Search results for "rape"

showing 10 items of 2178 documents

Desensitization of cAMP Accumulation via Human β3-Adrenoceptors Expressed in Human Embryonic Kidney Cells by Full, Partial, and Biased Agonists

2019

β3-Adrenoceptors couple not only to cAMP formation but, at least in some cell types, also to alternative signaling pathways such as phosphorylation of extracellular signal-regulated kinase (ERK). β3-Adrenoceptor agonists are used in long-term symptomatic treatment of the overactive bladder syndrome; it is only poorly understood which signaling pathway mediates the clinical response and whether it undergoes agonist-induced desensitization. Therefore, we used human embryonic kidney cells stably transfected with human β3-adrenoceptors to compare coupling of ligands with various degrees of efficacy, including biased agonists, to cAMP formation and ERK phosphorylation, particularly regarding des…

0301 basic medicineAgonistMAPK/ERK pathwaymedicine.drug_classmedicine.medical_treatmentdesensitization03 medical and health scienceschemistry.chemical_compoundpartial agonism0302 clinical medicinecAMPIsoprenalinemedicinePharmacology (medical)β3-adrenoceptorOriginal ResearchDesensitization (medicine)PharmacologyForskolinKinaselcsh:RM1-950extracellular signal-related kinaseCell biologylcsh:Therapeutics. Pharmacology030104 developmental biologybiased agonismchemistry030220 oncology & carcinogenesisPhosphorylationSignal transductionmedicine.drugFrontiers in Pharmacology
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5-HT1A Receptor Function Makes Wound Healing a Happier Process

2018

Skin wound healing is a multistage phenomenon that is regulated by cell–cell interplay and various factors. Endogenous serotonin is an important neurotransmitter and cytokine. Its interaction with the serotonin 1A receptor (5-HTR1A) delivers downstream cellular effects. The role of serotonin (5-hydroxytryptamine, 5-HT) and the 5-HT1A receptor has been established in the regeneration of tissues such as the liver and spinal motor neurons, prompting the investigation of the role of 5-HT1A receptor in skin healing. This study assessed the role of 5-HT1A receptor in excisional wound healing by employing an excisional punch biopsy model on 5-Ht1a receptor knockout mice. Post-harvest analysis reve…

0301 basic medicineAgonistmedicine.drug_classmedicine.medical_treatmentwound healingPharmacology03 medical and health scienceschemistry.chemical_compound0302 clinical medicineskin regenerationmedicine5-HT1A receptorPharmacology (medical)NeurotransmitterReceptor5-Ht1a receptor knockout mice modelOriginal ResearchPharmacologySkin repairintegumentary systembusiness.industrylcsh:RM1-950serotonin3. Good healthlcsh:Therapeutics. Pharmacology030104 developmental biologyCytokinenervous systemchemistry030220 oncology & carcinogenesisKnockout mouse5-HT1A receptorWound healingbusinessFrontiers in Pharmacology
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β(3)‐Adrenoceptors in the normal and diseased urinary bladder—What are the open questions?

2019

β(3)‐Adrenoceptor agonists are used in the treatment of overactive bladder syndrome. Although the relaxant response to adrenergic stimulation in human detrusor smooth muscle cells is mediated mainly via β(3)‐adrenoceptors, the plasma concentrations of the therapeutic dose of mirabegron, the only clinically approved β(3)‐adrenoceptor agonist, are considerably lower than the EC(50) for causing direct relaxation of human detrusor, suggesting a mechanism of action other than direct relaxation of detrusor smooth muscle. However, the site and mechanism of action of β(3)‐adrenoceptor agonists in the bladder have not been firmly established. Postulated mechanisms include prejunctional suppression o…

0301 basic medicineAgonistmedicine.medical_specialtyAdrenergic receptormedicine.drug_classUrinary BladderAdrenergic beta-3 Receptor Agonistsurologic and male genital diseasesThemed Section: Review Articles03 medical and health sciences0302 clinical medicineTherapeutic indexDesensitization (telecommunications)Internal medicineMedicineAnimalsHumansPharmacologyUrinary bladderRelaxation (psychology)business.industry030104 developmental biologymedicine.anatomical_structureEndocrinologyMechanism of actionReceptors Adrenergic beta-3medicine.symptombusinessMirabegron030217 neurology & neurosurgerymedicine.drug
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Dual Role of Endogenous Serotonin in 2,4,6-Trinitrobenzene Sulfonic Acid-Induced Colitis.

