Search results for "porter"

showing 10 items of 920 documents

Interactions between artemisinin derivatives and P-glycoprotein

2019

Abstract Background Artemisinin was isolated and identified in 1972, which was the starting point for a new era in antimalarial drug therapy. Furthermore, numerous studies have demonstrated that artemisinin and its derivatives exhibit considerable anticancer activity both in vitro, in vivo, and even in clinical Phase I/II trials. P-glycoprotein (P-gp) mediated multi-drug resistance (MDR) is one of the most serious causes of chemotherapy failure in cancer treatment. Interestingly, many artemisinin derivatives exhibit excellent ability to overcome P-gp mediated MDR and even show collateral sensitivity against MDR cancer cells. Furthermore, some artemisinin derivatives show P-gp-mediated MDR r…

ATP Binding Cassette Transporter Subfamily BPharmaceutical ScienceAntineoplastic AgentsPharmacology03 medical and health sciences0302 clinical medicineCombined treatmentIn vivoNeoplasmsparasitic diseasesDrug DiscoverymedicineHumansATP Binding Cassette Transporter Subfamily B Member 1Artemisinin030304 developmental biologyP-glycoproteinPharmacology0303 health sciencesbiologyChemistryArtemisininsDrug Resistance MultipleCancer treatmentMultiple drug resistanceComplementary and alternative medicine030220 oncology & carcinogenesisCancer cellbiology.proteinMolecular Medicinemedicine.drugPhytomedicine
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Putative molecular determinants mediating sensitivity or resistance towards carnosic acid tumor cell responses.

2020

Abstract Background Carnosic acid (CA) is one of the main constituents in rosemary extract. It possesses valuable pharmacological properties, including anti-oxidant, anti-inflammatory, anti-microbial and anti-cancer activities. Numerous in vitro and in vivo studies investigated the anticancer profile of CA and emphasized its potentiality for cancer treatment. Nevertheless, the role of multidrug-resistance (MDR) related mechanisms for CA's anticancer effect is not yet known. Purpose We investigated the cytotoxicity of CA against known mechanisms of anticancer drug resistance (P-gp, ABCB5, BCRP, EGFR and p53) and determined novel putative molecular factors associated with cellular response to…

ATP Binding Cassette Transporter Subfamily BPharmaceutical ScienceBiologyFlow cytometry03 medical and health sciences0302 clinical medicineWestern blotCell Line TumorDrug DiscoverymedicineATP Binding Cassette Transporter Subfamily G Member 2HumansATP Binding Cassette Transporter Subfamily B Member 1Cytotoxicity030304 developmental biologyPharmacology0303 health sciencesmedicine.diagnostic_testABCB5Antineoplastic Agents PhytogenicDrug Resistance MultipleNeoplasm ProteinsBlotErbB ReceptorsComplementary and alternative medicineApoptosisDrug Resistance NeoplasmPharmacogenetics030220 oncology & carcinogenesisCancer cellAbietanesCancer researchMolecular MedicineSignal transductionTumor Suppressor Protein p53Phytomedicine : international journal of phytotherapy and phytopharmacology
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Alkamides from Echinacea angustifolia Interact with P-Glycoprotein of Primary Brain Capillary Endothelial Cells Isolated from Porcine Brain Blood Ves…

2013

The blood-brain barrier prevents the passage of toxic compounds from blood circulation into brain tissue. Unfortunately, drugs for the treatment of neurodegenerative diseases, brain tumors, and other diseases also do not cross the blood-brain barrier. In the present investigation, we used isolated porcine brain capillary endothelial cells and a flow cytometric calcein-AM assay to analyze inhibition of P-glycoprotein, a major constituent of the blood-brain barrier. We tested 8 alkamides isolated from Echinacea angustifolia and found that four of them inhibited P-glycoprotein-mediated calcein transport in porcine brain capillary endothelial cells.

