Search results for "Drug resistance"

showing 10 items of 953 documents

Human ABCB1 confers cells resistance to cytotoxic guanidine alkaloids from Pterogyne nitens.

2015

Multidrug resistance (MDR) caused by human ABCB1 (P-glycoprotein/MDR1) is one of the major obstacles in chemotherapy. To understand the mechanism of MDR by ABCB1 and circumvent the MDR, in the present study, we established human ABCB1-expressing cells (Flp-In-293/ABCB1 cells) and examined the cytotoxic effects of four guanidine alkaloids from Pterogyne nitens (galegine, nitensidine A, pterogynidine and pterogynine) using Flp-In-293/Mock and Flp-In-293/ABCB1 cells. The activity of ABCB1 in Flp-In-293/ABCB1 cells were confirmed by typical substrates for ABCB1 (taxol and vinblastine) in MTT assay. Flp-In-293/ABCB1 cells were also resistant to the four guanidine alkaloids as well as taxol and v…

ATP Binding Cassette Transporter Subfamily BCell SurvivalATPaseBiomedical EngineeringGuanidinesBiomaterialschemistry.chemical_compoundAlkaloidsmedicineCytotoxic T cellHumansMTT assayGuanidineCytotoxicityP-glycoproteinCaesalpiniabiologyDose-Response Relationship DrugCytotoxinsGeneral MedicineDrug Resistance MultipleVinblastineMultiple drug resistanceHEK293 CellschemistryBiochemistrybiology.proteinMultidrug Resistance-Associated Proteinsmedicine.drugBio-medical materials and engineering
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Cytotoxicity of 35 medicinal plants from Sudan towards sensitive and multidrug-resistant cancer cells

2015

Abstract Background Cancer is a complex disease with multiple genetic and epigenetic alterations. Since decades, the hallmark of cancer therapy is chemotherapy. Cytotoxic drugs erase rapidly dividing cells without sufficient differentiation between normal and cancerous cells resulting in severe side effects in normal tissues. Recently, strategies for cancer treatment focused on targeting specific proteins involved in tumor growth and progression. The present study was designed to investigate the cytotoxicity of 65 crude extracts from 35 Sudanese medicinal plants towards various cancer cell lines expressing molecular mechanisms of resistance towards classical chemotherapeutics (two ATP-bindi…

ATP Binding Cassette Transporter Subfamily BCytoskeleton organizationCell SurvivalDNA repairBiologyPharmacologySudanSesquiterpenes GuaianeImmune systemCell Line TumorOxazinesDrug DiscoveryHumansATP Binding Cassette Transporter Subfamily B Member 1EpigeneticsCytotoxicityPharmacologyPlants MedicinalComputational BiologyAntineoplastic Agents PhytogenicDrug Resistance MultipleGene expression profilingXanthenesDrug Resistance NeoplasmPharmacogeneticsCell cultureCancer cellCancer researchIndicators and ReagentsTumor Suppressor Protein p53SesquiterpenesJournal of Ethnopharmacology
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Nitensidine A, a guanidine alkaloid from Pterogyne nitens, is a novel substrate for human ABC transporter ABCB1.

2014

The Pterogyne nitens (Fabaceae) tree, native to South America, has been found to produce guanidine alkaloids as well as bioactive flavonols such as kaempferol, quercetin, and rutin. In the present study, we examined the possibility of interaction between human ATP-binding cassette (ABC) transporter ABCB1 and four guanidine alkaloids isolated from P. nitens (i.e., galegine, nitensidine A, pterogynidine, and pterogynine) using human T cell lymphoblast-like leukemia cell line CCRF-CEM and its multi-drug resistant (MDR) counterpart CEM/ADR5000. In XTT assays, CEM/ADR5000 cells were resistant to the four guanidine alkaloids compared to CCRF-CEM cells, although the four guanidine alkaloids exhibi…

