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https://www.readbyqxmd.com/read/29346283/the-biological-role-of-hyaluronan-rich-oocyte-cumulus-extracellular-matrix-in-female-reproduction
#1
REVIEW
Eva Nagyova
Fertilization of the mammalian oocyte requires interactions between spermatozoa and expanded cumulus extracellular matrix (ECM) that surrounds the oocyte. This review focuses on key molecules that play an important role in the formation of the cumulus ECM, generated by the oocyte-cumulus complex. In particular, the specific inhibitors (AG1478, lapatinib, indomethacin and MG132) and progesterone receptor antagonist (RU486) exerting their effects through the remodeling of the ECM of the cumulus cells surrounding the oocyte have been described...
January 18, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29340053/indomethacin-based-stimuli-responsive-micelles-combined-with-paclitaxel-to-overcome-multidrug-resistance
#2
Shuanghu Wang, Xueying Tan, Shujuan Li, Yunfang Zhou, Peiwu Geng, Ailian Hua, Aiping Deng, Zhihong Yu
Development of multidrug resistance against antitumor agents is a major limiting factor for the successful chemotherapy. Currently, both amphiphilic polymeric micelles and chemosensitizers have been proposed to overcome MDR during chemotherapy. Herein, the redox-responsive polymeric micelles composed of dextran and indomethacin (as chemosensitizer) using a disulfide bond as the linker are prepared (DEX-SS-IND) for delivery of antitumor agent paclitaxel (PTX). The high level of glutathione in tumor cells selectively breaks the disulfide bond, leading to the rapid breakdown and deformation of redox-responsive polymeric micelles...
December 19, 2017: Oncotarget
https://www.readbyqxmd.com/read/29337669/gastroprotective-effects-of-the-isopropanol-extract-of-artemisia-princeps-and-its-gastroretentive-floating-tablets-on-gastric-mucosal-injury
#3
Joo-Il Kim, Sang-Wook Park, Jhong-Jae Lim, Se-Il Sohn, Ji-Su Shin, Sang Cheol Park, Young Pyo Jang, Eun Kyoung Chung, Hong-Woo Lee, Kyung-Tae Lee
In this study, we investigated the gastroprotective effect of an isopropanol extract from the aerial parts of Artemisia princeps (IPAP) and developed a gastroretentive floating tablet of IPAP (IPAP-FR) for maximized local gastroprotective effects. Pre-treatment with IPAP ameliorated the gastric mucosal hemorrhagic lesions in ethanol/HCl- or indomethacin- treated rats. IPAP decreased mucosal hemorrhage of gastric ulcers induced by ethanol or indomethacin plus pyloric ligation in rats. The optimized floating tablet, IPAP-FR, floated on medium surface with more sustained eupatilin release compared to the non-floating control tablet...
December 20, 2017: Acta Pharmaceutica
https://www.readbyqxmd.com/read/29333034/antinociceptive-and-anti-inflammatory-effects-of-triterpenes-from-pluchea-quitoc-dc-aerial-parts
#4
Francisco Alcione Nobre da Silva, Sônia Maria de Farias Freire, Marilene Oliveira da Rocha Borges, Francisco Erivaldo Vidal Barros, Maria da de Sousa, Maria Nilce de Sousa Ribeiro, Giselle Maria Skelding Pinheiro Guilhon, Adolfo Henrique Müller, Antonio Carlos Romão Borges
Background: Pluchea quitoc DC. (Asteraceae), a medicinal plant known as "quitoco," "caculucage," "tabacarana" and "madre-cravo," is indicated for inflammatory conditions such as bronchitis, arthritis, and inflammation in the uterus and digestive system. Objective: This study evaluated the analgesic and anti-inflammatory activities of the triterpenes compounds obtained from P. quitoc aerial parts. Materials and Methods: The triterpenes compounds β-amyrin, taraxasterol and pseudo-taraxasterol in a mixture (T); β-amyrin, taraxasterol and pseudo-taraxasterol acetates in a mixture (Ta); β-amyrin, taraxasterol, pseudo-taraxasterol acetates in a mixture with β-amyrin, taraxasterol and pseudo-taraxasterol myristates (Tafe) were analyzed in the models of nociception and inflammation...
December 2017: Pharmacognosy Research
https://www.readbyqxmd.com/read/29318292/synthesis-and-structure-activity-relationship-of-some-indole-derivatives-as-potential-anti-inflammatory-agents
#5
Samar S Fatahala, Mohammed A Khedr, Mossad S Mohamed
A series of fused pyrroles were synthesized and tested for their in vivo anti-inflammatory activity. Among 14 examined derivatives, 5 derivatives (1b-e, g and 5b), showed a promising anti-inflammatory activity equivalent to reference anti-inflammatory drugs (indomethacin and ibuprofen). A molecular docking study was conducted to interpret the biological activities of the tested compounds. The docking results were complementary with the phase of the biological survey and confirmed the biological effects.