2016

Background and Aims: Changes in gut serotonin content have been described in Inflammatory Bowel Disease and in different experimental models of colitis: the critical role of this monoamine in the pathogenesis of chronic gastrointestinal inflammation is gradually emerging. Aim of the present study was to evaluate the contribution of endogenous serotonin through the activation of its specific receptor subtypes to the local and systemic inflammatory responses in an experimental model of Inflammatory Bowel Disease. Methods: Colitis was induced by intrarectal 2,4,6-TriNitroBenzene Sulfonic acid in mice subacutely treated with selective antagonists of 5-HT1A (WAY100135), 5-HT2A (Ketanserin), 5-HT…

0301 basic medicineAgonistmedicine.medical_specialtyKetanserinmedicine.drug_classInflammationBiology5-HT2A receptorInflammatory bowel diseaseProinflammatory cytokine03 medical and health sciences0302 clinical medicineInternal medicinemedicinePharmacology (medical)5-HT1A receptorColitisReceptorintestineOriginal ResearchPharmacologylcsh:RM1-950apoptosismedicine.disease030104 developmental biologyEndocrinologylcsh:Therapeutics. Pharmacologyinflammation030211 gastroenterology & hepatologySerotoninmedicine.symptommedicine.drugFrontiers in pharmacology
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Corrigendum: Resolvin D1 Modulates the Intracellular VEGF-Related miRNAs of Retinal Photoreceptors Challenged With High Glucose

2020

Abstract Stimulation of retinal photoreceptors with elevated glucose concentration (30 mM) for 96 hours, served as diabetic retinopathy in-vitro model to study Resolvin D1 (50 nM) effects on neovascularization. VEGF and anti-angiogenic miR-20a-3p, miR-20a-5p, miR-106a-5p and miR-20b expression was assessed either in photoreceptors exposed to HG or in exosomes released by those cells. High glucose increased VEGF levels and concurrently decreased anti-angiogenic miRNAs content in photoreceptors and exosomes. RvD1 reverted the effects of glucose damage in photoreceptors and exosomal pro-angiogenic potential, tested with the HUVEC angiogenesis assay. By activating FPR2 receptor, RvD1 modulated …

0301 basic medicineAngiogenesisStimulationexosomesretinal photoreceptors exosomes miRNAs resolvin D1 VEGFNeovascularization03 medical and health scienceschemistry.chemical_compoundretinal photoreceptors0302 clinical medicinemedicinePharmacology (medical)ReceptorOriginal ResearchPharmacologyChemistrylcsh:RM1-950CorrectionRetinalTransfectionVEGFMicrovesiclesCell biology030104 developmental biologylcsh:Therapeutics. Pharmacology030220 oncology & carcinogenesismiRNAsresolvin D1medicine.symptomIntracellularFrontiers in Pharmacology
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Thymoquinone as a Potential Adjuvant Therapy for Cancer Treatment: Evidence from Preclinical Studies

2017

Thymoquinone (TQ), the main bioactive component of Nigella sativa, has been found to exhibit anticancer effects in numerous preclinical studies. Due to its multitargeting nature, TQ interferes in a wide range of tumorigenic processes and counteracts carcinogenesis, malignant growth, invasion, migration, and angiogenesis. Moreover, TQ can specifically sensitize tumor cells toward conventional cancer treatments (e.g., radiotherapy, chemotherapy, and immunotherapy) and simultaneously minimize therapy-associated toxic effects in normal cells. In this review, we summarized the adjuvant potential of TQ as observed in various in vitro and in vivo animal models and discussed the pharmacological pro…

