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https://www.readbyqxmd.com/read/28820051/bisthiourea-derivatives-of-dipeptide-conjugated-benzo-d-isoxazole-as-a-new-class-of-therapeutics-synthesis-and-molecular-docking-studies
#1
H K Kumara, D M Suyoga Vardhan, J Shiva Kumar, D Channe Gowda
We have synthesized a series of bisthiourea derivatives of dipeptides (Lys/lys-Asp and Lys/lys-Trp) conjugated benzo[d]isoxazole and the structures of synthesized compounds were confirmed by correlating their physical and spectroscopic data with earlier data. The molecules 1-24 were examined for their in vitro anti-inflammatory activity by employing human erythrocyte suspension test and it was found that the IC50 values of 9, 12, 21 and 24 were lower than the IC50 of standard references indomethacin and ibuprofen...
August 16, 2017: Anti-inflammatory & Anti-allergy Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28820025/interaction-between-progesterone-and-interleukin-1%C3%AE-in-modulating-progesterone-receptor-expression-and-the-inflammatory-phenotype-in-human-cervical-fibroblasts
#2
Stephanie Pierce, Amy E Roberson, Kimberly Hyatt, Krista Singleton, David Deschamps, Dean A Myers
Progesterone helps maintain cervical structure during pregnancy via the progesterone receptor (PR). Two PR isoforms exist, PR-A and PR-B, which have overlapping as well as isoform-specific target genes. During late gestation, leukocytes infiltrate the cervical stroma accompanied by increased cervical cytokine levels, resembling an inflammatory process. We examined interleukin (IL)-1β regulation of the expression of PR-A, PR-B, and genes governing prostaglandin synthesis in human cervical fibroblasts (HCFs)...
January 1, 2017: Reproductive Sciences
https://www.readbyqxmd.com/read/28816560/gastroprotective-and-antiulcer-effects-of-celastrus-paniculatus-seed-oil-against-several-gastric-ulcer-models-in-rats
#3
Suresh Palle, A Kanakalatha, Ch N Kavitha
Peptic ulcer is a recurrent chronic illness and has become almost a hallmark of the so-called civilized life. In folk medicine, the Celastrus paniculatus plant has been used for the prevention and treatment of various diseases and gastrointestinal disturbances, including dyspepsia and stomach ulcers. The aim of this study is to evaluate the gastroprotective and antiulcer effects of Celastrus paniculatus seed oil (CPO) against several gastric ulcer models in rats. The gastroprotective and antiulcer effects of CPO were evaluated using pylorus-ligated ulcer ethanol- and indomethacin-induced ulcers using rantidine (40 mg/kg per os [PO]) as standard...
August 17, 2017: Journal of Dietary Supplements
https://www.readbyqxmd.com/read/28808397/genistein-attenuated-gastric-injury-on-indomethacin-induced-gastropathy-in-rats
#4
Sarocha Vivatvakin, Duangporn Werawatganon, Kanjana Somanawat, Naruemon Klaikeaw, Prasong Siriviriyakul
OBJECTIVES: To investigates the mucoprotective effect of genistein on gastric injury in rats with indomethacin (IMN)-induced gastropathy. METHODS: Male Sprague-Dawley rats were randomly divided into three groups. Group 1 (control; n = 6) was given distilled water (DW). Group 2 (IMN; n = 6) was given indomethacin (IMN) 150 mg/kg dissolved in 5% sodium bicarbonate (NaHCO3(-)) 1 mL/rat via intragastric tube at time 0 and 4 h. Group 3 (genistein; n = 6) was given genistein 100 mg/kg dissolved in 0...
July 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28807848/hydroalcoholic-extract-from-bark-of-persea-major-meisn-l-e-kopp-lauraceae-exerts-antiulcer-effects-in-rodents-by-the-strengthening-of-the-gastric-protective-factors
#5
Lincon Bordignon Somensi, Thaise Boeing, Benhur Judah Cury, Viviane Miranda Bispo Steimbach, Rivaldo Niero, Lauro Mera de Souza, Luisa Mota da Silva, Sérgio Faloni de Andrade
ETHOPHARMACOLOGICAL RELEVANCE: The Persea major (Meisn.) L.E. Kopp (Lauraceae) (botanical synonym: Persea pyrifolia (D. Don) Spreng, Persea pyrifolia Nees and Mart., Persea cordata var. major (Meisn.) Mez and Persea willdenovii Kosterm) is a medicinal plant native in the south of Brazil, where is popularly known as Pau de Andrade, Maçaranduba or Abacate-do-Mato. Its barks are commonly used to prepare an infusion which is administered orally or topically to treat ulcers and wounds, respectively...
