Search results for "Mace"

showing 10 items of 4713 documents

Powerful tumor cell growth-inhibiting activity of a synthetic derivative of atractyligenin: Involvement of PI3K/Akt pathway and thioredoxin system

2014

The semi-synthetic ent-kaurane 15-ketoatractyligenin methyl ester (SC2017) has been previously reported to possess high antiproliferative activity against several solid tumor-derived cell lines. Our study was aimed at investigating SC2017 tumor growth-inhibiting activity and the underlying mechanisms in Jurkat cells (T-cell leukemia) and xenograft tumor models. METHODS: Cell viability was evaluated by MTT assay. Cell cycle progression, reactive oxygen species (ROS) elevation and apoptotic hallmarks were monitored by flow cytometry. Inhibition of thioredoxin reductase (TrxR) by biochemical assays. Levels and/or activation status of signaling proteins were assessed by western blotting. Xenogr…

CellBiophysicsAntineoplastic AgentsApoptosisAtractylosideBiologyCell cycleBiochemistryJurkat cellsMicePhosphatidylinositol 3-KinasesThioredoxinsTumor Cells CulturedmedicineAnimalsHumansMTT assayViability assaySettore BIO/15 - Biologia FarmaceuticaMolecular BiologyProtein kinase BPI3K/AKT/mTOR pathwayCell ProliferationPI3K/AktHCT 116 xenograftCytochromes cApoptosiThioredoxin systemSettore CHIM/06 - Chimica OrganicaCell cycleXenograft Model Antitumor AssaysCell biologymedicine.anatomical_structureCaspasesCancer researchThioredoxinDiterpenes KauraneProto-Oncogene Proteins c-aktEnt-kaurane
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Comparison between tumors in plants and human beings: Mechanisms of tumor development and therapy with secondary plant metabolites

2019

Abstract Background Human tumors are still a major threat to human health and plant tumors negatively affect agricultural yields. Both areas of research are developing largely independent of each other. Treatment of both plant and human tumors remains unsatisfactory and novel therapy options are urgently needed. Hypothesis The concept of this paper is to compare cellular and molecular mechanisms of tumor development in plants and human beings and to explore possibilities to develop novel treatment strategies based on bioactive secondary plant metabolites. The interdisciplinary discourse may unravel commonalities and differences in the biology of plant and human tumors as basis for rational …

Cellular immunityPhytochemicalsPlant TumorsPhysical CarcinogenesisSecondary MetabolismPharmaceutical ScienceBiologymedicine.disease_cause03 medical and health sciences0302 clinical medicineImmune systemCancer stem cellNeoplasmsDrug DiscoveryBiological CarcinogenesisPlant defense against herbivorymedicineAnimalsHumansPlant ImmunityPlant Physiological PhenomenaPlant Diseases030304 developmental biologyPharmacology0303 health sciencesAntibiotics Antineoplasticfungifood and beveragesPlantsAntineoplastic Agents PhytogenicComplementary and alternative medicineAgrobacterium tumefaciensDrug Resistance Neoplasm030220 oncology & carcinogenesisCancer researchMolecular MedicineCarcinogenesisPhytomedicine
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Novel Lipid and Polymeric Materials as Delivery Systems for Nucleic Acid Based Drugs

2015

Nucleic acid based drugs (NADBs) are short DNA/RNA molecules that include among others, antisense oligonucleotides, aptamers, small interfering RNAs and micro-interfering RNAs. Despite the different mechanisms of actions, NABDs have the ability to combat the effects of pathological gene expression in many experimental systems. Thus, nowadays, NABDs are considered to have a great therapeutic potential, possibly superior to that of available drugs. Unfortunately, however, the lack of effective delivery systems limits the practical use of NABDs. Due to their hydrophilic nature, NABDs cannot efficiently cross cellular membrane; in addition, they are subjected to fast degradation by cellular and…

