Search results for "HCT116 Cells"

showing 10 items of 50 documents

Bioactive pyrrole alkaloids isolated from the Red Sea : marine sponge Stylissa carteri

2017

Abstract Fifteen pyrrole alkaloids were isolated from the Red Sea marine sponge Stylissa carteri and investigated for their biological activities. Four of them were dibrominated [(+) dibromophakelline, Z-3-bromohymenialdisine, (±) ageliferin and 3,4-dibromo-1H-pyrrole-2-carbamide], nine compounds were monobrominated [(−) clathramide C, agelongine, (+) manzacidin A, (−) 3-bromomanzacidin D, Z-spongiacidin D, Z-hymenialdisine, 2-debromostevensine, 2-bromoaldisine and 4-bromo-1H-pyrrole-2-carbamide)] and finally, two compounds were non-brominated derivatives viz., E-debromohymenialdisine and aldisine. The structure elucidations of isolated compounds were based on 1D & 2D NMR spectroscopic …

StereochemistryCell Survival01 natural sciencesGeneral Biochemistry Genetics and Molecular BiologyCell LineRSchemistry.chemical_compoundAlkaloidsAnimalsHumansPyrrolesProtein kinase ACytotoxicityIndian OceanAgeliferinPyrrolebiologyMolecular Structure010405 organic chemistryKinasebiology.organism_classificationHCT116 Cells0104 chemical sciencesPorifera010404 medicinal & biomolecular chemistrySpongechemistryStylissa carteriDrug Screening Assays AntitumorTwo-dimensional nuclear magnetic resonance spectroscopy
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Steroidal saponins from two species of Dracaena.

2010

Four new steroidal saponins (1-4) were isolated from the stem and bark of two species of Dracaena: deistelianosides A and B (1 and 2) from D. deisteliana and arboreasaponins A and B (3 and 4) from D. arborea. Six known saponins and one known sapogenin were also isolated. The structures of 1-4 were established as diosgenin 3-O-[3-O-sulfate-alpha-l-rhamnopyranosyl-(1-->4)]-beta-d-glucopyranoside (1), 1-O-beta-d-xylopyranosyl-(1-->2)-[alpha-l-rhamnopyranosyl-(1-->3)]-beta-d-fucopyranosyl(23S,24S)-spirosta-5,25(27)-diene-1beta,3beta,23alpha,24alpha-tetrol 24-O-alpha-l-arabinopyranoside (2), pennogenin-3-O-alpha-l-rhamnopyranosyl-(1-->2)-[alpha-l-rhamnopyranosyl-(1-->3)]-[6-O-acetyl]-beta-d-gluc…

StereochemistryChemical structureSaponinPharmaceutical ScienceSapogeninPharmacognosyAnalytical Chemistrychemistry.chemical_compoundDrug DiscoveryHumansCameroonNuclear Magnetic Resonance BiomolecularDracaenaPharmacologychemistry.chemical_classificationPlants MedicinalbiologyMolecular StructurePlant StemsChemistryOrganic ChemistryGlycosideStereoisomerismDiosgeninSaponinsbiology.organism_classificationHCT116 CellsComplementary and alternative medicinevisual_artvisual_art.visual_art_mediumPlant BarkMolecular MedicineBarkSteroidsDracaenaHT29 CellsJournal of natural products
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Cytotoxicity and modes of action of four naturally occuring benzophenones: 2,2′,5,6′-Tetrahydroxybenzophenone, guttiferone E, isogarcinol and isoxant…

2012

Abstract Introduction The emergence of drug-resistant cancer cells drastically reduces the efficacy of many antineoplasic agents and, consequently, increases the frequency of therapeutic failure. Benzophenones are known to display many pharmacological properties including cytotoxic activities. The present study was aimed at investigating the cytotoxicity and the modes of action of four naturally occurring benzophenones 2,2′,5,6′-tetrahydroxybenzophenone ( 1 ), isogarcinol ( 2 ), isoxanthochymol ( 3 ) and guttiferone E ( 4 ) on a panel of eleven cancer cell lines including various sensitive and drug-resistant phenotypes. Methods The cytotoxicity of the compounds was determined using a resazu…

