0000000001301965

AUTHOR

Rosalia Busà

showing 10 related works from this author

Loading and release of the complex [Pt(DTBTA)(DMSO)Cl]Cl·CHCl3 with the 2,2′-dithiobis(benzothiazole) ligand into mesoporous silica and studies of an…

2018

Abstract Synthetic delivery systems have great potential for overcoming problems associated with systemic toxicity that accompanies chemotherapy with the use of cisplatin and family of platinum anticancer drugs. Mesoporous silicates have been studied in context of drug delivery and drug targeting. In this paper we report the studies of loading and release of a platinum complex, [Pt(DTBTA)(DMSO)Cl]Cl∙CHCl3 (1) where DTBTA = 2,2′-dithiobis(benzothiazole), that was recently synthesized and structurally characterized. Evaluation in vitro of antitumor activity against a human breast cancer cell line (MCF-7) showed a very potent activity of complex(1). Therefore, we thought to incorporate this co…

02 engineering and technologyMesoporous silica010402 general chemistry021001 nanoscience & nanotechnology01 natural sciencesControlled release0104 chemical sciencesInorganic ChemistryAntiproliferative activityControlled releaseLoadingMCM41Platinum(II) complexchemistry.chemical_compoundTargeted drug deliveryBenzothiazolechemistrySettore CHIM/03 - Chimica Generale E InorganicaDrug deliveryMaterials ChemistryPhysical and Theoretical Chemistry0210 nano-technologyCytotoxicityMesoporous materialConjugateNuclear chemistrySettore CHIM/02 - Chimica Fisica
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ATTIVITA’ CITOTOSSICA DI COMPLESSI ORGANOSTAGNO(IV) CON TRIAZOLOPIRIMIDINE CONTENENTI ATOMI DI OSSIGENO ESOCICLICO

2019

Le triazolopirimidine sono leganti eterociclici di crescente interesse. I composti di organostagno(IV) sono caratterizzati dalla presenza di un atomo di stagno (Sn) legato covalentemente ad uno o più sostituenti organici. In questo studio1 sono stati sintetizzati: Me3Sn(5tpO)(1); n-Bu3Sn(5tpO)(2); Me3Sn(mtpO)(3); n-Bu3Sn(mtpO)(4); n-Bu3Sn(HtpO2)(5); Ph3Sn(HtpO2)(6) e la loro citotossicità valutata su tre differenti linee cellulari tumorali umane: HCT-116 (carcinoma del colon retto), HepG2 (epatocarcinoma) e MCF-7 (carcinoma mammario). I complessi 2, 4, 5 e 6 hanno mostrato attività citotossica di 1-2 ordini di grandezza superiore al cis-platino, sulle 3 linee cellulari tumorali. Il meccanis…

triazolopirimidine attività citotossica
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Indicaxanthin from Opuntia ficus indica (L. Mill) Inhibits Oxidized LDL-Mediated Human Endothelial Cell Dysfunction through Inhibition of NF-κB Activ…

2019

Oxidized low-density lipoproteins (oxLDL) play a pivotal role in the etiopathogenesis of atherosclerosis through the activation of inflammatory signaling events eventually leading to endothelial dysfunction and senescence. In the present work, we investigated the effects of indicaxanthin, a bioavailable, redox-modulating phytochemical from Opuntia ficus indica fruits, with anti-inflammatory activity, against oxLDL-induced endothelial dysfunction. Human umbilical vein cord cells (HUVEC) were stimulated with human oxLDL, and the effects of indicaxanthin were evaluated in a range between 5 and 20 μM, consistent with its plasma level after a fruit meal (7 μM). Pretreatment with indicaxanthin si…

0301 basic medicineAgingArticle SubjectTranscription GeneticCell SurvivalPyridineHuman Umbilical Vein Endothelial Cell030204 cardiovascular system & hematologyPharmacologyBiochemistryUmbilical vein03 medical and health scienceschemistry.chemical_compound0302 clinical medicineSettore BIO/10 - BiochimicamedicineRNA MessengerReactive Nitrogen SpecieEndothelial dysfunctionlcsh:QH573-671CytotoxicityReactive nitrogen specieschemistry.chemical_classificationReactive oxygen specieslcsh:CytologyNF-kappa BOpuntiaHydrogen PeroxideCell BiologyGeneral MedicineNFKB1medicine.diseaseSettore CHIM/08 - Chimica FarmaceuticaUp-RegulationLipoproteins LDLEndothelial stem cell030104 developmental biologychemistryCell Adhesion MoleculeBetaxanthinThiobarbituric Acid Reactive SubstanceReactive Oxygen SpecieOxidation-ReductionIndicaxanthinATP Binding Cassette Transporter 1HumanOxidative Medicine and Cellular Longevity
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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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Inhibitory effects of cynaropicrin on human melanoma progression by targeting MAPK, NF-κB, and Nrf-2 signaling pathways in vitro