Cellular membranePolymersAntisense oligonucleotides aptamers carbon nanotubes exososomes liposomes miRNA polymers siRNAAptamerClinical BiochemistryNanotechnologyAnimals; Humans; Lipids; Nanoparticles; Nanotubes Carbon; Nucleic Acids; Polymers; Drug Delivery SystemsBiologyNanoparticleDrug Delivery SystemsNucleic AcidsAnimalsHumansAvailable drugsPolymerPharmacologyNanotubesNucleic AcidAnimalNanotubes CarbonCarbon chemistryRNALipidLipidsCarbonSettore CHIM/09 - Farmaceutico Tecnologico ApplicativoAntisense oligonucleotidesNucleic acidNanoparticlesHuman
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Volatile constituents of aerial parts of three endemic Centaurea species from Turkey: Centaurea amanicola Hub.-Mor., Centaurea consanguinea DC. and C…

2008

The volatile constituents of the aerial parts of Centaurea amanicola Hub.-Mor., Centaurea consanguinea DC. and Centaurea ptosimopappa Hayek were extracted by hydrodistillation and analysed by GC and GC-MS. Altogether 94 components were identified. Sesquiterpenoids, fatty acids and carbonylic compounds were the most abundant components in the oils. Hexadecanoic acid and (Z,Z )-9,12-octadecadienoic acid were the main fatty acids in all the examined samples, that showed different patterns of composition. The study on the biological activity of the oils showed an action mainly against the Gram-positive pathogens.

Centaurea amanicola Centaurea consanguinea Centaurea ptosimopappa essential oil GC/MS antimicrobial activityChromatography GasTurkeyOils VolatilePlant OilsCentaureaSettore CHIM/06 - Chimica OrganicaSettore BIO/15 - Biologia FarmaceuticaMicrobial Sensitivity TestsPlant Components AerialGram-Positive BacteriaGas Chromatography-Mass SpectrometryAnti-Bacterial AgentsNatural product research
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Chemical composition of the essential oils of Centaurea formanekii and Centaurea orphanidea ssp. thessala, two Centaurea species growing wild in Gree…

2012

The volatile constituents of the aerial parts of Centaurea formanekii Halacsy and the aerial parts, capitula and roots of C. orphanidea Heldr. & Sart. ex Boiss. ssp. thessala (Hausskn.) Dostál from Greece were extracted by hydrodistillation and analyzed. The main components in C. formanekii were hexadecanoic acid (13.6%), δ-elemene (9.1%), and spathulenol (6.9%). The main components in C. orphanidea ssp. thessala were γ-elemene (26.1%) and caryophyllene oxide (13.2%) in the aerial parts, hexadecanoic acid (33.5%) and heptacosane (6.3%) in the capitula, and hexadecanoic acid methyl ester (22.0%) and α-chamigrene (14.0%) in the roots. The chemotaxonomic significance with respect to other …

Centaurea formanekiiCaryophyllene oxideC. orphanidea ssp. thessalaγ-elemeneSettore CHIM/06 - Chimica OrganicaSettore BIO/15 - Biologia FarmaceuticaAsteraceaeHexadecanoic acidMusk xyleneEssential oil
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Chemical composition of the essential oil of the local endemics Centaurea davidovii and C. parilica (Asteraceae, sect. Lepteranthus) from Bulgaria

2014

In the present study the chemical compositions of the essential oils from aerial parts of Centaurea davidovii Urum. and C. parilica Stoj. & Stef., both endemic to Bulgaria, were evaluated by GC and GC-MS. The main components of C. davidovii were β-eudesmol (13.9%), spathulenol (13.3%), caryophyllene oxide (10.1%) and ( Z)-phytol (5.4%). The main components of C parilica were hexadecanoic acid (39.2%), ( Z, Z)-9,12-octadecadienoic acid (11.9%), caryophyllene oxide (6.8%) and spathulenol (6.6%). In order to compare the essential oils composition of these taxa and of related species a PCA analysis was carried out.