ATP Binding Cassette Transporter Subfamily BPolyunsaturated AlkamidesSwinePharmaceutical ScienceATP-binding cassette transporterCapillary endothelial cellsPharmacologyBlood–brain barrierEchinaceaAnalytical Chemistrychemistry.chemical_compoundDrug DiscoverymedicineAnimalsCells CulturedP-glycoproteinPharmacologyDose-Response Relationship DrugMolecular StructurebiologyEchinacea angustifoliaOrganic ChemistryBrainEndothelial CellsBiological TransportFlow CytometryFluoresceinsbiology.organism_classificationCalceinmedicine.anatomical_structureComplementary and alternative medicinechemistryBlood-Brain BarrierBlood circulationbiology.proteinMolecular MedicinePorcine brainPlanta Medica
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Cytotoxicity of the indole alkaloid reserpine from Rauwolfia serpentina against drug-resistant tumor cells.

2015

Abstract Background: The antihypertensive reserpine is an indole alkaloid from Rauwolfia serpentina and exerts also profound activity against cancer cells in vitro and in vivo. The present investigation was undertaken to investigate possible modes of action to explain its activity toward drug-resistant tumor cells. Material and methods: Sensitive and drug-resistant tumor cell lines overexpressing P-glycoprotein (ABCB1/MDR1), breast cancer resistance protein (ABCG2/BCRP), mutation-activated epidermal growth factor receptor (EGFR), wild-type and p53-knockout cells as well as the NCI panel of cell lines from different tumor origin were analyzed. Reserpine's cytotoxicity was investigated by res…

ATP Binding Cassette Transporter Subfamily BReserpineAngiogenesisPharmaceutical SciencePharmacologyBiologyRauwolfiaGene Knockout TechniquesCell Line TumorDrug DiscoverymedicineATP Binding Cassette Transporter Subfamily G Member 2HumansCytotoxicityPharmacologyWnt signaling pathwayReserpineAntineoplastic Agents PhytogenicDrug Resistance MultipleNeoplasm ProteinsErbB ReceptorsMolecular Docking SimulationComplementary and alternative medicineCell cultureApoptosisDoxorubicinDrug Resistance NeoplasmCancer cellMolecular MedicineATP-Binding Cassette TransportersErlotinibTumor Suppressor Protein p53medicine.drugPhytomedicine : international journal of phytotherapy and phytopharmacology
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Selective downregulation of the MDR1 gene product in Caco-2 cells by stable transfection to prove its relevance in secretory drug transport.

2005

Considerable interest is focused on overcoming multidrug resistance (MDR) in cancer chemotherapy. The in vitro experiments to characterize P-glycoprotein's (P-gp) function and to decrease its effects have led to a variety of strategies such as addition of competitors or supplementation of the medium with oligonucleotides complementary to the 5'-end of the MDR1-mRNA. For the Caco-2 cell line, an in vitro model for absorption screening, expressing multiple transporters including P-gp, which pumps substances back into the apical solution, P-gp activity might mask other relevant transport proteins' activity. The objective of the present study was to construct a Caco-2 subline with reduced P-gp …

ATP Binding Cassette Transporter Subfamily BTime FactorsPharmaceutical ScienceDown-RegulationBiologyTransfectionPermeabilityPropanolaminesDownregulation and upregulationDrug DiscoveryHumansNorthern blotOligonucleotideReverse Transcriptase Polymerase Chain ReactionElectroporationBiological TransportTransfectionFlow CytometryMolecular biologyIn vitroTransport proteinClone CellsMutagenesis InsertionalVerapamilCell cultureMolecular MedicineCaco-2 CellsGenes MDRMolecular pharmaceutics
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Pharmacogenomic Characterization of Cytotoxic Compounds from Salvia officinalis in Cancer Cells.

