0000000000199344

AUTHOR

Alfonso De Giulio

0000-0002-4799-1011

showing 4 related works from this author

Suppression of leukotriene B4 and tumour necrosis factor alpha release in acute inflammatory responses by novel prenylated hydroquinone derivatives.

1998

A series of prenyl hydroquinone derivatives synthesized as structural analogs of marine products were tested for their effects on inflammatory responses in vitro and in vivo. 2-Prenyl-1,4-hydroquinone (H1), 2-diprenyl-1,4-hydroquinone (H2), 2-triprenyl-1,4-hydroquinone (H3) and 2-tetraprenyl-1,4-hydroquinone (H4) scavenged reactive oxygen species and inhibited 5-lipoxygenase (5-LO) activity in human neutrophils. The inhibition of 5-LO activity was demonstrated in vivo in the mouse air pouch injected with zymosan and arachidonic acid-induced ear inflammation. The four compounds suppressed the production of tumour necrosis factor alpha (TNFalpha) in J774 cells stimulated with lipopolysacchari…

MaleNecrosisLipopolysaccharideLeukotriene B4Anti-Inflammatory AgentsPharmacologyLeukotriene B4Dinoprostonechemistry.chemical_compoundMiceIn vivomedicineAnimalsEdemaHumansCells CulturedNitritesPharmacologyInflammationArachidonic AcidbiologyTumor Necrosis Factor-alphaZymosanGeneral MedicineHydroquinonesNitric oxide synthasechemistryBiochemistryDepression ChemicalArachidonate 5-lipoxygenaseLuminescent Measurementsbiology.proteinTumor necrosis factor alphamedicine.symptomNaunyn-Schmiedeberg's archives of pharmacology
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Modulation of acute and chronic inflammatory processes by cacospongionolide B, a novel inhibitor of human synovial phospholipase A2

1999

Cacospongionolide B is a novel marine metabolite isolated from the sponge Fasciospongia cavernosa. In in vitro studies, this compound inhibited phospholipase A2 (PLA2), showing selectivity for secretory PLA2 (sPLA2) versus cytosolic PLA2 (cPLA2), and its potency on the human synovial enzyme (group II) was similar to that of manoalide. This activity was confirmed in vivo in the 8 h zymosan-injected rat air pouch, on the secretory enzyme accumulating in the pouch exudate. Cacospongionolide B, that is bioavailable when is given orally, reduced the elevated levels of sPLA2 present in paw homogenates of rats with adjuvant arthritis. This marine metabolite showed topical anti-inflammatory activit…

PharmacologybiologyMetaboliteZymosanBiological activityPharmacologyManoalidechemistry.chemical_compoundPhospholipase A2EicosanoidchemistryEnzyme inhibitorIn vivoImmunologybiology.proteinBritish Journal of Pharmacology
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A New Cacospongionolide Inhibitor of Human Secretory Phospholipase A2 from the Tyrrhenian Sponge Fasciospongia cavernosa and Absolute Configuration o…

1998

A new inhibitor of human secretory phospholipase A2 (PLA2), cacospongionolide E (4a), has been isolated from the Tyrrhenian sponge Fasciospongia cavernosa. The structure was proposed on the basis of spectroscopic data and by chemical transformations. The absolute configuration of cacospongionolides 2a-4a was established using the modified Mosher's method. Cacospongionolide E was the most potent inhibitor toward human synovial PLA2, showing higher potency than the reference compound manoalide and exerting no signs of toxicity on human neutrophils. It showed high activity in the Artemia salina bioassay and moderate toxicity in the fish (Gambusia affinis) lethality assay.

Magnetic Resonance SpectroscopySpectrophotometry InfraredMolecular ConformationPharmaceutical ScienceMass SpectrometryPhospholipases AAnalytical ChemistryCyprinodontiformesManoalidechemistry.chemical_compoundPhospholipase A2Synovial FluidDrug DiscoveryAnimalsHumansBioassayEnzyme InhibitorsFuransPancreasPyransPharmacologybiologyVenomsOrganic ChemistryAbsolute configurationBiological activitybiology.organism_classificationPoriferaPhospholipases A2SpongeComplementary and alternative medicinechemistryBiochemistryEnzyme inhibitorbiology.proteinMolecular MedicineSpectrophotometry UltravioletDrug Screening Assays AntitumorArtemia salinaJournal of Natural Products
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Effects of marine 2-polyprenyl-1,4-hydroquinones on phospholipase A2 activity and some inflammatory responses.

1995

Three 2-polyprenyl-1,4-hydroquinone derivatives (2-heptaprenyl-1,4-hydroquinone: IS1, 2-octaprenyl-1,4-hydroquinone: IS2 and 2-[24-hydroxy]-octaprenyl-1,4-hydroquinone: IS3) isolated from the Mediterranean sponge Ircinia spinosula, were evaluated for effects on phospholipase A2 activity of different origin (Naja naja venom, human recombinant synovial fluid and bee venom), as well as on human neutrophil function and mouse ear oedema induced by 12-O-tetradecanoylphorbol 13-acetate (TPA). IS1 interacted minimally with these responses. In contrast, IS2 and IS3 inhibited human recombinant synovial phospholipase A2 in a concentration-dependent manner, with minor effects on the rest of the enzymes…

Blood PlateletsLeukocyte migrationLeukotriene B4Cell SurvivalNeutrophilsPharmacologyBiologyIn Vitro TechniquesLeukotriene B4Phospholipases Achemistry.chemical_compoundMicePhospholipase A2SuperoxidesMicrosomesSynovial fluidAnimalsEdemaHumansPharmacologyPhospholipase AL-Lactate DehydrogenasePancreatic ElastaseAnti-Inflammatory Agents Non-SteroidalDegranulationBiological activityHydroquinonesPoriferaThromboxane B2Thromboxane B2Phospholipases A2Biochemistrychemistrybiology.proteinTetradecanoylphorbol AcetateEuropean journal of pharmacology
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