CentaureaC. davidoviiPlant Scienceβ-eudesmolessential oilSpathulenollaw.inventionlawDrug DiscoveryBotanyhexadecanoic acidspathulenolOils VolatileCentaurea specieSettore BIO/15 - Biologia FarmaceuticaC. parilicaBulgariaEndemismChemical compositionessential oilsEssential oilPharmacologybiologyPlant ExtractsGeneral MedicineSettore CHIM/06 - Chimica OrganicaCentaurea davidoviiAsteraceaebiology.organism_classificationComplementary and alternative medicineCaryophyllene oxideCentaureaCentaurea parilica
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Essential oil of Citrus lumia Risso: Phytochemical profile, antioxidant properties and activity on the central nervous system

2018

Citrus lumia Risso Essential oil Antioxidant properties Anti-cholinesterase activity Cytotoxicity Neuroactive effects 1. Introduction Plants that produce essential oils (EOs) represent a large part of natural flora and an important resource in various fields such as pharmaceutical, food and cosmetic industries, due to their flavor, fra- grance and biological activity (Swamy et al., 2016). EOs play a pivotal role in the growth and colonization of plants, giving color and scent to reproductive organs, attracting pollinators, favoring seed dispersion (Sharifi-Rad et al., 2017), and defending the plant against abiotic (light, temperature, etc.) and biotics (herbivores, harmful insects and pa- t…

Central Nervous System0106 biological sciences0301 basic medicineCitrusAntioxidantCytotoxicitymedicine.medical_treatmentToxicology01 natural sciencesAntioxidantsEssential oillaw.inventionTerpeneMicechemistry.chemical_compoundLinaloollawSettore BIO/15 - Biologia FarmaceuticaFood scienceCitrus lumia Risso Essential oil Antioxidant properties Anti-cholinesterase activity Cytotoxicity Neuroactive effectsbiologyGeneral MedicineNeuroprotective AgentsPhytochemicalNeuroactive effectsAnti-cholinesterase activityAcyclic MonoterpenesAntioxidant propertiesNeuroprotectionGas Chromatography-Mass SpectrometryCell Line03 medical and health sciencesCyclohexenesOils VolatilemedicineAnimalsRats WistarIC50Essential oilCholinesteraseCell-Free SystemTerpenesAnti-cholinesterase activity; Antioxidant properties; Citrus lumia Risso; Cytotoxicity; Essential oil; Neuroactive effects; Food Science; Toxicology030104 developmental biologychemistryMicroscopy Electron ScanningMonoterpenesbiology.proteinCitrus lumia RissoCholinesterase InhibitorsLimonene010606 plant biology & botanyFood ScienceFood and Chemical Toxicology
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Lavandula angustifolia Essential Oil and Linalool Counteract Social Aversion Induced by Social Defeat

2018

Many vegetable extracts, essential oils, and their main constituents are active on the Central Nervous System (CNS). In fact, they have been used as sedatives, hypnotics, or tranquilizers for their activity in treating CNS disorders. In this research, we studied the possible activities of Lavandula angustifolia (LA) essential oil and of its main constituent, linalool, as anti-stress compounds on anxiety and social interaction and their in vitro effects on proteins (pERK and PKA) involved in the transmission of the signal. An acute intraperitoneal injection of linalool (100 mg/kg) and of LA essential oil (200 mg/kg) reduced motor activity without any anxiolytic effect, but significantly incr…