2015

Salvia officinalis is used as a dietary supplement with diverse medicinal activity (e.g. antidiabetic and antiatherosclerotic effects). The plant also exerts profound cytotoxicity toward cancer cells. Here, we investigated possible modes of action to explain its activity toward drug-resistant tumor cells. Log10IC50 values of two constituents of S. officinalis (ursolic acid, pomolic acid) were correlated to the expression of ATP-binding cassette (ABC) transporters (P-glycoprotein/ABCB1/MDR1, MRP1/ABCC1, BCRP/ABCG2) and epidermal growth factor receptor (EGFR) or mutations in RAS oncogenes and the tumor suppressor gene TP53 of the NCI panel of cell lines. Gene expression profiles predicting se…

ATP Binding Cassette Transporter Subfamily BTumor suppressor geneLeupeptinsPharmaceutical ScienceATP-binding cassette transporterBreast NeoplasmsBiologymedicine.disease_causeAnalytical Chemistrychemistry.chemical_compoundfoodUrsolic acidDrug DiscoveryGene expressionmedicineHumansOleanolic AcidSalvia officinalisPharmacologyMutationPlants MedicinalMolecular StructureOrganic ChemistrySalvia officinalisNF-kappa BGenes erbB-1Antineoplastic Agents Phytogenicfood.foodTriterpenesComplementary and alternative medicinechemistryBiochemistryDrug Resistance NeoplasmPharmacogeneticsCancer cellMolecular MedicineATP-Binding Cassette TransportersSignal transductionSignal TransductionJournal of natural products
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Binding mode analysis of ABCA7 for the prediction of novel Alzheimer's disease therapeutics

2021

Graphical abstract

ATP Adenosine-triphosphateNBD nucleotide binding domainGSH reduced glutathionePolypharmacologyAlzheimer’s disease (AD)ATP-binding cassette transporterHTS high-throughput screeningBiochemistryABCA7Structural BiologyPLIF protein ligand interactionMSD membrane spanning domainPDB protein data bankTM transmembrane helixABC ATP-binding cassetteMultitarget modulation (PANABC)RMSD root mean square distanceABC transporter (ABCA1 ABCA4 ABCA7)Computer Science ApplicationsMOE Molecular Operating EnvironmentPharmacophoreSNP single-nucleotide polymorphismBiotechnologyResearch ArticleBBB blood-brain barrierBiophysicsDrug designComputational biologyBiologyAD Alzheimer’s diseasePET positron emission tomographyIC intracellular helixAPP amyloid precursor proteincryo-EM cryogenic-electron microscopyGeneticsHomology modelingBinding siteRational drug design and developmentComputingMethodologies_COMPUTERGRAPHICSNBD-cholesterol 7-nitro-2-13-benzoxadiazol-4-yl-cholesterolTransporterPSO particle swarm optimizationPET tracer (PETABC)ECD extracellular domainR-domain/region regulatory domain/regionABCA1biology.proteinEH extracellular helixTP248.13-248.65BODIPY-cholesterol 44-difluoro-4-bora-3a4a-diaza-s-indacene-cholesterolComputational and Structural Biotechnology Journal
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Inhibition of ATP-Binding Cassette Transporters by Chinese Herbs and Phytochemicals

2012

The gene family of ATP-binding cassette (ABC) transporters is widely distributed over the evolutionary tree of life from bacteria to man. In cancer, several ABC transporters are involved in the transport of anticancer drugs. This leads to the development of resistance to a broad spectrum of anticancer agents, termed multidrug resistance. An attractive strategy to overcome multidrug resistance is to block the transport function of ABC transporters leading to lethal intracellular concentrations of anticancer drugs. Efforts to identify transport inhibitors lead to a huge amount of chemical substances, none of which successfully passed clinical trials in cancer patients because of high toxicity…

Abcg2CancerATP-binding cassette transporterTransporterBiologymedicine.diseaseMultiple drug resistancechemistry.chemical_compoundchemistryBiochemistrymedicinebiology.proteinGene familyXenobioticFunction (biology)
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Cytotoxicity of cucurbitacin E from Citrullus colocynthis against multidrug-resistant cancer cells

