Search results for "HT29 Cell"

showing 10 items of 45 documents

A review of natural and modified betulinic, ursolic and echinocystic acid derivatives as potential antitumor and anti-HIV agents.

2003

The aim of this review is to update current knowledge on the betulinic, ursolic and echinocystic acids and their natural and semisynthetic analogs, focussing on their cytotoxic and anti-HIV activities. Then, the last results of the authors' team on unusual semisynthetic derivatives of these triterpenoids will be presented in order to establish structure/activity relationships.

PharmacologyMolecular StructureAnti hivChemistryAnti-HIV AgentsTumor cellsAntineoplastic AgentsGeneral MedicinePharmacologyTriterpenesStructure-Activity RelationshipTriterpenoidDrug DiscoveryHIV-1Tumor Cells CulturedStructure–activity relationshipHumansEchinocystic acidOleanolic AcidBetulinic AcidPentacyclic TriterpenesHT29 CellsMini reviews in medicinal chemistry
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New ursolic and betulinic derivatives as potential cytotoxic agents.

2003

Fifteen new ursolic and betulinic triterpenoids, bearing various functionalities at C-3 and C-28 were synthesized as potential cytotoxic agents. All compounds were obtained by a hemisynthetic route via ursolic and betulinic acids. Preliminary screening of these compounds on human HT 29 colon cancer cells revealed inhibitory activity for three of them. Beta-D-Glucopyranosyl-3beta-hydroxyurs-12(13)-en-28-oate 1c, 3beta-3-(3-pyridyl)-prop-2-enoyloxyurs-12(13)-en-28-oic acid 1i and the potassium salt of 3beta-cinnamoyloxylup-20(29)-en-28-oic acid 2d demonstrated cytotoxic activity in the micromolar range: 8.0, 45.0 and 8.0 microM, respectively.

PharmacologyMolecular StructureStereochemistryCell SurvivalAntineoplastic AgentsGeneral MedicineTriterpeneschemistry.chemical_compoundInhibitory Concentration 50Structure-Activity RelationshipTriterpenoidUrsolic acidchemistryBetulinic acidDrug DiscoveryCytotoxic T cellHumansDrug Screening Assays AntitumorBetulinic AcidCytotoxicityPentacyclic TriterpenesHT29 CellsJournal of enzyme inhibition and medicinal chemistry
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Tributyltin(IV) ferulate, a novel synthetic ferulic acid derivative, induces autophagic cell death in colon cancer cells: From chemical synthesis to …

2020

Ferulic acid (FA) is a natural phenolic phytochemical that has low toxicity and exhibits therapeutic effects against various diseases, behaving as an antioxidant. FA also displays modest antitumor properties that have been reported at relatively high concentrations. With the aim of improving the anti-tumor efficacy of FA, we synthesized the novel compound tributyltin(IV) ferulate (TBT-F). The coordination environment at the tin center was investigated spectroscopically. Following synthesis, chemical characterization and computational analysis, we evaluated TBT-F effects in colon cancer cells. The results showed that TBT-F, at nanomolar range concentrations, was capable of reducing the viabi…

Programmed cell deathAntioxidantCoumaric AcidsAutophagic Cell Deathmedicine.medical_treatmentAntineoplastic AgentsOrganotin(IV)VacuolePharmacology010402 general chemistry01 natural sciencesBiochemistryInorganic ChemistryFerulic acidchemistry.chemical_compoundColon cancer cytotoxicityLC3medicineHumansViability assay010405 organic chemistryChemistryp62AutophagyFerulic acidHCT116 Cells0104 chemical sciencesApoptosisCell Death ProcessColonic NeoplasmsCaco-2 CellsTrialkyltin CompoundsHT29 CellsJournal of Inorganic Biochemistry
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Tumor cell specific toxicity of Inula helenium extracts.

2006

The aim of the research program was to identify botanical extracts with antineoplastic activity. In this respect extracts prepared from Inula helenium roots showed a remarkable activity. As evidenced by the MTT assay, the Inula helenium extract revealed a highly selective toxicity toward four different tumor cell lines (HT-29, MCF-7, Capan-2 and G1), but a much lower toxicity against healthy human peripheral blood lymphocytes (PBLs) from two donors. The extract-induced death of tumor cells was studied extensively by electron microscopy. There was a remarkable similarity of morphological alterations observed in the four cell lines: patchy chromatin condensations, cytoplasmic vesiculation, sw…

Programmed cell deathCell SurvivalContext (language use)Plant RootsLethal Dose 50Cell Line TumorToxicity Tests AcuteHumansMTT assayLymphocytesAnnexin A5CytotoxicityPharmacologyInulabiologyMutagenicity TestsPlant Extractsbiology.organism_classificationMolecular biologyAntineoplastic Agents PhytogenicApoptosisCell cultureImmunologyInulaHT29 CellsHeleniumPhytotherapy research : PTR
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Cytotoxic Acacic Acid Glycosides from the Roots of Albizia coriaria

2009

Two new oleanane-type saponins, coriariosides A (1) and B (2), along with a known saponin, gummiferaoside C (3), were isolated from the roots of Albizia coriaria. Their structures were established by extensive analysis of 1D and 2D NMR experiments (COSY, ROESY, TOCSY, HSQC, and HMBC) and mass spectrometry. Compounds 1 and 3 when tested for cytotoxicity against two colorectal human cancer cells showed activity against the HCT 116 (IC50 4.2 microM for 1 and 2.7 microM for 3) and HT-29 (IC50 6.7 microM for 1 and 7.9 microM for 3) cell lines.

