Search results for "betulin"

showing 10 items of 35 documents

Reciprocal regulation of endothelial nitric-oxide synthase and NADPH oxidase by betulinic acid in human endothelial cells.

2007

Nitric oxide (NO) produced by endothelial NO synthase (eNOS) is a protective principle in the vasculature. Many cardiovascular diseases are associated with reduced NO bioactivity and eNOS uncoupling due to oxidative stress. Compounds that reverse eNOS uncoupling and increase eNOS expression are of therapeutic interest. Zizyphi Spinosi semen (ZSS) is one of the most widely used traditional Chinese herbs with protective effects on the cardiovascular system. In human umbilical vein endothelial cells (HUVEC) and HUVEC-derived EA.hy 926 cells, an extract of ZSS increased eNOS promoter activity, eNOS mRNA and protein expression, and NO production in a concentration- and time-dependent manner. Maj…

Nitric Oxide Synthase Type IIIBlotting Westernmedicine.disease_causeNitric OxideGene Expression Regulation EnzymologicNitric oxidechemistry.chemical_compoundEnosBetulinic acidmedicineHumansNitric Oxide DonorsEnzyme InhibitorsBetulinic AcidCyclic GMPCells CulturedPharmacologyNADPH oxidaseBetulinbiologyDose-Response Relationship DrugReverse Transcriptase Polymerase Chain ReactionNOX4AcetophenonesEndothelial CellsNADPH OxidasesZiziphusSaponinsbiology.organism_classificationTriterpenesNG-Nitroarginine Methyl EsterchemistryBiochemistryNADPH Oxidase 4biology.proteinMolecular MedicineSpermineP22phoxPentacyclic TriterpenesReactive Oxygen SpeciesOxidative stressDrugs Chinese HerbalThe Journal of pharmacology and experimental therapeutics
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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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Enhanced Accumulation of Betulinic Acid in Transgenic Hairy Roots of Senna obtusifolia Growing in the Sprinkle Bioreactor and Evaluation of Their Bio…

2021

Betulinic acid, which is found in transgenic roots of Senna obtusifolia (L.) H.S.Irwin & Barneby, is a pentacyclic triterpene with distinctive pharmacological activities. In this study, we report the differences in the content of betulinic acid and selected anthraquinones in transgenic S. obtusifolia hairy roots with overexpression of the PgSS1 gene (SOPSS2 line) and in transformed hairy roots without this genetic construct (SOA41 line). Both hairy root lines grew in 10 L sprinkle bioreactor. Additionally, the extracts obtained from this plant material were used for biological tests. Our results demonstrated that the SOPSS2 hairy root cultures from the bioreactor showed an increase in the c…

Senna PlantTransgeneBioengineeringAnthraquinonesApoptosisMicrobial Sensitivity TestsGram-Positive BacteriaBiochemistryModels BiologicalPlant Rootschemistry.chemical_compoundBioreactorsTriterpeneGene Expression Regulation PlantBetulinic acidCell Line TumorAnthraquinonesGene expressionGram-Negative BacteriaBioreactorHumansAntiviral activityBetulinic AcidMolecular BiologyCell ProliferationPlant Proteinsbcl-2-Associated X Proteinchemistry.chemical_classificationbiologyPlant ExtractsSprinkle bioreactorGeneral ChemistryGeneral Medicinebiology.organism_classificationAntimicrobialPlants Genetically ModifiedBiodiversitatAnticancerchemistryBiochemistryGlucosyltransferasesTransgenic hairy rootsMolecular MedicineAntimicrobialGene expressionTumor Suppressor Protein p53Senna obtusifoliaPentacyclic TriterpenesChemistrybiodiversity
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Cytotoxicity of Artesunic Acid Homo- and Heterodimer Molecules toward Sensitive and Multidrug-Resistant CCRF-CEM Leukemia Cells

2010

A novel approach to circumvent multidrug resistance is hybridization of natural products in dimers. We analyzed homodimers of two artesunic acid molecules and heterohybrids of artesunic acid and betulin in human CCRF-CEM and multidrug-resistant P-glycoprotein-overexpressing CEM/ADR5000 leukemia cells. Multidrug-resistant cells were not cross-resistant to the novel compounds. Collateral sensitivity was observed for artesunic acid homodimer. Artesunic acid and artesunic acid homodimer induced G0/G1 cell cycle arrest, apoptosis, and formation of reactive oxygen species.

