Search results for "TERPENES"

showing 10 items of 470 documents

Cytotoxic and protein kinase inhibiting nakijiquinones and nakijiquinols from the sponge Dactylospongia metachromia.

2014

Chemical investigation of the sponge Dactylospongia metachromia afforded five new sesquiterpene aminoquinones (1-5), two new sesquiterpene benzoxazoles (6 and 7), the known analogue 18-hydroxy-5-epi-hyrtiophenol (8), and a known glycerolipid. The structures of all compounds were unambiguously elucidated by one- and two-dimensional NMR and by MS analyses, as well as by comparison with the literature. Compounds 1-5 showed potent cytotoxicity against the mouse lymphoma cell line L5178Y with IC50 values ranging from 1.1 to 3.7 μM. When tested in vitro for their inhibitory potential against 16 different protein kinases, compounds 5, 6, and 8 exhibited the strongest inhibitory activity against AL…

Pharmaceutical ScienceAntineoplastic AgentsMarine BiologySesquiterpeneAnalytical Chemistrychemistry.chemical_compoundInhibitory Concentration 50MiceDrug DiscoveryAnimalsHumansProtein kinase ACytotoxicityIC50Nuclear Magnetic Resonance BiomolecularProtein Kinase InhibitorsPharmacologyBenzoxazolesMolecular StructureKinaseOrganic ChemistryQuinonesIn vitroPoriferaComplementary and alternative medicineBiochemistrychemistryCell cultureMolecular MedicineDrug Screening Assays AntitumorSesquiterpenesProto-oncogene tyrosine-protein kinase SrcJournal of natural products
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Cytotoxic Compounds from the Fruits of Uapaca togoensis towards Multifactorial Drug-Resistant Cancer Cells

2014

Cancer cells may rapidly acquire multidrug resistance, mainly due to the presence of adenosine triphosphate-binding cassette transporters, epidermal growth factor receptor, or mutations in the p53 tumor suppressor gene. This work was designed to assess the cytotoxicity of the methanol crude extracts and compounds from the fruits of Uapaca togoensis, namely, β-amyryl acetate (1), 11-oxo-α-amyryl acetate (2), lupeol (3), pomolic acid (4), futokadsurin B (5), arborinin (6), and 3-O-β-D-glucopyranosyl sitosterol (7) against nine drug sensitive and multidrug-resistant cancer cell lines. The resazurin reduction assay was used to evaluate the cytotoxicity of the fruits of U. togoensis and compound…

Pharmaceutical ScienceBiologyLignansAnalytical ChemistryInhibitory Concentration 50chemistry.chemical_compoundCell Line TumorDrug DiscoveryHumansCytotoxic T cellOleanolic AcidCytotoxicityLupeolMembrane Potential MitochondrialPharmacologyMolecular StructurePlant ExtractsAlkaloidOrganic ChemistryEuphorbiaceaeCell cycleAntineoplastic Agents PhytogenicDrug Resistance MultipleTriterpenesComplementary and alternative medicinechemistryBiochemistryDoxorubicinDrug Resistance NeoplasmApoptosisCell cultureCancer cellAcridinesMolecular MedicineDrug Screening Assays AntitumorPentacyclic TriterpenesReactive Oxygen SpeciesPlanta Medica
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Chemical Composition and Possible in Vitro Phytotoxic Activity of Helichrsyum italicum (Roth) Don ssp. italicum

2011

The chemical composition of the essential oil of Helichrysum italicum (Roth) Don ssp. italicum, collected in the National Park of Cilento and Diano Valley, Southern Italy, was studied by means of GC and GC/MS. Forty four compounds of 45 constituents were identified in the oil, mainly oxygenated sesquiterpenes. The essential oil was evaluated for its potential in vitro phytotoxic activity against germination and early radicle elongation of radish and garden cress. The radicle elongation of radish was significantly inhibited at the highest doses tested, while germination of both seeds was not affected.

Pharmaceutical ScienceGerminationphytotoxicityHelichrysum italicum (Roth) Don ssp. italicumPlant RootsHelichrysum italicumArticleLepidium sativumessential oilRaphanusAnalytical Chemistrylaw.inventionlcsh:QD241-441lcsh:Organic chemistrylawDrug DiscoveryBotanyOils VolatileRadiclePhysical and Theoretical ChemistryChemical compositionEssential oilHelichrysumbiologyHerbicidesPlant ExtractsOrganic Chemistryfood and beverages<em>Helichrysum italicum </em>(Roth) Don ssp.<em> italicum</em>; essential oil; phytotoxicitybiology.organism_classificationChemistry (miscellaneous)GerminationMolecular MedicinePhytotoxicitySesquiterpenesMolecules; Volume 16; Issue 9; Pages: 7725-7735
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Antibacterial Activity and Anticancer Activity of Rosmarinus officinalis L. Essential Oil Compared to That of Its Main Components