August 12, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28806653/novel-microemulsion-based-gels-for-topical-delivery-of-indomethacin-formulation-physicochemical-properties-and-in-vitro-drug-release-studies
#6
Anna Froelich, Tomasz Osmałek, Agnieszka Snela, Paweł Kunstman, Barbara Jadach, Marta Olejniczak, Grzegorz Roszak, Wojciech Białas
HYPOTHESIS: Microemulsion-based semisolid systems may be considered as an interesting alternative to the traditional dosage forms applied in topical drug delivery. Mechanical properties of topical products are important both in terms of application and dosage form effectiveness. In this study we designed and evaluated novel microemulsion-based gels with indomethacin and analyzed the factors affecting their mechanical characteristics and drug release. EXPERIMENTS: The impact of the microemulsion composition on the extent of isotropic region was investigated with the use of pseudoternary phase diagrams...
August 4, 2017: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/28801264/vasoactive-properties-of-antihypertensive-lactoferrin-derived-peptides-in-resistance-vessels-effects-in-small-mesenteric-arteries-from-shr-rats
#7
Aurora García-Tejedor, Paloma Manzanares, María Castelló-Ruiz, Antonio Moscardó, José F Marcos, Juan B Salom
AIMS: Bovine lactoferrin (LF) hydrolysates and peptides identified thereof have shown antihypertensive effects in rat models, mainly but not exclusively by angiotensin-converting enzyme inhibition. In this study we aimed to assess the vasoactive effects and mechanisms of an ultrafiltered (<3kDa) pepsin LF hydrolysate (LFH) and a heptapeptide identified in a LF hydrolysate produced by yeast proteolysis (DPYKLRP) in peripheral resistance arteries from spontaneously hypertensive rats (SHRs)...
August 8, 2017: Life Sciences
https://www.readbyqxmd.com/read/28795057/side-effects-of-indomethacin-in-refractory-post-traumatic-intracranial-hypertension-a-comprehensive-case-study-and-review
#8
REVIEW
Daniel Agustín Godoy, Pablo David Guerrero Suarez, Luis Rafael Moscote-Salazar, Mario Di Napoli
Intracranial hypertension (IH) is one of the final pathways of acute brain injury. In severe traumatic brain injury (sTBI), it independently predicts poor outcomes. Its control represents a key aspect of the management. Lack of response to conventional therapies signals a state of ''refractory IH'', with an associated mortality rate of 80-100%. In such cases, hypothermia, barbiturates at high doses (BBT), decompressive craniectomy (DC), and extreme hyperventilation are utilized. However, none of them has proven efficacy...
July 2017: Bulletin of Emergency and Trauma
https://www.readbyqxmd.com/read/28793049/possible-mechanisms-involved-in-the-vasorelaxant-effect-produced-by-clobenzorex-in-aortic-segments-of-rats
#9
J Lozano-Cuenca, A González-Hernández, O A López-Canales, J R Villagrana-Zesati, J D Rodríguez-Choreão, R Morín-Zaragoza, E F Castillo-Henkel, J S López-Canales
Clobenzorex is a metabolic precursor of amphetamine indicated for the treatment of obesity. Amphetamines have been involved with cardiovascular side effects such as hypertension and pulmonary arterial hypertension. The aim of the present study was to investigate whether the direct application of 10-9-10-5 M clobenzorex on isolated phenylephrine-precontracted rat aortic rings produces vascular effects, and if so, what mechanisms may be involved. Clobenzorex produced an immediate concentration-dependent vasorelaxant effect at the higher concentrations (10-7...
August 7, 2017: Brazilian Journal of Medical and Biological Research, Revista Brasileira de Pesquisas Médicas e Biológicas
https://www.readbyqxmd.com/read/28792072/synthesis-of-some-novel-2-6-disubstituted-pyridazin-3-2h-one-derivatives-as-analgesic-anti-inflammatory-and-non-ulcerogenic-agents
#10
Tamer H Ibrahim, Yasser M Loksha, Hosam A Elshihawy, Dina M Khodeer, Mohamed M Said
Some novel 2,6-disubstituted pyridazine-3(2H)-one derivatives were synthesized and evaluated for in vitro cyclooxygenase-2 (COX-2) inhibitory efficacy. Compounds 2-{[3-(2-methylphenoxy)-6-oxopyridazin-1(6H)-yl]methyl}-1H-isoindole-1,3(2H)-dione (5a), 2-propyl-6-(o-tolyloxy)pyridazin-3(2H)-one (6a), and 2-benzyl-6-(3,5-dimethyl-1H-pyrazol-1-yl)pyridazin-3(2H)-one (16a) showed the most potent COX-2 inhibitory activity with IC50 values of 0.19, 0.11, and 0.24 μM, respectively. The synthesized compounds with the highest COX-2 selectivity indices were evaluated for their anti-inflammatory, analgesic, and ulcerogenic activities...
