Search results for "Silybin"

showing 5 items of 5 documents

Synthesis and antioxidant evaluation of novel silybin analogues

2006

In this work, we evaluated the antioxidant properties of the eight novel silybin analogues for their capacity to scavenge free radicals including superoxide anion radicals and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals in vitro. Compound 7d demonstrated an excellent antioxidant effect in scavenging superoxide anion free radical with an IC50 value of 26.5 microM, while the IC50 of quercetin (the reference compound) was 38.1 microM. Compounds 7b, 7e, 7h showed certain scavenging activities for both types of free radicals.

AnionsAntioxidantDPPHRadicalmedicine.medical_treatmentDrug Evaluation PreclinicalMedicinal chemistryAntioxidantsInhibitory Concentration 50chemistry.chemical_compoundPicratesSuperoxidesDrug DiscoverymedicineOrganic chemistryIC50PharmacologyDose-Response Relationship DrugSuperoxideBiphenyl CompoundsAnion radicalsFree Radical ScavengersGeneral MedicineIn vitroHydrazinesModels ChemicalchemistrySpectrophotometrySilybinQuercetinQuercetinSilymarinJournal of Enzyme Inhibition and Medicinal Chemistry
researchProduct

Preparation of C-23 esterified silybin derivatives and evaluation of their lipid peroxidation inhibitory and DNA protective properties.

2009

A diverse series of C-23 esterified silybin derivatives (1a-n) were designed and synthesized. The antioxidative properties of these compounds were evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH) and superoxide anion radical scavenging, ferrous ion chelation, and inhibition of rat liver homogenate lipid peroxidation. Their protective effects on the prevention of hydrogen peroxide induced DNA damage were also investigated. Most of the synthesized compounds exhibited more effective antioxidant activities than silybin. The esterified silybin analogues displayed satisfactory performance especially on iron chelation and antiperoxidative activity. Compound 1n in particular exhibited remarkable a…

AntioxidantDNA damageDPPHmedicine.medical_treatmentClinical BiochemistryPharmaceutical ScienceSilibininBiochemistryLipid peroxidationchemistry.chemical_compoundStructure-Activity RelationshipDrug DiscoverymedicineAnimalsChelationMolecular BiologyChemistryOrganic ChemistryFree Radical ScavengersFree radical scavengerRatsBiochemistrySilybinMolecular MedicineLipid PeroxidationQuercetinNuclear chemistryDNA DamageSilymarinBioorganicmedicinal chemistry
researchProduct

Silibinin improves hepatic and myocardial injury in mice with nonalcoholic steatohepatitis

2012

Abstract Background Nonalcoholic fatty liver disease is a chronic metabolic disorder with significant impact on cardiovascular and liver mortality. Aims In this study, we examined the effects of silibinin on liver and myocardium injury in an experimental model of nonalcoholic fatty liver disease. Methods A four-week daily dose of silibinin (20 mg/kg i.p.) was administrated to db/db mice fed a methionine–choline deficient diet. Hepatic and myocardial histology, oxidative stress and inflammatory cytokines were evaluated. Results Silibinin administration decreased HOMA-IR, serum ALT and markedly improved hepatic and myocardial damage. Silibinin reduced isoprostanes, 8-deoxyguanosine and nitrit…

MaleGene ExpressionIsoprostanesmedicine.disease_causeGastroenterologyAntioxidantsMicechemistry.chemical_compoundMethionineNon-alcoholic Fatty Liver DiseaseNonalcoholic fatty liver diseasePhosphorylationGastroenterologyAlanine TransaminaseGlutathioneCholine DeficiencyMitochondrial respiratory chainLiverHeart Inflammation NAFLD Oxidative stress SilibininCytokinesmedicine.symptomSilymarinmedicine.medical_specialtySilibininInflammationStatistics NonparametricProinflammatory cytokineInsulin resistanceInternal medicinemedicineAnimalsNitritesAnalysis of VarianceNitratesHepatologySettore BIO/16 - Anatomia Umanabusiness.industryMyocardiumJNK Mitogen-Activated Protein KinasesGlutathionemedicine.diseaseDietFatty LiverOxidative StressEndocrinologychemistrySilybinInsulin ResistancebusinessOxidative stressDigestive and Liver Disease
researchProduct

Silibinin modulates lipid homeostasis and inhibits nuclear factor kappa B activation in experimental nonalcoholic steatohepatitis.

2012

Nonalcoholic steatohepatitis (NASH) is associated with increased liver-related mortality. Disturbances in hepatic lipid homeostasis trigger oxidative stress and inflammation (ie, lipotoxicity), leading to the progression of NASH. This study aimed at identifying whether silibinin may influence the molecular events of lipotoxicity in a mouse model of NASH. Eight-week-old db/db mice were fed a methionine-choline deficient (MCD) diet for 4 weeks and treated daily with silibinin (20 mg/kg intraperitoneally) or vehicle. Liver expression and enzyme activity of stearoyl-CoA desaturase-1 and acyl-CoA oxidase, and expression of liver fatty acid-binding protein were assessed. Hepatic levels of reactiv…

Malemedicine.medical_specialtyMice ObeseSilibininmedicine.disease_causeAntioxidantsTranslational Research BiomedicalMicechemistry.chemical_compoundMethionineNon-alcoholic Fatty Liver DiseasePhysiology (medical)Internal medicineNonalcoholic fatty liver diseasemedicineTBARSAnimalsHomeostasisNASH MCD Silibinin lipotoxicity.Reactive nitrogen speciesLiver injurychemistry.chemical_classificationReactive oxygen speciesAnti-Inflammatory Agents Non-SteroidalBiochemistry (medical)NF-kappa BPublic Health Environmental and Occupational HealthGeneral MedicineLipid Metabolismmedicine.diseaseCholine DeficiencyFatty LiverDisease Models AnimalOxidative StressEndocrinologyLiverchemistryLipotoxicitySilybinOxidative stressSilymarin
researchProduct

Silymarin and Cancer: A Dual Strategy in Both in Chemoprevention and Chemosensitivity

2020

Silymarin extracted from milk thistle consisting of flavonolignan silybin has shown chemopreventive and chemosensitizing activity against various cancers. The present review summarizes the current knowledge on the potential targets of silymarin against various cancers. Silymarin may play on the system of xenobiotics, metabolizing enzymes (phase I and phase II) to protect normal cells against various toxic molecules or to protect against deleterious effects of chemotherapeutic agents on normal cells. Furthermore, silymarin and its main bioactive compounds inhibit organic anion transporters (OAT) and ATP-binding cassettes (ABC) transporters, thus contributing to counteracting potential chemor…

Programmed cell deathsilymarinCellChemosensitizerPharmaceutical SciencechemopreventiveATP-binding cassette transporterApoptosisReviewProtective AgentsChemopreventionsilybinAnalytical Chemistrylcsh:QD241-44103 medical and health sciences0302 clinical medicinelcsh:Organic chemistryDrug DiscoverymedicineHumansPhysical and Theoretical ChemistryReceptor030304 developmental biology0303 health sciencesChemistryOrganic ChemistryCancerCell Cycle CheckpointsCell cyclemedicine.diseasemedicine.anatomical_structureChemistry (miscellaneous)intrinsic and extrinsic pathwayDrug Resistance Neoplasm030220 oncology & carcinogenesisCancer cellchemosensitizerCancer researchMolecular Medicinemetabolizing enzymesATP-Binding Cassette Transporterscell cycleABC transporterSignal TransductionMolecules
researchProduct