2012

In this study, Rosmarinus officinalis L. essential oil and three of its main components 1,8-cineole (27.23%), α-pinene (19.43%) and β-pinene (6.71%) were evaluated for their in vitro antibacterial activities and toxicology properties. R. officinalis L. essential oil possessed similar antibacterial activities to α-pinene, and a little bit better than β-pinene, while 1,8-cineole possessed the lowest antibacterial activities. R. officinalis L. essential oil exhibited the strongest cytotoxicity towards three human cancer cells. Its inhibition concentration 50% (IC50) values on SK-OV-3, HO-8910 and Bel-7402 were 0.025‰, 0.076‰ and 0.13‰ (v/v), respectively. The cytotoxicity of all the test sampl…

Pharmaceutical ScienceRosmarinusAnalytical Chemistrylaw.inventionchemistry.chemical_compoundlawDrug DiscoveryFood scienceCytotoxicityBicyclic Monoterpenesbiologyantibacterial activities18-cineoleAnti-Bacterial AgentsChemistry (miscellaneous)α-pineneOfficinaliscytotoxicityMolecular MedicineAntibacterial activityCell SurvivalMicrobial Sensitivity TestsRosmarinus officinalis L.Articlelcsh:QD241-441Bridged Bicyclo CompoundsInhibitory Concentration 50lcsh:Organic chemistryCell Line TumorBotanyOils Volatile<em>Rosmarinus officinalis </em>L.; 18-cineole; α-pinene; β-pinene; antibacterial activities; cytotoxicityHumansPhysical and Theoretical ChemistryIC50Essential oilEucalyptolBacteriaPlant ExtractsOrganic ChemistryCyclohexanolsbiology.organism_classificationAntineoplastic Agents PhytogenicRosmarinusβ-pineneEucalyptolchemistryMonoterpenesDrug Screening Assays AntitumorHuman cancerMolecules; Volume 17; Issue 3; Pages: 2704-2713
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Euphosantianane A–D: Antiproliferative Premyrsinane Diterpenoids from the Endemic Egyptian Plant Euphorbia Sanctae-Catharinae

2018

Euphorbia species are rich in diterpenes. A solvent extraction of Euphorbia sanctae-catharinae, a species indigenous to the Southern Sinai of Egypt, afforded several premyrsinane diterpenoids (1&ndash

Pharmaceutical ScienceTumor cells01 natural sciencesAnalytical ChemistryTDDTF-ECDlcsh:QD241-441tumor anti-proliferative activitylcsh:Organic chemistryDrug DiscoveryPhysical and Theoretical ChemistrySolvent extractionA549 cellEuphorbiabiologyTraditional medicine010405 organic chemistryChemistryOrganic ChemistryEuphorbiaceaeEuphorbiaceaediterpenesEuphorbia sanctae-catharinaebiology.organism_classification0104 chemical sciences010404 medicinal & biomolecular chemistryChemistry (miscellaneous)flavonoidsMolecular Medicine<i>Euphorbia sanctae-catharinae</i>Molecules
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Sterelactones: New Isolactarane Type Sesquiterpenoids with Antifungal Activity from Stereum sp. IBWF 01060

2008

Four members of a new family of tetracyclic sesquiterenoids possessing the isolactarane skeleton have been isolated from mycelial cultures of Stereum sp. IBWF 01060. Their structure elucidation and their antifungal activity against several plant pathogens as well as other microorganisms are reported.

PharmacologyAntifungalAntifungal AgentsMagnetic Resonance Spectroscopymedicine.drug_classBasidiomycotaBasidiomycotaBiologybiology.organism_classificationFungicideStereum sp.Drug DiscoveryBotanymedicineHumansSesquiterpenesMyceliumThe Journal of Antibiotics
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Effects of triterpenes on the immune system.

2010

Ethnopharmacological relevance: Triterpenes, which comprise a broad chemical group of active principles, are implicated in the mechanisms of action and pharmacological effects of many medicinal plants used in folk medicine against diseases in which the immune system is implicated. They have been described as anti-inflammatory, antiviral, antimicrobial, and antitumoral agents, as well as being immunomodulator compounds. Several of them are implicated in the resolution of immune diseases, although their effects have not always been clearly correlated. Aim of the review: The aim of this review is to compile relevant data on the mechanisms of action of triterpenes isolated from active ethnomedi…

PharmacologyMechanism (biology)Anti-HIV AgentsInflammationNF-κBComputational biologyBiologyAntimicrobialMajor histocompatibility complexTriterpeneschemistry.chemical_compoundImmune systemCucurbitacinschemistryAdjuvants ImmunologicImmune SystemDrug DiscoveryImmunologymedicinebiology.proteinAnimalsHumansmedicine.symptomMedicinal plantsTranscription FactorsJournal of ethnopharmacology
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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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Synthetic derivatives of aromatic abietane diterpenoids and their biological activities

2014

Naturally occurring aromatic abietane diterpenoids (dehydroabietanes) exhibit a wide range of biological activities. A number of synthetic studies aimed at modifying the abietane skeleton in order to obtain new potential chemotherapeutic agents have been reported. In this study, the biological activities of synthetic derivatives of aromatic abietane diterpenoids are reviewed.

PharmacologyMolecular StructureSynthetic derivativesOrganic ChemistryCarnosic acidGeneral MedicineTerpenoidFerruginolchemistry.chemical_compoundchemistryDrug DiscoveryOrganic chemistryDehydroabietic acidDiterpenesAbietaneEuropean Journal of Medicinal Chemistry
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