August 9, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28782581/anti-inflammatory-phenylpropanoids-and-phenolics-from-ficus-hirta-vahl
#11
Jun Cheng, Xiaomin Yi, Haiying Chen, Yihai Wang, Xiangjiu He
Four new phenylpropanoids (1-4) along with ten known phenolics were isolated and purified from the roots of hairy fig (Ficus hirta Vahl.). Their structures were elucidated by the extensive spectroscopic analysis and chemical degradation. The anti-inflammatory activities of the purified compounds were evaluated. Results indicated that the extracts and some purified compounds exhibited pronounced inhibitory effects on the lipopolysaccharides (LPS) induced nitric oxide (NO) production in murine macrophage RAW 264...
August 4, 2017: Fitoterapia
https://www.readbyqxmd.com/read/28780058/endothelial-nitric-oxide-synthase-and-cyclooxygenase-are-activated-by-hydrogen-peroxide-in-renal-hypertensive-rat-aorta
#12
B R Silva, L Pernomian, T D De Paula, M D Grando, L M Bendhack
In this work, we hypothesized that cyclooxygenase (COX) activity can be regulated by nitric oxide (NO) and hydrogen peroxide (H2O2). In the renal hypertension (2K-1C), phenylephrine (PE)-induced contraction was lower than in normotensive (2K) rat aortas. This impaired contraction is due to NO/H2O2- induced vasodilation. We evaluated the effects of H2O2 on the activity of COX and endothelial NO-Synthase (eNOS) in 2K-1C rat aortas stimulated with PE. Responses for PE or H2O2 were evaluated in 2K-1C and 2K rat aortas, without or with inhibitors for COX (Indomethacin) or eNOS (L-NAME)...
August 2, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28777516/hyperbaric-oxygenation-affects-the-mechanisms-of-acetylcholine-induced-relaxation-in-diabetic-rats
#13
Sanela Unfirer, Martina Mihalj, Sanja Novak, Aleksandar Kibel, Ava Cavka, Zrinka Mijalevic, Mario Gros, Ivica Brizic, Danijela Budimir, Anita Cosic, Mladen Boban, Ines Drenjancevic
The effects of hyperbaric oxygenation (HBO₂) on acetylcholine-induced vasorelaxation (AChIR) were evaluated in male Sprague-Dawley (SD) rats randomized into four groups: healthy controls (Ctrl), diabetic rats (DM), and control and diabetic rats that underwent hyperbaric oxygenation (Ctrl+HBO₂ and DM+HBO₂). AChIR was measured in aortic rings, with L-NAME, indomethacin, or MS-PPOH and a combination of inhibitors. mRNA expression of eNOS, iNOS, COX-1 and COX-2 was assessed by qPCR, and protein expression of CYP4A(1-3) by Western blot...
November 2016: Undersea & Hyperbaric Medicine: Journal of the Undersea and Hyperbaric Medical Society, Inc
https://www.readbyqxmd.com/read/28776721/synergistic-interaction-of-matricaria-chamomilla-extract-with-diclofenac-and-indomethacin-on-carrageenan-induced-paw-inflammation-in-rats
#14
Mario I Ortiz, Raquel Cariño-Cortés, Héctor A Ponce-Monter, Martha P González-García, Gilberto Castañeda-Hernández, Mireya Salinas-Caballero
Preclinical Research The coadministration of non-steroidal anti-inflammatory drugs (NSAIDs) with medicinal plant extracts may increase anti-inflammatory activity, thus permitting the use of lower NSAID doses and limiting the side effects. The aim of this study was to explore the interactions between an ethanolic extract of M. chamomilla extract (MCE) with two NSAIDs, diclofenac and indomethacin on carrageenan-induced paw inflammation and gastric injury in rats. Diclofenac, indomethacin and MCE, or combinations with MCE produced an anti-inflammatory effect...
August 4, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28776720/some-novel-mannich-bases-of-5-3-4-dichlorophenyl-1-3-4-oxadiazole-2-3h-one-and-their-anti-inflammatory-activity
#15
Meric Koksal, Irem Ozkan-Dagliyan, Tugce Ozyazici, Beril Kadioglu, Hande Sipahi, Ayhan Bozkurt, Suleyman S Bilge
Non-steroidal anti-inflammatory drugs (NSAIDs), which are widely used for the treatment of rheumatic arthritis, pain, and many different types of inflammatory disorders, cause serious gastrointestinal (GI) side effects. The free carboxylic acid group existing on their chemical structure is correlated with GI toxicity related with all routine NSAIDs. Replacing this functional group with the 1,3,4-oxadiazole bioisostere is a generally used strategy to obtain an anti-inflammatory agent devoid of GI side effects...