StereochemistryPharmaceutical ScienceApoptosisHL-60 CellsPharmacologyCaspase 8BenzophenonesInhibitory Concentration 50NeoplasmsDrug DiscoveryHumansCytotoxic T cellCytotoxicityCaspaseCell ProliferationPharmacologyCaspase-9LeukemiabiologyPlant ExtractsChemistryCarcinomaHCT116 CellsAntineoplastic Agents PhytogenicMatrix MetalloproteinasesPhenotypeComplementary and alternative medicineDoxorubicinDrug Resistance NeoplasmApoptosisCell cultureCaspasesColonic NeoplasmsCancer cellbiology.proteinMolecular MedicineReactive Oxygen SpeciesPhytotherapyPhytomedicine
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Triterpenoid saponins from Hydrocotyle bonariensis Lam

2011

Abstract Phytochemical investigation of the under-ground parts of Hydrocotyle bonariensis led to the isolation of five oleanane-type triterpenoid saponins, 3- O -{β- d -glucopyranosyl-(1 → 2)-[α- l -arabinopyranosyl-(1 → 3)]-β- d -glucuronopyranosyl}-21- O -(2-methylbutyroyl)-22- O -acetyl-R 1 -barrigenol, 3- O -{β- d -glucopyranosyl-(1 → 2)-[α- l -arabinopyranosyl-(1 → 3)]-β- d -glucuronopyranosyl}-21- O -(2-methylbutyroyl)-28- O -acetyl-R 1 -barrigenol, 3- O -{β- d -glucopyranosyl-(1 → 2)-[α- l -arabinopyranosyl-(1 → 3)]-β- d -glucuronopyranosyl}-21- O -acetyl-R 1 -barrigenol, 3- O -{β- d -glucopyranosyl-(1 → 2)-[α- l -arabinopyranosyl-(1 → 3)]-β- d -glucuronopyranosyl}-R 1 -barrigenol, a…

StereochemistryPlant ScienceHorticultureBiochemistryHydrocotyle bonariensisTriterpenoidHumansCameroonNuclear Magnetic Resonance BiomolecularMolecular BiologyMolecular StructurebiologyChemistryStereoisomerismGeneral MedicineSaponinsHCT116 Cellsbiology.organism_classificationAntineoplastic Agents PhytogenicTriterpenesHuman colon cancerDrug Screening Assays AntitumorHT29 CellsTwo-dimensional nuclear magnetic resonance spectroscopyRhizomeApiaceaePhytochemistry
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Steroidal saponins from Chlorophytum orchidastrum.

2009

Six new spirostane-type saponins (1−6), named orchidastrosides A−F, and chloromaloside D were isolated from an ethanol extract of the roots of Chlorophytum orchidastrum. The saponins have neotigogenin or neogitogenin as the aglycon and oligosaccharidic chains possessing seven to nine sugar units. Their structures were elucidated mainly by 2D NMR spectroscopic analyses (COSY, TOCSY, NOESY, HSQC, and HMBC) and FABMS and HRESIMS. Compounds 1−6 were tested for cytotoxicity against two human colon cancer cell lines, HCT 116 and HT-29.

Stereochemistrymedicine.medical_treatmentChemical structureSaponinPharmaceutical SciencePharmacognosyPlant RootsAnalytical ChemistrySteroidchemistry.chemical_compoundDrug DiscoverymedicineLiliaceaeSpirostansHumansPharmacologychemistry.chemical_classificationMolecular StructureOrganic ChemistryAcetalGlycosideOligosaccharideSaponinsHCT116 CellsAntineoplastic Agents PhytogenicComplementary and alternative medicinechemistryMolecular MedicineFranceDrug Screening Assays AntitumorTwo-dimensional nuclear magnetic resonance spectroscopyHT29 CellsJournal of natural products
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Cytotoxic phytochemicals from the crude extract of Tetrapleura tetraptera fruits towards multi-factorial drug resistant cancer cells.

