Search results for " DISCOVERY"

showing 10 items of 4082 documents

Effects of resveratrol on the ultrastructure of Botrytis cinerea conidia and biological significance in plant/pathogen interactions

2012

International audience; Many roles have been ascribed to stilbenes, namely as antimicrobial, deterrent or repellent compounds in plants, protecting them from attacks by fungi, bacteria, nematodes or herbivores, acting both as constitutive and active defense (phytoalexin) compounds. More recently, stilbenes (especially resveratrol and its derivatives) were acclaimed for their wondrous effects and wide range of purported healing and preventive powers as cardioprotective, antitumor, neuroprotective and antioxidant agents. Although there is a huge number of works concerning the role of resveratrol in human health, reports on the antifungal activity of this compound are still scarce. This study …

0106 biological sciences[SDV]Life Sciences [q-bio]Resveratrol01 natural sciencesConidiumchemistry.chemical_compoundBotrytis cinereaDrug DiscoveryStilbenesDISEASE RESISTANCEVitisPathogenBotrytis cinereachemistry.chemical_classificationELECTRON-MICROSCOPY0303 health sciencesbiologyPhytoalexinfood and beveragesBiological activityGeneral MedicineSpores FungalVITIS-VINIFERA LEAVESAntimicrobialABC TRANSPORTER BCATRB3. Good healthHost-Pathogen Interactions[SDE]Environmental SciencesGrapevineBotrytisSTILBENE PHYTOALEXINSMETABOLISMMicrobiology03 medical and health sciencesPhytoalexinsBotany[SDV.BV]Life Sciences [q-bio]/Vegetal BiologyPLANTSPHYTOALEXIN PHASEOLLINMode of action030304 developmental biologyPlant DiseasesPharmacologyBiological activityfungibiology.organism_classificationchemistryResveratrolGRAPEVINE LEAVESCAUSAL AGENT010606 plant biology & botany
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The Potential Role of Medicinal Mushrooms in the Prevention and Treatment of Gynecological Cancers: A Review

2019

A review of scientific information about the potential role of medicinal mushrooms in the prevention and treatment of gynecological cancers, human immunodeficiency virus, and human papillomavirus infections is reported here. The results of in vivo and in vitro experiments on 16 different species of Basidiomycetes and three Ascomycetes, which possess chemopreventive potential and are effective in clinical application in combination with chemotherapy, are also discussed. Medicinal mushroom extracts confirm an evident efficacy on the reduction of tumor cell proliferation and side effects in patients with gynecological tumors who are undergoing chemotherapy treatments. This review, the first on…

0106 biological sciencesanimal structuresVaginal NeoplasmsGenital Neoplasms Femalemedicine.medical_treatmentHuman immunodeficiency virus (HIV)Uterine Cervical NeoplasmsTumor cellsmedicine.disease_cause01 natural sciencesApplied Microbiology and BiotechnologyAntioxidantsMiceMedicinal mushroomAscomycotaIn vivo010608 biotechnologyDrug DiscoverymedicineAnimalsHumansIn patientHuman papillomavirusPapillomaviridaeCell ProliferationPharmacologyChemotherapyBiological ProductsClinical Trials as Topicbusiness.industryBasidiomycotafungiHIVSettore BIO/03 - Botanica Ambientale E ApplicataCancer researchFemalebusinessAgaricalesmedicinal mushrooms gynecological cancers human immunodeficiency virus human papillomavirus Basidiomycetes Ascomycetes
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2021

Centaurothamnus maximus (family Asteraceae), is a leafy shrub indigenous to the southwestern Arabian Peninsula. With a paucity of phytochemical data on this species, we set out to chemically characterize the plant. From the aerial parts, two newly identified guaianolides were isolated: 3β-hydroxy-4α(acetoxy)-4β(hydroxymethyl)-8α-(4-hydroxy methacrylate)-1αH,5αH, 6αH-gual-10(14),11(13)-dien-6,12-olide (1) and 15-descarboxy picrolide A (2). Seven previously reported compounds were also isolated: 3β, 4α, 8α-trihydroxy-4-(hydroxymethyl)-lαH, 5αH, 6βH, 7αH-guai-10(14),11(13)-dien-6,12-olide (3), chlorohyssopifolin B (4), cynaropikrin (5), hydroxyjanerin (6), chlorojanerin (7), isorhamnetin (8), …