0301 basic medicineAngiogenesismedicine.medical_treatmentthymoquinoneReviewPharmacologycancer treatment03 medical and health scienceschemistry.chemical_compound0302 clinical medicineAdjuvant therapyMedicinePharmacology (medical)preclinical studiesThymoquinonePharmacologyChemotherapybusiness.industrylcsh:RM1-950Canceradjuvant therapyImmunotherapymedicine.diseaseRadiation therapylcsh:Therapeutics. Pharmacology030104 developmental biologychemistry030220 oncology & carcinogenesisCancer researchbusinessAdjuvantFrontiers in Pharmacology
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Lyophilized Maqui (Aristotelia chilensis) Berry Induces Browning in the Subcutaneous White Adipose Tissue and Ameliorates the Insulin Resistance in H…

2019

Maqui (Aristotelia Chilensis) berry features a unique profile of anthocyanidins that includes high amounts of delphinidin-3-O-sambubioside-5-O-glucoside and delphinidin-3-O-sambubioside and has shown positive effects on fasting glucose and insulin levels in humans and murine models of type 2 diabetes and obesity. The molecular mechanisms underlying the impact of maqui on the onset and development of the obese phenotype and insulin resistance was investigated in high fat diet-induced obese mice supplemented with a lyophilized maqui berry. Maqui-dietary supplemented animals showed better insulin response and decreased weight gain but also a differential expression of genes involved in de novo…

0301 basic medicineAnthocyaninFGF21Physiologymedicine.medical_treatmentClinical BiochemistryWhite adipose tissueWhite adipose tissueBiochemistryMaqui berryAnthocyanins0302 clinical medicinemaqui berrybiologyChemistryanthocyaninsHigh-fat diethigh-fat dietLipogenesisObesitatmedicine.medical_specialtyRatolins (Animals de laboratori)030209 endocrinology & metabolismfibroblast growth factor 21carbohydrate-responsive element binding protein bArticle03 medical and health sciencesAristotelia chilensisInsulin resistancewhite adipose tissueInternal medicinemedicineObesityCarbohydrate-responsive element-binding proteinMolecular BiologybrowningdelphinidinInsulinlcsh:RM1-950Adipose tissuesCell Biologybiology.organism_classificationmedicine.diseaseTeixit adipós030104 developmental biologyEndocrinologylcsh:Therapeutics. PharmacologyMice (Laboratory animals)AlimentsThermogenesisAntioxidants
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Evaluation of Antioxidant, Anti-Inflammatory and Cytoprotective Properties of Ethanolic Mint Extracts from Algeria on 7-Ketocholesterol-Treated Murin…

2018

The present study consisted in evaluating the antioxidant, anti-inflammatory and cytoprotective properties of ethanolic extracts from three mint species (Mentha spicata L. (MS), Mentha pulegium L. (MP) and Mentha rotundifolia (L.) Huds (MR)) with biochemical methods on murine RAW 264.7 macrophages (a transformed macrophage cell line isolated from ascites of BALB/c mice infected by the Abelson leukemia virus). The total phenolic, flavonoid and carotenoid contents were determined with spectrophotometric methods. The antioxidant activities were quantified with the Kit Radicaux Libres (KRLTM), the ferric reducing antioxidant power (FRAP) and the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assays. The …