Spectrometry Mass Electrospray IonizationMagnetic Resonance SpectroscopyCell SurvivalApoptosischemistry.chemical_compoundCell Line TumorDrug DiscoverymedicineHumansCytotoxicitychemistry.chemical_classificationReactive oxygen speciesFormazansLeukemiaBetulinCell CycleSuccinatesCell cycleFlow Cytometrymedicine.diseaseArtemisininsTriterpenesMultiple drug resistanceLeukemiachemistryBiochemistryDrug Resistance NeoplasmCell cultureApoptosisMolecular MedicineReactive Oxygen SpeciesJournal of Medicinal Chemistry
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Activity of lupane triterpenoids from Maytenus species as inhibitors of nitric oxide and prostaglandin E2

2005

In the present study, we report that three new lupane triterpenes (1-3), in addition to 16 known ones (4-19), were isolated from the root bark of Maytenus cuzcoina and the leaves of Maytenus chiapensis. Their structures were elucidated by spectral analysis, including homonuclear and heteronuclear correlation NMR experiments (COSY, ROESY, HSQC, and HMBC). The natural compounds and derivatives 6a, 6b, 9a, and 9b have been tested for potential anti-inflammatory activity, and several compounds including 3-epicalenduladiol (2), 11alpha-hydroxy-glochidone (3), rigidenol (6), acetoxy-rigidenol (6a), 11alpha-acetoxy-30-chloro-3-oxo-lup-20(29)-ene (6b), betulin (9), 28-acetoxy-betulin (9a), epibetul…

StereochemistryClinical BiochemistryPharmaceutical SciencePharmacognosyNitric OxideBiochemistryDinoprostoneTerpeneCelastraceaeMiceStructure-Activity Relationshipchemistry.chemical_compoundTriterpeneDrug DiscoveryAnimalsMolecular Biologychemistry.chemical_classificationBetulinbiologyMaytenusMacrophagesSpectrum AnalysisOrganic ChemistryBiological activityBacterial InfectionsMaytenusbiology.organism_classificationAntineoplastic Agents PhytogenicTriterpenesTerpenoidEndotoxinsPlant LeaveschemistryMolecular MedicineBioorganic & Medicinal Chemistry
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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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Pyrolysis-gas chromatography : mass spectrometry analysis of di- and triterpenoids

2017

The objective of this work was to study a specific class of extractives existing in lignocellulosic biomass and more precisely in wood materials, and their thermochemical behavior during pyrolysis. The focus was centered on the class of terpenes and terpenoids; specifically two model compounds, abietic acid and betulinol, were chosen to represent the subclasses of di- and triterpenoids, respectively. The model compounds were investigated via pyrolysis-gas chromatography/mass spectrometry (Py-GC/MS) and the main objective was to study their product profiles and characteristic fragmentations, as well as the influence of specific variables (pyrolysis temperature and time) on pyrolysis products…

abietic acidterpeenitterpenoidsbetulinolkuivatislausPy-GC/MSpyrolysistriterpeenit
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Chemical constituents from Anthocleista liebrechtsiana De Wild & T. Durand (Loganiaceae)

2018

Abstract A new steroid derivative, (24S)-3β-hydroxy-7β-methoxyergost-5-ene (1), was isolated along with eleven known compounds: 7α-hydroxysterol (2), β-sitosterol (3), oleanolic acid (4), betulinic acid (5), lupeol (6), swertiaperennin (7), decussatin (8), tetracosanoic acid (9) β-sitosterol-3-O-β- d -glucopyranoside (10), (2R,3S)-2,3-dihydro-2-(3,4-dimethoxyphenyl)-3-hydroxymethyl-5-(2-formylvinyl)-7-hydroxybenzofuran (11) and acacetin 6-C-β- d -glucopyranoside (12) from the tree bark and leaves of Anthocleista liebrechtsiana De Wild & T. Durand. Their structures were elucidated on the basis of spectroscopic (1D and 2D NMR) and mass spectrometric data. Compounds 2 and 7–10 have already bee…

biologyAcacetin010405 organic chemistryStereochemistryAnthocleistaLoganiaceaebiology.organism_classificationAntimicrobial01 natural sciencesBiochemistry0104 chemical sciences010404 medicinal & biomolecular chemistrychemistry.chemical_compoundchemistryBetulinic acidOleanolic acidEcology Evolution Behavior and SystematicsDerivative (chemistry)LupeolBiochemical Systematics and Ecology
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Mimonoside D: a new triterpenoid saponin from Mimosa diplotricha Sauvalle (Fabaceae)

2021

A new triterpenoid saponin (Mimonoside D: 3-O-��-L-arabinopyranosyl-3��-hydroxyolean-12-en-28-oic acid 28-O-��-D-xylopyranosyl-(1���2)-��-D- glucopyranoside ester (1)) was isolated from the aerial parts of Mimosa diplotricha Sauvalle together with nine known compounds: 7,4���-dihydroxyflavone (2), kaempferol (3), lupeol (4), betulinic acid (5), ��-sitosterol (6), ��-sitosterol-3-O-��-D-glucopyranoside (7), lutein (8), 5,2���-dihydroxy-7,4���,5���-trimethoxyflavone (9) and vitexin (10). Their structures were elucidated on the basis of spectroscopic (1 D and 2 D nuclear magnetic resonance) and high-resolution mass spectrometric data as well as by comparison of their spectral data with those o…

chemistry.chemical_classificationbiologyOrganic ChemistryVitexinPlant ScienceFabaceaebiology.organism_classificationBiochemistryProteus mirabilisAnalytical Chemistrychemistry.chemical_compoundchemistryBetulinic acidKaempferolMimosa diplotrichaLupeolNuclear chemistryTriterpenoid saponin
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