0106 biological sciencesbiologyStereochemistryOrganic ChemistryPharmaceutical ScienceDEPTAsteraceaeFast atom bombardmentCarbon-13 NMRSesquiterpenebiology.organism_classification01 natural sciences0104 chemical sciencesAnalytical Chemistry010404 medicinal & biomolecular chemistrychemistry.chemical_compoundchemistryChemistry (miscellaneous)Drug DiscoveryMolecular MedicineHydroxymethylPhysical and Theoretical ChemistryTwo-dimensional nuclear magnetic resonance spectroscopyIsorhamnetin010606 plant biology & botanyMolecules
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Isolation of a novel linalool disaccharide glycoside from Raspberry fruit

1991

Abstract A new linalool disaccharide glycoside ( 1a ) was isolated from raspberry fruit ( Rubus idaeus , cv. Heritage) and characterized as S-(+)-linalool 3-O-α-L-arabinopyranosyl-(1→6)-β-D-glucopyranoside by means of spectroscopic studies.

0106 biological scienceschemistry.chemical_classificationbiology010405 organic chemistryStereochemistryRosaceae[SDV]Life Sciences [q-bio]Organic ChemistryDisaccharideGlycosideFRAMBOISIERbiology.organism_classification01 natural sciencesBiochemistry0104 chemical sciencesBlowing a raspberry[SDV] Life Sciences [q-bio]chemistry.chemical_compoundchemistryLinaloolDrug DiscoveryRubusComputingMilieux_MISCELLANEOUS010606 plant biology & botany
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Essential Oils Extracted from Different Species of the Lamiaceae Plant Family as Prospective Bioagents against Several Detrimental Pests

2020

On the basis of the side effects of detrimental synthetic chemicals, introducing healthy, available, and effective bioagents for pest management is critical. Due to this circumstance, several studies have been conducted that evaluate the pesticidal potency of plant-derived essential oils. This review presents the pesticidal efficiency of essential oils isolated from different genera of the Lamiaceae family including Agastache Gronovius, Hyptis Jacquin, Lavandula L., Lepechinia Willdenow, Mentha L., Melissa L., Ocimum L., Origanum L., Perilla L., Perovskia Kar., Phlomis L., Rosmarinus L., Salvia L., Satureja L., Teucrium L., Thymus L., Zataria Boissier, and Zhumeria Rech. Along with acute to…

0106 biological sciencesfood.ingredientHyptisLavandulaPhytochemicalsPharmaceutical ScienceReviewacute toxicitysublethal effectsSatureja01 natural sciencesRosmarinusessential oilAnalytical Chemistrylaw.inventionTeucriumlcsh:QD241-441foodlcsh:Organic chemistrylawDrug DiscoveryOils Volatilesublethal effectPesticidesPhysical and Theoretical ChemistrymonoterpenoidsEssential oilLamiaceaeMolecular StructurebiologyTraditional medicineOrganic ChemistryOriganumbiology.organism_classification010602 entomologyChemistry (miscellaneous)Insect RepellentsSettore BIO/03 - Botanica Ambientale E ApplicataMolecular MedicineLamiaceae010606 plant biology & botanyMolecules
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Spray-Drying Performance and Thermal Stability of L-Ascorbic Acid Microencapsulated with Sodium Alginate and Gum Arabic

2019

[EN] The potential of sodium alginate (ALG) and gum arabic (GA) as wall polymers for Lascorbic acid (AA) encapsulation as a tool for their preservation against the thermo-oxidative degradation was investigated. The influence of such polymers used as wall material on the AAcontent, size, encapsulation efficiency, encapsulation yield and thermo-oxidative stability were evaluated. The AA-microparticles were obtained using the spray-drying technique. An experimental Taguchi design was employed to assess the influence of the variables in the encapsulation process. The microparticles morphology and size distribution were characterized by scanning electron microscopy and laser diffraction. The the…