2020

Abstract Ethnopharmacological relevance Tetrapleura tetraptera is an African medicinal spice used in traditional medicine to treat several ailments including cancer. Aim of the study The present study was designed to evaluate the cytotoxicity of the dichloromethane-methanol (1:1) extract of the fruits of Tetrapleura tetraptera (TTF) and its constituents: (3R, 4S)-3,4-dimethyloxetan-2-one (1), luteolin (2), stigmasterol (4), 3-O-[6′-O-undecanoyl-β-D-glucopyranosyl]stigmasterol (6), olean-12-en-3-β-O-D-glucopyranoside (7), 3-O-β-D-glucopyranosyl-(1 → 6)-β-D-glucopyranosylurs-12-en-28-oic acid (8), 3-O-β-D-glucopyranosyl-(1 → 3)-β-D-glucopyranosyl-27-hydroxyolean-12-ene-28-oic acid (9), methyl…

Tetrapleura tetrapteraPhytochemicalsApoptosis03 medical and health scienceschemistry.chemical_compoundInhibitory Concentration 500302 clinical medicineBetulinic acidNeoplasmsDrug DiscoveryCytotoxic T cellHumansTetrapleuraCytotoxicity030304 developmental biologyPharmacologychemistry.chemical_classificationMembrane Potential Mitochondrial0303 health sciencesReactive oxygen speciesbiologyDose-Response Relationship DrugPlant ExtractsHep G2 Cellsbiology.organism_classificationHCT116 CellsMolecular biologyAntineoplastic Agents PhytogenicDrug Resistance MultipleMatrix MetalloproteinasesOxidative StresschemistryApoptosisDrug Resistance Neoplasm030220 oncology & carcinogenesisCaspasesFruitCancer cellReactive Oxygen SpeciesLuteolinSignal TransductionJournal of ethnopharmacology
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Synthesis of 5H-pyrido[3,2-b]pyrrolizin-5-one tripentone analogs with antitumor activity

2018

Abstract Pyrrolizinones represent an interesting class of compounds with varied degrees of structural complexity and pharmacological activity. Among these, 9H-pyrido[2,3-b]pyrrolizin-9-one, tripentone analogs, recently reported by us, showed significant antiproliferative activity against human tumor cell lines, inducing apoptosis and not affecting viability of Caco-2 differentiated in normal intestinal-like cells. Considering their interesting biological activity, their 5H-pyrido[3,2-b]pyrrolizin-5-one analogs were efficiently synthesized in good to excellent yields (61–91%). All tripentone derivatives were tested to assess their cytotoxicity against two human tumor cell lines, HCT-116 (hum…

TripentonesPyridinesAntineoplastic AgentsApoptosisAntiproliferative activity5H-pyrido[3; 2-b]pyrrolizin-5-ones; Antiproliferative activity; Antitumor; Apoptosis; Tripentones; Pharmacology; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry010402 general chemistry01 natural sciencesStructure-Activity Relationship2-b]pyrrolizin-5-onesCell Line TumorNeoplasmsDrug DiscoverymedicineHumansCytotoxic T cellPyrrolesCytotoxicityMitosisIC505H-pyrido[32-b]pyrrolizin-5-onePharmacology010405 organic chemistryChemistryDrug Discovery3003 Pharmaceutical ScienceOrganic Chemistry5H-pyrido[3ApoptosiTripentoneCancerBiological activityAntitumorGeneral MedicineHCT116 Cellsmedicine.disease0104 chemical sciencesCell cultureApoptosisMCF-7 CellsCancer researchCaco-2 CellsDrug Screening Assays AntitumorEuropean Journal of Medicinal Chemistry
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New 1,2,4-oxadiazole nortopsentin derivatives with cytotoxic activity