December 2017: Acta Chimica Slovenica
https://www.readbyqxmd.com/read/29315228/contribution-of-secondary-metabolites-to-the-gastroprotective-effect-of-aqueous-extract-of-ximenia-americana-l-olacaceae-stem-bark-in-rats
#6
Ticiana Parente Aragão, Lady Dayane Kalline Travassos Dos Prazeres, Samara Alves Brito, Pedro José Rolim Neto, Larissa Araújo Rolim, Jackson Roberto Guedes da Silva Almeida, Germana Freire Rocha Caldas, Almir Gonçalves Wanderley
Ximenia americana L. (Olacaceae) is used in ethnomedicine as cicatrizant and for the treatment of gastric disorders. This study identified the chemical constituents of the aqueous extract of X. americana (XaAE) and evaluated its antiulcerogenic activity. After lyophilization, XaAE was analyzed by liquid chromatography-mass spectrometry (LC-MS) and its antiulcerogenic effect was evaluated in acute gastric lesions induced by ethanol, acidified ethanol, and indomethacin. Antisecretory action, mucus production and the participation of sulfhydryl groups (-SH) and nitric oxide (NO) were also investigated...
January 9, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29305725/gelatin-nano-coating-for-inhibiting-surface-crystallization-of-amorphous-drugs
#7
Rattavut Teerakapibal, Yue Gui, Lian Yu
PURPOSE: Inhibit the fast surface crystallization of amorphous drugs with gelatin nano-coatings. METHODS: The free surface of amorphous films of indomethacin or nifedipine was coated by a gelatin solution (type A or B) and dried. The coating's effect on surface crystallization was evaluated. Coating thickness was estimated from mass change after coating. RESULTS: For indomethacin (weak acid, pKa = 4.5), a gelatin coating of either type deposited at pH 5 and 10 inhibited its fast surface crystal growth...
January 5, 2018: Pharmaceutical Research
https://www.readbyqxmd.com/read/29305664/effect-of-formulation-and-process-parameters-on-the-disproportionation-of-indomethacin-sodium-in-buffered-lyophilized-formulations
#8
Sampada Koranne, Seema Thakral, Raj Suryanarayanan
PURPOSE: (i) To investigate buffer salt crystallization and the consequent pH shifts during the freezing stage of the lyophilization of indomethacin sodium (IMCNa) in aqueous sodium phosphate buffer. (ii) To determine the effect of pH shift on the disproportionation of IMCNa in lyophilized formulations. METHODS: Prelyophilization solutions containing IMCNa in sodium phosphate buffer, at initial buffer concentrations ranging from 10 to 100 mM (pH 7.0), and at IMCNa concentrations of 5, 10 & 15 mg/ml, were investigated...
January 5, 2018: Pharmaceutical Research
https://www.readbyqxmd.com/read/29305070/alginate-as-a-potential-diphase-solid-dispersion-carrier-with-enhanced-drug-dissolution-and-improved-storage-stability
#9
Jian Guan, Qiaoyu Liu, Xiaofei Zhang, Yeli Zhang, Rina Chokshi, Haiyang Wu, Shirui Mao
The objective of this study was to explore the feasibility of using alginate as a promising diphase solid dispersion carrier to enhance dissolution rate of BCS II drugs with improved stability. Taking lovastatin and indomethacin as model drugs, solvent evaporation method was used to prepare solid dispersions. The drug/polymer compatibility was predicted by Hansen solubility parameter and the drug/polymer ratio was screened based on dissolution study, drug existing state in solid dispersion was characterized by DSC and XRPD...
January 2, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29300492/photoredox-catalyzed-decarboxylative-alkylation-of-silyl-enol-ethers-to-synthesize-functionalized-aryl-alkyl-ketones
#10
Weiguang Kong, Changjiang Yu, Hejun An, Qiuling Song
Photoredox-catalyzed decarboxylative alkylation of silyl enol ethers has been developed. Diverse functionalized aryl alkyl ketones were afforded in modest to good yields using N-(acyloxy)phthalimide as an easy access alkyl radical source under mild and operationally simple conditions. The excellent performance of drug molecules such as fenbufen and indomethacin and naturally occurring carboxylic acids such as stearic acid and dehydrocholic acid further demonstrated the practicability of the reaction.