August 4, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28771355/peptide-half-life-extension-divalent-small-molecule-albumin-interactions-direct-the-systemic-properties-of-glucagon-like-peptide-1-glp-1-analogues
#16
Esben M Bech, Manuel C Maldonado, Pernille Wismann, Kasper K Sørensen, Søren Blok van Witteloostuijn, Mikkel B Thygesen, Niels Vrang, Jacob Jelsing, Søren L Pedersen, Knud J Jensen
Noncovalent binding of biopharmaceuticals to human serum albumin protects against enzymatic degradation and renal clearance. Herein, we investigated the effect of mono- or divalent small-molecule albumin binders for half-life extension of peptides. For proof-of-principle, the clinically relevant glucagon-like peptide 1 (GLP-1) was functionalized with diflunisal, indomethacin, or both. In vitro, all GLP-1 analogues had subnanomolar GLP-1 receptor potency. Surface plasmon resonance revealed that both small molecules were able to confer albumin affinity to GLP-1 and indicated that affinity is increased for divalent analogues...
August 16, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28770976/non-steroidal-anti-inflammatory-drugs-nsaids-for-chronic-non-cancer-pain-in-children-and-adolescents
#17
REVIEW
Christopher Eccleston, Tess E Cooper, Emma Fisher, Brian Anderson, Nick Mr Wilkinson
BACKGROUND: Pain is a common feature of childhood and adolescence around the world, and for many young people, that pain is chronic. The World Health Organization guidelines for pharmacological treatments for children's persisting pain acknowledge that pain in children is a major public health concern of high significance in most parts of the world. While in the past pain was largely dismissed and was frequently left untreated, views on children's pain have changed over time, and relief of pain is now seen as important...
August 2, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28768046/carbon-monoxide-released-from-its-pharmacological-donor-tricarbonyldichlororuthenium-ii-dimer-corm-2-accelerates-the-healing-of-pre-existing-gastric-ulcers
#18
Magierowski Marcin, Magierowska Katarzyna, Hubalewska-Mazgaj Magdalena, Sliwowski Zbigniew, Ginter Grzegorz, Pajdo Robert, Chmura Anna, Kwiecien Slawomir, Brzozowski Tomasz
BACKGROUND AND PURPOSE: Carbon monoxide (CO), gaseous mediator produced by heme oxygenases (HO), has been shown to prevent stress-, ethanol-, aspirin- or alendronate-induced gastric damage, however, its role in the gastric ulcer healing has not been fully explained. We investigated whether CO released from tricarbonyldichlororuthenium (II) dimer (CORM-2) can affect gastric ulcer healing and determined mechanisms involved in healing action of this compound. EXPERIMENTAL APPROACH: Gastric ulcers were induced in Wistar rats by serosal application of acetic acid...
August 2, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28765519/effect-of-naringin-on-monosodium-iodoacetate-induced-osteoarthritis-pain-in-rats
#19
Qiang Xu, Zuo-Fu Zhang, Wei-Xue Sun
BACKGROUND The aim of the current study was to evaluate the anti-osteoarthritic and anti-inflammatory effect of naringin in a monosodium iodoacetate (MIA)- induced osteoarthritis (OA) model in rats. The anti-osteoarthritic potential of naringin was evaluated against the MIA-induced OA rat model. MATERIAL AND METHODS Wistar rats were used for the study and were divided into the following groups: normal control (saline-treated); group II (MIA-treated): group III (MIA+Naringin), and group IV (MIA+Indomethacin)...
August 2, 2017: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/28765512/a-cluster-of-immunoresolvents-links-coagulation-to-innate-host-defense-in-human-blood
#20
Paul C Norris, Stephania Libreros, Nan Chiang, Charles N Serhan
Blood coagulation is a protective response that prevents excessive bleeding upon blood vessel injury. We investigated the relationship between coagulation and the resolution of inflammation and infection by lipid mediators (LMs) through metabololipidomics-based profiling of human whole blood (WB) during coagulation. We identified temporal clusters of endogenously produced prothrombotic and proinflammatory LMs (eicosanoids), as well as specialized proresolving mediators (SPMs). In addition to eicosanoids, a specific SPM cluster was identified that consisted of resolvin E1 (RvE1), RvD1, RvD5, lipoxin B4, and maresin 1, each of which was present at bioactive concentrations (0...
August 1, 2017: Science Signaling
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