ATP Binding Cassette Transporter Subfamily BLeukemia T-CellStereochemistryATPasePharmaceutical ScienceATP-binding cassette transporterGuanidineschemistry.chemical_compoundStructure-Activity RelationshipCell Line TumorDrug DiscoveryHumansheterocyclic compoundsBinding siteGuanidineCytotoxicityP-glycoproteinPharmacologyAdenosine TriphosphatasesbiologyPlant ExtractsAlkaloidFabaceaeFluoresceinsAntineoplastic Agents PhytogenicDrug Resistance MultipleMolecular Docking SimulationComplementary and alternative medicinechemistryBiochemistryVerapamilDrug Resistance Neoplasmbiology.proteinMonoterpenesMolecular MedicineATP-Binding Cassette TransportersKaempferolPhytotherapyPhytomedicine : international journal of phytotherapy and phytopharmacology
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The lignan, (-)-sesamin reveals cytotoxicity toward cancer cells: pharmacogenomic determination of genes associated with sensitivity or resistance.

2013

(-)-Sesamin is a lignan present in sesam oil and a number of medicinal plants. It exerts various pharmacological effects, such as prevention of hyperlipidemia, hypertension, and carcinogenesis. Moreover, (-)-sesamin has chemopreventive and anticancer activity in vitro and in vivo. Multidrug resistance (MDR) of tumors leads to fatal treatment outcome in many patients and novel drugs able to kill multidrug-resistant cells are urgently needed. P-glycoprotein (MDR1/ABCB1) is the best known ATP-binding cassette (ABC) drug transporter mediating MDR. ABCB5 is a close relative to ABCB1, which also mediates MDR. We found that the mRNA expressions of ABCB1 and ABCB5 were not related to the 50% inhibi…

ATP Binding Cassette Transporter Subfamily BPharmaceutical ScienceATP-binding cassette transporterDioxolesBiologyPharmacologymedicine.disease_causeLignanschemistry.chemical_compoundSesaminCell Line TumorNeoplasmsDrug DiscoverymedicineCluster AnalysisHumansATP Binding Cassette Transporter Subfamily B Member 1GenePharmacologyPlant ExtractsGene Expression ProfilingABCB5Multiple drug resistanceMitochondrial respiratory chainHEK293 CellsComplementary and alternative medicinechemistryDrug Resistance NeoplasmCancer cellMolecular MedicineDrug Screening Assays AntitumorCarcinogenesisPhytotherapyPhytomedicine : international journal of phytotherapy and phytopharmacology
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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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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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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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Acid sensitivity of neomycin-resistant mutants ofOenococcus oeni: a relationship between reduction of ATPase activity and lack of malolactic activity

1999

Mutants of Oenococcus oeni were isolated as spontaneous neomycin-resistant mutants. Three of these mutants harbored a significantly reduced ATPase activity that represented 50% of that of the wild-type strain. Their growth rates were also impaired at pH 5.3 (46-86% of the wild-type level). However, the profiles of sugar consumption appeared identical to those of the parental strain. At pH 3.2, all the mutant strains failed to grow and a drastic decrease in viability was observed after an acid shock. Surprisingly, all the isolated mutants were devoid of malolactic activity. These results suggest that the ATPase and malolactic activities of O. oeni are linked to each other and play a crucial …

ATPaseMutantMalatesMicrobiologyMicrobiologyGeneticsmedicineMalolactic fermentationLactic AcidMolecular BiologyHeat-Shock ProteinsOenococcus oeniAdenosine Triphosphataseschemistry.chemical_classificationbiologyStrain (chemistry)Drug Resistance MicrobialNeomycinNeomycinHydrogen-Ion Concentrationbiology.organism_classificationAnti-Bacterial AgentsGram-Positive CocciEnzymeBiochemistrychemistrybiology.proteinHeat-Shock ResponseLeuconostocBacteriamedicine.drugFEMS Microbiology Letters
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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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