January 4, 2018: Organic Letters
https://www.readbyqxmd.com/read/29299942/docking-assisted-design-of-novel-4-adamantanyl-2-thiazolylimino-5-arylidene-4-thiazolidinones-as-potent-nsaids
#11
O Kouatly, Ph Eleftheriou, A Petrou, D Hadjipavlou-Litina, A Geronikaki
Docking analysis was used to predict the effectiveness of adamantanyl insertion in improving cycloxygenase/lipoxygenase (COX/LOX) inhibitory action of previously tested 2-thiazolylimino-5-arylidene-4-thiazolidinones. The crystal structure data of human 5-LOX (3O8Y), ovine COX-1 (1EQH) and mouse COX-2 (3ln1) were used for docking analysis. All docking calculations were carried out using AutoDock 4.2 software. Following prediction results, 11 adamantanyl derivatives were synthesized and evaluated for biological action...
January 4, 2018: SAR and QSAR in Environmental Research
https://www.readbyqxmd.com/read/29289887/novel-click-modifiable-thioquinazolinones-as-anti-inflammatory-agents-design-synthesis-biological-evaluation-and-docking-study
#12
Ghandoura Moussa, Rana Alaaeddine, Lynn M Alaeddine, Rasha Nassra, Ahmed S F Belal, Azza Ismail, Ahmed F El-Yazbi, Yasser S Abdel-Ghany, Aly Hazzaa
Click chemistry was used to synthesize a new series of thioquinazolinone molecules equipped with propargyl moiety,1,2,3-triazolyl and isoxazolyl rings. Our design was based on merging pharmacophores previously reported to exhibit COX-2 inhibitory activities to a thioquinazolinone-privileged scaffold. The synthesized compounds were subjected to in vitro cyclooxygenase COX-1/COX-2 and 15-LOX inhibition assays. Compounds 2c, 3b, 3h, 3j, and 3k showed COX-2 inhibition with IC50 (μM) 0.18, 0.19, 0.11, 0.16 and 0...
December 18, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29289470/prostanoid-dependent-bladder-pain-caused-by-proteinase-activated-receptor-2-activation-in-mice-involvement-of-trpv1-and-t-type-ca2-channels
#13
Maho Tsubota, Tomoka Ozaki, Yuko Hayashi, Yasumasa Okawa, Ayaka Fujimura, Fumiko Sekiguchi, Hiroyuki Nishikawa, Atsufumi Kawabata
We studied the pronociceptive role of proteinase-activated receptor-2 (PAR2) in mouse bladder. In female mice, intravesical infusion of the PAR2-activating peptide, SLIGRL-amide (SL), caused delayed mechanical hypersensitivity in the lower abdomen, namely 'referred hyperalgesia', 6-24 h after the administration. The PAR2-triggered referred hyperalgesia was prevented by indomethacin or a selective TRPV1 blocker, and restored by a T-type Ca2+ channel blocker. In human urothelial T24 cells, SL caused delayed prostaglandin E2 production and COX-2 upregulation...
December 15, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/29284502/reciprocal-interactions-between-prostaglandin-e2-and-estradiol-dependent-signaling-pathways-in-the-injured-zebra-finch-brain
#14
Alyssa L Pedersen, Colin J Saldanha
BACKGROUND: Astrocytic aromatization and consequent increases in estradiol are neuroprotective in the injured brain. In zebra finches, cyclooxygenase-activity is necessary for injury-induced aromatase expression, and increased central estradiol lowers neuroinflammation. The mechanisms underlying these influences are unknown. Here, we document injury-induced, cyclooxygenase-dependent increases in glial aromatase expression and replicate previous work in our lab showing increases in central prostaglandin E2 and estradiol following brain damage...
December 29, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/29283047/is-it-all-said-for-nsaids-in-alzheimer-s-disease-role-of-mitochondrial-calcium-uptake
#15
Sara Sanz-Blasco, Maria Calvo-Rodríguez, Erica Caballero, Monica Garcia-Durillo, Lucía Nunez, Carlos Villalobos
Epidemiological data suggest that non-steroidal anti-inflammatory drugs (NSAIDs) may protect against Alzheimer's disease (AD). Unfortunately, recent trials have failed in providing compelling evidence of neuroprotection. Discussion as to why NSAIDs effectivity is uncertain is ongoing. Possible explanations include the view that NSAIDs and other possible disease-modifying drugs should be provided before the patients develop symptoms of AD or cognitive decline. In addition, NSAID targets for neuroprotection are unclear...