2019

Abstract Background Cucurbitacin E (CuE) is an oxygenated tetracyclic triterpenoid isolated from the fruits of Citrullus colocynthis (L.) Schrad. Purpose This study outlines CuE's cytotoxic activity against drug-resistant tumor cell lines. Three members of ABC transporters superfamily, P-glycoprotein (P-gp), breast cancer resistance protein (BCRP) and ABCB5 were investigated, whose overexpression in tumors is tightly linked to multidrug resistance. Further factors of drug resistance studied were the tumor suppressor TP53 and the epidermal growth factor receptor (EGFR). Methods Cytotoxicity assays (resazurin assays) were used to investigate the activity of Citrullus colocynthis and CuE towar…

Abcg2Drug ResistancePharmaceutical ScienceATP-binding cassette transporterMicroarraySubfamily Gchemistry.chemical_compoundGene Knockout Techniques0302 clinical medicineEpidermal growth factorPhytogenicDrug DiscoveryATP Binding Cassette Transporter Subfamily G Member 2Cancer0303 health sciencesTumorLeukemiabiologyChemistryABCB5TransfectionCell cycleNeoplasm ProteinsGene Expression Regulation NeoplasticErbB ReceptorsMolecular Docking SimulationSubfamily B030220 oncology & carcinogenesisMolecular MedicineCitrullus colocynthiMember 2Member 1ATP Binding Cassette Transporter Subfamily BATP Binding Cassette TransporterAntineoplastic AgentsCell Line03 medical and health sciencesCell Line TumorHumansATP Binding Cassette Transporter Subfamily B Member 1030304 developmental biologyCucurbitacin EPharmacologyNeoplasticTraditional herbal medicineCancer; Citrullus colocynthis; Drug resistance; Microarray; Traditional herbal medicine; ATP Binding Cassette Transporter Subfamily B; ATP Binding Cassette Transporter Subfamily B Member 1; ATP Binding Cassette Transporter Subfamily G Member 2; Antineoplastic Agents Phytogenic; Cell Line Tumor; Citrullus colocynthis; Doxorubicin; Drug Resistance Neoplasm; ErbB Receptors; Gene Expression Regulation Neoplastic; Gene Knockout Techniques; Humans; Leukemia; Molecular Docking Simulation; Neoplasm Proteins; Triterpenes; Tumor Suppressor Protein p53Antineoplastic Agents PhytogenicTriterpenesComplementary and alternative medicineGene Expression RegulationDrug Resistance NeoplasmDoxorubicinCancer cellbiology.proteinCancer researchNeoplasmCitrullus colocynthisTumor Suppressor Protein p53
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Trans-epithelial transport of the betalain pigments indicaxanthin and betanin across Caco-2 cell monolayers and influence of food matrix.

2012

Purpose: This study investigated the absorption mechanism of the phytochemicals indicaxanthin and betanin and the influence of their food matrix (cactus pear and red beet) on the intestinal transport. Methods: Trans-epithelial transport of dietary-consistent amounts of indicaxanthin and betanin in Caco-2 cell monolayers seeded on TranswellR inserts was measured in apical to basolateral (AP-BL) and basolateral to apical (BL-AP) direction, under an inwardly directed pH gradient (pH 6.0/7.4, AP/BL) mimicking luminal and serosal sides of human intestinal epithelium. The effect of inhibitors of membrane transporters on the absorption was also evaluated. Contribution of the paracellular route was…

Absorption (pharmacology)Cell Membrane PermeabilityChemical PhenomenaPyridinesBetalainsindicaxanthinMedicine (miscellaneous)Plant RootsIntestinal absorptionAntioxidantsCaco-2 cellchemistry.chemical_compoundPigmentSettore BIO/10 - BiochimicaHumansbetalains;intestinal absorption; Caco-2 cells; betalainic food; indicaxanthin; betaninFood scienceIntestinal MucosaBetaninbetalainic foodPEARNutrition and DieteticsbetaninbetalainCell PolarityFood Coloring AgentsOpuntiaBiological TransportPigments BiologicalBetaxanthinsIntercellular JunctionschemistryIntestinal AbsorptionCaco-2visual_artFruitFood Fortifiedvisual_art.visual_art_mediumATP-Binding Cassette TransportersDigestionBetacyaninsBeta vulgarisCaco-2 CellsDigestionIndicaxanthinEuropean journal of nutrition
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