Central Nervous System30030301 basic medicinelinaloolLavandulaVolatilePharmaceutical SciencePharmacologyAnalytical Chemistrylaw.inventionSocial defeatMicechemistry.chemical_compound0302 clinical medicineAnti-Anxiety AgentsLinaloolCentral Nervous System Diseasessocial defeatlawDrug DiscoveryHypnotics and SedativesEssential oil; Lavandula angustifolia; Linalool; Social defeat; Animals; Anti-Anxiety Agents; Antidepressive Agents; Central Nervous System; Central Nervous System Diseases; Humans; Hypnotics and Sedatives; Interpersonal Relations; Lavandula; Mice; Monoterpenes; Oils Volatile; Analytical Chemistry; Chemistry (miscellaneous); Molecular Medicine; 3003; Drug Discovery3003 Pharmaceutical Science; Physical and Theoretical Chemistry; Organic ChemistryLavandula angustifolia<i>Lavandula angustifolia</i>Antidepressive AgentsLavandulaChemistry (miscellaneous)Molecular MedicineAntidepressantmedicine.drug_classAnxiolyticArticleessential oillcsh:QD241-44103 medical and health scienceslcsh:Organic chemistrymedicineAnimalsHumansInterpersonal RelationsPhysical and Theoretical ChemistryEssential oilbusiness.industryDrug Discovery3003 Pharmaceutical ScienceOrganic Chemistry030104 developmental biologyAnti-Anxiety AgentschemistryLavandula angustifoliaMonoterpenesbusinessOils030217 neurology & neurosurgeryMolecules
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Hunting for the high-affinity state of G-protein-coupled receptors with agonist tracers: Theoretical and practical considerations for positron emissi…

2019

Abstract The concept of the high‐affinity state postulates that a certain subset of G‐protein‐coupled receptors is primarily responsible for receptor signaling in the living brain. Assessing the abundance of this subset is thus potentially highly relevant for studies concerning the responses of neurotransmission to pharmacological or physiological stimuli and the dysregulation of neurotransmission in neurological or psychiatric disorders. The high‐affinity state is preferentially recognized by agonists in vitro. For this reason, agonist tracers have been developed as tools for the noninvasive imaging of the high‐affinity state with positron emission tomography (PET). This review provides an…

Central Nervous SystemBETA-ADRENERGIC-RECEPTORpositron emission tomographyagonist high-affinity stateD-2/3 AGONISTG-protein-coupled receptorsReview ArticleReceptors G-Protein-Coupledchemistry.chemical_compound0302 clinical medicineDrug DiscoveryReceptorNeurotransmitterReview Articles0303 health sciencesmedicine.diagnostic_testNONHUMAN PRIMATE BRAINEndocytosisTEST-RETEST REPRODUCIBILITYPositron emission tomographyG‐protein‐coupled receptors030220 oncology & carcinogenesisENDOGENOUS OPIOID RELEASEMolecular MedicineIN-VIVO BINDINGSignal TransductionAgonistNoninvasive imagingexperimental designmedicine.drug_classNeurotransmissionRAT-BRAINneurotransmittersagonist high‐affinity state03 medical and health sciencesIn vivomedicineAnimalsHumanshuman brain030304 developmental biologyG protein-coupled receptorPharmacologyDOPAMINE D2(HIGH) RECEPTORS5-HT1A RECEPTORSchemistryPositron-Emission TomographyPET RADIOLIGANDRadiopharmaceuticalsNeuroscienceMedicinal research reviews
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In silico prediction of central nervous system activity of compounds. Identification of potential pharmacophores by the TOPS–MODE approach

2004

The central nervous system (CNS) activity has been investigated by using a topological substructural molecular approach (TOPS-MODE). A discriminant analysis to classify CNS and non-CNS drugs was developed on a data set (302 compounds) of great structural variability where more than 81% (247/302) were well classified. Randic's orthogonalization procedures was carried out to allow the interpretation of the model and to avoid the collinearity among descriptors. The discriminant model was assessed by a leave-n-out (when n varies from 2 to 20) cross-validation procedure (79.94% of correct classification), an external prediction set composed by 78 CNS/non-CNS drugs (80.77% of correct classificati…

Central Nervous SystemMolecular modelChemistryStereochemistryIn silicoOrganic ChemistryClinical BiochemistryPharmaceutical ScienceCollinearityComputational biologyLinear discriminant analysisModels BiologicalBiochemistryCross-validationPolar surface areaStructure-Activity RelationshipPredictive Value of TestsDrug DiscoveryMolecular MedicinePharmacophoreMolecular BiologyOrthogonalizationCentral Nervous System AgentsBioorganic &amp; Medicinal Chemistry
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