December 27, 2017: Current Alzheimer Research
https://www.readbyqxmd.com/read/29281684/candida-albicans-derived-mannoproteins-activate-nf-%C3%AE%C2%BAb-in-reporter-cells-expressing-tlr4-md2-and-cd14
#16
Traci Ness, Mahmud Abdallah, Jaime Adams, Claudia Alvarado, Edwin Gunn, Brittany House, John Lamb, Jack Macguire, Emily Norris, Rebekah Robinson, Morgan Sapp, Jill Sharma, Ronald Garner
The ability of soluble C. albicans 20A (serotype A) mannoprotein (CMP) to serve as a ligand for toll-like receptor 4 (TLR4) and its co-receptors was examined using commercially available and stably-transfected HEK293 cells that express human TLR4, MD2 and CD14, but not MR. These TLR4 reporter cells also express an NF-κB-dependent, secreted embryonic alkaline phosphatase (SEAP) reporter gene. TLR4-reporter cells exhibited a dose-dependent SEAP response to both LPS and CMP, wherein peak activation was achieved after stimulation with 40-50 μg/mL of CMP...
2017: PloS One
https://www.readbyqxmd.com/read/29281657/indoles-induce-metamorphosis-in-a-broad-diversity-of-jellyfish-but-not-in-a-crown-jelly-coronatae
#17
Rebecca R Helm, Casey W Dunn
Many animals go through one or more metamorphoses during their lives, however, the molecular underpinnings of metamorphosis across diverse species are not well understood. Medusozoa (Cnidaria) is a clade of animals with complex life cycles, these life cycles can include a polyp stage that metamorphoses into a medusa (jellyfish). Medusae are produced through a variety of different developmental mechanisms-in some species polyps bud medusae (Hydrozoa), in others medusae are formed through polyp fission (Scyphozoa), while in others medusae are formed through direct transformation of the polyp (Cubozoa)...
2017: PloS One
https://www.readbyqxmd.com/read/29277718/effect-of-allantoin-on-experimentally-induced-gastric-ulcers-pathways-of-gastroprotection
#18
Dayane Moreira da Silva, José Luís Rodrigues Martins, Danillo Ramos de Oliveira, Iziara Ferreira Florentino, Daiany Priscilla Bueno da Silva, Fernanda Cristina Alcântara Dos Santos, Elson Alves Costa
Gastric ulcer affects people worldwide, and its inefficacy and recurrence have fueled the search for new therapeutic strategies. Despite the well-known use of allantoin in medicines and cosmetic products, its effect has not yet been studied with regard to gastric ulcer. Hence, the aim of the present study was to explore the pharmaco-mechanistic efficacy of allantoin against commonly harmful agents that cause injuries to the stomach. Ethanol, indomethacin, and stress-induced gastric ulcer models were adopted, in addition to pylorus ligature, a quantification of vascular permeability, glutathione (GSH), gastric adhered mucus, prostaglandin (PGE2), pro-inflammatory cytokines levels, myeloperoxidase (MPO), and catalase (CAT) activities...
December 22, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29276647/low-dose-intravenous-paracetamol-for-patent-ductus-arteriosus-in-indomethacin-resistant-or-contraindicated-preterm-infants-three-cases-reports
#19
Shun Matsumura, Ayumi Oshima, Sumie Fujinuma, Kosuke Tanaka, Nobuhiko Nagano, Fuyu Miyake, Satoshi Masutani, Masanori Tamura, Keiko Ueda, Fumihiko Namba
Background  Although indomethacin (IND) is the standard treatment for hemodynamically significant patent ductus arteriosus (hsPDA) in Japan, it may be associated with renal impairment and gastrointestinal complications. The use of paracetamol for hsPDA closure has recently increased. Unlike IND, paracetamol does not have a peripheral vasoconstrictive effect and can be given to infants with contraindications to IND. Based on limited data available from randomized trials, paracetamol and IND seem to have similar effects...
October 2017: American Journal of Perinatology Reports
https://www.readbyqxmd.com/read/29273868/involvement-of-tlr3-dependent-pges-expression-in-immunosuppression-by-human-bone-marrow-mesenchymal-stem-cells
#20
Dae Seong Kim, Whi Hyeong Lee, Myoung Woo Lee, Hyun Jin Park, In Keun Jang, Ji Won Lee, Ki Woong Sung, Hong Hoe Koo, Keon Hee Yoo
Human mesenchymal stem cells (MSCs) are known for their prostaglandin E2 (PGE2)-mediated immunosuppressive function but the precise molecular mechanisms underlying PGE2 biosynthesis during inflammation have not been completely elucidated. In this study, we have investigated the involvement of PGE2 pathway members in PGE2 production by bone marrow (BM)-MSCs in response to inflammatory stimuli, and their role in immunosuppression mediated by BM-MSCs. We found that IFN-γ and TNF-α increased cyclooxygenase (COX)-2 expression but not that of prostaglandin E synthase (PGES), or PGE2 production...
December 22, 2017: Stem Cell Reviews
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