2021

Malignant melanoma is the deadliest skin cancer, due to its propensity to metastasize. MAPKs and NF-κB pathways are constitutively activated in melanoma and promote cell proliferation, cell invasion, metastasis formation, and resistance to therapeutic regimens. Thus, they represent potential targets for melanoma prevention and treatment. Phytochemicals are gaining considerable attention for the management of melanoma because of their several cellular and molecular targets. A screening of a small library of sesquiterpenes lactones selected cynaropicrin, isolated from the aerial parts of Centaurea drabifolia subsp. detonsa, for its potential anticancer effect against melanoma cells. Treatment…

MAPK/ERK pathwayApoptosisBiologymedicine.disease_causeLactones03 medical and health scienceschemistry.chemical_compound0302 clinical medicineSettore BIO/10 - Biochimicasesquiterpene lactonesmedicinemelanomaHumansoxidative stresschemopreventionTranscription factorCell ProliferationMitogen-Activated Protein Kinase KinasesPharmacology0303 health sciencesoxidative streCell growthMelanoma030302 biochemistry & molecular biologyNF-kappa BNF-κBmedicine.diseaseMAPKCynaropicrinchemistry030220 oncology & carcinogenesiscynaropicrinDisease ProgressionCancer researchSignal transductionCarcinogenesisSesquiterpenesSignal Transduction
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Cytotoxic Activity of Organotin(IV) Derivatives with Triazolopyrimidine Containing Exocyclic Oxygen Atoms

2020

In this study cytotoxicity of organotin(IV) compounds with 1,2,4-triazolo[1,5-a]pyrimidines, Me3Sn(5tpO) (1), n-Bu3Sn(5tpO) (2), Me3Sn(mtpO) (3), n-Bu3Sn(mtpO) (4), n-Bu3Sn(HtpO2) (5), Ph3Sn(HtpO2) (6) where 5HtpO = 4,5-dihydro-5-oxo-[1,2,4]triazolo-[1,5-a]pyrimidine, HmtpO = 4,7-dihydro-5-methyl-7-oxo-[1,2,4]triazolo-[1,5-a]pyrimidine, and H2tpO2 = 4,5,6,7-tetrahydro-5,7- dioxo-[1,2,4]triazolo-[1,5-a]-pyrimidine, was assessed on three different human tumor cell lines: HCT-116 (colorectal carcinoma), HepG2 (hepatocarcinoma) and MCF-7 (breast cancer). While 1 and 3 were inactive, compounds 2, 4, 5 and 6 inhibited the growth of the three tumor cell lines with IC50 values in the submicromolar …

DenticityCellPharmaceutical Science01 natural sciencesAnalytical Chemistrychemistry.chemical_compoundDrug DiscoveryOrganotin CompoundstriazolopyrimidineCytotoxicityMembrane Potential MitochondrialCytotoxinsapoptosisBiological activityHep G2 CellsG2 Phase Cell Cycle CheckpointsGene Expression Regulation Neoplasticmedicine.anatomical_structureChemistry (miscellaneous)Mitochondrial MembranesMCF-7 CellsMolecular MedicineCyclin-Dependent Kinase Inhibitor p21crystal structurein vitro anticancer activityPyrimidineCell SurvivalStereochemistryorganotin(iv)010402 general chemistryArticlelcsh:QD241-441Inhibitory Concentration 50Structure-Activity Relationshiplcsh:Organic chemistrymedicineHumansPhysical and Theoretical ChemistryMetallodrug010405 organic chemistryLigandOrganic ChemistryTriazolesHCT116 CellsapoptosiG1 Phase Cell Cycle Checkpoints0104 chemical sciencesPyrimidineschemistrymetallodrugsCell cultureApoptosisDrug DesignTumor Suppressor Protein p53Reactive Oxygen SpeciesMolecules
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Klebsiella pneumoniae Lipopolysaccharides Serotype O2afg Induce Poor Inflammatory Immune Responses Ex Vivo