SaponinPharmaceutical ScienceAlbizziaPharmacognosyPlant RootsAnalytical ChemistryTriterpeneCoriariaDrug DiscoveryBotanyHumansCameroonOleanolic AcidMedicinal plantsNuclear Magnetic Resonance BiomolecularPharmacologychemistry.chemical_classificationPlants MedicinalMolecular StructurebiologyOrganic ChemistryGlycosideSaponinsHCT116 Cellsbiology.organism_classificationAlbiziaAntineoplastic Agents PhytogenicTriterpenesTerpenoidComplementary and alternative medicinechemistryMolecular MedicineDrug Screening Assays AntitumorHT29 CellsJournal of Natural Products
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Novel Acylated Triterpene Glycosides from Muraltia heisteria

2002

Four new acylated triterpene glycosides (1-4) have been isolated as two inseparable mixtures of the trans- and cis-3,4,5-trimethoxycinnamoyl derivatives (1,2 and 3,4) from the roots of Muraltia heisteria. The structures of these compounds were elucidated by various 1D and 2D NMR techniques, including (1)H and (13)C, COSY, NOESY, HSQC, TOCSY, and HMBC experiments and FABMS. Compounds 3 and 4 were shown to be cytotoxic in a human colon cancer cell line but did not show any ability to potentiate in vitro cisplatin cytotoxicity.

StereochemistryAcylationSaponinPharmaceutical ScienceStereoisomerismPharmacognosyPlant RootsAnalytical ChemistrySouth AfricaTriterpeneDrug DiscoveryTumor Cells CulturedHumansOrganic chemistryNuclear Magnetic Resonance BiomolecularChromatography High Pressure LiquidPharmacologychemistry.chemical_classificationMolecular StructureChemistryHydrolysisOrganic ChemistryGlycosideStereoisomerismBiological activitySaponinsAntineoplastic Agents PhytogenicTriterpenesTerpenoidPolygalaceaeComplementary and alternative medicineMolecular MedicineCisplatinDrug Screening Assays AntitumorHT29 CellsTwo-dimensional nuclear magnetic resonance spectroscopyJournal of Natural Products
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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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Gold(I) Biscarbene Complexes Derived from Vascular-Disrupting Combretastatin A-4 Address Different Targets and Show Antimetastatic Potential

2014

Gold N-heterocyclic carbene (NHC) complexes are an emerging class of anticancer drugs. We present a series of gold(I) biscarbene complexes with NHC ligands derived from the plant metabolite combretastatin A-4 (CA-4) that retain its vascular-disrupting effect, yet address different cellular and protein targets. Unlike CA-4, these complexes did not interfere with tubulin, but with the actin cytoskeleton of endothelial and cancer cells. For the highly metastatic 518A2 melanoma cell line this effect was accompanied by a marked accumulation of cells in the G1 phase of the cell cycle and a suppression of active prometastatic matrix metalloproteinase-2. Despite these mechanistic differences the co…

StereochemistryNeovascularization PhysiologicAntineoplastic AgentsBiologyBiochemistryMicechemistry.chemical_compoundCoordination ComplexesTubulinCell Line TumorBibenzylsDrug DiscoveryHuman Umbilical Vein Endothelial CellsAnimalsHumansGeneral Pharmacology Toxicology and PharmaceuticsMelanomaCell ProliferationPharmacologyCombretastatin A-4Tube formationCombretastatinMice Inbred BALB COrganic ChemistryCell cycleActin cytoskeletonG2 Phase Cell Cycle CheckpointsActin CytoskeletonChorioallantoic membranechemistryDrug Resistance NeoplasmCell cultureCancer cellMCF-7 CellsCancer researchMolecular MedicineGoldHT29 CellsMethaneChemMedChem
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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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Two Triterpene Saponins from Achyranthes bidentata.

2001

Bidentatoside II (1) and chikusetsusaponin V methyl ester (2) are two further triterpene saponins isolated from the roots of Achyranthes bidentata. Chemical and homo and heteronuclear two-dimensional (2D) NMR techniques have led to the structural elucidation of 1 which is a new seco-glycoside of oleanolic acid and the full 1H- and 13C-NMR assignments of 2. These compounds did not show any potentiation of the in vitro cytotoxicity of cisplatin in the HT 29 human colon cancer cell line.

StereochemistrySaponinPharmacognosyPlant Rootschemistry.chemical_compoundGlucosideTriterpeneDrug DiscoveryHumansOleanolic acidAchyranthes bidentataAchyrantheschemistry.chemical_classificationbiologyPlant ExtractsGlycosideGeneral ChemistryGeneral MedicineSaponinsbiology.organism_classificationAntineoplastic Agents PhytogenicTriterpenesTerpenoidBiochemistrychemistryHT29 CellsChemical and Pharmaceutical Bulletin
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