0301 basic medicineAntioxidantLipopolysaccharidePhysiologymedicine.drug_classDPPHmedicine.medical_treatmentClinical BiochemistryFlavonoidantioxidant activityphenolic compoundsPharmacologyBiochemistryArticleAnti-inflammatory03 medical and health scienceschemistry.chemical_compoundcytoprotectionmedicineanti-inflammatory activityMolecular Biology7-ketocholesterolchemistry.chemical_classificationMentha sp. ethanolic extractslcsh:RM1-950<i>Mentha</i> sp. ethanolic extractscarotenoidsInterleukinCell Biologylcsh:Therapeutics. Pharmacology030104 developmental biologychemistryflavonoidsCytokine secretionTumor necrosis factor alphaAntioxidants
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Hepatoprotective effects of extracts, fractions and compounds from the stem bark of Pentaclethra macrophylla Benth: Evidence from in vitro and in viv…

2021

Abstract Aim To identify the bioactive hepatoprotective components of the ethanol extract of Pentaclethra macrophylla stem bark using in vitro and in vivo approaches. Methods The bioguided-fractionation of the ethanol extract was based on the substances’ capacity to prevent in vitro, the lipid peroxidation of hepatocytes’ membranes induced by hydrogen peroxide. For the in vivo hepatoprotective test, mice were treated orally with the ethyl acetate (EtOAc) fraction of the ethanol extract at doses of 50 and 75 mg/kg/day for one week and subjected to d -galactosamine/lipopolysaccharide (GaIN/LPS)-induced hepatotoxicity. Blood samples were collected for alanine aminotransferase (ALAT), aspartate…

0301 basic medicineAntioxidantPentaclethra macrophyllaIsolated compoundsmedicine.medical_treatmentInterleukin-1betaLipid peroxidationStructure-activity relationshipsRM1-950AntioxidantsLipid peroxidationSuperoxide dismutase03 medical and health scienceschemistry.chemical_compoundMice0302 clinical medicineIn vivomedicineAnimalsAspartate AminotransferasesRats WistarPharmacologybiologyTraditional medicinePlant StemsChemistryPlant ExtractsTumor Necrosis Factor-alphaBergeninAlanine TransaminaseFabaceaeGeneral MedicineGlutathioneDisease Models Animal030104 developmental biologyHepatoprotectionLiverCatalase030220 oncology & carcinogenesisbiology.proteinHepatocytesPlant BarkTherapeutics. PharmacologyChemical and Drug Induced Liver InjuryGaIN/LPSHepatoprotectionBiomedicine & Pharmacotherapy
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Colon bioaccessibility under in vitro gastrointestinal digestion of a red cabbage extract chemically profiled through UHPLC‐Q‐Orbitrap HRMS

2020

Red cabbage is a native vegetable of the Mediterranean region that represents one of the major sources of anthocyanins. The aim of this research is to evaluate the antioxidant capability and total polyphenol content (TPC) of a red cabbage extract and to compare acquired data with those from the same extract encapsulated in an acid-resistant capsule. The extract, which was qualitatively and quantitatively profiled by UHPLC-Q-Orbitrap HRMS analysis, contained a high content of anthocyanins and phenolic acids, whereas non-anthocyanin flavonoids were the less abundant compounds. An in vitro gastrointestinal digestion system was utilized to follow the extract&rsquo

0301 basic medicineAntioxidantPhysiologyAcid‐resistant capsulemedicine.medical_treatmentClinical BiochemistryIn vitro gastrointestinal digestionBioaccessibilityPronaseOrbitrapBiochemistryArticlelaw.invention03 medical and health sciences0404 agricultural biotechnologyfoodNutraceuticallawmedicineUHPLC-Q-Orbitrap HRMSUHPLC‐Q‐Orbitrap HRMSFood scienceacid-resistant capsuleMolecular Biology030109 nutrition & dieteticsRed cabbageChemistrylcsh:RM1-950fungifood and beveragesCapsule04 agricultural and veterinary sciencesCell BiologyMetabolism040401 food sciencefood.foodcarbohydrates (lipids)lcsh:Therapeutics. PharmacologyantioxidantsPolyphenolUHPLC-Q-Orbitrap HRMS.AntioxidantRed cabbage
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