2021

Currently, Klebsiella pneumoniae is a pathogen of clinical relevance due to its plastic ability of acquiring resistance genes to multiple antibiotics. During K. pneumoniae infections, lipopolysaccharides (LPS) play an ambiguous role as they both activate immune responses but can also play a role in immune evasion. The LPS O2a and LPS O2afg serotypes are prevalent in most multidrug resistant K. pneumoniae strains. Thus, we sought to understand if those two particular LPS serotypes were involved in a mechanism of immune evasion. We have extracted LPS (serotypes O1, O2a and O2afg) from K. pneumoniae strains and, using human monocytes ex vivo, we assessed the ability of those LPS antigens to in…

0301 basic medicineMicrobiology (medical)SerotypeChemokineQH301-705.5Klebsiella pneumoniae<i>Klebsiella pneumoniae</i>030106 microbiologyMicrobiologyArticleNF-κBMicrobiology03 medical and health scienceschemistry.chemical_compoundImmune systemAntigenVirologyantimicrobial resistanceBiology (General)Pathogenimmune evasionbiologylipopolysaccharideNF-κBSettore CHIM/06 - Chimica Organicalipopolysaccharidesbiology.organism_classificationKlebsiella pneumoniae030104 developmental biologychemistrynosocomial infectionbiology.proteinlipids (amino acids peptides and proteins)Ex vivoMicroorganisms
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Synthesis, properties, antitumor and antibacterial activity of new Pt(II) and Pd(II) complexes with 2,2′-dithiobis(benzothiazole) ligand

2017

Mono- and binuclear Pt(II) and Pd(II) complexes with 2,20-dithiobis(benzothiazole) (DTBTA) ligand are reported. [Pt(DTBTA)(DMSO)Cl]Cl∙CHCl3 (1) and [Pd2(m-Cl)2(DTBTA)2]Cl2 (2) have been synthesized and structurally characterized by elemental analysis, IR, 1H and 13C NMR spectroscopy, MS spectrometry and the content of platinum and palladium was determined using a flame atomic spectrometer. Two different coordination modes of 1 and 2 complexes were found; in both complexes, the coordination of Pt(II) and Pd(II) ions involves the N(3) atoms of the ligand but the binuclear complex 2, is a cis-chloro-bridged palladium complex. Evaluation of their in vitro antitumor activity against two human tu…

StereochemistryPlatinum complex Palladium complex Heterocyclic nitrogen ligand Anticancer activity Antimicrobial activityClinical BiochemistryPharmaceutical Sciencechemistry.chemical_elementPlatinum CompoundsMicrobial Sensitivity TestsLigands010402 general chemistry01 natural sciencesBiochemistrychemistry.chemical_compoundCell Line TumorDrug DiscoveryEscherichia coliHumansBenzothiazolesMolecular Biology010405 organic chemistryLigandSpectrum AnalysisOrganic ChemistryCell cycleIn vitroAnti-Bacterial Agents0104 chemical sciencesBenzothiazolechemistrySettore CHIM/03 - Chimica Generale E InorganicaMolecular MedicineDrug Screening Assays AntitumorPlatinumAntibacterial activityPalladiumIntracellularPalladiumBioorganic &amp; Medicinal Chemistry
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CCDC 1908619: Experimental Crystal Structure Determination

2020

Related Article: Alessandro Attanzio, Simone D’Agostino, Rosalia Busà, Anna Frazzitta, Simona Rubino, Maria Assunta Girasolo, Piera Sabatino, Luisa Tesoriere|2020|Molecules|25|859|doi:10.3390/molecules25040859

Space GroupCrystallographycatena-[(mu-5-oxo-5H-[124]triazolo[15-a]pyrimidin-3-ido)-tributyl-tin]Crystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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CCDC 1908620: Experimental Crystal Structure Determination

2020

Related Article: Alessandro Attanzio, Simone D’Agostino, Rosalia Busà, Anna Frazzitta, Simona Rubino, Maria Assunta Girasolo, Piera Sabatino, Luisa Tesoriere|2020|Molecules|25|859|doi:10.3390/molecules25040859

Space GroupCrystallographycatena-[(mu-5-oxo-5H-[124]triazolo[15-a]pyrimidin-3-ido)-trimethyl-tin]Crystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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