0106 biological sciencesfood.ingredientMaterials scienceChemical PhenomenaScanning electron microscopeAlginatesDrug Compoundinggum arabicPharmaceutical ScienceAscorbic AcidL-ascorbic acid01 natural sciencesArticleAnalytical Chemistrysodium alginatelcsh:QD241-4410404 agricultural biotechnologyfoodDifferential scanning calorimetryDrug Stabilitylcsh:Organic chemistry010608 biotechnologyDrug DiscoveryThermal stabilityspray-dryingPhysical and Theoretical ChemistryParticle Sizechemistry.chemical_classificationAnalysis of VarianceMolecular StructurenanotechnologySpectrum AnalysisOrganic ChemistryTemperature04 agricultural and veterinary sciencesPolymerAscorbic acid040401 food scienceThermogravimetrychemistryChemical engineeringChemistry (miscellaneous)Spray dryingMAQUINAS Y MOTORES TERMICOSMolecular MedicineGum arabicencapsulation
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Synthesis and Cytotoxicity of 1,4-Dihydropyridines and an Unexpected 1,3-Oxazin-6-one

2016

Eight heterocycles have been prepared in a one-pot reaction manner based on the Hantzsch dihydropyridine synthesis. The synthesis afforded seven dihydropyridines (DHP) and one unexpected 1,3-oxazin-6-one. Their structures were confirmed based on NMR spectroscopy and mass spectrometry. The obtained products have been evaluated for their cytotoxicity against eight cancer cell lines and one normal cell line. Two halogenated DHPs (7 and 8) displayed cytotoxicity toward all the nine tested cancer cell lines with IC50 values from 4.10 to 58.90 μm, while others showed selective activities. DHPs (7 and 8) bearing a Me group at C(2) and C(6) as well as a halogenated substituent at C(4′) were more an…

0301 basic medicine010405 organic chemistryStereochemistryChemistryOrganic ChemistrySubstituentDihydropyridineDHPSNuclear magnetic resonance spectroscopy01 natural sciencesBiochemistryCatalysis0104 chemical sciencesInorganic ChemistryNormal cell03 medical and health scienceschemistry.chemical_compound030104 developmental biologyDrug DiscoveryIc50 valuesmedicinePhysical and Theoretical ChemistryCancer cell linesCytotoxicitymedicine.drugHelvetica Chimica Acta
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Investigation of Isoindolo[2,1-a] quinoxaline-6-imines as Topoisomerase I Inhibitors with Molecular Modeling Methods

2017

Background: Isoindolo[2,1-alpha] quinoxalines constitute an important class of compounds which demonstrated potent antiproliferative activity against different human tumor cell lines and topoisomerase I inhibitors. In particular, their water soluble imine or iminium salts recently synthesized showed potent growth inhibitory effect on NCI-60 tumor cell line panel and biological studies performed on the most active compounds demonstrated that they cause DNA damage via topoisomerase I poisoning. Objective: Herein, we investigate with molecular modeling methods, the common features responsible for topoisomerase I inhibition of the water-soluble isoindolo[2,1-alpha] quinoxalin-6-imines, by compa…

0301 basic medicine030103 biophysicsMolecular modelStereochemistryDNA damageAntineoplastic AgentsIsoindolesTopoisomerase-I InhibitorCrystallography X-RayaromatechinStructure-Activity Relationship03 medical and health scienceschemistry.chemical_compoundQuinoxalinetopotecanantiproliferativeCell Line TumorNeoplasmsQuinoxalinesquinoxalineDrug DiscoveryHumansCell Proliferationbiologypharmacophore modelTopoisomeraseIminiumGeneral MedicineSettore CHIM/08 - Chimica FarmaceuticaMolecular Docking SimulationTopoisomerase IindenoisoquinolineDNA Topoisomerases Type IchemistryDocking (molecular)dockingbiology.proteinMolecular MedicineTopoisomerase I; quinoxaline; antiproliferative; topotecan; aromatechin; indenoisoquinoline; docking; pharmacophore modelIminesTopoisomerase I InhibitorsPharmacophore
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2,3-Dihydrobenzofuran privileged structures as new bioinspired lead compounds for the design of mPGES-1 inhibitors

2016

International audience; 2,3-Dihydrobenzofurans are proposed as privileged structures and used as chemical platform to design small compound libraries. By combining molecular docking calculations and experimental verification of biochemical interference, we selected some potential inhibitors of microsomal prostaglandin E2 synthase (mPGES)-1. Starting from low affinity natural product 1, by our combined approach we identified the compounds 19 and 20 with biological activity in the low micromolar range. Our data suggest that the 2,3-dihydrobenzofuran derivatives might be suitable bioinspired lead compounds for development of new generation mPGES-1 inhibitors with increased affinity.