2019

New analogs of nortopsentin, a natural 2,4-bis(3&prime

anti-cancer agentCell SurvivalAnti-cancer agentsPharmaceutical ScienceAntineoplastic AgentsAntiproliferative activity01 natural sciencesArticlechemistry.chemical_compoundStructure-Activity RelationshipMarine alkaloidsSettore BIO/10 - BiochimicaDrug DiscoveryMoietyHumansPharmacology Toxicology and Pharmaceutics (miscellaneous)lcsh:QH301-705.5Cell ProliferationIndole testMolecular Structure010405 organic chemistryAcridine orangeImidazoles2 4-oxadiazole derivativesnortopsentin analogs2 4-oxadiazole derivatives; Anti-cancer agents; Antiproliferative activity; Marine alkaloids; Nortopsentin analogs 1; Antineoplastic Agents; Caco-2 Cells; Cell Cycle Checkpoints; Cell Proliferation; Cell Survival; HCT116 Cells; Humans; Imidazoles; MCF-7 Cells; Molecular Structure; Structure-Activity RelationshipPhosphatidylserineCell Cycle CheckpointsNortopsentin analogs 1HCT116 CellsSettore CHIM/08 - Chimica Farmaceutica0104 chemical sciences124-oxadiazole derivative010404 medicinal & biomolecular chemistrychemistryBiochemistry124-oxadiazole derivativeslcsh:Biology (General)ApoptosisCell cultureCancer cellMCF-7 CellsMarine alkaloid2 4-oxadiazole derivativeCaco-2 CellsEthidium bromide
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Synthesis and Antitumor Activity of New Thiazole Nortopsentin Analogs

2016

New thiazole nortopsentin analogs in which one of the two indole units was replaced by a naphthyl and/or 7-azaindolyl portion, were conveniently synthesized. Among these, three derivatives showed good antiproliferative activity, in particular against MCF7 cell line, with GI50 values in the micromolar range. Their cytotoxic effect on MCF7 cells was further investigated in order to elucidate their mode of action. Results showed that the three compounds act as pro-apoptotic agents inducing a clear shift of viable cells towards early apoptosis, while not exerting necrotic effects. They also caused cell cycle perturbation with significant decrease in the percentage of cells in the G0/G1 and S ph…

antiproliferative activitybis-indolyl alkaloidsIndolesStereochemistryPopulationPharmaceutical ScienceAntineoplastic AgentsAntiproliferative activity; Apoptosis; Bis-indolyl alkaloids; Marine alkaloids; Thiazolyl-indolesBis-indolyl alkaloid010402 general chemistry01 natural sciencesArticlechemistry.chemical_compoundCell Line TumorDrug DiscoveryHumansCytotoxic T cellThiazolyl-indoleThiazoleMode of actioneducationlcsh:QH301-705.5Pharmacology Toxicology and Pharmaceutics (miscellaneous)Antitumor activityIndole testeducation.field_of_study010405 organic chemistryChemistryCell CycleImidazolesapoptosisApoptosiHCT116 CellsSettore CHIM/08 - Chimica Farmaceutica0104 chemical sciencesThiazoleslcsh:Biology (General)BiochemistryApoptosisCell cultureMCF-7 Cellsmarine alkaloidsMarine alkaloidthiazolyl-indolesDrug Screening Assays Antitumormarine alkaloids; bis-indolyl alkaloids; thiazolyl-indoles; apoptosis; antiproliferative activityMarine Drugs
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EGF-Induced Acetylation of Heterogeneous Nuclear Ribonucleoproteins Is Dependent on KRAS Mutational Status in Colorectal Cancer Cells.

2015

KRAS mutational status is considered a negative predictive marker of the response to anti-EGFR therapies in colorectal cancer (CRC) patients. However, conflicting data exist regarding the variable response to EGFR-targeted therapy. The effects of oncogenic KRAS on downstream targets were studied in cell lines with different KRAS mutations. Cells harboring a single KRASG13D allele showed the most tumorigenic profile, with constitutive activation of the downstream pathway, rendering them EGF-unresponsive. Conversely, KRASA146T cells showed a full EGF-response in terms of signal transduction pathways, cell proliferation, migration or adhesion. Moreover, the global acetylome of CRC cells was al…

lcsh:MedicineBiologymedicine.disease_causeHeterogeneous-Nuclear RibonucleoproteinsProto-Oncogene Proteins p21(ras)Epidermal growth factorCell Line TumormedicineHumansCell adhesionlcsh:ScienceMutationMultidisciplinaryEpidermal Growth FactorCell growthlcsh:RAcetylationCell migrationHCT116 CellsGene Expression Regulation NeoplasticDrug Resistance NeoplasmAcetylationMutationCancer researchlcsh:QKRASSignal transductionColorectal NeoplasmsResearch ArticleSignal TransductionPLoS ONE
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