yoon, Eun Jung Sohn, Jung Hyo Kim, Jai Wha Seo, Sung-Hoon Kim
Although Kaejadan (KJD), an herbal cocktail of three medicinal plants (Lithospermum erythrorhizon, Cinnamomum loureirii, and Salvia miltiorrhiza), has been traditionally used for the treatment of rheumatoid arthritis, its scientific evidence is not fully understood. Hence, we investigated antiinflammatory and analgesic mechanism of KJD in vivo and in vitro. Kaejadan suppressed the number of writhing responses in mice treated by acetic acid and showed antinociceptive effect by tail-flick test. Kaejadan abrogated serotonin or carrageenan or Freund's complete adjuvant (FCA)-induced paw edema and also reduced the level of Evans Blue for vascular permeability...
January 9, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28070488/transcriptome-profiling-of-elettaria-cardamomum-l-maton-small-cardamom
#20
F Nadiya, N Anjali, Jinu Thomas, A Gangaprasad, K K Sabu
Elettaria cardamomum (L.) Maton, known as 'queen of spices, is a perennial herbaceous monocot of the family Zingiberaceae, native to southern India. Cardamom is an economically valuable spice crop and used widely in culinary and medicinal purposes. In the present study, using Ion Proton RNA sequencing technology, we performed transcriptome sequencing and de novo transcriptome assembly of a wild and five cultivar genotypes of cardamom. RNA-seq generated a total of 22,811,983 (92 base) and 24,889,197 (75 base) raw reads accounting for approximately 8...
March 2017: Genomics Data
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