0301 basic medicine300323-Dihydrobenzofuran privileged structure; Cancer; Inflammation; Molecular docking; mPGES-1 inhibitors; Biochemistry; Clinical Biochemistry; Molecular Biology; Molecular Medicine; Organic Chemistry; Drug Discovery3003 Pharmaceutical Science; 3003Amino Acid MotifsClinical BiochemistryGene ExpressionPharmaceutical Science01 natural sciencesClinical biochemistryBiochemistry[ CHIM ] Chemical SciencesProtein Structure Secondary[ SDV.CAN ] Life Sciences [q-bio]/Cancerchemistry.chemical_compoundLow affinityDrug DiscoveryEnzyme Inhibitors23-Dihydrobenzofuran privileged structure; Molecular docking; mPGES-1 inhibitors; Cancer; InflammationProstaglandin-E SynthasesCancerAnti-Inflammatory Agents Non-SteroidalBiological activityProto-Oncogene Proteins c-metIntramolecular OxidoreductasesMolecular Docking SimulationMolecular dockingMolecular Medicinelipids (amino acids peptides and proteins)Cell SurvivalStereochemistryMolecular Sequence Data2Antineoplastic Agents[SDV.CAN]Life Sciences [q-bio]/Cancer3-Dihydrobenzofuran privileged structureInhibitory Concentration 50Structure-Activity Relationship03 medical and health sciencesCell Line TumorMicrosomesHumans[CHIM]Chemical SciencesMolecular BiologyBenzofuransInflammationNatural product010405 organic chemistryDrug Discovery3003 Pharmaceutical ScienceOrganic ChemistryEpithelial CellsmPGES-1 inhibitorsCombinatorial chemistryCombined approach0104 chemical sciences030104 developmental biologychemistryDrug DesignDrug Screening Assays Antitumor
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Indicaxanthin from Opuntia Ficus Indica (L. Mill) impairs melanoma cell proliferation, invasiveness, and tumor progression.

2018

Abstract Background: A strong, reciprocal crosstalk between inflammation and melanoma has rigorously been demonstrated in recent years, showing how crucial is a pro-inflammatory microenvironment to drive therapy resistance and metastasis. Purpose: We investigated on the effects of Indicaxanthin, a novel, anti-inflammatory and bioavailable phytochemical from Opuntia Ficus Indica fruits, against human melanoma both in vitro and in vivo. Study Design and Methods: The effects of indicaxanthin were evaluated against the proliferation of A375 human melanoma cell line and in a mice model of cutaneous melanoma. Cell proliferation was assessed by MTT assay, apoptosis by Annexin V-Fluorescein Isothio…

0301 basic medicine3003MaleSkin NeoplasmsPyridinesPyridinePhytochemicalsMelanoma ExperimentalPharmaceutical ScienceIndicaxanthinApoptosisBcl-2 B cell lymphoma gene-2 (Bcl-2)chemistry.chemical_compoundMice0302 clinical medicineOpuntia Ficus Indica (L.Mill)Settore BIO/10 - BiochimicaDrug DiscoveryCXCL1 chemokine (C-X-C motif) ligand 1MelanomaNF-κB nuclear factor kappa BMTT 3-[45-dimethyltiazol-2-yl]-25-diphenyl tetrazolium bromideMelanomaNF-kappa BOpuntiaComplementary and Alternative Medicine2708 DermatologyBetaxanthinsCXCL1030220 oncology & carcinogenesisMolecular MedicinePhC phytochemicalGrowth inhibitionIndicaxanthinHumanBiologyPhytochemicalNHEM normal human epidermal melanocyte03 medical and health sciencesc-FLIP FLICE-inhibitory proteinIn vivoCell Line TumormedicineAnimalsHumansNeoplasm InvasivenessSkin NeoplasmCell ProliferationNeoplasm InvasiveneInflammationPharmacologyCell growthAnimalDrug Discovery3003 Pharmaceutical ScienceApoptosimedicine.diseaseMice Inbred C57BL030104 developmental biologyComplementary and alternative medicinechemistryTumor progressionList of Abbrevations: AxV-FITC annexin V-fluorescein isothiocyanateBetaxanthinFruitCutaneous melanomaCancer researchPI propidium iodide PIPhytomedicine : international journal of phytotherapy and phytopharmacology
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